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Y2 > 11 Hypertension > Flashcards

11 Hypertension Flashcards

1
Q

Define hypertension

A

High blood pressure

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2
Q

Define cardiovascular disease (CVD)

A

Includes all the disease of heart and blood vessels

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3
Q

Define cardiovascular risk

A

The likelihood of developing angina,myocardial infarction or stroke

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4
Q

What is blood pressure?

A

The force of the blood pushing against the walls of the arteries

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5
Q

What is systolic pressure?

A

The pressure of blood in the vessels when the heart beats

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6
Q

What is diastolic pressure?

A

The pressure between beats when the heart relaxes

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7
Q

What is the unit blood pressure is measured in?

A

Millimeters of mercury/mmHg

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8
Q

What is considered to be high blood pressure?

A

140/90mmHg or higher

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9
Q

What blood pressure is considered to be prehypertension?

A

Between 120-139mmHg and/or 80/89 mmHg

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10
Q

What is considered normal blood pressure?

A

Less than 120/80 mmHg

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11
Q

What is the most common intervention in primary care?

A

Management

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12
Q

What some risk factors of hypertension?

A
  • age
  • co-morbidities
  • ethnicity
  • family history
  • gender (M>F)
  • hypertension in pregnancy
  • poor diet (too much salt)
  • smokers
  • e.c.t.
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13
Q

What are the consequences of high blood pressure?

A
  • stroke
  • heart failure
  • erectile dysfunction
  • vision loss
  • heart attack
  • kidney disease/failure
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14
Q

What is Left ventricular hypertrophy?

A

It is the thickening of the heart’s main pumping chamber and is a consequence of hypertension.

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15
Q

What is a result of left ventricular hypertrophy?

A

The thickening of the wall may result in elevation of pressure within the heart and sometimes poor pumping action

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16
Q

How do we estimate CVD risk?

A

QRISK3-risk calculator

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17
Q

What is the QRISK3-risk calculator?

A

It calculates risk of having a ‘heart attack or stroke’ over the next ten years and is based on data from UK GPs

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18
Q

What patients would use QRISK3-risk calculator?

A

This is for primary prevention patients

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19
Q

What can consistently high blood pressure lead to?

A

Damage in the arteries and organs and is a leading cause of stroke, heart disease and kidney disease

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20
Q

Why is lowering blood pressure significant?

A

By lowering blood pressure by even 5 mmHg can significantly lower the chance of developing serious health problems

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21
Q

In 2017, what was the estimation of people in the UK have high blood pressure?

A

1 in 4 people, however, many people are undiagnosed

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22
Q

What is the NHSE Ambition target for people being treated with hypertension?

A

80% of people to be treated to target by March 25

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23
Q

What is the cause of PRIMARY hypertension?

A

In most cases (90-95%) there is no identifiable cause

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24
Q

What are the causes of SECONDARY hypertension?

A
  • diseases (e.g. chronic kidney disease, Crushing syndrome, Parathyroid disease)
  • drugs (e.g. corticosteroids, decongestants, NSAIDs)
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25
Q

What are the symptoms of high blood pressure?

A
  • dizziness
  • headache
  • vomiting, nausea
  • blurred vision
  • shortness of breath
    But most people are ASYMPTOMATIC
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26
Q

What ways can hypertension cases be found?

A
  • opportunistic (patients present in health care settings)
  • proactive methods
  • ambulatory blood pressure monitoring
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27
Q

What are the proactive methods of finding hypertension cases?

A
  • NHS health checks
  • Community Pharmacy case finding services
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28
Q

What is the NHS health checks for?

A

It is for adults in England aged 40-74
Designed to spot early signs of stroke, kidney disease, type 2 diabetes or dementia

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29
Q

What is the purpose of community pharmacy case finding service?

A

To identify people over 40y years old with high blood pressure, who have previously NOT had a confirmed diagnosis of hypertension

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30
Q

Describe ambulatory blood pressure monitoring (ABMP)

A
  • takes blood pressure every 30 minutes (day and night)
  • need at least 14 daytime readings for diagnosis
  • mean daytime BP
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31
Q

Describe home blood pressure monitoring (HBPM)

A
  • alternative to ABPM and is increasing in use
  • Patient does BP monitoring for at least 4 days and ideally seven days
  • 2 readings each morning and 2 readings each evening at least 1 minute apart
  • Discard day one readings and then average BP from all other days
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32
Q

What are some tips for taking blood pressure?

A
  • patient should be relaxed
  • take the pulse for 1 minute
  • the arm should be supported at heart level
  • no talking with the back supported and feel flat on the floor
  • take 2 or 3 readings
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33
Q

Give examples of lifestyle advice for all

A
  • DASH eating plan
  • exercise
  • reduced dietary sodium intake
  • moderation of alcohol intake as needed
  • weight loss if warrented
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34
Q

What can be tested to flag target organ damage?

A
  • urine
  • blood tests
  • eyes
  • ECG
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35
Q

What would you look at in URINE to spot target organ damage?

A
  • albumin - creatinine ration (ACR)
  • haematuria
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36
Q

What would you look at in blood tests to spot target organ damage?

A
  • electrolytes, creatinine, eGFR
  • lipid profile
  • liver function and thyroid function
  • HbA1c
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37
Q

What would you be looking at in the eyes to spot target organ damage?

A

Examination of fundi for hypertensive retinopathy

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38
Q

What would you be looking at with an ECG to spot target organ damage?

A
  • 12 lead ECG: looking for hypertrophy
  • signs of ischaemic changes (arrhythmias)
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39
Q

How would you estimate cardiovascular risk in people aged 25-84 without CVD, CKD or familial hypercholesterolaemia?

A

QRisk3 tool valid for UK population

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40
Q

What is the treatment plan for a patient with a blood pressure reading of under 135/85 mmHg?

A

You would check at least every 5 years and more often if clinic BP is close to 140/90 mmHg
If there’s evidence of target organ damage, consider alternative causes

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41
Q

What is the risk of using beta-blockers and thiazides together?

A

Increase risk of diabetes

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42
Q

Wha can newer drugs used to treat hypertension offer?

A

Offer slightly better stroke risk reduction in high risk patients

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43
Q

What is the first line of treatments for hypertension?

A

ACD:
- ACE inhibitors or ARB
- Calcium channel blocks
- Thiazide-like diuretics

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44
Q

What is white coat?

A

Blood pressure higher in clinical settings

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45
Q

What is masked hypertension?

A

Blood pressure is higher at home

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46
Q

Give examples of ACE inhibitors

A

Perindopril & Ramipril

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47
Q

In hypertension, when is ACE inhibitors given?

A

First line in younger (<55 years) Caucasian people and people who are diabetic

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48
Q

Apart from hypertension, when is ACE inhibitors used?

A

Primary and secondary prevention of CVD, heart failure and diabetic neuropathy

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49
Q

What are some side effects of ACE inhibitors?

A
  • dry cough
  • renal impairment
  • angio-oedema
  • HYPERkalaemia
  • HYPOnatraemia
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50
Q

What must be monitored when taking ACE inhibitors?

A

Baseline renal function and electrolytes (Na and K) and they should be rechecked 1-2 weeks after starting and after any dose increase

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51
Q

What should you avoid taking with ACE inhibitors?

A

Avoid K+ sparing diuretics and NSAIDs

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52
Q

What cautions must you take with ACE inhibitors?

A
  • care with diuretic therapy
  • caution aortic stenosis (postural hypotension)
  • do not use in pregnancy
  • contraindications include bilateral renal artery stenosis
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53
Q

ACE inhibitors are the leading cause of what?

A

Drug induced angio-oedema (incidence 0.1-0.7% of patients)

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54
Q

What do you usually see (signs) with angio-oedema?

A
  • swelling of the lips, tongue, face and upper airway without itching or urticaria
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55
Q

What is urticaria?

A

Hives - itching welts

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56
Q

When does angio-oedema present after starting prescription?

A

Half of cases occur in the 1st week of starting but can occur at anytime (hours-years)

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57
Q

When does the swelling in angio-oedema develop?

A

Over mins-hours to a peak with each episode lasting 2-5 days

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58
Q

Why does ACE inhibitors cause angio-edema?

A

CLASS EFFECT
ACE inhibitors cause angioedema by blocking the breakdown of bradykinin, leading to its accumulation. Elevated bradykinin levels increase vascular permeability, causing fluid to leak into tissues and result in swelling.

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59
Q

What does bradykinin do?

A

It’s a potent endothelium-dependent vasodilator and mild diuretic which may cause the lowering of blood pressure

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60
Q

What is the incidence of cross reaction between ACEi and ARBs?

A

Low incidence

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61
Q

Give examples of angiotensin II receptor blockers (ARBs)

A

Irbesartan & Losartan

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62
Q

What are ARBs an alternative to?

A

Alternative to ACE inhibitors
- DO NOT use in combination

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63
Q

Who are usually prescribed ARBs (angiotensin II receptor blockers)?

A

For black patients of African or Caribbean origin (in preference to ACEi) WITH DIABETES

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64
Q

What are the side effects of ARBs?

A
  • cough
  • lower risk of angio-edema than ACEi
  • renal impairment
  • HYPERkalemia
  • headache
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65
Q

Who is offered calcium channel blocker for hypertension?

A

First line treatment for non-diabeteic patients aged >55 or black African or Afro-Caribbean

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66
Q

What are the two distinct classes of calcium channel blockers?

A

Dihydropyridine & non-dihydropyridine

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67
Q

Give examples of dihydropyridine CCBs?

A
  • amlodipine
  • lacidipine
  • lercanidipine
  • nifedipine
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68
Q

What does Dihydropyridine do?

A

It causes vasodilatation of coronary and peripheral arteries and relaxes smooth muscles

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69
Q

Apart from hypertension, what else can dihydropyridine be used for?

A

Treatment of stable angina

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70
Q

What are some of the effects of dihydropyridine CCBs?

A
  • flushing and headaches
  • ankle swelling
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71
Q

Where are CCBs metabolized?

A

By the liver

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72
Q

What blood tests are needed for dihydropyridine?

A

No specific tests are needed

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73
Q

Give examples of non-dihydropyridines?

A
  • phenylalkalamines (verapamil)
  • benzothiazepines (diltiazem)
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74
Q

How does non-dihydropyridines work to lower hypertension?

A
  • interferes with myocardial conduction
  • slows the heart rate
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75
Q

What should you not combine verapamil with and why?

A

Because it is a non-dihydropyridine, it should not be combined with beta-blockers as it slows the heart

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76
Q

What condition should you not use non-dihydropyridine in?

A

Heart failure as it may cause contractility to be reduced

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77
Q

What is a common side effect of non-dihydropyridine?

A

Constipation

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78
Q

What else can non-dihydropyridine be used for?

A

Treat stable angina and for arrhythmias (rate control)

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79
Q

What steps in hypertension treatment is thiazide like diuretics offered?

A

Step 2 or 3

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80
Q

What thiazide-like diuretics would be prescribed?

A

Indapamide 2.5 od (or chlorthalidone)

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81
Q

When would thiazide like diuretics not be effective?

A

Poor renal function (eGFR <30 ml/min)

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82
Q

What do you need to be careful of when taking thiazide like diuretics?

A
  • electrolyte disturbances (Na, K, Ca)
  • renal impairment
    THEREFORE baseline U&E tests must be don’t and repeat within 1 month
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83
Q

What are some side effects of thiazide like diuretics?

A
  • may cause skin rashes
  • may unmask/exacerbate gout
  • increases risk of diabetes (esp. w/ beta-blockers)
  • loss of efficacy in CKS (eGFR <30 ml/min)
  • increase in urate, glucose and blood lipids
  • HYPOkalaemia
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84
Q

What is a 4th line drug of choice to treat hypertension?

A

Spironolactone - aldosterone antagonist

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85
Q

What is the risk of taking spironalactone?

A

Risk of HYPERkalaemia and renal impairment

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86
Q

What effect does NSAIDs have on blood pressure?

A

Increases it

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87
Q

What is the dosing advice for spironolactone?

A

Low doses only - max dose 50 mg/day

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88
Q

What tests should be done when taking spironolactone?

A

Baseline U&E and repeat in 2-4 weeks

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89
Q

Apart form hypertension, what else an spironolactone be used for?

A

Also used in heart failure (max 50 mg/day) and ascites (higher doses may be Rx)

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90
Q

Give examples of loop diuretics

A

Furosemide & bumetanide

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91
Q

Compare the potency of loop diuretics to thiazides

A

Loop diuretics are more potent than thiazides

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92
Q

Apart from hypertension, when else can loop diuretics be used?

A

Used in pulmonary oedema or heart failure

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93
Q

What is the mode of action of loop diuretics?

A

Loop diuretics inhibit the Na⁺-K⁺-2Cl⁻ cotransporter in the thick ascending limb of the loop of Henle, reducing sodium, chloride, and water reabsorption. This leads to increased urine output and decreased fluid volume, helping to lower blood pressure and reduce edema.

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94
Q

What are some unwanted effects of loop diuretics?

A
  • renal impairment
  • electrolyte disturbances (Na+, K+, Ca++, Mg++)
  • may exacerbate diabetes
  • may lead to gout
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95
Q

What must be monitored when taking loop diuretics?

A

Monitor U&E baseline and within 1 month after starting

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96
Q

What do alpha blockers do?

A

Vasodilatation of vascular smooth muscle

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97
Q

Why must there be care with dosing of alpha blockers?

A

It can cause postural hypotension

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98
Q

What is the usual choice of alpha blockers?

A

Doxazosin

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99
Q

Apart from hypertension, what else can alpha blockers be used for?

A

Benign prostatic hypertrophy (BPH) - there are alpha receptors in the prostate and urethra

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100
Q

Give examples of beta blockers

A

Atenolol, bisoprolol and metoprolol

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101
Q

Are any beta-blockers cardio-specific?

A

No but they may be CARDIO-SELECTIVE

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102
Q

How effective are beta-blockers?

A

Not as effective at reducing stroke, MI and mortality (HTN patients) compared to other drugs

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103
Q

What cautions do you need to keep in mind regarding beta-blockers?

A

Caution in lung disease and diabetes
Contraindications with severe asthma

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104
Q

What are some of the side effects of beta-blockers?

A
  • bronchospasm + potential bronchoconstriction
  • vasoconstriction via blockage of B2-R
  • increase blood lipids
  • nightmares (lipid soluble)
  • fatigue
  • cold extremities
  • impotence
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105
Q

Why does beta blockers have contraindications with severe asthma?

A

Beta blockers are contraindicated in severe asthma because they block beta-2 adrenergic receptors in the lungs, which are responsible for bronchodilation. By inhibiting these receptors, beta blockers can cause bronchoconstriction, worsening asthma symptoms and potentially leading to severe respiratory distress.

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106
Q

What other methods would specialists use/special situations to treat hypertension?

A
  • vasodilators
  • centrally acting vasodilators
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107
Q

What do centrally acting vasodilators do?

A

They work directly on the part of the brain that controls blood pressure and are also known as CENTRAL ALPHA ANTAGONISTS

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108
Q

Give examples of vasodilators and centrally acting vasodilators

A

Vasodilators: hydralazine & minoxidil
Centrally acting vasodilators: moxonidine & clonidine

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109
Q

What should you consider with hypertension in pregnancy?

A

Need to use medicines with safety

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110
Q

Give examples of medication you can prescribe in pregnancy with hypertension

A
  • labetalol
  • methyldopa
  • nifedipine
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111
Q

What hypertensive medication should be avoided in pregnancy?

A

Avoid ACEi/ARB in pregnancy

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112
Q

Are NICE targets or order of medicines always appropriate?

A

No - adapt your management plan to the patient

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113
Q

For what types of patients may you have to adapt their management plan for hypertension?

A
  • elderly (limited evidence age >80)
  • frailty
  • postural hypotension
  • renal disease
  • other cardiac conditions
  • one medicine for two indications
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114
Q

What would you potential have to adapt in management plan of hypertension for patients who are frail?

A

May need to relax targets

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115
Q

What does postural hypotension increase the risk of?

A
  • risk of falls
  • dementia
  • stroke
  • all-cause mortality
  • significant impact on activities of daily living
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116
Q

What is postural hypotension?

A

When you measure blood pressure lying/sitting vs standing, there is a sustained drop (SBP >20 mmHg and/or DBP >10 mmHg) within 3 minutes

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117
Q

What part of the management plan for hypertension would be changed for a patient with renal disease?

A
  • blood pressure targets may be lower
  • choice of medication for CKD rather than following ‘NICE’ order
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118
Q

What would you need to consider in the management plan of hypertension for people with cardiac conditions?

A

If medicines have prognostic benefit e.g. heart failure, secondary prevention of CVD

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119
Q

Give an example of when one medicine having two indications need to be considered

A

Beta-blockers in the rate control in atrial fibrillation with lower the blood pressure

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120
Q

What is the formula for blood pressure?

A

BP = CO x TPR

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121
Q

What is the formula for cardiac output?

A

Cardiac output = stroke volume x heart rate

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122
Q

What is stroke volume regulated by?

A

The ventricles

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123
Q

What regulates heart rate?

A

The SA node

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124
Q

What is Starling’s Law?

A

The stroke volume of the left ventricle will increase as the left ventricular volume increases due to the myocyte stretch. This links with the force of contraction.

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125
Q

Describe the RAAS system

A

Low BP Trigger: Kidneys release renin.
Renin Action: Converts angiotensinogen (from liver) to angiotensin I.
ACE Enzyme: Converts angiotensin I to angiotensin II (in lungs).
• Aldosterone: Increases sodium/water retention in kidneys (raises blood volume/BP).
• ADH Release: Promotes more water reabsorption in kidneys.
• RAAS Blockers: ACE inhibitors/ARBs reduce BP.

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126
Q

Describe the RAAS system

A

Low BP Trigger: Kidneys release renin.
Renin Action: Converts angiotensinogen (from liver) to angiotensin I.
ACE Enzyme: Converts angiotensin I to angiotensin II (in lungs).
Aldosterone: Increases sodium/water retention in kidneys (raises blood volume/BP).
ADH Release: Promotes more water reabsorption in kidneys.
RAAS Blockers: ACE inhibitors/ARBs reduce BP.

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127
Q

What is the effect of angiotensin II?

A

Angiotensin II Effects: Vasoconstriction (raises BP) & Stimulates aldosterone release (from adrenal glands).

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128
Q

How is the total peripheral resistance regulated?

A

Increases in Ang II —> increase in IP3 —> increases intracellular [Ca2+]
This causes constriction of arterioles and and increase in total peripheral resistance

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129
Q

How is preload regulated?

A

Constriction of venues via AT1-R
RAAS also facilitates Na+ and H2O retention

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130
Q

What is the role of aldosterone?

A
  • activates cytoplasmic receptors
  • these receptors bind to the nucleus
  • increase expression of Na+ channels
  • H2O and Na+ retention is aided by
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131
Q

What is the treatment of hypertension dependent on?

A
  • age
  • ethnicity
  • co -existing diseases
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132
Q

What are the main classes of anti-hypertensives?

A
  • ACE inhibitors, Angiotensin receptor blockers, renin antagonists
  • calcium channel blockers
  • diuretics (no longer frontline)
  • beta blockers (no longer frontline)
  • vasodialators
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133
Q

What would be the first line choice of antihypertensive for a patient with type 2 diabetes?

A

ACEi or ARBs

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134
Q

What would be the first line choice of antihypertensives for a patient under 55 and not of black family origin?

A

ACEi or ARBs

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135
Q

What would be the first line choice of antihypertensives for a patient age 55 and over?

A

Calcium channel blockers

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136
Q

What would be the first line choice for a patient who is black-African or Afro-Caribbean?

A

Calcium channel blockers

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137
Q

What happens when a patient takes their first dose of ACEi?

A

Hypotension

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138
Q

Who would ACEi not be as effective for?

A

Black African/Caribbean patients

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139
Q

What are ACEi contraindicated in?

A

Bilateral renal artery stenosis

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140
Q

Why are ACEi frontline treatments for diabetic patients?

A

No adverse effects on serum glucose/lipids

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141
Q

What do angiotensin receptor blockers do?

A

Block the actions of Ang II on AT1-R
(-ARTAN)

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142
Q

Give an example of an aldosterone antagonist

A

Spironolactone - used to treat hypertensive patients with primary aldosteronism

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143
Q

What is the mechanism of spironolactone?

A
  • inhibits the ability of aldosterone to produce new Na+ channels
  • loss of Na+ and H2O
  • decreased preload and reduced blood pressure
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144
Q

What do the main classes of dihydropyridine target? (-DIPINE)

A

Targets L-type Ca2+ channels on smooth muscle of blood vessels

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145
Q

What do non-dihydropyridine such as phenylalkylamines and benzothiazepines target?

A

Target L-type channels in the heart and decrease the frequency and force of contraction
- less used to treat hypertension

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146
Q

What are some side effects of CCBs?

A
  • flushing and headaches
  • peripheral oedema
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147
Q

What is the interaction between grapefruit juice and CCBs?

A

Grapefruit juice enhances action (CYP3A4)
-furanicomarins

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148
Q

Combinations of what is not recommended in regards to CCBs?

A

Combinations of Ca2+ channel antagonists are not recommended

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149
Q

What is peripheral oedema?

A

Impairment of the function of the pre-capillary sphincter increases hydrostatic pressure across the capillary and reduces fluid reabsorption

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150
Q

When would furosemide be used?

A

ONLY in resistant hypertension

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151
Q

What is the mode of action of thiazide-like diuretics?

A

• Inhibit the sodium-chloride symporter (NCC) in the distal convoluted tubule
• Decrease reabsorption of sodium and chloride
• Increase excretion of sodium, chloride, and water
• Reduce blood volume and lower blood pressure
• Mild vasodilatory effect contributes to antihypertensive properties

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152
Q

What is the mode of action of beta-blockers?

A

• Block beta-adrenergic receptors (mainly β1 and β2)
• Reduce the effects of adrenaline and noradrenaline
• Decrease heart rate (negative chronotropic effect)
• Reduce the force of heart contractions (negative inotropic effect)
• Lower blood pressure by reducing cardiac output and renin release from kidneys

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153
Q

Describe the link between beta-blockers and hypoglycemia

A
  • blood glucose is low it activates the release of adrenaline, mobilizes glucose release from the liver
  • beta blockers block this process
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154
Q

What are some symptoms of hypoglycemia?

A
  • tremor
  • palpitations
  • sweats
  • feeling tired or weak
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155
Q

“Combining X with beta blockers should be used with caution for diabetic patients.”
What is X?

A

Thiazides

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156
Q

Give an example of a non selective (B1 & B2) beta blocker

A

PropranOLOL - you wouldn’t give this to a patient with serious asthma as it is associated with asthma attacks

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157
Q

Give an example of a selective B1 antagonist

A

AtenOLOL

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158
Q

What are A1 antagonists?

A

Vasodilators

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159
Q

What are vasodilators?

A
  • Used to treat hypertension in patients with benign prostatic hypertrophy
  • Other vasodilators open K+ channels
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160
Q

Give an example of a vasodilator used to treat hypertension in patients with benign prostatic hypertrophy

A

doxAZOSIN

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161
Q

Give an example of a vasodilator used to open K+ channels.

A

minoxidil

162
Q

What is the mechanism of action of amlodipine in the treatment of hypertension?

A

CALCIUM CHANNEL BLOCKERS
- Inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle cells.
- Causes vasodilation by relaxing smooth muscle in the arterial walls.
- Lowers peripheral vascular resistance, leading to reduced blood pressure.
- Has minimal effects on heart rate or cardiac contractility at therapeutic doses.
- Primarily acts on the peripheral vasculature, making it effective for long-term blood pressure control.

163
Q

Spironolactone being prescribed depends on what?

A

Potassium levels

164
Q

What is a particle?

A

Any unit of matter having defined physical dimensions, not a molecule

165
Q

Solids are not what?

A

Static systems

166
Q

What can alter the physical state of particles?

A

Physical manipulation

167
Q

What is the lifetime of a drug?

A
  1. Drug synthesis
  2. Development of formulated medicine
  3. Production of formulated medicine flow and packing properties
  4. Administration of medicines
  5. Drug in body
  6. Drug removed from body
168
Q

What implications does particle size have for tableting and capsule filling?

A

Particle size can affect flow properties of a powder and its packaging properties which has implications since machinery relies on a set volume entering the die at a given time. This is to avoid filling problems

169
Q

What 10 things can particles affect?

A
  1. Rate of chemical reaction
  2. Dissolution rate
  3. Bioavailability (via dissolution rate)
  4. Packing density
  5. Flow characteristics
  6. Suspendabilty
  7. Texture
  8. Deposition site in lung
  9. Colour
  10. Taste
170
Q

What effect does surface area have on the rate of reaction?

A
  • reactions with solids take place on the surface of the solid
  • when the solid is split into several pieces, the SA increases which increases the area for the reactant particles to collide with
  • therefore are more collisions and a higher chance of reaction
171
Q

Particle size can affect the rate of a chemical reaction which in turn affects what?

A

The stability of a drug

172
Q

What is dissolution rate?

A

The speed/rate at which a drug substance can dissolve in a medium

173
Q

Micronisation of solid particle
can increase its dissolution
rate – why?

A

when particle size is reduced, the total effective surface area is increased and thereby dissolution rate is enhanced.

174
Q

What can happen with excessive particle reduction?

A

This can cause particle to re-aggregate into larger molecules

175
Q

How can you prevent re-aggregation of particles that have been reduced excessively in size?

A

They can be dispersed in polyethylene glycol (PEG), polyvinylpyrrolidine (PVP) dextrose or other agents

176
Q

What two types of uniformity of distribution can particle size effect?

A
  • drug in powder mixture
  • drum of drug or excipient in warehouse
177
Q

Flow characteristic can affect what?

A

content uniformity when the tablet die is filled by volume

178
Q

What does suspendability affect?

A

The dispersion of the API in a liquid vehicle where they remain undissolved but evenly distributed

179
Q

Does dissolution rate affect the solubility of solid particles?

A

No, because solubility is a concentration not a rate so would not be effected

180
Q

What are two types of equivalent sphere diameters?

A
  • projected area diameter (da)
  • perimeter diameter (dp)
181
Q

What are equivalent sphere diameters used for?

A

To describe irregular particles

182
Q

The method used to measure particle size determines what?

A

The type of equivalent sphere diameters measured

183
Q

What does sieving measure?

A

Measures sieve diameter, dA
Generally used for dr powders

184
Q

What does mono size mean?

A

All particles are the same size

185
Q

What are the different distributions shown on a histogram when showing the range of particle sizes?

A
  • Normal distribution
  • Bimodal distribution
  • Positively/negatively skewed
186
Q

Describe normal distribution on a histogram for particle sizes

A

Can be normally distributed about a central value where the MODE (peak frequency value) separates the curve into 2 equal halves.

187
Q

Give examples of techniques used for particle sizing

A
  • sieving
  • microscopy
  • sedimentation rate
  • electrical sensing zone method
  • laser diffraction
  • photon correlation spectroscopy
  • cascade impaction
188
Q

The choice of particle sizing depends on what? (5)

A
  1. Size range of the particles to be measured
  2. Wet or dry methods
  3. Manual or automated methods
  4. Cost of analysis
  5. Speed of analysis
189
Q

What does the range of analysis for microscopy measure?

A

Measures projected area diameter (da), perimeter diameter (dp), Feret’s diameter (dF) and Martin’s diameter (dM)

190
Q

Why is it important that the particles in a powder mixture are the same size?

A

It would affect dosage

191
Q

What are powders?

A

Solid particles of the same or different chemical composition

192
Q

Why are powders so important?

A

Virtually all pharmaceutical preparations involve handling of powder ingredients at some stage e.g. tablets, hard capsules, solutions/suspensions and creams

193
Q

Why is it important that powders have good flow properties?

A

So they can be packaged quickly and the dosage is uniformed
Free flowing order —> same volume
It also affects the mechanical strength of the tablets and encourages good content and weight uniformity

194
Q

What is the importance of characterization in regard to powder flow?

A

It enables batter prediction for flow which is important for powder handling, equipment design & predicting formulation behaviour early on in the formulation process

195
Q

How can flow behaviour be modified?

A

It can be made to flow better by adding excipients (e.g. glidant) or changing the size/shape of the powder particles

196
Q

What are the forces acting in powder flow with examples?

A

DRIVING FORCES; gravity, mechanical forces etc.
DRAG FORCES: cohesion, adhesion, friction, surface tension

197
Q

What is cohesion vs adhesion?

A

Cohesion is when the particles stick to each other which adhesion is the particles sticking to a surface

198
Q

List some factors affecting powder flow?

A
  1. Particle size
  2. Particle shape
  3. Particle density
  4. Packaging geometry
  5. Moisture content
  6. Electrostatic forces
199
Q

How does particle size affect particle flow?

A

The larger the particle, the better the flow as they have a SMALLER surface area, therefore lower cohesion/adhesion forced and gravity has a greater influence leading to better flow

200
Q

How does particle shape affect flow?

A

Spherical particles have a better flow as they have smallest SA to volume ratio, less adhesion/cohesion and less friction.
Irregular shaped particles have larger SA, greater cohesion/adhesion, mechanical locking which lead to poor flow

201
Q

How does particular density lead to better flow?

A

Denser particles lead to better flow as they are generally less cohesive than particles of lower density. More gravity acts on them as a driving force for powder flow.

202
Q

What’s the equation for particle density?

A

Particle density (p) = particle mass (m)/particle volume (v)

203
Q

What is packing geometry affected by?

A
  • particle size and size distribution
  • particle shape and texture
    More tightly packed powders require a higher diving force to produce powder flow
204
Q

How does packing geometry effect flow?

A

Looser packing leads to better flow
Particles closer together, greater cohesion/adhesion (van der Waals)

205
Q

Define packing

A

Position of particles relative to each other in a defined volume

206
Q

What is true density (p)?

A
  • characteristic of individual particles
  • mass per unit volume (g/cm3)
  • intrinsic property of the material
207
Q

What is bulk density?

A
  • characteristic of the powder as a whole
  • linked to porosity
  • mass of powder/ bulk (fluff) volume (kg/m3 or g/cm3)
  • The higher the porosity (spaces between particles the lower the bulk density)
208
Q

What impact does moisture content & electrostatic forces on flow?

A

high moisture & electrostatic forces lead to poor flow as it makes the powder particles more cohesive

209
Q

How can we measure powder flow if it is good or bad?

A
  1. Angle of repose
  2. Bulk density (packing geometry)
    - Carr’s index (of compressibility)
    - Hausner ration
  3. Shear strength
  4. Flow rate through orifice
210
Q

What is the equation for the angle of repose (AOR)?

A

a = Tan -1 (h/r)

h = height
r = radius
a = AOR

211
Q

Describe the link between AOR and co(ad)hesion

A

MORE CO(AD)HESION: stacks up, steeper slope, larger AOR and poor flow

LESS CO(AD)HESION: slides down slope, less steep slope, smaller AOR and better flow

212
Q

What can you use to measure AOR?

A
  • static AOR
  • drained AOR
  • dynamic AOR
    Different methods and handling may produce different values for the same powder
213
Q

What is the equation for bulk density?

A

Bulk density = mass of bulk powder (MB)/volume occupied by the bulk powder (VB)

214
Q

Why is bulk density < true density?

A

This is because bulk density = k x true value where k is the packing fraction and is the void space as particles cannot fill the volume 100%. As k is variable so is bulk density

215
Q

What does bulk density measure?

A

Measures how readily/to what extent a powder consolidates as consolidated powders flow poorly

216
Q

What would you use to quantify bulk density?

A
  1. Hausner ratio
  2. Carr’s index (of compressibility)
217
Q

Why can Hausner ratio only be bigger than one?

A

As fluff volume can never be smaller than tapped a when tapped the volume decreases.
You want the value to be as close as possible to 1

218
Q

“The higher the Hausner ratio, the ____ the flow.”

A

Poorer

219
Q

What is the equation for Hausner ratio?

A

Tapped bulk density/ fluff bulk density
OR
Fluff bulk volume/tapped bulk volume

220
Q

“The ____ the Carr’s index, the ____ the flow

A

Higher & Poorer

221
Q

“The ____ the Carr’s index, the ____ the flow

A

Higher & Poorer

222
Q

What is the equation for Carr’s index?

A

100 (VF - VT)/VF

VT = tapped volume
VF = fluff volume

223
Q

In regards to shear strength, what is shear cell?

A

Measures shear strength of powder bed —> powder cohesion/adhesion

224
Q

What is the general rule of shear strength?

A

Greater shear strength —> more cohesive —> poorer flow

225
Q

What is flow rate through orifice?

A

It’s the amount (mass/volume) of powder discharged through an orifice from a hopper, per unit time

226
Q

For flow rate through an orifice, what is the general rule?

A

The higher the flow rate the better the flow

227
Q

Flow rate through orifice is influenced by what?

A
  • orifice diameter
  • hopper wall angle
  • hopper width
  • height of powder head
228
Q

How can we improve powder flow?

A
  1. Use larger particles (granulation or remove fine particles)
  2. Use more spherical particles (spray drying)
  3. Avoid/remove electrostatic charges (earthing)
  4. Remove excess moisture )drying)
  5. Add a glidant (colloidal SiO2 to the powder mixture
229
Q

How can we improve powder flow?

A
  1. Use larger particles (granulation or remove fine particles)
  2. Use more spherical particles (spray drying)
  3. Avoid/remove electrostatic charges (earthing)
  4. Remove excess moisture )drying)
  5. Add a glidant (colloidal SiO2 to the powder mixture
230
Q

How do glidants wok?

A

They work by reducing friction or cohesion between particles or by making the powder particles more spherical. However, there is a certain range of conc and once above this, they will inhibit powder flow

231
Q

What is a capsule?

A

Solid dosage form, shells obtaining active ingredient

232
Q

What are capsules used for?

A

Mostly for oral administration but may be formulated for other routes such as inhalation, rectal or vaginal

233
Q

What are the two main types of capsules?

A

Hard & soft (softgels)

234
Q

Describe the shell material of hard capsules

A
  • 2 piece hard shell
  • contains gelatin, water, opacifier, plasticiser and surfactant
235
Q

What are the basic features of a hard capsule?

A

Cap and body
The body is smaller in diameter, longer and inserts into the cap

236
Q

What are some advanced features of hard capsules?
*look back at lecture for their benefits

A
  1. Tapered trim
  2. Notches/dimples
  3. Circle grooves
  4. Air vent
237
Q

How are hard capsules made?

A
  1. Dip metal pins in gelatin solution
  2. Dry to form capsule halves
  3. Remove from metal pins
  4. Trim to desired size
  5. Assemble for transit
238
Q

What is gelatin?

A

Hydrolysed collagen derived from connective tissue such as skin, bone and ligaments

239
Q

What are the two types of gelatin?

A

A Acid-hydrolysed
B Alkali-hydrolysed

240
Q

What are some alternatives to gelatin?

A

HPMC or PVA

hydroxypropyl methylcellulose or Polyvinyl alcohol

241
Q

Give examples of fill material

A
  • powder
  • granules
  • pellets
  • liquid
  • tablets
  • capsule
  • there are filling combinations
242
Q

What are the requirements for the filling material for capsules?

A
  • homogeneity
  • physicochemical properties
  • capsule size
  • flow properies
243
Q

What are the two types of dosing systems?

A

Dependent and Independent

244
Q

What is dependent dosing systems?

A

The capsule body volume is used for accurate filling

245
Q

What is independent dosing systems?

A

It’s when the fill material is weighed independently of the capsule body volume

246
Q

What are two examples of independent dosing systems?

A
  1. Dosator - measures the exact mass of powder using a dosing tube in a dosing chamber
  2. Tamping fingers - force plugs (compacted powder) through holes in dosing disc
247
Q

What are the advantages of hard capsules?

A
  • versatility
  • product stability
  • product efficiency
  • clinical trial blinding
  • user acceptance/adherence
248
Q

Give examples of types of soft gels

A
  • orally administered
  • chewable
  • suckable
  • twist-off
  • meltable
249
Q

Describe the shell material of soft gel capsules

A

Continuous one piece of gelatin
Usually ovoid or oblong

250
Q

How is dry cough produced by ACEi?

A

Ace enzyme converts Ang I —> Ang II and breaks down bradykinin to inactive peptide

ACEi reduce production of Ang II which reduces the conversion of bradykinin to inactive peptide —> this reduces irritation which reduces production of dry cough

251
Q

How is total peripheral resistance regulated?

A

Increase in Ang II -> bins to AT 1 receptors which is coupled with G protein —> increases IP3 —> increases intracellular Ca —> calcium binds with calmodulin —> actives actin and myosin —> cross bridges made leading to contraction of smooth muscle of arterioles —> increase in TPR —> increase in BP

252
Q

What are the fill materials of soft capsules?

A
  • drug in lipophilic solution/suspensions
  • drug in hydrophilic solution/suspensions
  • self-emulsifying systems
  • lipolysis systems
253
Q

What is a self-emulsifying system?

A

Concentrates of drug-oil-surfactant form micro/nano sized droplets instantaneously in contact with GI fluid

254
Q

What are lipolysis systems?

A

Lipid bases matrix susceptible to lipolysis in the GI tract which results in enhanced drug dissolution in lipolysis products facilitates absorption.

255
Q

What requirements must the fill matrix meet?

A
  • dissolves/suspends drug
  • disperses drug following softgel rupture in GI tract
  • it retains drug in solution in the GI tract
  • it’s compatible with softgel shell
  • enhances drug absorption characteristics
256
Q

What are some advantages of soft capsules?

A
  • improved drug absorption
  • user preference/adherence
  • enhanced safety in manufacture or handling
    -provided ideal formulations of oily drug
  • dose uniformity
  • dose stability
257
Q

What are the quality parameters when producing softgel capsules?

A

Impurities in gel (e.g. aldehydes)
Gel ribbon thickness
Shell seal thickness
Fill matrix weight
Shell weight
Shell moisture content
Shell hardness

258
Q

What are the in-process control parameters when producing soft gelatin capsules?

A
  1. Gelatin viscosity and thickness
    1. Temperature
    2. Capsule sealing
    3. Filling accuracy
    4. Rotary die speed
    5. Drying conditions
    6. Moisture content
259
Q

What is a tablet?

A

A solid dosage form containing a single dose of one or more API and suitable formulations aids (excipients)

260
Q

How are tablets manufactured?

A

Usually by compression
Other techniques: extrusion, moulding, lyophilization and 3D printing

261
Q

What are tablets usually used for?

A

Usually used for oral administration of drugs for systemic delivery by some are used for oral action

262
Q

What are the components of a tablet?

A

Active pharmaceutical ingredient & excipients (binder, glindant, lubricant, filler)

263
Q

What are excipients?

A

Inert substances used as formulation aids

264
Q

What percentage of API would be considered a high dose and a low dose?

A

Low dose: <5% of tablet weight
High dose: >50% of tablet weight

265
Q

What is the function of tablet excipients?

A

Aids the production of tablets with required quality specifications such as:
- content uniformity
- stability of API and finished product
- enhancement an control of bioavailability
- smooth operation of the tableting procedure

266
Q

What properties should tablet excipients have?

A
  • non-toxic
  • inactive (chemically and physiologically)
  • cost effective
  • required physiochemical properties
  • correct standard/quality
267
Q

What is bulking agent used for?

A

Used to increase bulk volume of powder when handling small quantities of API.
This helps increase tablet size to make it suitable for processing and manufacturing

268
Q

Binding of the drug to the filler may affect ___

A

Bioavailability

269
Q

Give examples of filler or dilutent

A
  • lactose (not suitable for lactose intolerant people)
  • sucrose, glucose, mannitol
  • cellulose
  • inorganic
270
Q

What is binder used for in making tablets?

A

For production of granules and tablets of required mechanical strength and is added to drug-filler powder mix before granulation

271
Q

What does binder improve when making tablets?

A

Improved flow properties by formation of granules and ensure tablet integrity after compression

272
Q

What is the typical conc. of binder and what would happen if you went over or below?

A

Typical conc. 2-10% w/w
Insufficient binder conc. - production of weak tablets
Excessive amounts - tablets may be too strongly bound

273
Q

If a tablet is too strongly bound what effect would this have?

A
  • negatively impact dissolution and drug release from the tablet
274
Q

For binders, what are the two modes of addition?

A

As a dry powder or as a solution

275
Q

What is glidant used for?

A

Used to increase flow ability of powder mixture and is added to granules before tableting to ensure optimum flow ability for high-speed production runs

276
Q

What does glidant improve and how?

A

Improves powder flow by reducing friction between particles, cohesion and surface charge

277
Q

What is the role of lubricant? (3)

A
  • help reduce friction between the tablet surface and the die wall
  • ensures smooth formation and ejection of the tablets and reduces wear on tablet machine’s punches and dies
  • prevents capping, fragmentation or scratches which can effect the quality of the tablet or halt production
278
Q

Are lubricants hydrophobic or hydrophilic in nature?

A

Hydrophobic

279
Q

What would happen if lubricants when making tablets were in high concentrations?

A

They would slow down tablet disintegration and dissolution

280
Q

What is the function of antiadherent?

A

Reduces adhesion between powder and punch surface, preventing sticking or picking

281
Q

What is picking?

A

When there is a build up of thin powder layer on punches which results in uneven and matte surfaces with unclear symbols and markings

282
Q

What is the function of flavour in making tablets?

A

Used to improve or mask unpleasant taste

283
Q

When making tablets, why must flavour be added before processes that involve heat?

A

They are frequently THERMOLABILE - sensitive to heat

284
Q

What is the function of colourant?

A

Improves tablet appearance
Helps with identification and adherence

285
Q

What does disintergrant do in tableting?

A

Facilitates break up (deaggregation) of tablet compact into smaller components when in contact with liquid

286
Q

Why is deaggregation of tablets important?

A

It increases the exposed surface area to GI fluids which enables faster drug release and dissolution

287
Q

What are the modes of action of disintergrants?

A
  • facilitates water uptake which leads to deaggregation —> tablet rupture occurs which is the mechanical consequence of water uptake
  • production of gas - releases gas in contact with water e.g. effervescent tablets
288
Q

What are two types of releases of tablets?

A

Immediate release and modified release

289
Q

Give examples of immediate release tablets?

A

Disintegrating
Chewable
Effervescent
Sublingual
Buccal

290
Q

Give examples of modified release tablets

A

Prolonged release
Pulsatile release
Delayed release

291
Q

Why is sublingual or buccal administration beneficial for drugs with high first-pass metabolism?

A

It’s good for drugs with high first pass metabolism so you can bypass it by making it enter the bloodstream within the vessels in the mouth

292
Q

Why would excipients in specialised tablets be different?

A

Because it would be absorbed differently
You would need to consider how quickly we would need the API and how long you would like the effect

293
Q

What are the advantages of tablets?

A
  • oral delivery with is safe and convenient
  • stability
  • dosage form containing accurate doses of drug can be reproduced
  • mass produced at a low cost
  • versatility and convenience
294
Q

What are the disadvantages of tablets?

A
  • compression difficulties due to powder physical properties
  • poor/variable bioavailability
  • unsuitable for some patients
295
Q

When manufacturing tablets what qualities must powders have?

A
  • COMPRESSIBLE - when subjected with force from the punches, the particles must cohere to form a compact
  • able to MAINTAIN THE COMPACT - must remain as a tablet without breaking up when removing the punch
296
Q

What is the manufacturing process?

A

Weighing —> mixing —> granulation —> tableting —> coating —> quality control (uniformity of mass —> dissolution)

297
Q

How are tablets formed through compression?

A

Pressure is applied to a powder for force particles close together by confined compression to cohere to form a solid compact of define geometry

298
Q

What are some tablet machines?

A
  • single punch
  • rotary press
299
Q

What are the two ways of preparing a powder for compression?

A
  • granulation
  • direct compression
300
Q

What is the method of wet granulation when preparing powders for compression?

A

Adding solvent and binder to powder, mix, dry and break up through screen to produce particle aggregates

301
Q

What is the tableting journey?

A

Mixing powders —> (granulation if needed) —> compression —> coating —> packing

302
Q

What is comminution?

A

The process of converting solid particles from an initial (larger) size into a smaller size or size range and requires the application of mechanical force

303
Q

Why is comminution important?

A
  • tablet production uses solid particulate drugs and excipients and the raw materials often have larger particles than requires
  • particle size has an effect on: material handling, manufacturing efficiency and biopharmaceutical properties
304
Q

What is the effect of comminution?

A
  • increases specific surface area
  • improves content uniformity in tablets
  • increases bulk density
305
Q

What is the result of improving content uniformity in tablets?

A
  • easier to distribute particles across entire volume when more subdivisions available
  • more even (uniform) distribution of particles within tablet
306
Q

For a given mass, the smaller the particle size leads to…

A

… more subdivisions and the larger the specific surface area will be

307
Q

In what two ways will particles within a batch vary in size and what would effect them?

A
  • central diameter (e.g. mean, mode, median)
  • distribution (e.g. standard deviation, range)

BOTH affected by comminution

308
Q

Comminution starts with _____ _______ and initiates _____ _______ explained by ______ _______ of brittle fractures

A
  1. Crack propagation
  2. Particle fracture
  3. Griffith’s theory
309
Q

What would different particles of offered sizes exhibit?

A
  • different fracture behaviours and is susceptible to various extents to the effect of a comminution method
310
Q

What does Griffith’s theory describe?

A

describes the mechanism of brittle fractures

  • material have microscopic flaws
  • energy applied during comminution concentrated at tip of crack
  • energy at crack tip overcomes bond strength
  • bond rupture cascades along region with most flaws to dissipates energy
  • almost instantaneous brittle fracture
311
Q

What are some of the various equipment and techniques of comminution?

A
  • cutting
  • compression
  • impact
  • attrition
312
Q

What should you consider when hosing a method of comminution?

A
  • target particle size
  • material properties
  • cost (smaller target size is generally more costly)
313
Q

What is toughness is regard to material properties for comminution?

A

Ability to absorb energy by deforming
- tough (non-brittle) materials are difficult to comminute

314
Q

What is surface hardness in regard to material properties for comminution?

A

Ability to resist permanent deformation
- hard materials are difficult to comminute, may damage equipment parts

315
Q

What is mixing?

A

Combining particles of different ingredients which are initially separated or partially much such that each particle of one ingredient will be positioned as close as possible to a particle of each of the other ingredients.

316
Q

What are the four degrees of mixing?

A
  1. complete segregation
  2. Partial mix
  3. Ideal or perfect mix
  4. Random mix
317
Q

Why do we need uniformity when mixing?

A

To avoid issue with therapeutic effects and safety/toxicity issues

318
Q

How would you minimise content variation when mixing and remain with acceptable limits?

A
  • increasing proportion of drug particles relative to excipients in mixture
  • increasing total number of particles in mixture (e.g. comminution)
  • using an efficient mixing procedure
319
Q

What is powder segregation?

A

Demixing - separation of components
Where random mix becomes a non-random mix or there is a failure to achieve. Random mix

320
Q

When would powder segregation occur?

A

Can occur due to handling due to the differences in particle properties

321
Q

What is the effect of powder segregation?

A

Quality of mix is reduced, content variation and unacceptable weight variations

322
Q

What is ordered mixing?

A

Adsorption of small (micronised) powder particles on larger particles

323
Q

What are the effects of ordered mixing?

A

It minimises segregation and ensure good flow properties
Likely to occur in every powder mix

324
Q

Describe pharmaceutical powder mixes

A

Partly random and ordered

325
Q

Why is ordered mixing better than random mixing?

A
  • beneficial for potent drugs
  • direct compression tablets - prevents segregation
326
Q

Give examples of when ordered mixing is used

A
  1. Dry antibiotic (fine powder) formulation for reconstitution in water is adsorbed on the surface of sucrose or sorbitol (larger molecules)
  2. Dry inhalation powder (micronised) adsorbed on larger carrier particles e.g. lactose
327
Q

What are some examples of powder mixing?

A
  • tumbling mixers
  • agitator mixers
  • fluidized bed mixers
  • high speed mixer-granulators
328
Q

What are the advantages of the direct compression method?

A
  • no granulation process needed
  • thus cheaper and preferred by manufactures
329
Q

What factors would you need to consider when directly compressing tablets?

A
  • % 250mg tablet
  • content uniformity
  • flow
  • compaction
330
Q

What are granules?

A

Aggregates of powder particles with a particle size of 200um - 4mm

331
Q

What are the uses of granules?

A
  • standalone dosage form
  • intermediate product in tablet/capsule manufacture
332
Q

Why do we granulate?

A
  1. Prevent segregation
  2. Improve flow properties
  3. Improve compaction characteristics
  4. Reduce fines (toxic drugs)
333
Q

What are the types of granulation methods?

A
  1. Wet granulation
  2. Dry granulation
  3. Melt granulation
334
Q

What is wet granulation & the process?

A

Wet messaging using granulation fluid
1. Spraying with granulating fluid which is usually a volatile solvent with binder which evaporated as granules dry, leaving behind the binder holding them together
2. Agglomeration - particles collide and stick together
3. Finished granulate

335
Q

What are the methods of wet granulation on a larger scale?

A
  1. Low shear method
  2. High shear method
  3. Fluidised bed method
336
Q

When would you use dry granulation?

A

When wet granulation is unsuitable for moisture/heat-sensitive materials e.g aspirin

337
Q

What should you avoid in melt granulation?

A

Avoid use of water or organic solvents

338
Q

The particle bonds for granulation must be what?

A

They must be strong enough to prevent granules from breaking down into powder during subsequent processes

339
Q

The particle bonds for granulation must be what?

A

They must be strong enough to prevent granules from breaking down into powder during subsequent processes

340
Q

What are the five primary bonding mechanisms for granulation?

A
  1. Adhesion and cohesion in immobile films
  2. Interfacial forces in mobile liquid films
  3. Formation of solid bridges
  4. Attractive forces between solid particles
  5. Mechanical interlocking
341
Q

How does adhesion/cohesion in immobile films result in granulation?

A

Adsorbed material e.g. moisture results in:
1. greater particle diameter, SA
2. Thus reduced inter-particulate distance
3. Resulting in greater van der Waals forces

342
Q

What do interfacial forces in mobile liquid films give rise to?

A

Various states of inter-particulate water distribution

343
Q

What are the states of inter-particulate water distribution from weakest interfacial forces to strongest?

A

Pendular state —> Funicular state —> capillary state

344
Q

The stronger the interfacial forces, the ____ the granules

A

Stronger

345
Q

Solid bridges can arise from what?

A
  • hardening of binder
  • crystallisation of dissolved substances following drying
  • partial melting und pressure + solidification - dry granulation
346
Q

What are the attractive forces between solid particles?

A
  • van der Waals forces
  • electrostatic forces
347
Q

In mixing, van der Waals forces increases as what decreases?

A

Inter-particulate distance decreases e.g. applying pressure

348
Q

What does electrostatic forces contribute to?

A

May contribute to initial agglomeration e.g. during mixing

349
Q

How is drying powders and granules done?

A
  • with controlled heat
  • The energy input is to provide latent heat of vaporisation/sublimination with minimal temperature rise
350
Q

What do you need to be cautious of when drying powders and granules?

A

Caution taken to minimise thermal degradation and to not cause unwanted effects on the API

351
Q

What is FMC?

A

Free moisture content refers to unbound water which is readily removed by evaporation

352
Q

What is EMC?

A
  • Equilibrium moisture comtent refers to bound water which is difficult to remove by evaporation.
  • Adsorbed/absorbed water exists in equilibrium with moisture in ambient atmosphere
353
Q

What does EMC depend on?

A
  • temperature
  • relative humidity
  • nature of solid
354
Q

What is the equation for relative humidity?

A

RH (%) = p/ps x 100
p (Pa) = vapour pressure of water in air
ps (Pa) = Vapour pressure of water in air saturated with water vapour at same temperature (temperature-dependent)

355
Q

During drying, what could change temperature and moisture content (therefore RH)?

A
  • evaporated water from a drying solid
  • evaporative cooling of air via latent heat transfer to drying solid
356
Q

Once FMC is removed extended drying times will not remove ____ unless ____ is lowered

A
  1. EMC
  2. RH
357
Q

How can relative humidity be lowered?

A
  • air conditioning
  • desiccators
358
Q

Why do pharmaceutical solids work best with some residual moisture content?

A

Moisture prevents build up of statics in powders thus promoting flow

359
Q

What are some methods of drying wet solids - granules?

A
  • convective drying (gas)
  • conductive drying (e.g. vacuume ovens)
  • radiation drying
360
Q

What would you need to consider when selecting a drying method?

A
  • thermostability
  • physical properties
  • nature of liquid
  • scale of operation
  • need for asepsis/sterility
361
Q

What are the principles of efficient drying?

A
  • large SA for heat transfer
  • efficient heat transfer
  • efficient mass transfer
  • efficient vapour removal
362
Q

What solute migration?

A

Solute redistribution towards drying surface, following solvent movement (intergranular and intragranular)

363
Q

What are the two types if solvent movement between solid particles?

A

IINTRAgranular and INTERgranular

364
Q

What is solute migration affected by?

A
  • granule formulation
  • drying method
  • moisture content
365
Q

What is the effects of solute migration?

A
  • migration of drug plus attrition leads to variability in drug content, thus drug loss
  • migration of colouring leads to mottling
366
Q

What is the feature of ordered mix?

A

It prevents segregation

367
Q

Tablet compression is made up of what materials?

A
  • granules
  • primary powder particles (direct compression)
368
Q

What are the processes of tablet compression?

A
  • powder compression
  • powder compaction
369
Q

What is the process of tablet compaction?

A
  1. Filling
  2. Clearing excess powder
  3. Compression
  4. Ejection of tablet
370
Q

What are two important powder characteristics?

A

Compressibility & compactibility

371
Q

What is compressibility?

A

Propensity of powder to reduce in volume when subjected to pressure in a confined space

372
Q

What is compactability?

A

Propensity to form coherent tablet when compressed

373
Q

What is the mechanism of powder (granule) compression?

A
  1. Reposition
  2. Deformation
  3. Fragmentation
  4. Densification
  5. Attrition
  6. Deformation of primary particles in granules
374
Q

Briefly list the tablet compaction cycle

A
  1. Die filling
  2. Tablet formation
  3. Tablet ejection
375
Q

What excipients can be added to aid the compression process?

A
  • glidant
  • lubricant/anti-adherent
376
Q

What are the 5 bonding types in tablets according to Rumpf classification?

A
  1. Solid bridges
  2. Bonding by liquids
  3. Binder bridges
  4. Intermolecular and electrostatic forces
    5 mechanical interlocking
377
Q

Various dies and punches produce different tablet shapes, scoring, embossing etc. Why are these features important?

A

Helps with identification, and aid with accuracy in a pharmacy setting

378
Q

Powder compatibility determines what?

A
  • fracture tendency & mechanical strength of tablets (e.g. capping and lamination)
379
Q

What is capping and what are the reasons for it?

A

Top of tablet separates from body.

Reasons:
- air entrapment
- fines deposition along upper edge of tablet
- insufficient moisture/binder
- poor mixing

380
Q

What is lamination and what are the causes of it?

A

Splitting of tablet body, not limited to cap

Reasons:
- over compression
- poor powder cohesion

381
Q

What is the definition of tablet coating?

A

Process by which an essentially dry outer layer of material is applied to a tablet surface

382
Q

What are the uses of tablet coating?

A
  • enhance tablet strength
  • protect product (e.g. from light & moisture)
  • protect handles (e.g. from toxic drug)
  • modify drug release
  • improve patient acceptability (e.g. taste, appearance, ease of swallowing)
  • product identification
383
Q

What are the methods of application of the coating material for tablets?

A

Poured & sprayed

384
Q

What are the different types of coating?

A
  1. Film coating
  2. Sugar coating
  3. Compression coating
385
Q

Why might film coating be popular?

A
  • thin and is negligible in thickness and mass
386
Q

What are the main methods of coating?

A

Coating pan and fluidised bed coating

387
Q

What are the two types of film coating?

A
  1. Immediate release (non-functional) coating
  2. modified release (functional) coating
388
Q

What is the use of immediate release coating?

A

Used to modify appearance, taste or for identification

389
Q

What is the use of modified release coating?

A

Used to modify release of drug from tablet

390
Q

What is the difference between delayed release and extended release?

A

Delayed release medication is SELECTIVELY SOLUBLE at pH > 5-6 while extended release medication is relatively INSOLUBLE IN WATER and drug is usually released over 6-12 hours

391
Q

What are the types of film coating polymers?

A
  1. Immediate release (soluble in water, drug release quickly)
  2. Delayed release (water soluble at high pH but to low pH, drug is released in intestines)
  3. Extended release (relatively insoluble in water, drug released slowly)
392
Q

What are the 5 film coating characteristics and why are they important?

A
  1. Solubility - dictates bioavailability
  2. Viscosity - ideal for spaying if low
  3. Permeability - important for taste, drug stability and bioavailability
  4. Strength and flexibility - must not crack easily
  5. Adhesion - must not stick to tablet core and not peel of easily
393
Q

What are some film coating defects?

A
  1. Peeling
  2. Orange peel effect
  3. Mottling
  4. Bridging
  5. Core erosion
394
Q

What is peeling in reference to film coating defects?

A

When film fragments flake off coated surface possibly due to excess moisture in tablet

395
Q

What is bridging in reference to film coating defects?

A

Obscuring of indented markings

396
Q

What is core erosion in reference to film coating defects?

A

Disfiguration of core due to overexposure to film coating solution

397
Q

What is sugar coating?

A

Usually achieved by using a pan coating apparatus and creates a thick coat.

398
Q

What are the stages of sugar coating?

A
  1. Sealing
  2. Sub-coating
  3. Smoothing
  4. Colouring
  5. Polishing
  6. Printing
399
Q

Compare sugar coating to film coating

A

Sugar coating: round and polished in appearance, with a weighting increase of 30-50% with no embossed logo or breakline

Film coating: retains contour of core tablet and is less shiny in appearance, with a weighting increase of 2-3% with a possible embossed logo or breakline Film coating

400
Q

Describe compression coating

A

It is a novel drug delivery application when two drugs are used (one in core tablet , other in coating)
It is dry with no heat coat for liable drugs
Fast and slow release components in the formulation

401
Q

What is the process of compression coating?

A
  1. Primary compaction
  2. Transfer core tablet to larger die
  3. Fill die around core table
  4. secondary compaction

Y2 (6 decks)

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