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TPN, syringe drivers, Lab Results > Advanced Formulations > Flashcards

Advanced Formulations Flashcards

1
Q

Time for action IV

A

30-60 seconds

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2
Q

Time for action sublingual

A

3-5 minutes

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3
Q

IM

A

10-20 minutes

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4
Q

Rectal

A

5-30 minutes

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5
Q

Oral

A

immediate to extended

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6
Q

GTN Sublingual tablets vs spray

A

tablet can be spat out when vasodilation has occurred

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7
Q

counselling GTN

A

patient should sit down
spray under tongue, wait 5 mins
if symptoms haven’t relieved administer again
if same after 5 mins call ambulance

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8
Q

Advantages of:

  1. Oral
  2. IV
A
  1. Easy-to-use, Extended formulation available

2. 100% bioavailability, fast onset

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9
Q

Advantages of

  1. Topical
  2. Pulmonary
A
  1. easy, non-invasive

4. rapid absorption, inhaled with low systemic absorption

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10
Q

Barriers to oral drug delivery

A

GIT - pH, enzyme degradation, binding
Mucus - diffusion, binding, electrostatic repulsion
Membrane transport - diffusion, recognition, enzymes - brush border
Liver - 1st pass

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11
Q

Routes of absorption across epithelia

A

Paracellular - between cells
Transcellular - through cells (passive, carrier-mediated, endocytosis)
EFFLUX (P-gp)

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12
Q

Transcellular carrier-mediated

A

Large neutral amino acid carrier system
requires energy
against gradient
may require associated ions H+ Na+

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13
Q

Transcytosis comparion of types

A

Receptor-mediated - specific, saturable

Adsorptive endocytosis - non-specific, unsaturable

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14
Q

Mechanism of enteric coating

A

e.g. SI, use polymer insoluble pH<4 but soluble above. Use plasticiser to avoid the coat cracking

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15
Q

Colon-specific release strategies (3)

A
  1. enzyme triggered - polymers or prodrugs
  2. pH controlled - polymers using above 7 as the trigger
  3. time-controlled - polymers
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16
Q

Sustained release systems (4)

A

Bio-erosion
Gastro-retentive - floating, swelling+expandable
Diffusion - reservoir, matrix
Dissolution - increase particle size, use slow dissolving matrix, tablet coating

17
Q

Disadvantages

  1. Oral
  2. Rectal
A
  1. unsuitable - vomiting, difficulty swallowing
    slow, unpredictable absorption
    hard to mask taste
  2. Patient acceptability
18
Q

Disadvantages

  1. SC or IM
  2. IV
A

3.Unpredictable absorption, sore
4. requires functioning cannula, can be distressing
local infection, reaction

19
Q

Disadvantages:

  1. topical - desired MW log P
  2. Inhaled
A
  1. MW<500 moderate log P 1-4 desired
    slow absorption
  2. Inhaler technique
    size of drug particles delivered
20
Q

Onset of action of GTN formulations

A

Spray>tablets>Parenteral injection>Patches and ointment

21
Q

SL tablets - description of administration, advantages and disadvantages

A

Formulation: Held within the oral cavity, below the tongue and slowly dissolve. Designed to dissolve slowly and not disintegrate.
Advantages; Give rapid absorption into the systemic circulation. Avoids first pass metabolism.
Disadvantages; issues with eating, drinking or smoking, as can affect how the drug is absorbed and how well it works.

22
Q

Buccal absorption of basic drugs change according to increase of pH of their solutions

A

Buccal absorption of basic drugs increases with increasing pH of their solutions

23
Q

Are weakly acidic or weakly basic drugs absorbed when the pH is well below pKa?

A

Weakly acidic

24
Q

IM and SC administration,
muscle tissue
oily vehicles
lower MW + dispersion rate

A

Muscle tissue is more acidic than normal physiological fluids
Oily vehicles may be used to provide diffusion over a prolonged period
Dispersion of soluble drugs from the injection site is more rapid the lower the molecular weight of the drug

25
Q

Compare advantages/disadvantages of MDI with DPI

A

Both particle size <5um
MDI - cheaper, hermetically sealed reducing contamination. Stability issues, need co-ordination.
DPI - less co-ordination, no propellant, less irritation.
Require excipients, cannot be used with spacer

26
Q

Regarding the physiology of the respiratory tract, which of the following statements are true?

  1. The diameters of the conducting airways decreases towards the alveoli
  2. Drug absorption from the respiratory tract occurs at the alveoli
  3. The surface area of the alveoli is > 100 meters squared.
  4. The primary mechanism of elimination of particles > 5 um is expiration.
A

1 and 2

27
Q

Concerning the formulation and use of MDI, which of the following statements are true?

  1. Oxidation of drugs is minimised.
  2. MDI are usually formulated to ensure that the drug is soluble within the propellant system.
  3. MDI require the inclusion of a preservative
  4. MDI may be easily formulated to contain water
A

1

28
Q

Concerning the formulation of DPI, which of the following are true?

  1. Liquid propellants are not required.
  2. The Mass Median Aerodynamic diameter of the therapeutic agents should be < 5 um
  3. Lactose is commonly used to improve the flow properties of the powdered drug
  4. Following inspiration, both lactose and the powdered drug reach the site of action.
A

1,2,3

29
Q

True statements regarding MDI:

  1. Administration of high doses of therapeutic agent
  2. Convenience for the patient
  3. Requirement for patient’s ability to co-ordinate actuation and inhalation
  4. Greater efficiency than nebulisers.
A

2,3,4

30
Q

Advantages/disadvantages of colon-specific drug strategies?

A

Advantages: avoid enzyme degradation in the low pH of the stomach and SI
Disadvantages: - drug still subject to 1st pass
-concentration of microorganisms in the colon is very high and little is known about the possibility of pre-systemic drug metabolism by these molecules

31
Q

Advantages of tablets

A
  • can contain multiple APIs
  • accurate dose
  • easy, convenient
  • control where drug is released
  • offer taste masking to a degree
  • generally most stable format for an API (water accelerates the breakdown)
32
Q

In relation to buccal and SL formulation which statements are true:

  1. Drugs absorbed by these routes bypass the liver
  2. absorption through the buccal epithelium is not affected by the partition coefficient of the drug
  3. buccal absorption of basic drugs increases with increasing pH of their solutions
  4. buccal absorption of acidic drugs increases with increasing pH of their solutions
  5. there is an optimum log P for SL absorption
A

1,3,5

33
Q

In relation to absorption of drugs from i.m. and s.c. injections, which of the following statements are correct?

a) Dispersion of soluble drugs from the injection site is more rapid the lower the molecular weight of the drug
b) Binding to muscle protein increase the rate of absorption
c) Hydrophilic drugs bind strongly to muscle protein
d) Muscle tissue is more acidic than normal physiological fluids
e) Oily vehicles may be used to provide diffusion over a prolonged period

A

A,D,E

34
Q

IV and tumour targeting strategies

A

nanoparticles. Cancer drugs typically need to reach cancer but can damage normal healthy cells producing undesired side effects
e. g. doxorubicin - liposome

35
Q

liposomes

A

IV into bloodstream where they accumulate at tumour (leakier blood vessels). Increases solubility, stability.
Silicone degrades releasing doxorubicin at site of action. Favourable biodistribution, pKa, safety profile.
These molecules spontaneously formed nanoparticles which were taken up by tumour

36
Q

What are liposomes?

A

A liposome is a spherical-shaped vesicle that is composed of one or more phospholipid bilayers, which closely resembles the structure of cell membranes. The ability of liposomes to encapsulate hydrophilic or lipophilic drugs have allowed these vesicles to become useful drug delivery systems.

37
Q

timed colon release mechanism

A

The drug is incorporated into pellets. These are coated with slow-release polymer then a second coat is applied. This is then compressed into a tablet

TPN, syringe drivers, Lab Results (13 decks)

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