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Pharmacotherapy > Medication Sticks > Flashcards

Medication Sticks Flashcards

1
Q

Commonly accepted cosmetic formulations

A

Pain relief roll on sticks
Lip balms
Speciality compounds

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2
Q

Why is medical sticks not as common

A

We have replacement therapies that are far more superior

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3
Q

What is a soft stick?

A

Generally a cosmetic preparation
Convenient to apply topical drugs

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4
Q

What is hard sticks?

A

➔ Crystalline powders fused by heat or held together with binders such as cocoa butter or petrolatum

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5
Q

What is needed to activate hardsticks/

A

Moisture

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6
Q

What is the general bases for medicaiton sticks?

A

Fatty bases or water soluble bases

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7
Q

What are the fatty bases used in stick bases?

A
  • cocoa butter
  • Vegetable oils – rancidity; mineral oil
  • hydrogenated vegetable oil - Witepsol
  • Waxes (carnauba wax, candelilla wax, beeswax)
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8
Q

What are the water-soluble bases used in stick bases?

A
  • Sodium stearate/glycerol PEGs
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9
Q

What is the preparation for medicaiton stick?

A

Molding/fusion

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10
Q

What is a solid dosage form suppository?

A

used for rectal, vaginal, urethral administration

Consists of a dispersion of the active ingredient in an inert matrix (a rigid or semi-rigid base)

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11
Q

What are the advantages of a suppository over other dosage forms?

A

➔ Less invasive than injectables
➔ Limit first pass hepatic metabolism
➔ Limit drug interactions when given in combination with other therapies
➔ Can be used for both local and systemic effects
➔ accommodates patients who have difficulty
swallowing pills
➔ Accommodates administration in unconscious patients or infants
➔ increased bioavailability of drugs

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12
Q

What are the limitations of suppositories?

A

➔ Not for long-term treatment (NOT PHARMACEUTICAL LIMITATION BUT due to lower user acceptance)

➔ User discomfort

➔Special storage conditions like low
temperature (risk of melting)

➔For some patient population, dosage form is difficult for self-administration

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13
Q

As compared to other environments whats unique about the rectum environment?

A

constant and static

Neutral pH

Normal bacterial flora

Rich vasculature that increases bioavailability

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14
Q

What is the inferior/middle rectal vein?

A

drains into the inferior vena cava and, therefore, directly into the systemic circulation.

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15
Q

What is the superior rectal vein?

A

drains into portal vein which passes the blood through the liver prior to reaching the systemic circulation.

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16
Q

Take some time to look at the picture on the next slide

A
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17
Q

What are the factors that may contribute to the absorption of drugs via the rectal routes?

A

Formulation factors
Physiological factors

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18
Q

Most transport in the rectum will be?

A

Transcellular

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19
Q

Formulation factors with suppositories need to incorporate both?

A

Drug and the vehicle.

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20
Q

What is important with suppositorie vehicles?

A

(REMEMBER vehicle should be inert and thus have no interaction with the API)

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21
Q

What does a high Partition coefficient indicate?

A

High lipophilicity

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22
Q

If we have high lipophilicity what does that mean?

A

slow release of the drug from formulations that have fatty bases BUT fast release from hydrophilic bases (VEHICLE FACTOR)

Like base and like vehicle is slow

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23
Q

What determiens the maximum concentration available for absorption?

A

Solubility of the drug in the rectal fluid

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24
Q

Acid dissociation constant (pKa) of the drug near or above the physiological pH means

A

Higher absorption since it is in the unionized form and more in favor for transcellular route

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25
Q

Lower the particle size means?

A

The better dissolution in the rectal fluid

26
Q

What physiological factors affect absorption?

A

anatomical size difference between the rectum of adults and children

site of drug delivery in the rectum

Changes in rectal pH based on age or disease conditions

presence of stool in the rectum affects the viscosity of the rectal contents

Frequency of bowel movements

Pathological changes in tissue integrity changes the thickness of the mucosal membrane

27
Q

What are the three different types of suppositories

A

Rectal (1.5 inches
Vaginal suppositories
Urethral suppositories

28
Q

What is the only urethral suppository available?

A

Muse (For ED)

29
Q

With respect to the choice of drug which should be chosen for suppositories

A

➔Poorly absorbing orally
➔Taste unacceptable
➔Irritating to GI mucosa
➔Drug of abuse
➔Acid labile drugs
➔Drugs prone to enzymatic degradation

30
Q

With respect to the vehicle/base of the suppository what should it be able to do?

A
  • Melt
  • Soften
  • dissolve at body temperature,
  • Promote drug release
  • Stay stable during manufacturing and storage
  • INERT
  • Esthetically acceptable
31
Q

What are the fatty bases used in suppository bases

A
  • cocoa butter
  • hydrogenated vegetable oil - Witepsol
  • hydrogenated palm oil - Suppocire suppository base (Gattefosse)
32
Q

What are the water soluble bases used in suppository bases?

A
  • glycerine based suppositories
  • PEGs
33
Q

With respect to the choice of the base. If our drug has low solubility in the fat, but more soluble in the water, what vehicle should we use?

A

Fatty base, Faster release (Always doing the opposite)

34
Q

With respect to the choice of the base. If our drug has low solubility in water, but more soluble in the fat, what vehicle should we use?

A

Water-miscible base

35
Q

What is the melting point for Cocoa butter?

A

31-35

36
Q

What is the disadvantage of Cocoa butter?

A
37
Q

What is a common hydrogenated vegetable oils?

A

Witepsol

38
Q

Review the next table

A

Although they all are fatty bases, they have different intensity of hydrophilic and lipophilic character → THIS is an important parameter in selecting the base which depends on the physicochemical characteristics of the drug.

39
Q

Why do we want to use a water soluble bases?

A

If we want a laxative effect

40
Q

What are the limitiations of PEG?

A

a. Hygroscopic→storageconditionsneedscriticalcontrol
b. Several incompatibilities with APIs
c. May become brittle on storage

41
Q

To improve incorporation of active ingredients

A

➔Fixed oils – to levigate solids
➔Water

42
Q

Ti improve viscosity

A

➔Al-monostearate, glyceryl monostearate ➔Stearyl-, myristyl-, cetyl alcohols ➔Bentonite, colloidal silica

43
Q

When would you CONSIDER rectal route

A
  • Pediatric patients
  • Patients experiencing dysphagia
  • Intractable nausea and vomiting
  • Refusing oral medications or spitting
    out tablets
  • Patients with gastrointestinal
    obstruction
  • Patients with esophageal stricture or
    malignancy
  • Loss of consciousness/palliative care
  • Decreased mental status
44
Q

When would you AVOID rectal route

A
  • Neonatal patients
  • Patients who may have conditions
    associated with neutropenia (due
    to risk of infection)
  • Thrombocytopenia (due to risk of
    bleeding)
  • Chronic constipation
  • Increased GI motility (Diarrhea)
  • When placement of medication per
    rectum will cause pain (e.g., inflamed/bleeding hemorrhoids (rectal creams and ointments are preferred), fissures or lesions of the anus or rectum)
45
Q

What is the general suppository for compounding steps?

A

➔ Mold preparation
➔ Mold calibration
➔ Base preparation
➔ Incorporation of active (drug displacement factor)
➔ Mixing and pouring
➔ Cooling and finishing
➔ Packaging, storage and labelling

46
Q

What is the Displacement factor?

A

➔ measure of the amount of active substance (in grams) that displaces 1 g of suppository base.

➔Affects final suppository weight and dosing uniformity of the formulation especially for drugs which exhibit high displacement factors.

47
Q

What are the techniques for suppositories preparation

A

➔ 1. Molding (fusion)
➔ 2. Compression (Cold compression)
➔ 3. Hand rolling

48
Q

Packaging and Storage for suppositories

A

MOST SUPPOSITORIES ARE
INDIVIDUALLY WRAPPED

49
Q

Fatty base suppositories must be stored

A

Store in a cool place 2-8°C – strict temperature control

50
Q

What causes Splitting, pitting and cracking

A

Excipient contracts strongly
Large time gap between pouring and cooling→temperature fluctuations

51
Q

What causes Sticking to mold

A

Faulty molds (gaps between molds upon closure)
Premature removal from mold Insufficient cooling Insufficient lubrication

52
Q

What causes Thickening prior to pouring

A

high proportion of finely powdered active ingredients
High viscosity base mixtures

53
Q

What causes poor product homogeneity?

A

Displacement factor not taken into account
Cooling too slow or too weak leading to drug sedimentation

54
Q

What causes Product insufficiently solid

A

Inclusion of air

55
Q

What causes Surface anomalies (fat bloom, whitening)

A

(high melting points) → Excipient melting at more than 60°C → longer residence in the molds→shape absormalities
Excipient/ active ratio

56
Q

What is the solution for splitting pitting and cracking?

A

Use an excipient which crystallizes slower
Maintain optimum control of steps pouring and cooling→minimize temperature fluctuations

57
Q

What is the solution for sticking to the mold?

A

Use appropriate equipment (inspect before begin) Prolong molding period/cooling period
Use an excipient which crystallized more rapidly Reduce cooling temperature
Sufficient lubrication

58
Q

What is the solution for thickening prior to pouring?

A

PEG: select the mixture of right PEGs
Adjust the concentration of the API in the dosage form

59
Q

What is the solution for poor porduct homogeneity?

A

Calculation should be carefully performed Increase viscosity of the base

60
Q

What is the solution ofr product insufficiently solid?

A

Check the stirring level and limit the formation of air bubbles

61
Q

What is the solution for surface anomalies?

A

Ensure mold is appropriately sealed
Use excipients to stabilize the system like surfactants

62
Q
A

Pharmacotherapy (6 decks)

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