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PHAR 224 > Suppositories > Flashcards

Suppositories Flashcards

1
Q

what are medication sticks

A

dosage form for administering topical drugs

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2
Q

what are common soft sticks

A 
cosmetic preparations (lip balm, deodorant) 
convenient to apply topical drugs
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3
Q

What are hard sticks made of

A

Crystalline powders fused or bound together with cocoa butter or petrolatum
ex: styptic pencil

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4
Q

what is a suppository

A

A solid dosage form 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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5
Q

Disadvantages of suppositories

A

More invasive
Sometimes absorption is variable
They may be a bit more to manufacture

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6
Q

advantages of suppositories

A

Can be used in people who can’t take oral medication

Unconscious patients

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7
Q

What are some applications of suppositories

A

Local effect: antihaemorrhoidal, contraceptive preps

Systemic effect: analgesics, antiasthmatics

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8
Q

where are drugs absorbed in the rectum?

A

Inferior/middle rectal vein to the general circulation

Miss first pass metabolism
Need to make sure that most of the drug is administered in the lower part of the rectum

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9
Q

Drug factors that affect drug absorption from suppositories

A

Degree of ionization (unionized is better)
Solubility of drug (lipophilic is better)
Particle size (smaller is better)
Partition coefficient of drugs between vehicle and rectal fluid

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10
Q

Vehicle factors that affect drug absorption from suppositories

A

Melting point and liquefaction (need them to melt at body temp so drug can be released)
Viscosity (make sure that the active ingredient mixes with the vehicle so it needs to be viscous enough to maintain homogenous mix of drug and vehicle (no sedimentation)

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11
Q

physiological factors that affect drug absorption

A 
pH of rectal fluids 
Colonic content (better for it to be empty)
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12
Q

what is the rate limiting step in drug absorption from the rectum?

A

THICKNESS OF MUCOSAL MEMBRANE

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13
Q

physiochemical considerations for formulating suppositories (9)

A

spreadability
melting temperature (need melting for absorption)
presence of water (optimize water content: without water the fats may be hydrolyzed, can have drug excipient interactions, or bacterial contamination)
Hygroscopicity (PEG: might cause irritation because of the hygroscopic properties, add water right before administration and then administer)
Viscosity (low viscosity can cause sedimentation can add aluminum monostearate)
Brittleness (synthetic fat bases, overcome by adding plasticity imparting compounds-Tween 80, Castor oil)
Density
Volume contraction
Incompatibilities

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14
Q

Drugs that are good choices for suppositories

A 
Poorly absorbed orally 
Unacceptable taste 
Irritating to the GI mucosa
Drug of abuse 
Properties of the drug (physical appearance: liquid, pasty, solid; Bulk density; Solubility)
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15
Q

What are properties to consider when choosing a base

A 
Physiochemical properties 
Release characteristics 
Inertness 
Stability during manufacturing 
Essential properties during production, storage, and use
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16
Q

When to use a fatty base

A

when the drug is highly soluble in water

17
Q

when to use a water-miscible base

A

when the drug is highly soluble in fat

18
Q

Fatty bases used in suppositories

A

Cocoa butter

Hydrogenated vegetable oil: adeps solidus, Witepsol

19
Q

what is cocoa butter

A

Natural triglyceride
melts at body temp, solidifies at 25 degrees C
Has 4 polymorphic forms
Requires mold lubrication

20
Q

what is hydrogenated vegetable oil

A

semi-synthetic
waxy solids
self-lubricating and contract in mold
NO polymorphism

21
Q

what are water-soluble bases used in suppositories

A

glycerin based

PEGs

22
Q

what is PEG

A

has a melt point above body temp but dissolves and mixes with rectal fluid
chemically stable, inert
no mold lubricant needed

23
Q

What is an additive that improves incorporation of active ingredients

A

MgCO3: for glycerol into lipidic base
Fixed oils: to levigate solids
Water

24
Q

what is an additive that increases hydrophilicity

A 
Ionic surfactants (anionic, SDS, sodium-lauryl sulfate, TEA-stearate) 
Non-ionic surfactants (Tween, Labrafil, Cremophor)
25
Q

what are some additives that improve viscosity

A

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

26
Q

what are some additives that modify melting points

A

Fatty acids, fatty alcohols, waxes
Sometimes the base may have a melting point range but addition of drug may change the melting point
Adding these brings the formulation back to a certain melt point

27
Q

what is an additive that increases mechanical strength

A

Synthetic bases

28
Q

what are additives that protect against degradation

A

Antimicrobial, antifungal, antioxidant

29
Q

what are the general compounding steps

A

Mold preparation
Mold calibration
Base preparation Preparation of the active drug
Mixing and pouring
Cooling and finishing Packaging, storage, and labelling

30
Q

what are the steps of fusion

A 
Melt base 
Incorporate drug 
Pour melt into molds while stirring 
Allow to melt and congeal 
Remove suppositories from mold

Can lubricate the molds with mineral oil silicones

31
Q

what is compression

A

No problems with sedimentation
Increased rate of production
Elimination of temperature change related problems
Disadvantage: requires finely powdered excipients

32
Q

what is hand rolling

A

Doesn’t require special calculation
Mostly for cocoa butter
Tedious, requires experience
Not very uniform

33
Q

steps of hand rolling

A

Triturate drug and base together in mortar
Use your hand to make a round shape with the mixture
Flatten to a rod shape and then cut from there

34
Q

how do fatty based suppositories need to be stored?

A

Individually wrapped to prevent contact (wrapping material: plastic/aluminum foil)
Store in a cool place

35
Q

how do water soluble based suppositories need to be stored

A

Individually wrapped
Tightly closed containers to prevent moisture absorption (water soluble bases are hygroscopic in nature)
Store in a cool place EXCEPT for PEG which can be stored at room temp

36
Q

steps to insert a rectal suppository

A
  1. lubricate the tapered end of the suppository with lube or water
  2. Lay on one side with one leg bent and the other straight or with one leg on a chair
  3. seperate buttocks
  4. gently press the suppository into the rectum until it passes the sphincter
  5. close your legs or stay still for 15 minutes and avoid emptying bowels for at least one hour also avoid excessive movement for 1 hour
37
Q

steps to insert a vaginal suppository

A
  1. Place suppository in applicator
  2. Lay on your back with your knees bent or stand with feet spread apart
  3. Gently insert the applicator into the vagina as far as it will go comfortably

PHAR 224 (7 decks)

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