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Compounding Exam 1 > Lecture 7 - Suppositories > Flashcards

Lecture 7 - Suppositories Flashcards

1
Q

in suppositories, the drug is incorporated into a base which ___ or ____ at body temp to release the drug

A

melts or dissolves

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2
Q

TRUE OR FALSE

suppositories are really only used for their systemic effects

A

FALSE - local or systemic

local irritation, hemorrhoids

systemic hormone delivery or pain relief

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3
Q

vaginal suppositories are also called….

A

pessaries

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4
Q

an adult rectal suppository weighs around…..

A

2 grams

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5
Q

what is usually the shape of rectal suppositories vs vaginal

A

rectal are long and cylindrical with 1 tapered end

vaginal is usually globular oviform or cone shaped

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6
Q

around how much do vaginal suppositories typically weigh

more or less than rectal?

A

more than rectal - around 5g

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7
Q

uses of vaginal suppositories

A

hormone delivery
birth control
combat infection
restore vagina lmucosa to normal state

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8
Q

major advantages of suppositories***

A

NO pH degradation or enzymatic degradation of the drug (like in the gut)

very limited 1st pass effect

drugs that irritate the stomach can be delivered this wat to bypass the stomach

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9
Q

what is the approximate rectal pH and what is the advantage of this***

A

around 6.8

drugs that are degraded by low pH in the stomach thus won’t be affected by rectal administration

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10
Q

true or false

if a drug is susceptible to degradation in acidic environment, rectal suppositories are not a good chouce

A

false - they are

rectal pH is close to neutral at 6.8

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11
Q

major issues of suppositories*****

A

UNPREDICTABLE ABSORPTION - results can vary from patient to patient

can be slow and incomplete absoroption

mucosal irritation

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12
Q

give 3 reasons why absorption from suppositories is unpredictable***

A

contents of the colon
placement of suppository
GI probelms

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13
Q

which has larger surface area for absorption and what does this mean - GI or rectum***

A

GI

therefore, absorption may be incomplete and slow when things given rectally

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14
Q

true or false

suppositories do not require special storage requirements

A

FALSE - they do – this is disadvantage

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15
Q

the rectum is the terminal portion of the_____

A

large intestine

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16
Q

***volume of the rectal fluid

A

1-3mL

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17
Q

TRUE OR FALSE

the rectum has high buffer capacity

what is significance

A

false - low buffer capacity

therefore, the drug inserted must be extremely close to neutral

if basic, can turn fluid alkaline by adding a base which can cause irritation

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18
Q

what position are rectal suppositories supposed to be inserted and why – explainnnn**

A

in the LOWER AND MIDDLE VEINS
this is bc it drains directly into the inferior vena cava and bypasses the liver and first pass effects to go DIRECTLY into circulation

upper rectal vein drains directly into hepatic portal vein – goes right to liver and subject to hepatic metabolism

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19
Q

blood supply of rectum**

A

upper, middle, and lower hemorrhoidal veins

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20
Q

what is the MAIN ingredient in a suppository

what is the purpose of it

A

the base

helps to formulate drug in suppository and allows for drug release and bioavailability

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21
Q

explain how a suppository base should behave at room temp vs at body temp

A

should remain solid at room temp and melt or dissolve at body temp

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22
Q

name 2 different classifications of suppository bases and give examples

A

oleaginous/fatty base - COCOA BUTTER

hydrophilic bases – glycerinated gelatin and PEG

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23
Q

we want drugs with ______ partition coefficients to be absorbed through the rectum

A

HIGH

the rectal membrane is lipophilic - want lipophilic drug

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24
Q

what can you say about the desired particle size of a drug in a suppository

A

want pretty small to be able to permeate the membrane and leave the base

smaller particles = higher surface area — BETTER DISSOLUTION AND RAPID ABSORPTION

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25
Q

*** a fatty base will release a lipophilic drug quickly or slowly????

A

SLOWLY – also slower absorption

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26
Q

true or false

a lipophilic drug will have quick drug release from a PEG or glycerinated gelatin suppository base***

A

TRUE - hydrophilic base and lipophilic drug will allow for quick release

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27
Q

As mentioned, small particle size is desired for drugs incorporated into suppository bases

what is the most common way this is done

A

trituration

28
Q

approximate body temp in celsius

approximate room temp in celsius

A

body - 37

room temp - 22-25

29
Q

true or false

the suppository base should not interact with the drug

A

true

30
Q

aside from causing pain, why must the suppository base not irritate the mucous membrane

A

may initiate a bowel movement and eliminate chance of drug release and absorption

31
Q

suppository bases should be _____ viscosity when melted

A

high

32
Q

true or false

suppository bases should be physically stable

A

true

33
Q

water dispersable suppository base example

A

cocoa-butter substitutes with surfactans

34
Q

aside from cocoa butter name other fatty/oleaginous bases

A

hydrogenated fatty acids of vegetable oils (palm kernal oil, cottonseed oil)

35
Q

true or false

water soluble/water miscible bases dissolve in the rectum

A

true

36
Q

when preparing suppository with cocoa butter, it is VERY IMPORTANT NOT TO EXCEED……

A

60 degrees celsius

excess heating can form an unstable and low melting point crystalline form — may melt even at low temp

37
Q

name 2 substances that lower the melting point of cocoa butter and thus should not be used

A

phenol

chloralhydrate

38
Q

if worried about cocoa butter melting at room temp, what can we do?

A

add solidifying agents – cetyl ester wax and beeswax

39
Q

of the 2 main types of suppository bases, which is mainly used rectally and which is mainly used vaginally

A

gelatinated glycerin and PEG are typically VAGINAL

cocoa butter typically RECTAL

40
Q

name 3 COMMERCIAL NAMES of other fatty bases (not cocoa butter)***

all are___

A

fattibase
wecobee base
witepsol base

triglycerides

41
Q

glycerinated gelatin is ______ in nature

what does this mean?

A

hygroscopic

will absorb water from the body fluids to DISSOLVE

if you put in rectum pt will lose fluid and have stinging and laxative effect (may be desired)

42
Q

*******ratio of glycerinated gelatin

A

70 glycerin: 20 gelatin: 10 water

43
Q

true or false

glycerinated gelatin is most frequently used for VAGINAL

A

true

44
Q

time range that glycerinated gelatin dissolves vs time that cocoa butter melts

A

gly. gelatin dissolves SLOWLY - 30-40 mins

cocoa butter melts much faster - 10-15 mins

45
Q

storage of glycerinated gelatin and why

A

TIGHT CONTAINERS - it’s hygroscopic!!

46
Q

explain what should be done before applying suppositories with glyc. gelatin as the base and why

A

moisten before applying —- reduce initial tendency of the base to draw water from the mucous membrane and cause tissue irritation

47
Q

glycerinated gelatin bases intended for extended shelf life should have what and why?

A

PRESERVATIVES like methyl/propyl paraben – bc of water content

48
Q

PEG ________ and HIGHER are wax like white solids

A

1000

less than 1000 are liquid at room temp

mix both to get good consistency - achieved by FUSION

49
Q

with increasing molecular weight of polyethylene glycol bases………

_____increases
____ decreases

A

hardness increases and water solubility decreases

50
Q

true or false

for PEG bases, there is no risk of melting so no refrigeration is required

A

true

51
Q

true or false

PEG bases take 10-15 mins to dissolve

A

false 30-40 mins (like glyc. gelatin)

52
Q

what does PEG interact with and what does this mean

A

polystyrene (prescription vials)

therefore, can only be dispensed in them if first wrapped in foil

53
Q

what drug forms a complexation with PEG and what does this mean

A

Aspirin

THEREFORE, if we use PEG + Aspirin, there will not be quick release

use diff base if we want quick

54
Q

high concentrations of ________ will soften PEG

A

salicylic acid

55
Q

what 3 things will cause crystallization of PEG base

A

salicylic acid
camphor
sodium barbital

56
Q

3 methods of suppository preparation

A

molding (most common) - melt and pour and allow to cool and congeal

compression

hand molding and shaping

57
Q

when using the molding method for preparing suppositories, the mold should be filled at what temp?

A

room temp

if cold, could make fractures and fissures in suppositories

58
Q

______ may be required for some molds and bases

give 2 examples

A

LUBRICATION

mineral oil and gelatin

not too much - will pool at supp tip

59
Q

micture should be poured into the mold right before reaching…..

A

congealing temperature

60
Q

how much mixture should be poured into the mold

A

add excessive amounts bc it will shrink when it cools

61
Q

when a drug is placed into a suppository base, it will…..

A

displace an amount of base (as a function of its density)

use density factor to determine how much base will be displaced by the drug!!!

weight drug/weight base displaced = density factor

62
Q

suppositories must be made to _____ before use

A

come to room temp

63
Q

counseling for PEG/cocoa butter/vaginal suppositories

A

PEG - moisten with water before use

cocoa butter - rub with fingers so upper surface melts

vaginal - moisten with water for good lubrication and disintegration

64
Q

how is strength of API in suppository expressed

A

amt/suppository

65
Q

which suppository base interacts with polystyrene

A

PEG

66
Q

true or false**

PEG bases may cause stinging and burning when used rectally

A

true

67
Q
A

Compounding Exam 1 (9 decks)

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