Pharm 125 Midterm Content

suppositories, powders/granules, tablets, capsules, modified release

What is the difference between a suppository and an insert?

an insert is for any body cavity that isnt the mouth or rectum

T/F suppositories are less irritating to the GI tract

T

Are suppositories intended for local or systemic effect?

both

T/F suppositories avoid 1st pass metabolism

T (if they are administered properly)

T/F poor compliance is associated with suppositories

T

T/F some suppositories can cause irritation to the mucous membranes

T

What is the shape of a rectal suppository?

bullet or torpedo shape

What is the weight of a baby, adult, and rectal rocket suppository?

1g, 2g, 4-5g

What is the shape of a vaginal suppository?

globular/oval shape

What is the weight of a vaginal suppository?

3-5g

What kind of vehicles are vaginal suppositories usually made from?

H2O soluble or H2O miscible vehicles (PEG, glycerinated gelatin)

What type of suppository can be used for infections, as contraceptives or for hormones?

vaginal

What is the weight of a female and male urethral suppository?

2g, 4g

What is the diameter of urethral suppositories?

3-6mm, longer for males

What type of suppository can be used to treat ED, bacterial infections or as a local anesthetic?

urethral

What type of excipient is 1-10% silica gel?

suspending agent

___________ are additives that prevent sinking during congealing

suspending agents

What type of excipients are mineral oil and glycerol?

mold lubricants

_____________ are additives that prevent suppositories from sticking to the mold

mold lubricants

What types of excipients are methylcellulose and colloidal silicon dioxide?

viscosity-enhancing agents

_____________ are additives that sustain drug release from the suppository base

viscosity-enhancing agents

What types of excipients are Tween (polysorbate) and Span (sorbitan ester)?

surfactants/emulsifying agents

_____________ are additives that improve wetting and spreading and may increase permeability of the rectal mucosal membrane

surfactants/emulsifying agents

What types of excipients are white wax, beeswax and cetyl esters wax?

solidifying agents

____________ are additives that raise the melting point

solidifying agents

T/F surfactants can be used as dispersants in suppositories

T

T/F an ideal suppository should be non-absorbable

T

What type of suppository base is Witepsol?

semi-synthetic fatty base w/ emulsifier

What type of suppository base is Fattibase?

semi-synthetic fatty base

What type of suppository base is glycerinated-gelatin?

hydrophilic/H2O soluble

What type of suppository base is PEG?

hydrophilic/H2O soluble

What type of suppository base is Polybase?

hydrophilic/H2O soluble (PEG + tween 80)

Another name for theobroma oil is?

cocoa butter

Cocoa butter is a mixture of glyceryl esters of _____, _____, _____, and other fatty acids.

stearic, palmitic, oleic

T/F cocoa butter is compatible with many ingredients

T

T/F cocoa butter is prone to polymorphism

T

What is the melting point of the a polymorph of cocoa butter?

<30*C

What is the melting point of the B polymorph of cocoa butter?

34-35*C

What is the most stable polymorph form of cocoa butter?

B polymorph

How are semi-synthetic fatty bases made?

hydrolyzing veggie oil + hydrogenation then re-esterifying the acids by heating with glycerol

T/F semi-synthetic fatty bases can experience polymorphism

F

T/F semi-synthetic fatty bases should be stored in the fridge

T

Semi-synthetic fatty bases may be more irritating than cocoa butter because they can have a ________ effect

dehydrating

What is the composition of glycerinated-gelatin base?

70% glycerin, 20% gelatin, 10% H2O

T/F glycerinated-gelatin bases will melt at body temperature

F, they slowly dissolve in the mucous lining of the rectum and vagina (~50*C)

Glycerinated-gelatin bases are used frequently for _________ suppositories

vaginal

Which base would be better as an antiseptic, glycerinated-gelatin or fatty bases?

glycerinated-gelatin, dissolves slowly

Glycerinated-gelatin are used as a suppository base but one disadvantage is they have their own therapeutic effect. What is it?

laxative effect

T/F glycerinated-gelatin bases are hygroscopic

T, need careful storage

Since glycerinated-gelatin bases are hygroscopic, what effect does this have on the mucosa?

dehydrating and irritating

Do PEG base suppositories require refrigeration?

No, mp > 42*C

T/F PEG suppositories melt at body temp

F

Which base has a shorter release time of drug, cocoa butter or PEG?

cocoa butter

Why does PEG have a prolonged release of drug compared to cocoa butter?

needs to dissolve first before diffusing

How can physical properties and mps be adjusted for PEG bases?

by varying the mixture of high and low MW polymers

If a PEG base was made of 95% PEG 1000 + 5% PEG 4000, would the mp be low or high?

low, large % of lower MW PEG

Will PEG base leak from the body?

no

PEG bases are ______, meaning they absorb moisture from their environment

hygroscopic

Why would a PEG base suppository be moistened with H2O before insertion?

hygroscopic nature can cause irritation go the rectal mucosa

T/F PEG base will not contract significantly during cooling

F, forms pits/holes

PEG bases are incompatible with ______ substances (ex: tannic acid, aspirin, benzocaine, salicylic acid)

phenolic

Why would you not use aspirin in a PEG base?

PEG is not compatible with phenolic substances

Does fluid in the rectal cavity have any buffer capacity?

no

The _______ rectal veins transport drug to the upper part of the rectal cavity and liver

superior

The _______ rectal veins transport drug to the IVC and bypass the liver

inferior

You should add a suppository to the _____ part of the rectum if you want to bypass the liver

lower

________ drugs will have good release from fatty base suppositories, resulting in better absorption and bioavailability

hydrophilic

_______ drugs tend to remain in fatty bases and lead to little absorption

lipophilic

________ drugs will have good release from hydrophilic/H2O soluble suppositories, resulting in better absorption and bioavailability

lipophilic

_______ drugs tend to remain in hydrophilic/H2O soluble bases and lead to little absorption

hydrophilic

If possible, the ______ form of a lipophilic drug should be used in a fatty base.

ionized salt, improved hydrophilic properties

PEG bases with _____ MWs have longer dissolution time

higher

Preparation of suppositories: ______ is a historic part of the art of the pharmacist

hand-rolling and shaping

Hand-rolling and shaping is usually done with __________ because it is easy to manipulate

cocoa butter

When could you use compression molding to make a suppository?

for heat-labile substances

for substances that are insoluble in base

Given the following steps, name the method of suppository preparation:

1. Triturate API with cocoa butter to make a paste

2. Add grated cocoa butter and triturate

3. Knead until pliable

4. Roll into cylinder then cut into suppository shape

hand-rolling and shaping

T/F compression molding is usually done by hand

F, need special machine

Given the following procedure, name the method of suppository preparation:

1. Mix the base and ingredients into a paste

2. Force the paste into a mold

compression molding

Which method of suppository preparation did we use in lab?

fusion molding

Given the following procedure, name the method of suppository preparation:

1. Melt the base

2. Add API and mix

3. Pour into a mold

4. Congeal at room temp then refrigerate

fusion molding

T/F hydroscopic products should be wrapped in grease-proof paper

F, dispense in plastic or tight glass container

We need to account for drug density when there is more than ____ mg of drug in the suppository

100

What is the density factor (DF)?

amount of API displaced by 1g of base

What is the estimated DF?

powders have an estimated displacement of 0.7g of base per 1g of drug

When do you use the double casting method?

when the DF is unknown and the drug has a systemic effect

What is the Paddock method equation (double casting)?

DF = B/(A-C)+B

A = blank weight avg

B = weight of API/supp

C = avg weight of final supp

Quiz:

A pharmacist prepares 6 suppositories using a PEG base, density 1.18g/mL. The total weight of the suppositories is found to be 13.81g. What is the volume of each cavity in the mold?

1.95mL

Quiz:

Correlate the best suppository base to use with the following drug types

____ PEG base 1. fat-soluble drugs

____ fatty base 2. H2O soluble drugs

1. PEG base

2. fatty base

Quiz:

T/F If a compound has a density factor of 1.3 compared with cocoa butter this means that 1 gram of the compound will displace 1.3 grams of cocoa butter.

F

Quiz:

Order the following steps for the preparation of suppositories with cocoa butter base:

When base is melted, sprinkle the API to the melted base and mix until homogeneous.

Shave cocoa butter into small pieces and weigh the amount needed.

Pour the mixture to cavities of the mold and let it congeal.

Transfer the base to a beaker and add it to a water bath to melt.

3, 1, 4, 2

Quiz:

What type of suppository base would provide the best bioavailability for a hydrophilic drug?

glycerinated gelatin

cocoa butter

polyethylene glycol

polyoxyl 40 stearate

cocoa butter

Quiz:

How much cocoa butter is required to prepare SEVEN suppositories, each containing 400 mg of API? The API density factor in cocoa butter is 1.65 and blank suppository weighs 1.8g).

10.9

Quiz:

You need to prepare SIX suppositories, each containing 500mg of API. After performing a double-casting procedure, your medicated suppositories weighed an average of 2.35g. How much suppository base will you need to prepare this prescription?

11.1g

Quiz:

How many polymorphic forms does cocoa butter have?

4+

3

2

1

4+

Quiz:

How much cocoa butter is required to prepare FIVE suppositories, each containing 200 mg of API? The API density factor in cocoa butter is 1.65 and blank suppository weighs 1.8g).

8.4g

Quiz:

Which of the following bases exhibit polymorphism?

glycerinated gelatin

polyethylene glycol

polyoxyl 40 stearate

cocoa butter

cocoa butter

A ______ is defined as a single or mixture of solids in a finely divided state

powder

A ______ is defined as a solid dosage form composed of agglomerations of smaller particles

granules

Powders are ______ in size

< 1000um

Granules are ____ to ____ in size

0.2-4mm