541 - Drug Delivery Systems Lab I - Exam Iii - Suppositories

Front 1

What are the general effects of suppositories?

Back 1

They may act as a protectant or palliative to the local tissues at the point of introduction OR as a carrier of therapeutic agents for systemic or local actions

Front 2

What happens to suppositories at body tempature?

Back 2

They usually melt, soften or dissolve

Front 3

Name the four routes of administration that utilize suppositories

Back 3

1) Rectal
2) Vaginal
3) Urethral
4) Nose (Bougies)

Front 4

Describe adult rectal suppositories

Back 4

Cylindrical or conical shaped with a taper or pointed end that are approximately 2 gm and 1-1.5 inches long

Front 5

Describe infant rectal suppositories

Back 5

Same as adult suppositories, but with one half the weight

Front 6

What makes the French "special"?

Back 6

They like rectal suppositories.

Yikes.

Front 7

What are the benefits of rectal suppositories?

Back 7

1) Local or systemic action
2) Preferred when drug is destroyed in the GI tract OR
3) When NPO due to vomiting OR
4) When patient is unconscious

Front 8

What are the drawbacks of rectal suppositories?

Back 8

1) Absorption of most drugs is frequently erratic and unpredictable
2) Some may "leak" or are expelled post-insertion
3) Seriously, who (besides the French) likes to stick things up their butt?

Front 9

What are the steps to inserting a suppository?

Back 9

1) If possible, empty bowels
2) Wash hands w/ warm & soapy water
3) Remove foil or any wrapping
4) Lubricate taped end or, if not possible, moisten with a small amount of water
5) Stand w/ one leg on a chair OR
6) Lay on one side with one leg bent towards your stomach
7) Separate the buttocks
8) Gently, but firmly, push to insert the suppository
9) Close legs and remain still for 15 minutes
10) Do not void bowels for 1 hour
11) Wash hands
12) Enjoy

Front 10

How far do you have to insert a rectal suppository?

Back 10

Adults - 1 inch
Infants - 1/2 to 1 inch

Front 11

What is the approximate weight of vagina suppositories?

Back 11

3 to 5 grams

Front 12

Why use polyethylene glycol in vaginal suppositories?

Back 12

They will minimize leakage

Front 13

What are the benefits to vaginal suppositories?

Back 13

1) Less drug degradation compared to PO
2) Dose can be retrieved if necessary
3) Potential of long term absorption (IUDs)

Front 14

What are the drawbacks to vagina suppositories?

Back 14

1) Variable absorption due to dynamic variations in pH and membrane permeability over time
2) A tendency of some forms to be expelled

Front 15

How do you insert vaginal suppositories?

Back 15

1) Wash hands w/ soap and warm water
2) Remove foil or wrapping
3) Place suppository in applicator
4) Hold applicator at opposite end of the suppository
5) Lay on your back with knees bent or while standing spread your feet a few inches apart w/ knees bent
6) Gently insert applicator, slowly pushing suppository in as far back as possible
7) Remove applicator
8) Wash hands

Front 16

Are urethral suppositories common

Back 16

No

Front 17

Describe urethral suppositories

Back 17

Females: 5 mm diameter, 50 mm length, 2 gm

Males: 5 mm diameter, 125 mm length, 4 gm

Front 18

What is the "Rectal Rocket"?

Back 18

Special design for hemorrhoids that:
1) Does not get lost in rectum
2) Treats both internally and externally
3) Patient can expel gas without losing suppository

Front 19

What are some local applications of suppositories used for?

Back 19

1) Hemorrhoids
2) Itching
3) Infections

Front 20

What are some systemic applications of suppositories used for?

Back 20

1) Anti-emetics
2) Anti-asthmatics
3) Analgesics
4) Hormones

Front 21

What is the largest concern about drug administration from suppositories?

Back 21

The unpredictable absorption, use as a last resort

Front 22

What are the desirable properties of suppository bases?

Back 22

1) Chem and Phys stable under normal conditions
2) Non-reactive and compatible w/ other drugs and agents
3) Free from objectionable odor (who smells these)
4) Aesthetically appealing appearance
5) Non-toxic, non-sensitizing, non-irritating
6) Expansion/contraction characteristics for molds
7) Melts or dissolves in intended body orifice
8) Non-binding of drugs
9) Mixes with or absorbs some water

Front 23

How are suppositories classified?

Back 23

Based upon their composition and physical properties (i.e. oil or water based)

Front 24

What makes cocoa butter unique?

Back 24

Polymorphism, main source of formulation difficulties

Front 25

What are some examples of synthetic triglycerides?

Back 25

1) Hydrogenated vegetable oils
2) Fattibase
3) Wecobee
4) Dehydag
5) Hydrokote
6) Suppocire
7) Witespol

(Who names this stuff?)

Front 26

What is glycerinated gelatin used for?

Back 26

For vaginal suppositories

Front 27

What are the benefits of glycerinated gelatin?

Back 27

1) Tend to dissolve or disperse slowly in mucous secretions - Does not melt at body temp
2) Absorb and dissolve in atmospheric moisture
3) Need to have a preservative added
4) Dip in water just before use

Front 28

Describe polyethylene glycol properties for suppositories

Back 28

Chemically stable, miscible with water and mucous secretions and can be formulated in a wide range of hardness and melting points -- Do not melt at body temperature, thus can be stored at room temperature

Front 29

What is Polybase?

Back 29

Pre-blended suppository base that is a white solid consisting of a homogeneous mixture of PEGs and Polysorb 80

Front 30

What are PEGs incompatible with?

Back 30

1) Silver salts
2) Tannic Acid
3) Aminopyrine
4) Quinine
5) Ichthammol
6) Aspirin
7) Benzocaine
8) Iodochlorhydroxyquin
9) Sulfonamides

Front 31

What will crystallize out of PEG suppositories?

Back 31

1) Sodium Barbital
2) Salicylic Acid (will soften)
3) Camphor

Front 32

What should suppositories containing PEG not be stored/dispensed in?

Back 32

Polystyrene prescription vials

Front 33

What do you consider when selecting a suppository base?

Back 33

1) Intended use (local/systemic)
2) Route of administration
3) Patient comfort and compatibility
4) Stability

Front 34

Are fatty bases or PEG bases more comfortable for patients?

Back 34

Fatty bases -- bland and nonirritating to sensitive areas. PEG can give a stinging and burning sensation... and no one wants that down there

Front 35

What is the big drawback to PEG bases in rectal suppositories?

Back 35

Can cause a defecating reflex

This can be minimized by adding 10% water and moistening prior to insertion

Front 36

What is an example of the addition of another drug or compound lowering the melting point of a fatty base?

Back 36

Chloral hydrate in cocoa butter

Front 37

What is a concern about storage of fatty bases?

Back 37

Sensitivity to warm temperatures as they melt at body temp

Front 38

What routes are PEG bases preferred for?

Back 38

Vaginal and urethral - Lack sphincter muscles preventing leakage

Front 39

What dictates the release of the drug and onset of action?

Back 39

1) Liquefaction of the base
2) Dissolution of the active drug through the mucosal layers

Front 40

Is the choice of base critical in regard to local action?

Back 40

Nope

Front 41

What are the methods of suppository preparation?

Back 41

1) Hand Rolling
2) Compression Molding
3) Fusion Molding

Front 42

What is "Hand Rolling"?

Back 42

1) Simplest and oldest method
2) Only use cocoa butter

Front 43

What is the procedure for "Hand Rolling"?

Back 43

1) Grate base
2) Active ingredients are finely powdered or dissolve in alcohol
3) Knead active ingredents into base w/ mortar and pestle
4) Roll mass into cylindrical rod on pill tile
5) Cut rod into slices and blunt end with finger heat
6) Individually wrap

Front 44

What is the procedure for "Fusion Molding"?

Back 44

1) Melt the base
2) Disperse/dissolve the drug into the base
3) Pour mixture into mold
4) When congealed, remove from mold
5) Can be used with all types of suppositories

Front 45

What is "displacement"?

Back 45

When a drug displaces an amount of base, based on its density

Front 46

What happens when the density of the drug is the same as the base?

Back 46

It will displace an equivalent amount of base

Front 47

What happens when the density of the drug is greater than the base?

Back 47

It will displace a proportionally smaller weight of the base.

Front 48

What are "Displacement Factors"?

Back 48

Substances with different densities will occupy different volumes. This is important for fixed volume dosage forms as there is only a set amount of space for the drug/base

Front 49

Can you use a mold when it is cold or frozen?

Back 49

No - This can cause fractures and fissures

Front 50

What is the "Double-Cast Method of Suppository Preparation"?

Back 50

When the drug makes up a large amount of the dosage unit and there is no reported density factor for the drug in this base