suppositories

Question 1

what are suppositories

Answer 1

are solid dosage forms intended for insertion into body orifices where they melt, soften or dissolve and exert local or systemic effect.

Question 2

Latin supponere meaning “to place under” Suppositories are commonly used rectally and vaginally, and occasionally urethrally

Answer 2

ok

Question 3

how are different suppositories are inserted

Answer 3

Rectal suppositories are inserted with the fingers.
Certain vaginal suppositories (particularly the inserts or
tablets prepared by compression) may be inserted high
in the tract with the aid of an appliance.

Question 4

what is the rectal suppositories physical appearance

Answer 4

Rectal suppositories are usually about 32 mm (1.5
inches) long, are cylindrical, and have one or both end
tapered ( bullet- or torpedo-shaped)

Question 5

on what does the weight of the suppository depend on

Answer 5

density of the base and the medicinal agent in the
suppository.

Question 6

adult suppositories—-2g when we use cocoa butter
infant and children—– half the weight and pencil shaped
vaginal suppositories—— globular, oviform and con shaped

Answer 6

ok

Question 7

what are the local effects for rectal supps

Answer 7

– Relieve constipation.
– Relieve pain, itching and inflammation associated
with hemorrhoids.

Question 8

what do antihemorrhoidal supps contain

Answer 8

– Local anesthetics
– Vasoconstrictors
– Astringents
– Analgesics
– Soothing emollients
– Protective agents

Question 9

what do anticonstipation supps contains

Answer 9

glycerin suppositories that promote laxation by local
irritation of the mucous membranes (probably by the
dehydrating effect of glycerin on these membranes)

Question 10

what do we use local vaginal supps for

Answer 10

-Contraceptives: nonoxynol-9
– Antiseptics
– Specific agents to combat invading pathogens
and treatment of vaginitis caused different
microorganisms.

Question 11

do we use the vagina or rectum for systemic effects

Answer 11

rectum

Question 12

what are the advantages for using rectal supps for systemic effects

Answer 12

1. Drugs that are destroyed by the pH or enzymatic
   activity of the stomach or intestine need not to be
   exposed to these destructive environments.
2. Drug irritating to the stomach may be given without
   causing such irritation.
3. Drugs destroyed by portal circulation may bypass
   the liver after rectal absorption.
4. This route is convenient for administration of drugs
   to patients who are unable to swallow medications.
5. It is an effective route for treatment of patients with
   vomiting

Question 13

examples for systemic supps

Answer 13

– Prochlorperazine and chlorpromazine: relief
of nausea and vomiting
– Oxymorphone HCl: opioid analgesic
– Ergotamine tartrate: relief of migraine.
– Indomethacin: NSAID analgesic and
antipyretic.
– Ondansetron: relief of nausea and vomiting.

Question 14

what are the factors that controls absorpriton in rectal supps

Answer 14

– Physiological factors.
– Physicochemical factors of the drug and the
base.

Question 15

The human rectum is approximately 15 to 20 cm long.
–
When empty of fecal material, the rectum contains only
2 to 3 ml of inert mucous fluid.
–
In the resting state, the rectum is not motile; there is no
villi or microvilli on the rectal mucosa.

Answer 15

ok

Question 16

what are the physiological factors

Answer 16

1. The colonic content
2. The circulation route
3. The pH and lack of buffering capacity of rectal
   fluids.

Question 17

how does the colonic content effect absorption

Answer 17

Greater absorption (↑ systemic effects) may be
expected from a rectum that is void than from one
that is distended with fecal matter.
(make contact with the absorbing surface of the rectum and colon in an empty rectum.)

other factors
– Diarrhea
– Colonic obstruction due to tumorous growths
– Tissue dehydration.

Question 18

how does the circulation route effect absorption

Answer 18

bypass the portal circulation during their first pass into the general
circulation  enabling drugs otherwise destroyed in the liver to exert systemic effects.

– The lower hemorrhoidal veins surrounding the
colon receive the absorbed drug and initiates its
circulation throughout the body, bypassing the liver.

– Lymphatic circulation also assists in the
absorption of rectally administered drugs.

Question 19

how does the ph effect absorption

Answer 19

Rectal fluids are essentially neutral in pH (7.5 – 8),
and have no effective buffer capacity  the form in
which the drug is administered (salt or free form) will
not generally be chemically changed by the
environment.

Question 20

why do we use and for what do we use cocca butter

Answer 20

While cocoa butter melts rapidly at body temperature, Because of its
immiscibility with rectal fluids  it fails to release fat-soluble drugs readily. using a cocoa butter base, it is preferable to incorporate the ionized (salt) form rather than the unionized (free) form

For hydrophilic, water miscible bases such as,
glycerinated gelatin and polyethylene glycol, the free
form (unionized form) or the salt form can be used 
these bases themselves tend to dissolve slowly and
thus retard the release of the drug regardless of the
form. (

Question 21

why do we use and for what do we use cocca butter

Answer 21

While cocoa butter melts rapidly at body temperature, Because of its
immiscibility with rectal fluids  it fails to release fat-soluble drugs readily. using a cocoa butter base, it is preferable to incorporate the ionized (salt) form rather than the unionized (free) form

For hydrophilic, water miscible bases such as,
glycerinated gelatin and polyethylene glycol, the free
form (unionized form) or the salt form can be used 
these bases themselves tend to dissolve slowly and
thus retard the release of the drug regardless of the
form. (

Question 22

what are the physicochemical factors

Answer 22

1. The relative solubility of the drug in lipid and in
   water:
2. Particle size of the dispersed drug:
3. Nature of the base:

Question 23

how does the particle size effect the absorption

Answer 23

 ↓in particle size  ↑ surface area, A
 ↑ surface area, A  ↑ increases dissolution
rate.
 ↑ increases dissolution rate  ↑ in rapid
absorption

Question 24

– As mentioned previously, water soluble bases (e.g.,
polyethylene glycol) that dissolves in the rectal fluids
releases for absorption both, water-soluble and lipidsoluble drugs.
– The more drug a base contain  the more drug will
be available for absorption.
until saturation

Answer 24

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Question 25

what are the properties of a good base

Answer 25

1. The base should be solid at room temperature, but must be capable of melting, softening or dissolving at body temperature to release the drugs for absorption 2. The base should not interact or complex with the drug  this will slow or even prevent drug release. 3.t should not irritate the mucous membrane of the rectum  this will initiate a colonic response and cause bowel movement. This will lead to elimination of the drug product outside the body

Question 26

give an example for long acting supps

Answer 26

morphine sulfate in slow-release suppositories. It can be compounded by the pharmacist by including alginic acid in the base which will prolong the release of morphine over several hours.

Question 27

give examples on the advantages of diffirent bases

Answer 27

cocoa butter melts quickly at body temperature and would release drugs very fast. Cocoa butter will give excellent release of water-soluble drugs. When irritation or inflammation is to be relieved (such as in hemorrhoids), cocoa butter appears to be the superior base because of its emollient or soothing effects. Fat soluble drugs seems to be more readily released from bases such as glycerinated gelatin and PEG.However, glycerinated gelatin and PEG bases dissolves slowly in body fluids. The release therefore is not as fast as for water-soluble drugs from cocoa butter base

Question 28

give examples on the advantages of diffirent bases

Answer 28

cocoa butter melts quickly at body temperature and would release drugs very fast. Cocoa butter will give excellent release of water-soluble drugs. When irritation or inflammation is to be relieved (such as in hemorrhoids), cocoa butter appears to be the superior base because of its emollient or soothing effects. Fat soluble drugs seems to be more readily released from bases such as glycerinated gelatin and PEG.However, glycerinated gelatin and PEG bases dissolves slowly in body fluids. The release therefore is not as fast as for water-soluble drugs from cocoa butter base

Question 29

what are the diffrent classes for bases

Answer 29

A. Fatty or oleaginous bases B. Water-soluble or water-miscible bases C. Miscellaneous bases: usually a combination of lipophilic and hydrophilic substances.

Question 30

give examples for fatty bases

Answer 30

cocca butter – Hydrogenated fatty acids of vegetable oils such as palm kernel oil and cottonseed oil. – Compounds containing glycerin with high￾molecular weight fatty acids(e.g., palmitic acid and stearic acid): examples include glyceryl monopalmitate and glyceryl monostearate

Question 31

talk about cocca butter

Answer 31

– Defined as the fat obtained from the roasted seed of theobroma cacao. – Appearance: at room temperature it is a yellowish white solid having a faint, agreeable chocolate-like odor – Chemical composition: it is a triglyceride primarily of oleopalmitostearin and oleodistearin. – Melting point: 30 to 36 C. – Because of its melting point, it is an ideal base as it melts just below the body temperature and yet maintaining solidity at usual room temperatures. – However, because of its triglyceride content, it exhibits marked polymorphism (existence in several crystalline forms). should be melt at 23 in a warm water bath Substances such as phenol and chloral hydrate have a tendency to lower the melting point of cocoa butter. – If the melting point is low enough (because of additives) that it is not feasible to prepare a solid suppository using cocoa butter alone as the base  solidifying agents like cetyl esters wax (~20%) or beeswax (~40%) may be melted with the cocoa butter to compensate for the softening effect of the added substance. – However, the hardening agent: • Must not be so excessive as to prevent the base from melting in the body • Must not interfere with the therapeutic agent in any way or alter the efficacy of the product.

Question 32

give examples for water soluble bases

Answer 32

– Glycerinated gelatin – Polyethylene glycol

Question 33

talk about Glycerinated gelatin

Answer 33

– Prepared by dissolving granular gelatin (20%/) in glycerin and adding water or a solution or a suspension of the medication (10%). – Most frequently used in preparation of vaginal suppositories  where prolonged action of the medicinal agent is usually desired – The reason of the prolonged action is that the glycerinated gelatin base is slower to soften and mix with the physiological fluids than is cocoa butter  slower drug release. – Glycerinated gelatin-based suppositories have a tendency to absorb moisture as a result of the hygroscopic nature of glycerin  they must be protected from atmospheric moisture if they are to maintain their shape and consistency. – Also a result of hygroscopicity, the suppository has a dehydrating effect and may irritate the tissue upon insertion. the water in the formula for the suppositories minimizes this effect.

Question 34

talk about polyethylene glycol

Answer 34

– Polymers of ethylene oxide and water – It is prepared at various: –Chain lengths –Molecular weights –Physical states – The are available in a number of molecular weight ranges, the most commonly used are summarized in the table 1. – Note: the numeric designation refers to the average molecular weight of each of the polymers. – Various combination of these polyethylene glycols may be combined by fusion Polyethylene glycol suppositories do not melt at body temperature but rather dissolve slowly in the body’s fluids. Therefore, the base need NOT to be formulated to melt at body temperature.

Question 35

what are the advantages of PEG

Answer 35

• Permits slower release of the medication from the base once the suppository is inserted. • Permit convenient storage of these suppositories without the need for refrigeration and without danger of softening excessively in warm weather. • Permits slow insertion without fear that they would melt in the fingertip (as cocoa butter suppositories sometimes do).

Question 36

what are miscellaneous bases

Answer 36

• These are mixtures of oleaginous and water-soluble or water-miscible materials. • These mixtures may be chemical or physical mixtures. • Some of these materials are preformed emulsions (generally w/o type) or they are capable of dispersing in aqueous fluids and making emulsions. • Example: polyoxyl 40 stearate.

Question 37

talk about Polyoxyl 40 stearate

Answer 37

it is a surface active agent that is employed in a number of commercial suppositories. – Compositions: it is a mixture of the following: • Monostearates ester of mixed polyoxyethylene diols. • Distearates ester of mixed polyoxyethylene diols. • Free glycols. – The average polymer length is about 40 oxyethylene units. – Appearance: it is white to light tan waxy solid – It is water soluble. – Melting point: 39 – 45 C.

Question 38

what are the methods of prepearing supps

Answer 38

1. Molding from a melt. 2. Compression 3. Hand rolling and shaping

Question 39

how do we prepare by molding

Answer 39

1. Melting the base. 2. Incorporating any required medicaments. 3. Pouring the melt into the mold. 4. Allowing the melt to cool and congeal into suppositories. 5. Removing the formed suppositories from the mold. • Most bases are suitable for preparation by molding such as, cocoa butter, glycerinated gelatin, polyethylene glycol.

Question 40

how do we prepare by molding

Answer 40

1. Melting the base. 2. Incorporating any required medicaments. 3. Pouring the melt into the mold. 4. Allowing the melt to cool and congeal into suppositories. 5. Removing the formed suppositories from the mold. • Most bases are suitable for preparation by molding such as, cocoa butter, glycerinated gelatin, polyethylene glycol.

Question 41

what are the diffirent molds

Answer 41

– Commercially available molds can produce individual or large numbers of suppositories of various shapes and sizes. – Plastic mold may be used to produce as little as a single suppository. – Metal molds that are commonly used for pharmacy or laboratory scale production are capable of producing 6, 12, or more suppositories in a single operation. – Industrial molds produce hundreds of suppositories in a single batch.

Question 42

what are the trades of now days molds

Answer 42

– Molds in common use today are made of stainless steel, aluminum, brass, or plastic. – The molds usually separates into sections, generally longitudinally. – The molds are opened for cleaning before and after preparation of a batch of suppositories. – The molds are closed when the melt is poured and opened again to remove the cold molded suppositories. – Care must be taken during cleaning the molds as any scratches on the molding will take away from the desired smoothness of the suppositories. It may cause the suppository to stick on the mold and get damaged while removing from the mold.

Question 43

why do we lubricate the molds

Answer 43

– Suppository molds may require lubrication before the melt is poured to facilitate clean and easy removal of the molded suppositories. This will depend on the formulation – When cocoa butter or polyethylene glycol are used as base, lubrication is usually unnecessary  these materials contract sufficiently on cooling to separate from the inner surfaces of the mold and allow easy removal. – Lubrication is necessary when glycerinated gelatin is used as the base. – A thin coating of mineral oil applied with the finger to the molding surfaces usually suffice.

Question 44

why do we and how do we calibrate molds

Answer 44

we calibrate them because the diffrence in density 1. Prepare molded suppositories from base material alone. 2. Remove the suppository from the mold. 3. Weigh the suppositories: record the total weight and the average weight. 4. The suppositories are then carefully melted in a calibrated beaker 5. Determine the volume for the total number as well as the average of one suppository.

Question 45

remember df= weight of the drug\the weight of the base dispalced

Answer 45

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