d.

Vaginal or Pessary
SUPPOSITORIES - Larger, more or less globular in form, weighs 5 g.
- Pessary is also applied to an instrument inserted into the
- Suppositories are solid dosage forms intended for insertion into
vagina to support the uterus
body orifices where they melt, soften or dissolve and exert local
- Usually globular, oviform or cone-shaped
or systemic effects.
- The word suppository is from the Latin supponere, meaning “to
place under” as derived from sub (under) and ponere (to place)
- Solid dosage forms in which one or more APIs are dispersed in a
suitable base and molded or otherwise formed into a suitable
shape for insertion into the rectum to provide local or systemic
effects.

Types of Suppositories:
a. Urethral Suppositories
- aka Bougie or bacillum or cereolus
- Slender, Pencil-shaped which actually weighs about 2 g and
are 7 cm (2 inches) long for female, and for male it weighs
about 4 g and measure 14 cm (5 inches)
- Bougie is also shaped to an instrument which is inserted into Uses and Applications:
the urethra or other body passages for the purpose of
1. First Pass Effect
dilatation or exploration.
- Avoiding, at least partially, the FPE that may result in higher
blood levels for those drugs subject to extensive first-pass
metabolism upon oral administration.
b. Nasal or Burginarium
2. Drug Stability
- Same as urethral but shorter and thinner
- Avoiding the breakdown of certain drugs that are
susceptible to gastric degradation
c. Rectal Suppository
3. Large Dose Drugs
- More or less conical with rounded apex, which weighs 2 g
- Ability to administer somewhat larger doses of drugs than
for adult and one half for infants
using oral administration
- Rectal suppositories are usually about 32 mm (1.5 inch) long,
4. Irritating Drugs
are cylindrical, and have one or both ends tapered. Some
- Ability to administer drugs that may have an irritating effect
rectal suppositories are shaped like a bullet, a torpedo or the
on the oral or gastrointestinal mucosa when administered
little finger.
orally.
- Rectal suppositories for use by infants and children are
5. Unpleasant tasting or smelling drugs
about half the weight and size of the adult suppositories and
- Ability to administer unpleasant tasting or smelling drugs
assume a more pencil-like shape
whose oral administration is limited.

Pharm 201 Laboratory | Duyen Page 1|5

 6. In children, the rectal route is especially useful. An ill child may
refuse oral medication and may fear injections.
7. In patients experiencing nausea and vomiting or when the patient
is unconscious
8. The presence of disease of the upper GIT that may interfere with
drug absorption.
9. Objectionable taste or odor of a drug (especially important to
children)
10. Achievement of a rapid drug effect systematically (as an alternate
to injection)
Disadvantages of Suppositories
1. A perceived lack of flexibility regarding dosage of commercially
available suppositories resulting in underuse and a lack of
availability.
2. If suppositories are made on demand, they may be expensive.
3. Suppositories as a dosage form are safe, but they exhibit variable
effectiveness.
4. Different formulations of a drug with a narrow therapeutic
margin, such as aminophylline, cannot be interchanged without
risk of toxicity.
5. The “bullet-shaped” suppository after insertion can leave the
anorectal site and ascend to the rectosigmoid and descending
colon. Hence, one may consider suppositories with this shape
should not be used at bedtime
6. Defecation may interrupt the absorption process of the drug; this
may especially occur if the drug is irritating.
7. The absorbing surface area of the rectum is much smaller than
that of the small intestine.
8. The fluid content of the rectum is much less than that of the small
intestine, which may affect dissolution rate
9. There is the possibility of degradation of some drugs by the
microflora present in the rectum.
10. The dose of the drug required for rectal administration may be
greater than or less than the dose of the same drug given orally.
This can be dependent upon such factors as the constitution and
condition of the patient, the physicochemical nature of the drug
Pharm 201 Laboratory | Duyen
and its ability to traverse the physiologic barriers to absorption ad
the nature of the suppository vehicle and its capacity to release
the drug and make it available for absorption
Local Action
- Once inserted, the suppository base melts, softens or dissolves,
distributing its medicaments to the tissues of the region.
- Rectal suppositories intended for local action are most frequently
used to relieve constipation or the pain, irritation, itching and
inflammation associated with hemorrhoids or other anorectal
conditions.
- Antihemorrhoidal suppositories frequently contain a number of
components, including local anesthetics, vasoconstrictors,
astringents, analgesics, soothing emollients, and protective
agents.
- A popular laxative, glycerin suppositories promote laxation by
local irritation of the mucous membranes, probably by the
dehydrating effect of the glycerin on those membranes.
- Vaginal suppositories or inserts intended for local effects are
employed mainly as contraceptives, as antiseptics in feminine
hygiene and as specific agents to combat invading pathogens.
Most commonly the drugs used are nonoxynol 9 for
contraception, trichomonacides to combat vaginitis caused by
__________________________, antifungals to treat
_____________________, and anti-infectives/ antibiotics
directed at other microorganisms
Systemic Action
- The mucous membranes of the rectum and vagina permit the
absorption of so many soluble drugs. Although the rectum is used
frequently as the site for systemic absorption of drugs, the vagina
is not as frequently used for this purpose.
Examples of Rectal Suppositories
Suppository Commercial Product Type of Effect
Bisacodyl Dulcolax Local
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 Hydrocortisone Anusol-HC Local - Cocoa butter is softened when phenol, camphor, chloral hydrate,
Hydromorphone Dilaudid Systemic volatile oils or similar substances from the medicating ingredients,
Indomethacin Indocin Systemic however, this is remedied by the addition of wax, spermaceti, etc.
Mesalamine Canasa Local to raise the melting point of cacao butter in the warmest weather.
Promethazine Phenergan Systemic
Paracetamol Opigesic Systemic Question: Why should Cocoa Butter, NF be melted slowly and
Faktu evenly?
Glycerin

_______________________________________________________ - Reading Assignment: Please read the examples of Fatty or

Oleaginous Bases in Table 12.5, page 372 of your Ansel.
Classification of Suppository Bases
A suppository base should be: Water-Soluble or Water-Miscible Base
1. Physically and chemically stable
- Water-soluble or water-miscible
2. Nonirritating
- Glycerinated gelatin and polyethylene glycols
3. Non-toxic
- Glycerinated Gelatin suppositories may be prepared by dissolving
4. Non-senstizing
granular gelatin (20%) in glycerin (70%) and adding water or a
5. Chemically and physiologically inert
solution or suspension of the medication (10%)
6. Compatible with a variety of drugs
- Glycerinated gelatin is frequently used in the preparation of vaginal
7. Stable during storage
suppositories, with which prolonged local action of the medicinal
8. Aesthetically acceptable (free from objectionable odor and a
agent is usually desired. The glycerinated gelatin base is slower to
pleasing appearance)
soften and mix with the physiologic fluids than is cocoa butter and
therefore provides a slower release.
Fatty or Oleaginous Base Question: What are the consequences of the hygroscopic nature of
- Fatty bases are the most frequently employed suppository bases, glycerin?
primarily because cocoa butter is a member of this group of
substances. _______________________________________________________
- Theobroma oil (Scientific name of the plant source?) or Cocoa
Preparation of Suppositories
Butter, NF, acts by melting at body temperature. At room
temperature, it is a yellowish-white solid having a faint agreeable - Suppositories are prepared by two methods:
chocolate-like odor. It is a bland, non-irritating fat, pressed from a. Molding from a melt
ground cacao beans, possessing remarkable quality of maintaining b. Hand rolling and shaping
its firmness, even exceptional hardness for a fatty substance, to - The method most frequently employed both on a small scal e and
within a few degrees of the body temperature, when it readily melts on an industrial scale is molding
to a liquid without passing through an appreciable softening stage.
- Melting point of Theobroma oil is 30°C to 35°C (86° to 95°F) making A. Molding
it an ideal suppository base melting at just below body temperature Steps:
and yet maintaining its solidity at usual room temperatures. a. Melting the Base
Pharm 201 Laboratory | Duyen Page 3|5
 b. Incorporating any required medicaments
c. Pouring the melt into molds
d. Allowing the melt to cool and congeal into suppositories
e. Removing the formed suppositories from the mold

Suppository Molds
- Commercially available molds can produce individual or large
numbers of suppositories of various shapes and sizes.
- Molds in common use today are made from stainless steel,
aluminum, brass, or plastic. The molds which separate into
sections, generally longitudinally, are opened for cleaning before
and after preparation of a batch of suppositories, closed when the
melt is poured, and opened again to remove the cold molded
suppositories
- Care must be exercised in cleaning the molds, as any scratches on
the molding surfaces will take away from the desired smoothness
of the suppository. Plastic molds are especially prone to scratching
Example of a hinged mold

Types of Molds:
1. The white, metal, individual type of mold. The draw backs to
the use of these forms are the difficulty to quickly and easily
removing the suppository, the trouble in cleaning the molds
and the liability of losing or misplacing them.
2. Divided Mold – AN elastic band holds the sections together
but the hinged is better
3. Hinged Mold – Constructed to produce 1 or 2 different sizes
of suppository. The manner of using it is similar to that of the
preceding molds

Example of a rubber mold

Lubrication of the Molds

- Suppository molds may require lubrication before the melt is
poured to facilitate clean and easy removal of the molded
suppository.
- Lubrication is seldom necessary when the base is
_________________ or ___________________, as these
Pharm 201 Laboratory | Duyen Page 4|5
 materials contract sufficiently on cooling to separate from the
inner surfaces and allow easy removal.
- Lubrication is usually necessary with glycerinated gelatin
- A thin coating of mineral oil applied with the finger to the molding
surfaces usually suffices. However, no material might irritate the
Packaging and Storage
mucous membranes should be employed as a mold lubricant
Preparing and Pouring the Melt
- Stir the melted mass and pour into a chilled mold, lightly
lubricated with mineral oil. Fill each opening of the mold exactly
and uniformly or the openings may all be overflowed so that the
tops run together on the mold. In the latter case, stand the mold
on the counter until the mass on top has solidified, then cut off
excess with a spatula.
- Place mold on ice and when sufficiently hardened suppositories
will be found to have contracted slightly so that light pressure on
the base of each suppository will cause it to loosen in the mold
and readily drop out when the mold is open. Never apply
continued pressure when removing the suppository as it will
cause it to melt. Cool the thumb by placing it on ice for a moment,
before giving the quick, firm pressure.
- Another good practice is to cool the suppository molds in the
freezing cabinet of the refrigerator. This method does not only
guarantee the cold mold but the degree of coldness is such that it
is not necessary to use a lubricant upon the mold, since the
suppository can usually be emptied from the mold without the
necessity of even opening it.
Pharm 201 Laboratory | Duyen
B. Hand Rolling and Shaping
- Hand rolling and shaping is a historic part of the art of the
pharmacist.
- Glycerin suppositories and glycerinated gelatin suppositories re
packaged in tightly closed glass containers to prevent a change in
moisture content.
- Suppositories prepared from a cocoa butter base are usually
individually wrapped or otherwise separated in compartmented
boxes to prevent contact and adhesion
- Suppositories containing light sensitive products are individually
wrapped in an opaque material such as a metallic foil
- Cocoa butter suppositories must be stored below
_________________ and preferably in a refrigerator.
- Glycerinated gelatin suppositories can be stored at
______________________
- Excessive softening is the major indication of instability in
suppositories, although some suppositories may dry out and
harden or shrivel. Evidence of oil stains on packaging material
should warn the pharmacist to examine individual suppositories
more closely be removing any foil covering. As a general rule,
suppositories should be stored in a refrigerator.
Question: What happens when a suppository is stored in high
humidity?
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