CHAPTER 12

SUPPOSITORIES, INSERTS, AND STICKS

1. Define suppositories and give the origin of the terms.

A suppository is a solid dosage form wherein 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 effect. The term suppository is derived from the Latin supponere,
meaning “to place under,” as derived from sub (under) and ponere (to place). Thus,
suppositories are meant both linguistically and therapeutically to be placed under the body,
as into the rectum.
2. Define inserts and sticks.
An insert is a solid dosage form that is inserted into a naturally occurring (nonsurgical)
body cavity other than the mouth or rectum, including the vagina and urethra. Medication
sticks are a convenient form for administering topical drugs. Their development is interesting
because it involves the history of cosmetics, which parallels human history.
3. Compare and contrast various suppository, inserts, and stick dosage forms in terms of
physical appearance, size, and shape.
Suppositories have various shapes and weights; the shape and size of a suppository must
be such that it can be easily inserted into the intended orifice without causing undue
distension, and once inserted, it must be retained for the appropriate period. Rectal
suppositories are usually about 32 mm (1.5 in) long, are cylindrical, and have one or both
ends tapered. Some rectal suppositories are shaped like a bullet, a torpedo, or the little
finger. Depending on the density of the base and the medicaments, the weight of the
suppository may vary. Adult rectal suppositories weigh about 2 g when cocoa butter is
employed as the base. Rectal suppositories for use by infants and children are about half the
weight and size of the adult suppositories and assume a more pencil-like shape.
Vaginal inserts are usually globular, oviform, or cone shaped and weigh about 5 g when
cocoa butter is the base. However, depending on the base and the manufacturer’s product,
the weight of vaginal inserts may vary widely.
 Urethral inserts are slender, pencil-shaped suppositories. Male urethral suppositories
may be 3 to 6 mm in diameter and approximately 140 mm long, although this may vary.
When cocoa butter is employed as the base, these suppositories weigh about 4 g. Female
urethral suppositories are about half the length and weight of the male urethral suppository,
being about 70 mm long and weighing about 2 g when made of cocoa butter.
Medication sticks are cylindrical in shape and generally range from 5 to 25 g. They are
generally packaged in an applicator tube for topical administration, and the applicator can
be adjusted to continually expose new, fresh stick from inside the tube.
4. Describe the advantages and disadvantages of suppository, insert, and stick drug delivery
versus oral drug delivery.
The advantages include first-pass effect, drug stability, and ability to administer large
doses of drugs, irritating drugs, unpleasant tasting or smelling drugs, or drugs with
objectionable taste or odor (especially important in children). It is also useful in children
because an ill child may refuse oral medication and may fear injections. Additionally, it is
advantageous in patients experiencing nausea and vomiting or when the patient is
unconscious, and when there is a presence of disease in the upper gastrointestinal tract that
may interfere with drug absorption. Rapid drug effect systemically can be achieved through
rectal administration. On the other hand, its disadvantages include the following: (a) a
perceived lack of flexibility regarding dosage of commercially available suppositories
resulting in underuse and a lack of availability, (b) suppositories may be expensive, (c)
suppositories exhibit variable effectiveness, depending upon many factors, (d) different
formulations of a drug with a narrow therapeutic margin cannot be interchanged without
risk of toxicity, (e) the bullet-shaped suppository after insertion can leave the anorectal site
and ascend to the rectosigmoid and descending colon, (f) defecation may interrupt the
absorption process of the drug, (g) the absorbing surface area of the rectum is much smaller
than that of the small intestine, (h) the fluid content of the rectum is much less than that of
the small intestine, which may affect dissolution rate, (i) possibility of degradation of some
drugs, (j) the dose of a drug required may be greater than or less than the dose of the same
 drug given orally, and (k) anatomic and physiologic factors and physicochemical factors of
the drug and the base may affect the rectal absorption of a drug administered.
5. Some localized actions for specific suppositories?
• 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.
• Glycerin suppositories promote laxation by local irritation of the mucous membranes,
probably by the dehydrating effect of the glycerin on those membranes.
• Sticks are commonly used for local effect and include hydration/emollient, antibacterial,
sunscreen, antipruritic, and other uses.
6. Pessaries and bougies
• Pessaries or vaginal suppositories intended for local effects are employed mainly as
contraceptives, as antiseptics in feminine hygiene, and as specific agents to combat an
invading pathogen.
• Urethral suppositories or bougies may be antibacterial or a local anesthetic preparative
for a urethral examination.
7. Some suppositories having systemic effects?
• Prochlorperazine and chlorpromazine are used for the relief of nausea and vomiting and
as a tranquilizer.
• Morphine and oxymorphone are used for opioid analgesia.
• Ergotamine tartrate is used for the relief of migraine syndrome.
• Indomethacin is a nonsteroidal anti-inflammatory analgesic and antipyretic.
• Ondansetron is for the relief of nausea and vomiting,
8. Explain the physiological factors of rectal drug absorption and vaginal/urethral insert
administration
 a. Circulation route: Drugs absorbed rectally can bypass the portal circulation. This
enables drugs that are otherwise destroyed in the liver to exert systemic effects.
b. pH and lack of buffering capacity of the rectal fluids: The pH of the rectal fluid is
generally in the range of 7.2 to 7.4, and it has negligible buffer capacity. The form
in which the drug is administered will not generally be chemically changed by the
rectal environment, therefore, the pH of the medium may be determined by the
characteristics of the drug.
c. Colonic content: When systemic effects are desired from the administration of a
medicated suppository, greater absorption may be expected from a rectum that
is void than from one that is distended with fecal matter. Other conditions such
as diarrhea, colonic obstruction due to tumorous growths, and tissue dehydration
can all influence the rate and degree of drug absorption from the rectal site.
9. The physicochemical factors that influence absorption for the following:
a. Drug
• The lipid-water partition coefficient of a drug is an important consideration in
the selection of the suppository base and in anticipating drug release from
that base.
• The smaller the particle size of the drug, the greater the surface area, the
more readily the dissolution and the greater chance for rapid absorption.
b. Suppository/insert base
• Nature of the base: The base must be capable of melting, softening, or
dissolving to release its drug for absorption. If the base interacts with the drug
to inhibit its release, drug absorption will be impaired or even prevented. Also,
if the base irritates the mucous membranes of the rectum, it may initiate a
colonic response and prompt a bowel movement, eliminating the prospect of
complete drug release and absorption. For most purposes, it’s convenient to
classify suppository bases according to their physical characteristics into two
main categories and a third miscellaneous group: (a) fatty or oleaginous bases,
 (b) water-soluble or water-miscible bases, and (c) miscellaneous bases,
generally combinations of lipophilic and hydrophilic substances.
10. The advantages and disadvantages of using cocoa butter as suppository base
Its advantage is that it is in ideal suppository base because it melts just below body
temperature and yet maintaining its solidity at usual room temperatures. It also appears to
be the superior base when irritation or inflammation is to be relieved because of its emollient
or soothing, spreading action. However, it exhibits polymorphism. Thus, when cocoa butter
is hastily or carelessly melted at a temperature greatly exceeding the minimum required
temperature and is then quickly chilled, the result is a metastable crystalline form with a
melting point much lower than that of the original cocoa butter. In fact, the melting point
may be so low that the cocoa butter will not solidify at room temperature. Cocoa butter must
be slowly and evenly melted, preferably over a bath of warm water, to avoid formation of
the unstable crystalline form and ensure retention in the liquid of the more stable beta
crystals that will constitute nuclei upon which the congealing may occur.
11. Enumerate the 3 methods of preparing suppositories/insert/stick.
a. Fusion molding: Suppositories are prepared using molding by melting the bases
and pouring into molds for shaping. They are allowed to cool and solidify to
produce the medication.
b. Compression molding: Suppositories are prepared using compression by applied
pressure to the mass placed in a cylinder. This method is preferable for heat-labile
medicaments.
c. Hand rolling and shaping: It is the traditional and simplest method where drugs
are mixed into the base and are consequently kneaded and triturated. The
resulting mass is then cut into several pieces and molded by hand to desired
shape.
12. The different steps in the preparation of suppositories by molding?
The steps in molding include (a) melting the base, (b) incorporating any required
medicaments, (c) pouring the melt into molds, (d) allowing the melt to cool and congeal into
suppositories, and (e) removing the formed suppositories from the mold.
13. When and why do suppository molds require lubrication
Even though cocoa butter is usually used and allow for clean removal from molds, adding
lubricants prevent chances of adherence to mold walls. This is mainly done for glycerinated
gelatin by using a thin layer of mineral oil.
14. Uses of glycerin suppositories?
Glycerin suppositories promote laxation by local irritation of the mucous membranes,
probably by dehydrating effect of the glycerin on those membranes. It is used to treat
occasional constipation or to cleanse the bowel before a rectal exam or other intestinal
procedure.
15. Generate a listing of key counseling points a pharmacist should share with the patient
prescribed a drug in a suppository/insert/stick drug delivery system
• The pharmacist must take into account the active drug and the method of application.
• Patients should be instructed on how to properly store the suppository, unwrap a
wrapped suppository, and resolidify a melted suppository.
• The pharmacist should discuss the proper method of disposing of unused suppositories.
• Generally, the patient should be told to apply the stick only to the involved area and not
to the surrounding skin.
• The patient should apply the medication liberally over the area but only as needed.
• The surface of the stick should be cleaned with a tissue after each use, and, to avoid
transmitting infection, the product should not be shared with others.
16. Give the appropriate packaging and storage condition for suppositories.
• Glycerin suppositories and glycerinated gelatin suppositories are packaged in tightly
closed glass containers to prevent a change in moisture content. They can be stored at
controlled room temperature.
• Suppositories prepared from a cocoa butter base are usually individually wrapped or
otherwise separated in compartmented boxes to prevent contact adhesion. They must
be stored below 30oC and preferably in a refrigerator.
• Suppositories containing light-sensitive drugs are individually wrapped in an opaque
material such as a metallic foil.
• Most commercial suppositories are individually wrapped in either foil or plastic. Some
are packaged in a continuous strip, separated by tearing along perforations.
Suppositories are also commonly packaged in slide boxes or in plastic boxes.
• Suppositories made from a base of polyethylene glycol may be stored at usual room
temperatures.
• Suppositories must not be stored in high humidity to prevent absorption of moisture nor
in places of extreme dryness to prevent moisture loss.