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SUPPOSITORIES, INSERTS, AND STICKS • Rectal Suppository

− Relieve constipation
SUPPOSITORY − Relieve pain, irritation, itching, and
• Latin: supponere; means to place under (sub inflammation associated with
– under; ponere – to place) hemorrhoids/anorectal conditions
• Solid dosage form in which API’s are
dispersed in a suitable base and molded into *see table 12.1 for examples*
a suitable shape
• Intended for insertion into body orifices • Vaginal Suppositories or Inserts
where they melt, soften, or dissolve − pessaries
• Exert local or systemic effects − Contraceptives, antiseptics

INSERTS Examples:
• Solid dosage form inserted into a naturally Nonoxynol 9 Contraception
occurring or nonsurgical body cavity rather Combat vaginitis
than the mouth or rectum, including the caused by
Trichomonacides
vagina and urethra Trichomonas
Vaginalis
Treat Candida
STICKS Antifungals
(Monilia) albicans
• Convenient form for administering topical Directed at other
Anti-infectives/antibiotics
drugs organisms
• Local effect
• hydration/emollient, antibacterial, sunscreen, *see table 12.2 for more examples*
antipruritic
• Involves the history of cosmetics • Urethral Inserts
− bougies
DIFFERENCES IN TERMS OF APPEARANCE, SIZE, − Antibacterial, local anesthetic
AND SHAPE
Appearance Size Shape Systemic Action
• Mucous membrane of the rectum and vagina
Suppositories Have one or permit the absorption of many soluble drugs.
32 mm cylindrical
a. Rectal both ends
tapered • NOTE: Rectum is used frequently as the site for
Globular, the systemic absorption of drug (vagina is nor
Inserts 5 g (with
oviform or frequently used)
a. Vaginal cocoa
cone
(pessaries) butter base
shaped
Male: 3- Examples:
6mm Prochlorperazine & Tranquilizer; relief of
diameter; Chlorpromazine N&V
b. Urethral 140mm Pencil-
(bougies)
slender Morphine &
long shaped Opioid analgesia
Oxymorphone
Female: 70 Indomethacin Analgesic, antipyretic
mm long Relief of migraine
Packed in Ergotamine tartrate
syndrome
Sticks applicator 5-25 g cylindrical
tubes
Ondansetron Relief of N&V
Hydromorphone Analgesic
Antihistamine,
USES AND APPLICATIONS OF SUPPOSITORIES Promethazine HCl
antiemetic, sedative
Local Action
• Once inserted, suppository base melts, softens FACTORS OF DRUG ABSORPTION FROM RECTAL
or dissolves. SUPPOSITORIES
• Medicaments are distributed to the tissues of Physiological Factors
the region. • Circulation Route
− Intended for retention within the cavities − Drugs absorbed rectally can bypass the
(local effect) portal circulation during their first pass
− Intended to be absorbed (systemic into the general circulation, which
effects)

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enables drugs that are otherwise
destroyed in the liver to exert systemic COCOA BUTTER AS SUPPOSITORY BASE
effects.
− The lower hemorrhoidal veins then Too fine particles
initiate its circulation throughout the
body, bypassing the liver.
− Lymphatic circulation assists absorption
of rectally administered drugs
high increase of viscosity of the melted
excipient
• 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 use of excessively small particles + possible
negligible buffer capacity difficulties in flow during production
Advantages:
• Colonic Content
1. melts at 30°C to 36°C (86°F to 97°F); melts
− A drug will have greater opportunity to
below body temperature, maintaining its
make contact with the absorbing
solidity
surface of the rectum and colon in the
2. has a metastable condition that allows slow
absence of the fecal matter
transition to the more stable beta form of
− Evacuant enema may be administered crystals having the greater stability and a
and allowed to act before the higher melting point
administration of a suppository 3. superior base for treating anorectal
PHYSIOCHEMICAL FACTORS AND DRUG EFFECTS disorders
Physicochemical factors of the bases include its:
a. ability to melt Disadvantages:
b. soften or dissolve at body temperature 1. immiscible with body fluids
c. ability to release drug substance 2. have little tendency to enter the aqueous
d. hydrophilic and hydrophobic character physiologic fluids
3. exhibits marked polymorphism or existence
• Lipid-Water Solubility in several crystalline forms
− Important consideration in the
PREPARATION OF SUPPOSITORIES
selection of the suppository base and
1. Molding from a melt
in anticipating drug release from that
a. Melting the base
base
b. incorporating any required
− Lipophilic drug
medicaments
✓ distributed in a fatty suppository
c. Pour the melt into the mold
base in low concentration
d. cool ang congeal into suppositories
✓ has less tendency to escape to
e. Remove formed suppositories
the surrounding aqueous fluids
than a hydrophilic substance in a
NOTE: Cocoa butter, glycerinated gelatin
fatty base
and polyethylene glycol are suitable for this
− NOTE: The more drug a base contains,
preparation.
the more drug it will be available for
absorption.
Lubrication of the Mold
• Lubricants are necessary for
• Particle Size
suppositories (usually with
− Size of the drug particle will influence
glycerinated gelatin), in order to
its rate of dissolution and its availability
facilitate clean and easy removal of
for absorption
the molded suppositories.
− NOTE: The smaller the particle, the
• A thin coating of mineral oil applied
greater the surface area, the more
with the finger to the molding surfaces
readily the dissolution of the particle
(suffices).
and the greater the chance for rapid
• However, it us seldom necessary for
absorption.
suppositories with cocoa butter or

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polyethylene glycol as its base as they
contract sufficiently when cooled and
easier to remove from the mold

2. Hand Rolling & Shaping


− Historic part of the art of the
pharmacist
− With the availability of suppository
molds, there is a little requirement
for today’s pharmacists to shape
suppositories by hand

GLYCERIN SUPPOSITORIES
• popular laxatives
• Promote laxation by local irritation of the
mucous membranes through the dehydrating
effect of the glycerin on those membranes.

CLINICAL CONSIDERATIONS
Regarding suppositories, patients should be
informed about the following:
1. proper storage conditions for both
prescription and nonprescription products
2. how to unwrap a wrapped suppository
3. how to resolidify a melted suppository
4. proper insertion of the suppository
5. reasonable estimate of the time after which
the medication should be discarded
suggested by the pharmacist

DIFFERENT TYPES OF PACKAGING AND STORAGE


CONDITIONS
tightly closed glass
Glycerin/Glycerinated containers to prevent
Gelatin Suppository alteration in moisture
content

individually wrapped;
separated in
Cocoa Butter Based
compartmented boxes
Suppository
to prevent contact or
adhesion

individually wrapped in
Suppository Containing
an opaque material
Light Sensitive Drugs
such as metallic foil

individually wrapped in
either foil or plastic
Other Commercial in continuous strip,
Suppositories separated by tearing
along perforations
slide or plastic boxes

NOTE: Suppositories must be stored in a cool place


since they are adversely affected by heat.

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