DOSAGE FORMS base.

Children: half the weight

and more pencil shaped.
SUPPOSITORIES
VAGINAL SUPPOSITORIES
 Is a dosage form in which one or
more APIs are dispersed in a  Aka pessaries
suitable base and molded or  Globular, oviform, cone shaped.
otherwise formed into a suitable  Weigh about 5 grams when cocoa
shape for insertion into the butter is in the base.
rectum to provide local or
URETHRAL INSERTS
systemic effect.
 Supponere, meaning “to place  Aka bougies
under” as derived from sub  Slender, pencil shaped
(under) and ponere (to place).  Male: 3-6mm in diameter and
140mm long. With cocoa butter it
INSERTS
weighs 4g.
 Is a solid dosage form that is  Female: half the length and
inserted into a naturally weight of the male. 70mm long
occurring (non surgical) body and 2g when made of cocoa
cavity other than the mouth or butter.
the rectum , including the vagina
Suppositories contain:
and the urethra.
 Aspirin and opiates for pain.
MEDICATION STICKS
 Ergotamine tartrate for migraine
 For administering topical drugs . and headaches.
 Cylindrical in shape  Provide systemic drug effects
 5-25g
Advantages:
 Packed in an applicator tube with
an applicator.  First pass effect: avoid first pass
effect that may result to higher
blood pressure.
RECTAL SUPPOSITORIES  Drug stability: avoiding
breakdown of drugs that are
 32mm (1.5in), cylindrical, one or
susceptible to gastric
both ends tapered. Some are
degradation.
shaped like a bullet/ torpedo.
 Large dose drugs: administer
Adults: 2g when Theobroma oil
large dose drugs as compared to
(cocoa butter) is employed as the
oral administration.

YSOBEL L SUMABAT | BS PHARMACY | SPUP

  Irritating drugs: ability to
administer drugs with irritating
Local action of suppositories: used to
effect on the oral or
relieve constipation, or the pain,
gastrointestinal mucosa.
irritation, itching and inflammation
 Unpleasant tasting or smelling
associated with hemorrhoids and other
drugs.
anorectal conditions.
 Easy for administration to
children.  Glycerin suppositories- provide
 For patients experiencing nausea laxation by local irritation of the
and vomiting or when patient is mucous membrane.
unconscious.  Vaginal suppositories -
 Used when the presence of contraceptives, antiseptic and
disease of the GI tract that may specific agent to combat an
interfere with drug absorption. invading pathogen. Most
 Objectionable taste or odor of a common: nonoxynol 9
drug. (contraception), trichomonacides
 Achievement of a rapid drug (combat vaginitis caused by
effect systemically. trichomonas vaginalis)
antifungals (to treat candida
Disadvantages:
monilial albicans).
 Lack of commercially available  Urethral spp.- may be
suppositories. antibacterial or a local anesthetic
 If they are on demand, they may for urethral examination.
be expensive.  Sticks- local effect and include
 May exhibit variable hydration/emollient,
effectiveness. antibacterial, sunscreen,
 Defecation may interrupt the antipruritic.
absorption process of the drug
Systemic action:
especially when the drug is
irritating. Examples:
 Fluid content of the rectum is
 Prochlorperazine and
much less that of the small
chlorpromazine for the relief of
intestine which may effect
nausea and vomiting and a
dissolution rate.
tranquilizer.
 There is possibility of derogation
 Morphine and oxymorphone for
of drug due to microflora present
opioid analgesia.
in the rectum.

YSOBEL L SUMABAT | BS PHARMACY | SPUP

  Ergotamine tartrate for the relief chemically and physiologically
of migraine. inert, compatible with a variety of
 Indomethacin an NSAI analgesic drugs, stable during storage and
and antipyretic. esthetically acceptable.
 Ondansetron for the relief of
FATTY/OLEAGINOUS BASE
nausea and vomiting.
 Most frequently used
PHYSIOLOGICAL FACTORS AND
suppository base, contains cocoa
DRUG EFFECT
butter, many hydrogenated fatty
a. Circulation route acids of vegetable oils (palm
b. pH and lack of buffering kernel oil and cottonseed oil),
capacity of the rectal fluids glycerin, high molecular weight
 Rectal fatty acids (palmitic and stearic
 Vaginal acids).
 Urethra  Cocoa butter, NF is fat obtained
c. Colonic content from roasted seed of Theobroma
cacao. Yellowish white color with
PHYSIOCHEMICAL FACTORS AND
chocolate like odor. Is a
DRUG EFFECT
triglyceride primarily of
a. Lipid- water solubility oleopalmitostearin and
b. Particle size oleodistearin. Melts at 30-36
degrees which makes it an ideal
suppository base.
SUPPOSITORY BASES
WATER SOLUBLE AND WATER
NATURE OF THE BASE MISCIBLE BASES
 Must be capable of melting,  Glycerinated gelatin and
softening or dissolving to release polyethylene glycols.
its drug for absorption.  Glycerinated gelatin may be
 Morphine sulfate- slow release prepared by dissolving granular
suppository. Is prepared In a base gelatin (20%) in glycerin (70%)
that includes alginic acid which and adding water or solution or
will prolong the release of the suspension of the medication
drug for several hours. (10%). Used frequently for
 Should be physically and vaginal spp. In which prolonged
chemically stable, nonirritating, local action of the medicinal
nontoxic, nonsensitizing, agent is usually desired. Urethral

YSOBEL L SUMABAT | BS PHARMACY | SPUP

 spp of glycerinated gelatin are  Water miscible base – based on
much easier to insert than those diffusion; all water soluble.
with cocoa butter.
 Polyethylene glycols are
polymers of ethylene oxide and PREPARATIONS OF
water. Have an average SUPPOSITORIES
molecular weight of 300, 400 and
MOLDING
600. Are clear, colorless liquids.
Those having an average 1. Melting the base
molecular weight of 1000 are wax 2. Incorporating any required
like white solids whose hardness medicaments
increases as molecular weight 3. Pour the melt into molds
increases. Do not melt due to 4. Allow the melt to cool and
body temperature but rather congeal into suppositories
dissolve slowly in body’s fluids. 5. Removing from mold
 Poloxamers (Pluronics) are water
soluble, block copolymers with a
wide range of uses. (L44, L62,  Suppository Molds - made from
L64, F68). Have no odor or taste. stainless steel, aluminum brass or
plastic. Plastic molds are
FORMULATION VARIABLES especially prone to scratching.
A. Physical state  Lubrication of the mold- e.g.
B. Particle size mineral oil
C. Viscosity  Calibration of the mold – total
D. Brittleness weight and average weight of
E. Volume contraction each suppository are recorded.
F. Drug release rate  Determination of the amount of
 Oil soluble drug (oily base) : base required
slow release, poor escaping
tendencies
 Water soluble drug (oily base) :
rapid release
 Oil soluble drug (water miscible
base)- moderate release
 Water miscible drug (water
miscible base)- moderate release
based

YSOBEL L SUMABAT | BS PHARMACY | SPUP

TRANSDERMAL DRUG
DELIVERY SYTEM:

 Facilitate the passage of

therapeutic quantities of
drug substances through
the skin and into the
general circulation for
their systemic effect.
 In 1965, Stoughton first
conceived of the
percutaneous absorption
of drug substances.
 The first transdermal
system: Transderm Scop
was approved by FDA in
1979 for prevention of
nausea and vomiting.

YSOBEL L SUMABAT | BS PHARMACY | SPUP