Suppositories,

Inserts, and Sticks

Razon
Recabo
Rendon
Sagun
Songcuya

36
37
38
39
40

Systemic Actions
For systemic effects, the mucous
membranes of the rectum and vagina
permits absorption of many soluble
drugs.

Prochlorperazine and Chlorpromazine:

nausea and vomiting and as tranquilizer
Morphine and Oxymorphine:
opioid analgesia
Ergotamine tartrate:
migraine syndrome
Indomethacin:
non steroidal, anti-inflammatory analgesic and antipyretic
Ondansetron:
nausea and vomiting
Chloral hydrate:
sedative and hypnotic
Belladonna and Opium:
Analgesia and antispasmodic effect
Aspirin:
analgesic and antipyretic
Aminophylline and Theophylline:
relief of asthma

Rectal Suppositories

Factors Affecting Drug Absorption of

Suppositories
1)Physiologic Factors
Colonic content
Circulation route
pH and Lack of Buffering Capacity of the
Rectal Fluids
2) Physicochemical Factors
Lipid-water solubility
Particle size
Nature of the Base

Colonic Content
It is more effective for a drug to be
absorbed systematically in an empty
rectum than from one that is filled
with
fecal matter
Diarrhea, colonic obstruction due to
tumors and tissue dehydration can
influence the rate and degree of
absorption

Circulation Route
Drugs absorbed rectally, unlike those
absorbed orally, bypass the portal
circulation during their first pass into the
general circulation, thereby enabling drugs
otherwise destroyed in the liver to exert
systemic effect.
The lower hemorrhoidal veins surrounding
the colon receive the absorbed drug and
initiate its circulation throughout the body, bypassing the liver.

Lymphatic circulation also assists in

the absorption of rectally administered
drugs.

pH and Lack of Buffering Capacity of

the Rectal Fluids
The rectal fluids are essentially neutral
in pH (ranges 7.2 to 7.4) and has no
effective buffer capacity so no
chemical change will occur in this area.
The form in which the drug is
administered will not generally be
chemically changed by the rectal
environment.

Rectal Hemmorrhoidal
Veins

Rectal Hemmorrhoidal
Veins
These veins act by transporting the
active principle absorbed in the rectum
to the blood system either directly by
means of iliac veins and the vena cava
(inferior and middle hemorrhoidal
veins) or indirectly by means of portal
vein and the liver (superior
hemorrhoidal vein).

Rectal Hemmorrhoidal
Veins
It is generally accepted that at least
50% to 70% of the active ingredients
administered rectally take the direct
pathway, thus bypassing the liver and
avoiding the first-pass effect. There is
also the possibility of absorption into
the lymphatic vessels that should not
be dismissed but may be minimal.

Vaginal

Urethra
The female urethra is supplied by
blood vessels called the internal
pudendal and vaginal arteries. The
male urethra is supplied by the inferior
vesical and middle rectal arteries. The
veins follow these blood vessels.

Physicochemical Factors of the Drug

and Suppository Base
A. Drug
1. Relative solubility of the drug in
lipid and in water
2. Particle size of a dispersed drug
B. Suppository base
1. Ability to melt, soften or dissolve
at body temperature
2. Ability to release the drug
substance
3. Its hydrophilic or hydrophobic
charact

Lipid-water solubility
A lipophilic drug that is distributed in a
fatty suppository base in low
concentration has less tendency to
escape to the surrounding aqueous
fluids than would a hydrophilic
substance present in fatty base to an
extent approaching the saturation.

Example of water soluble bases:

polyethylene glycols - which dissolve in
the anorectal fluids, release for
absorption both water-soluble and oilsoluble drugs.

Particle Size
For drugs present in a suppository in the
undissolved state, the size of the drug
particle will influence its rate of dissolution
and its availability for absorption.
The smaller the particle size, the more
readily the dissolution of the particle and
the greater the chance for rapid
absorption.

Suppository Base
Nature of the Base:
Base must be capable of melting,
softening
or dissolving to release its drug
absorption.
If the base interacts with the drug to
inhibit
its release, drug reaction will be
impaired
or prevented.

Undesirable Characteristics of a
Base
1. That which interact with the drug
inhibiting its release such that the
drug absorption will be prevented or
delayed.
2. That which is irritating to the
mucous membranes of the rectum
thus initiating a colonic response and
prompt a bowel movement, negating
the prospect of thorough drug release
and absorption.

Classification of Bases

Fatty or Oleaginous base

Cocoa butter- commonly used because it melts
quickly at body temperature.
Palm kernel oil & Cotton seed oil- have many
hydrogenated fatty acids of vegetable oil
Others:
Plamitic & Stearic acids-is one of the most common
saturated fatty acids found in nature
followingpalmitic acid.
Wecobee Bases- triglycerides derived from coconut
oil
Witepsol Bases- triglycerides from palm, palm
kernel, and coconut oils with self emulsifying

Water-soluble and watermiscible bases

The main members of this group
are based of
1. Glycerinated gelatin
2. Bases of polyethylene glycols

Water-soluble and water-miscible bases

Glycerinated gelatin
is most frequently used in the
preparation
of vaginal suppositories, where the
prolonged localized action of the
medicinal agent is usually desired.

Water-soluble and watermiscible bases

Polyethylene glycols
Polyethylene glycols are polymers of
ethylene oxide and water, prepared to various
chain lengths, molecular weights, and physical
states. They are available in a number of
molecular weights ranges 200, 400,
600, 1000, 1500, 1540, 3350, 4000, 6000 and 8000.
Polyethylene glycols with average MW of 200,
400, and 600 are clear, colorless liquids. Those
greater than 1000 are wax like, white solids with
hardness increasing with an increase in molecular
weight.
Example: Polybase

Miscellaneous bases
3) Miscellaneous bases
-mixtures of oleaginous and watersoluble or water-miscible materials,
-some are preformed emulsions,
generally of the water/oil type, or
they may be capable of dispensing in
aqueous fluids.
E.g. Polyoxyl 40 stearate