Suppositories

By
Ass.Prof. Mona Arafa
Presented by
Dr. Yomna Moussa
• Anatomy of the rectum:
- The rectum is part of the colon, forming the last 15 – 20 cm of the
GI tract.
- The rectum can be considered as a hollow organ with a relatively
flat wall surface, without villi.
- It contains only 2 – 3 ml of inert mucous fluid with pH of 7.5 .
 Suppositories
1) They are solid dosage forms
2) They contain one or more APIs are dispersed in a suitable base and
molded or otherwise formed into a suitable shape for insertion into the
rectum.
3) Intended for insertion into body orifices
4) They melt, soften or dissolve to give their effect
5) They have either local or systemic effects
6) They may be rectal, vaginal and urethral supp.
7) They have various shapes (torpedo, globular, oviform, tablet and pencil
shape). WHY?
8) Their weights varies from 2-5 gm
ADV:
1- They are accurate dosage forms
2- Used for systemic distribution and preferable than oral route in
some certain cases like unconscious conditions.
3- Suitable for administration of drugs not tolerated orally.
E.g. medications which are sensitive to gastric pH and enzymes
4- Suitable in case of medications that interrupt the GIT functions.
E.g. drugs that cause irritation to stomach
5- Convenient in certain cases.
E.g. nausea and vomiting
6- When local effect is desired such in case of rectal , vaginal and
urethral diseases.
7- Suppositories have faster onset of action than oral route as drug is
directly absorbed from mucosa into venous circulation.
8- Drugs by this route are not destroyed by liver due to the 1st pass
effect.
Disadv.:
1- Patient acceptance
2- Not suitable in some cases like Diarrhea
3- The total amount of the drug within supp. may cause irritation or is
too high to be found within supp.
4-Incomplete absorption of the drug that may need empty bowel.
5-Defecation may interrupt the absorption process of the drug; this
may especially occur if the drug is irritating.
6-The absorbing surface area of the rectum is much smaller than that
of the small intestine.
7- The fluid content of the rectum is much less than that of the small
intestine, which may affect dissolution rate.
8-There is the possibility of degradation of some drugs by the
microflora present in the rectum.
Indications:
1- To empty the bowel; before certain surgery
2- To relieve acute constipation
3- Before endoscopic examination
4- To soothe and treat hemorrhoids or anal pruritus
Contraindications :
1- Chronic constipation cause it needs repetitive use
2- Paralytic ileus
3- Colonic obstruction
4- Gastrointestinal operations
 the suppository Once inserted
the suppository base melts, softens, or dissolves, distributing its
medicaments to the tissues of the region.

These medicaments may be intended for

retention within the cavity for

absorption for systemic effects
local effects
 Local Action
❑ 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.
❑ 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 an invading pathogen.
❑ Urethral suppositories may be antibacterial or a local anesthetic
preparative for a urethral examination.
 Systemic Action
❑ For systemic effects, the mucous membranes of the rectum and
vagina permit the absorption of many soluble drugs.
❑ Although the rectum is used frequently as the site for the
systemic absorption of drugs, the vagina is not as frequently
used for this purpose.
❑ Examples of drugs administered rectally in the form of
suppositories for their systemic effects include
(a) prochlorperazine and chlorpromazine for the relief of nausea
and vomiting and as a tranquilizer;
(b) morphine and oxymorphone for opioid analgesia;
(c) ergotamine tartrate for the relief of migraine syndrome;
(d) indomethacin, a nonsteroidal anti-inflammatory analgesic and
antipyretic;
(e) ondansetron for the relief of nausea and vomiting.
➢ other types of suppositories:
1- Vaginal (inserts):
A) Tablets :
➢ Adv :
1- Easy to manufacture
2- More stable
4- Less messy
5- Easily disintegrate and disperse in surrounding media and slowly
release the medications
B) May be available as hard or soft gelatin capsules
• Inserts specifications:
1) Ovoid in shape which weigh 1-2 g
2) Wetted with water just before use
3) They are prepared by compression
4) Composed of :
➢ Lactose vehicle
➢ Starch disintegrate
➢ PVP(Polyvinylpyrrolidone) dispersing agent
➢ Magnesium stearate lubricant
II- Urethral suppositories
➢ Suppositories for urethral administration tend to be thinner and
tapered, often about 5 mm in diameter. They have been used in the
treatment of local infections
Factors affecting drug absorption from
rectal suppositories
Factors

1)Physiologic 2) Physicochemical
Factors Factors

•Lipid-water
•Circulation route
solubility

•pH and Lack of

Buffering Capacity •Particle size
of the Rectal Fluids

•Colonic content •Nature of the base

Factors affecting rectal absorption :
I-Physiologic factors:
1- Colonic content for systemic effect:
A- greater absorption is expected from empty rectum than that with
fecal matter why?
B- other conditions may affect the rate and degree of drug absorption
E.g. diarrhea &colonic obstruction
2- Circulation route
➢ Adv. Of drug absorbed rectally over those absorbed after oral
administration
A- they bypass the portal circulation,
B- so protect drug from destruction by liver,
C- then, they can exert their systemic circulation by being distributed
by veins surrounding the colon through the body
D- lymphatic circulation also assists in drug absorption.
that consists of a complex network of vessels, tissues, and organs. The
lymphatic system helps maintain fluid balance in the body by
collecting excess fluid and particulate matter from tissues and
depositing them in the bloodstream.
Rectal. The last few inches of the large intestine
constitute the rectum, terminating at the anus.
The rectum contains three types of hemorrhoidal
veins:
1. superior hemorrhoidal vein
2. middle hemorrhoidal vein
3. inferior hemorrhoidal vein
✓ inferior and middle hemorrhoidal veins →
transport the active principle absorbed in the
rectum to the blood system directly by means of
iliac veins and the vena cava.
✓ superior hemorrhoidal vein → transport the
active principle absorbed in the rectum to the
blood system indirectly by means of the portal vein
and the liver.
✓ it is not really possible to predict the position or
exact location of the suppository in the rectum, it is
not really possible to predict exactly which way the
active principle will be transported.
✓ 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.
• To summarize:
ABSORPTION OF DRUGS FROM THE RECTUM
• 3 separate veins

Lower Middle Upper

haemorrhoidal haemorrhoidal haemorrhoidal
vein vein vein

drain directly into the Drains into the

general circulation portal vein, which
flows to the liver
Thank you