Types of Suppositories, uses and examples. Suppository bases, uses and examples. Factors affecting rectal absorption of drugs.

1. Chapter 12:
SUPPOSITORIES
and
INSERTS
By:
Asst. Prof. MA. LOURDES L. MOJARES, R. Ph.
School of Pharmacy
CEU Manila

2. SUPPOSITORIES
 Solid dosage forms intended for insertion into
the body orifices where it;
1. melt
2. soften
3. dissolve
and exert localized or systemic effects

3. TYPES OF SUPPOSITORIES
RECTAL SUPPOSITORIES
 About 32 mm (1 ½ inches) in length,
cylindrical, one or both ends tapered and
some are bullet shaped
 Adult rectal suppositories weigh about 2
grams when cocoa butter is used as a base
 Intended for both local and systemic
actions

4. RECTAL SUPPOSITORIES
FOR LOCAL EFFECT
 Used to relieve constipation, as laxative.
Examples:
Glycerin suppositories
Dulcolax (Bisacodyl) suppositories

5. RECTAL SUPPOSITORIES

6. RECTAL SUPPOSITORIES

7. RECTAL SUPPOSITORIES
FOR LOCAL EFFECT
 Used to relieve pain, irritation, itching, and
inflammation associated with hemorrhoids
and other anorectal conditions
Examples:
Hydrocortisone suppositories
Mesalamine suppositories

8. RECTAL SUPPOSITORIES
FOR SYSTEMIC ACTIONS
 Relief of nausea and vomiting - Ondansetron
suppositories
 Tranquilizer - Prochlorperazine and Chlorpromazine
suppositories
 NarcoticAnalgesic – Oxymorphone suppositories
 NSAID (for migraine) – Ergotamine tartrate
suppositories
 Analgesic-antipyretic – Opigesic (Paracetamol)
suppositories

9. Systemic effects via rectal route:
ADVANTAGES
1. Drugs are not destroyed or inactivated by the
pH or enzymatic activity of the GIT
2. GI irritation is avoided
3. Bypass the liver
4. Convenient for administration of drugs to
patients who are unable to swallow
5. Effective route in treatment of patients with
vomiting

10. Factors affecting the absorption of drugs
from rectal suppositories
 Physiologic  Physicochemical
factors factors
 Colonic content  Lipid-water
 Circulation route solubility
 pH and Lack of  Particle size
buffering capacity  Nature of the base
of the rectal fluids

11. COLONIC CONTENT
For Systemic drug effect, absorption is
greater in a rectum that is void
/empty.
Diarrhea, Fecal matter
Slow down rectal
Tumor growth drug absorption
Tissue dehydration

12. pH and LACK OF BUFFERING
CAPACITY OF THE RECTAL
FLUIDS
 It is preferred to incorporate the
“ionized” salt form of the drug, to
maximize bioavailability.
 COCOA BUTTER – melts rapidly
at normal body temperature (due to
its immiscibility with fluids), it fails
to release fat-soluble drugs readily.

13. PHYSICO-CHEMICAL FACTORS
OF THE DRUG AND THE BASE
 Lipid – Water Solubility
The more drug the base contains, the
more drug will be available for
absorption.
If drug concentration in the intestinal
lumen is above a certain amount, the rate
of absorption is not changed by further
increase of the drug.

14. PHYSICO-CHEMICAL FACTORS
OF THE DRUG AND THE BASE
 Lipid – Water Solubility
A lipophilic drug that is distributed in
a fatty base (at low concentration) has
less tendency to be released into the
body fluid, than a hydrophilic drug in a
fatty base.

15. PHYSICO-CHEMICAL FACTORS
OF THE DRUG AND THE BASE
 Particle Size
The smaller the particle size, the greater
the surface area, the more readily the
dissolution of the particle, the greater the
chance for rapid absorption.

16. PHYSICO-CHEMICAL FACTORS
OF THE DRUG AND THE BASE
 Nature of the Base
If the base interacts with the drug to
inhibit its release, drug absorption will
be impaired or prevented.

17. PHYSICO-CHEMICAL FACTORS
OF THE DRUG AND THE BASE
 Nature of the Base
If the base irritates the mucous
membranes of the rectum, it may prompt
bowel movement, thus eliminating the
chance for complete bowel movement
and absorption

18. VAGINAL SUPPOSITORIES
Also called “ PESSARY / PESSARIES”
 Globular, oviform, or cone shaped
Weigh about 5 grams when cocoa butter is used
as the base
 Employed mainly as contraceptives,
antiseptics in feminine hygiene, and as specific
agents to combat invading pathogen
 More widely compounded than vaginal inserts

19. MONISTAT SUPPOSITORY
(Miconazole nitrate)

20. SHAPES and SIZES
of SUPPOSITORIES

21. VAGINAL
INSERTS / TABLETS
 Morewidely used than vaginal
suppositories.
 Easierto manufacture, more stable and
are less messy.
 Ovoid shaped
 Package includes a plastic inserting
device.

22. VAGINAL INSERTS
 Prepared by compression methods
 Contain lactose (filler); starch
(disintegrant); PVP (dispersing agent);
magnesium stearate (lubricant)
 Some may come in a form of gelatin
capsules of the drug, which is released
intravaginally.

23. VAGINAL INSERTS: EXAMPLES
PRODUCT NAME GENERIC NAME CATEGORY
SEMICID VAGINAL NONOXYNOL - 9 NON-SYSTEMIC
CONTRACPTIVE REVERSIBLE BIRTH
INSERTS CONTROL
ENCARE NONOXYNOL - 9 NON-SYSTEMIC
CONTRACEPTIVE REVERSIBLE BIRTH
INSERTS CONTROL

24. CANESTEN VAGINAL
TABLET
(Clotrimazole)

25. URETHRAL SUPPOSITORIES
 Also known as “BOUGIES”
 Slender, pencil-shaped
 May be antibacterial or a local
anesthetic preparative to urethral
examination

26. URETHRAL SUPPOSITORIES
1. Male Urethral suppository –
About 3 to 6 mm in diameter and approx.
140 mm in length; weigh about 4 grams
when cocoa butter is used as the base
2. Female Urethral suppository –
About 70 mm in length and weigh about 2
grams when cocoa butter is used as the
base

27. Alprostadil Urethral
Microsuppository (MUSE)
 A single-use medicated transurethral
system for the delivery of the drug,
Alprostadil to the male urethra.
 Indicated for the treatment of erectile
dysfunction (ED)

28. Alprostadil Urethral
Microsuppository (MUSE)

29. Alprostadil Urethral
Microsuppository (MUSE)

30. SUPPOSITORY BASES
I. BASES THAT MELT –
FATTY OR OLEAGINOUS BASES
COCOA BUTTER –Theobroma oil
Melts at 300C to 360C
Good base for rectal suppositories but less ideal
for vaginal and urethral suppositorries.
Exhibits polymorphism
Its melting can be lowered by certain drugs
(e.g. phenol and chloral hydrate)

31. COCOA BUTTER
(Theobroma cacao)
 CETYL ESTERS WAX
(20 %)
 BEESWAX (4 %)
May be added to
compensate for the
softening effect of
added substance to
Cocoa butter.

32. SUPPOSITORY BASES
I. BASES THAT MELT –
FATTY OR OLEAGINOUS BASES
WITEPSOL BASES – triglycerides of saturated
fatty acids C12 to C18.
WECOBEE BASES – triglycerides derived
from coconut oil
FATTIBASE® - triglycerides from palm, palm
kernel, and coconut oils with self
emulsifying glyceryl monostearate and
polyoxyl stearate

33. SUPPOSITORY BASES
II. WATER SOLUBLE AND WATER
MISCIBLE BASES
PEG POLYMERS
Use combination of PEG polymers of
varying molecular weights:
 PEG 400 –liquid
 PEG 1000 – semisolid

34. SUPPOSITORY BASES
II. WATER SOLUBLE AND WATER
MISCIBLE BASES
1. PEG POLYMERS
 PEG 1500 to 1540 – fairly firm semisolids
 PEG 4000 to 6000 – wax-like
These bases “do not leak” from the orifice.

35. SUPPOSITORY BASESI
2. GLYCERINATED GELATIN
 Frequentlyused base in vaginal
suppositories.
 Suppositories (using this base) should be
moistened first with water to avoid irritation
to the tissue upon insertion.

36. SUPPOSITORY BASES
III. MISCELLANEOUS BASES
 Mixtures of oleaginous and water-soluble or
water-miscible materials
 Hold water or aqueous solutions and are
said to be hydrophilic

37. PREPARATION OF
SUPPOSITORIES
1. HAND ROLLING
The oldest and simplest method of
suppository preparation.
Method of choice when only a few
suppositories are to be prepared in a
cocoa butter base.

38. HAND ROLLING METHOD
It has the advantage of avoiding the
necessity of heating the cocoa
butter.
A plastic-like mass is prepared by
“triturating” grated cocoa butter
and active ingredients in a mortar.

39. METAL SUPPOSITORY MOLD

40. HAND ROLLING METHOD
The mass is formed into a ball in the
palm of the hands, then rolled into a
uniform cylinder with a large spatula
or small flat board on a pill tile.
The cylinder is then cut into the
appropriate number of pieces which
are rolled on one end to produce a
conical shape.

41. COMPRESSION MOLDING
METHOD
A method of preparing suppositories
from a mixed mass of grated
suppository base and medicaments
which is forced into a special
compression mold.

42. RUBBER / LATEX
SUPPOSITORY MOLDS

43. COMPRESSION MOLDING
METHOD
The method requires that the capacity
of the molds first be determined by
compressing a small amount of the
base into the dies and weighing the
finished suppositories

44. FUSION MOLDING
METHOD
Involves the ff. steps;
1. melting the suppository base
2. dispersing or dissolving the drug in
the melted base.

45. BLISTER PACKAGING
FOR SUPPOSITORIES

46. FUSION MOLDING
METHOD
The mixture is removed from the
heat and poured into a suppository
mold.
When the mixture has congealed, the
suppositories are removed from the
mold.

47. FUSION MOLDING: steps
1. Melting the base
2. Incorporating any required
medicaments
3. Pouring the melt into molds
4. Allowing the melt to cool and congeal
to suppositories
5. Removing the formed suppositories

48. PACKAGING and STORAGE
of SUPPOSITORIES
1. COCOA BUTTER BASED
SUPPOSITORIES
 Individually wrapped
 Kept refrigerated

49. RECTAL SUPPOSITORIES

50. PACKAGING and STORAGE
of SUPPOSITORIES
2. GLYCERIN SUPPOSSITORIES AND
GLYCERINATED GELATIN BASED
SUPPOSITORIES
Packaged in a tightly closed containers
Stored at temperature below 35°F
Can be stored at controlled room
temperature (200C to 250C)

51. PACKAGING and STORAGE
of SUPPOSITORIES
3. PEG BASED SUPPOSITORIES
 Stored at usual room temperature
 NO REFRIGERATION required