SUPPOSITORIES

AND INSERTS
Prepared by MJMolina RPh
• Introduction
• Indications
• Types
• Advantages and Disadvantages
Suppositories
• solid dosage forms intended for
insertion into body orifices where they
melt, soften, or dissolve and exert local
or systemic effects
• Supponere - meaning to place under
• Routes: rectum, vagina, and urethra
 IDEAL CHARACTERISTICS
1. Melts at body temperature or dissolves in body
fluids.
2. Non-toxic and non-irritant.
3. Compatible with any medicament.
4. Releases any medicament readily
5. Easily molded and removed from the mould.
6. Stable to heating above the melting point.
7. Easy to handle.
8. Stable on storage.
Indications
1. Administering drugs to infants/small
children
2.Severely debilitated patients
3.Those who cannot take medications
orally
4.Those for whom the parenteral route
might be unsuitable
Local action
• Rectal suppositories used to relieve
constipation or the pain, irritation, itching,
and inflammation.
• A popular laxative, glycerin suppositories
promote laxation by the local irritation of the
mucous membranes.
• Vaginal suppositories for localized effects
are employed mainly as contraceptives,
antiseptics in feminine hygiene, and as
specific agents to combat as invading
pathogen.
Systemic action
➢ For systemic effects, the mucous
membranes of the rectum and vagina
permit the absorption of many soluble
drugs.
• Ex:
Ergotamine tartarate
Chlorpromazine
Indomethacin(NSAID)
Types of Suppositories
▪ Rectal Suppositories
- Intended for local action to relieve constipation, irritation, itching
and inflammatory
- Sedatives, tranquilizers, analgesic, most common – use for
hemorrhoid
▪ Vaginal Suppositories (Pessaries)
- Intended for local effects like contraceptives, antiseptics in feminine
hygiene
▪ Urethral Suppositories (Bougies)
- Intended for antibacterial or as local anesthetic preparative for
urethral examination
▪ Nasal Suppositories (Buginaria)
▪ Ear Cones (Aurinaria)
CHARACTERISITCS RECTAL VAGINAL URETHRAL

Other name --- Pessaries Bougies

M = 4g
Weight 2g 3g F = 2g

M = 140mm
Size 32nm vary F = 70mm

* Bullet shape Globular Pencil-like

Shape * Torpedo Oviform
* Pencil-like Cone
(children)
½ size and
Age difference weight for infant Adults Adults
and children

Gender Same Female only Same

Advantages of Suppositories
▪ Easily administered
▪ Convenient mode of administration for
drugs which irritate the GIT
▪ Faster onset of action as compared to oral
administration
▪ Produce local action at the site of insertion
▪ No variation of drug dose
▪ Effective route in treatment of patients with
vomiting
Advantages of Suppositories
❖ Can be used in unconscious patients
❖ Can be used for systemic absorption of
drugs and avoid first-pass metabolism.
❖Babies or old people who cannot
swallow oral medication.
❖Post operative people who cannot be
administered oral medication.
❖People suffering from severe nausea or
vomiting.
Disadvantages of Suppositories
• Drugs which are irritant to mucous
membrane (rectum) cannot be formulated
as suppository
• Demands stringent storage conditions
• Problematic in large scale production of
suppositories and achievement of suitable
shelf life
DISADVANTAGES OF SUPPOSITORIES:
➢ The problem of patient acceptability.
➢Suppositories are not suitable for patients suffering
from diarrhea.
➢In some cases the total amount of the drug must be
given will be either too irritating or in greater amount than
reasonably can be placed into suppository.
➢Incomplete absorption may be obtained because
suppository usually promotes evacuation of the
bowel.
Disadvantages of Suppositories
▪ Leaking problem of the material through
cavities causes embarrassment to the
patient
▪ Development of procitis (inflammation of
anus and lining of rectum)in some cases.
▪ Slow and incomplete absorption of drug
Composition of Suppositories
▪ Active ingredient

▪ Suppository base

▪ Additives
Composition of Suppositories
Active Ingredient
 Composition of Suppositories
Suppository base
▪ Play important role in the release of the
medication and therefore in the availability
of drug.
▪ Act as vehicle for medicaments
 SUPPOSITORY BASE

The suppository bases are used to

prepare the suppositories so that:
❖They can retain its shape
❖Firmness during the administration
❖And to give the suppositories a melting
point which is equal to the temperature of
the body cavity into which it is inserted
Ideal Suppository Vehicle / Base
▪ nontoxic and nonirritating
▪ compatible with variety of drugs
▪ melts or dissolves in body fluids
▪ stable on storage
▪ does not interfere with release or
absorption of drug substances
Classification of Suppository Bases
A. Fatty or Oleaginous Bases
B. Water-Soluble and Water-Miscible Bases
C. Miscellaneous Bases
Fatty or Oleaginous Bases
• Most frequently used
• Cocoa Butter, NF
• Fattibase
– (triglycerides from palm, palm kernel and coconut oils with self-
emulsifying glyceryl monostearate and polyoxyl stearate)
• Wecobee bases
– (triglycerides derived from coconut oil)
• Witepsol bases
– (triglycerides of saturated fatty acids C12-C18 with varied
portions of the corresponding partial glycerides)
Fatty or Oleaginous Bases
• Cocoa Butter, NF
– Fat obtained from the roasted seed of Theobroma
cacao
– At room temperature, it is a yellowish-white solid
having a faint, agreeable chocolate-like odor
– A triglyceride primarily of oleopalmistearin and
oleodistearin
– Ideal suppository base because it melts at 30°-
36°C, melting just below body temperature and yet
maintaining its solidity at usual room temperatures.
Disadvantages of Theobroma oil

Polymorphism
Rancidity
Adheres to the mould when
solidified
Leakage from body cavity on
melting
Costly
Immiscible with body fluids
 Water-Soluble and
Water-Miscible Bases
• Glycerinated gelatin
– Prepared by dissolving granular gelatin (20%) in
glycerin (70%) and adding water or a solution or
suspension of the medication (10%)
– Most frequently used in the preparation of vaginal
suppositories, with which prolonged local action
– Slower to soften and mix with the physiologic fluids
than is cocoa butter and therefore provides a a
slower rate.
 Water-Soluble and
Water-Miscible Bases
• Polyethylene glycols
– Polymers of ethylene oxide and water prepared to various
chain lengths, molecular weights, and physical states
– Do not melt at body temperature but rather dissolve slowly in
the body’s fluids.
– Should be dipped in water just before use to avoid irritation of
the mucous membranes after insertion.
 Miscellaneous Bases
Example: Polyoxyl 40 stearate
▪ mixture of the monostearate and distearate
esters of mixed polyoxyethylene diols and the
free glycols
▪ white to light tan waxy solid that is water soluble
▪ melting point, 39°-45°C
III. PREPARATION OF SUPPOSITORIES
 PREPARATION OF SUPPOSITORIES

❖Rolling method
❖Hot process or fusion method
❖Cold compression method
Hand molding & shaping
❖ Not really used much anymore
❖ Weigh ingredients
❖ Shred cocoa butter
❖ Mix together
❖ Apply gentle heat
❖ Shape and form
Molding/Fusion
1. Melting the base
2. Incorporating any required medicaments
3. Pouring the melt into molds
4. Allowing the melt to cool and congeal into
suppositories
5. Removing the formed suppositories from
the mold
❖ Suitable bases: cocoa butter, glycerinated
gelatin, polyethylene glycol
Compression
❖ Prepared by forcing the mixed mass of the
base and the medicaments into special
molds using suppository-making machines
❖ suited for suppositories containing heat-
labile medicinal substances or insoluble
substances in bases
Rectum
• 15-20cm long
• Empty: 2-3mL of inert mucous fluid
• No villi or microvilli on the rectal mucosa
(immobile at resting state)
• Abundant blood and lymphatic vessel
• Better absorbed in a void rectum
• The lower hemorrhoidal veins surrounding
the colon receive the absorbed & initiate its
circulation through the body, bypassing the
liver.
• Rectal fluids are essentially neutral in pH &
have no effective buffer capacity.
• The suppository base has a marked
influence on the release of active
constituents.
❖They are meant for the insertion into the
rectum for systemic or local action
❖For adults weigh 2 gm and are torpedo
shape. Children's suppositories weigh about
1g
❖Cocoa butter is generally used as the base
in these preparations
✓ Laxative suppository formulation
Glycerin 91g
Sodium Stearate 9 g
Purified Water 5g
FACTORS AFFECTING ABSORPTION OF DRUGS FROM RECTAL SUPPOSITORIES:

➢ Physical factors:
❖ Colonic content
❖ Circulation route
❖ pH and lack of buffering capacity of colon

➢ Physico-chemical factors:
❖ Particle size
❖ Nature of base
❖ Lipid- water solubility of drug
❖ Presence of adjuncts in the base
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 a hydrophilic substance in a fatty
base.
Particle Size
The smaller the particle, the greater the
surface area, the more readily the
dissolution of the particle and the greater
the chance for rapid absorption.
Nature of the Base
- The base must be capable of melting,
softening, or dissolving to release its drug
for absorption.
- Drug malabsorption
a) the base interacts with the drug
b) the base irritates the mucous
membranes of the rectum, it may initiate
a colonic response and prompt bowel
movement
Some Factors of Drug Absorption
from Rectal Suppositories
• Physiologic Factors
– Colonic Content
– Circulation Route
– pH and Lack of Buffering Capacity of the
Rectal Fluids
Rectal suppositories
• Prochlorperazine and Chlorpromazine
- relief of nausea & vomiting
• Oxymorphhone HCl
- opioid analgesic
• Ergotamine tartrate
- relief of migraine syndrome
• Indomethacin
- nonsteroidal anti-inflammatory analgesic
• Ondansentron
- relief of nausea & vomiting
Rectal suppositories
Patient counselling:
✓ Stored in the refrigerator and allowed to warm to RM
before insertion.
✓ Rub cocoa butter suppositories gently with the fingers
to melt the surface to provide lubrication for insertion.
✓ Remove the wrapping before insertion.
✓ Glycerinated gelatin or polyethylene glycol
suppositories should be moistened with water to
enhance lubrication.
✓ Bullet-shaped rectal suppositories should be inserted
pointed end first.
✓ The patient who is to use half of a suppository should
be told to cut the suppository lengthwise with a clean
razor blade.
Urethral suppositories
❑ thinner and tapered
❑ 5mm diameter
❑ Treatment of local infections
❑ Ex: MUSE microsuppository
- Alprostadil
- treatment of erectile dysfunction
 Urethral suppositories:-
❖They are meant for insertion into the
urethra
❖They are thin long and cylindrical at one
end to facilitate insertion
❖ They generally weigh about 2 -4 gm
❖ They are very rarely used
➢These are inserted into the vagina
➢weigh about 3-5gm and are molded in conical, rod
shaped, and oval.
➢These are generally used to combat infections
occurring in the female genitourinary area, to restore
the vaginal mucosa to its normal state and for
contraception
Rx
Progesterone 25 -600mg
PEG 400 60%
PEG 8000 40%
This formulation is used in suppository for the restoration of
the vaginal mucosa.
Vaginal suppositories

❑ employed to combat infection in the female

genitourinary tract (nystatin), to restore the
vaginal mucosa to its normal state (dienestrol),
and for contraception (nonoxynol-9)
Vaginal suppositories
Patient counselling:
1. Read the instructions with the product.
2. Inserted high into the vagina with the provided
applicator.
3. Notify her physician if burning, irritation, or any
signs of allergic reaction occur.
4. Wear sanitary napkin.
Vaginal inserts
❑ easier to manufacture
❑ more stable
❑ less messy
❑ aka vaginal tablets
❑ ovoid and accompanied
with a plastic inserter
❑ Advise the patient to
dip the tablet into water
quickly before insertion.
Nasal suppositories
➢They are meant for the
insertion into the nasal cavity
➢ They are thin cylindrical in shape
➢They are always prepared using
the glycero-gelatin base.
➢They are about 9-10CM long and
weigh about 1 gm
EAR CONES
€These are meant for
introduction into the ear
€They are long, thin, and
cylindrical in shape
€They weigh about 1gm
€Theobroma oil is generally
used as the base
I. SUPPOSITORIES
I. SUPPOSITORIES
Water soluble bases
➢Glycero-gelatin base:
✓Mixture of glycerin and water made stiff by
addition of gelatin
✓Used to prepare all type of Suppositories
but practically most suitable forpessaries
✓Prepared suppositories are translucent.
✓They dissolve slowly and release
medicament
Disadvantages
❖Gelatin is incompatible with many drugs
like tannic acid , ferric chloride, Gallic acid
etc.
❖Chances of bacterial , mouldgrowth.
❖Hygroscopic in nature
❖They have physiological action
❖More difficult to prepare and handle
 Emulsifying bases
These are synthetic bases
❖ Witepsol:
It consist of triglycerides of saturated
vegetable fatty acids and partial esters
❖ Massa estarinum:
It is a mixture of mono, di and triglycerides
of unsaturated fatty acids.
❖ Massupol:
It consist of glyceryl esters of lauric acid
with small amount of glyceryl stearate to
improve water absorbing capacity
Packaging and Storage
• Glass or plastic containers
– Glycerin suppositories and glycerinated gelatin
suppositories; to prevent a change in moisture content
• Wrapped or unwrapped
- cocoa butter; to prevent contact and adhesion
• Room temperature or under refrigeration
- brittle due to loss of moisture when exposed to extreme
dryness
• Moderate humidity
- spongy when stored at high humidity due to moisture
absorption
III. VAGINAL INSERTS
• Vaginal tablets, frequently
referred to as vaginal inserts, are
usually ovoid and are
accompanied in their packaging
w/ a plastic inserter, a device for
easy placement of the tablet w/in
the vagina.
• These are prepared by tablet
compression.
• The tablet is intended to w/in
the vagina, releasing their
medication.