SlideShare a Scribd company logo
SUPPOSITORIES and ENEMAS
Dr. Samia Ghani
M. Phil Pharmaceutics
•The word suppository is derived from Latin word
« suppositorium »
which means
« to place under »
Definition
• Suppositories are solid or semi-solid dosage forms intended for
insertion into the body cavities e.g. rectum, vaginal cavity,
occasionally into the urethral tract where these suppositories melt or
soften or dissolve in the cavity fluid and exert a localized or systemic
effects.
• The derivation of the word suppository is from the Latin supponere,
meaning “to place under,” as derived from sub (under) and ponere (to
place). Thus, suppositories are meant both linguistically and
therapeutically to be placed under the body, as into the rectum
• Suppositories are commonly employed rectally and vaginally,
occasionally they’re used uretharlly and rarely they are also used
nasally or orally.
• They have various shapes, sizes and weights.
• These are employed when a drug cannot tolerate orally or patient
cannot swallow a drug easily.
• The shape and size of suppository must be such that it is capable of
being easily inserted into the intended body cavity and once it is
intended it must be retained for an appropriate period of time.
• Suppository generally have been employed for three reasons to:
o Promote defecation
o Introduce drugs into body
o Treat anorectal diseases
THE THERAPEUTIC USES OF SUPPOSITORIES
1. The drugs may be administered in the suppository dosage form for
local or systemic effect.
2. Such health action depends on:
• Nature of drug
• Concentration of drug
• Rate of drug absorption which depends upon the blood supply and
• solubilities of the drugs
3. The lipid soluble or un-dissociated drugs are readily dissolved after
release from the base and fat.
Local Action:
1. The emollient (substances that soften the skin), the astringents
(chemical substances that constrict the body tissues to stop bleeding or
to make skin less oily – also called as protein precipitant), anti-bacterial
agents, hormones, steroids and local anesthetics are dispersed in the
suppositories for the treatment of local conditions of either vagina or
urethra.
2. The rectal suppositories are primarily intended for the localized
action and these are most frequently used or employed to relieve the
constipation, pain, irritation, itching and inflammation associated with
hemorrhoids (swollen or painful condition in which bleeding can
occur).
3. Anti-hemorrhoidalsuppositories frequently contain a number of
components including:
1.Local anesthetics
2.Astringents
3.Soothing agents
v. Vasoconstrictors vi. Analgesics
vii. Emollients
iv. Protective
E.g. glycerin suppository as a laxative (increase bowel movement)
4.Vaginal suppositories are used for the local action e.g. antiseptics,
contraceptives (to stop child birth) etc.
5.Urethral suppositories may be used as anti-bacterial and as local
anesthetics.
Systemic Action:
1. For systemic action, the mucous membrane of the rectum and
vagina permit the absorption of many soluble drugs.
2. Awiderangeofdrugsareemployedforsystemicactione.g.
o Analgesics
o Anti-spasmodic (to treat spasm - Biscopan)
o Sedatives (induce sleep)
o Tranquilizers
o Anti-bacterial agents
Advantages of Suppositories over Oral
Therapy:
1. Some drugs are destroyed by the GIT enzymes (or by the pH of GIT).
Such drugs are administered in suppository form.
2. Drugs which cause gastric irritation may be given rectally in the form
of suppository.
3. To bypass the first pass action (drugs destroyed by portal circulation
may bypass the liver after rectal absorption) e.g.
• Propranolol (Anti-hypersensitive)
• Glycerol trinitrate (used in angina attack–placed under tongue or given as
suppository)
4. The route of administrations are also convenient for:
• Adult patients
• Unconscious persons
• Mental retarded person
• For infants who may unable to swallow the medicines
5. In vaginal cavity, for local antiseptics and anti-bacterial action.
6. This route has ability to administer some what larger doses of drugs
than using oral administration.
7. This route ensures a rapid drug effect systematically (as an alternate
to injections).
8. This route avoids bad taste or odour of drug.
Disadvantages of Suppository:
• 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.
• A perceived lack of flexibility regarding dosage of commercially
available suppository resulting in underuse and a lack of availability.
• They’re expensive if made on demand.
• Different formulations of a drug with a narrow therapeutic margin,
such as aminophylline, cannot be interchanged without risk of
toxicity.
• Defecation may interrupt the absorption process of the drug, if drug
is irritating.
• There is possibility of degeneration of some drugs by the micro-flora
present in the rectum.
Examples of Drugs:
• Prochlorperazine (for nausea and vomiting)
• Chlorpromazine (as a tranquillizer)
• Oxymorphine HCl (narcotic analgesic)
• Indomethacin (NSAID analgesic and anti-pyretic)
• Ergotamine tartarate (relief of migraine)
Drugs Dispensing in Suppositories:
• Hormones
• Steroids
• Emollients
• Astringents
• Antibiotics
• Local anesthetics
• Local analgesics
FACTORS AFFECTING THE ACTION OF
SUPPOSITORIES
First Step of Dissolution Depends Upon:
i. Melting point of base used
ii. Liquefaction of base used
Second Step of Diffusion Depends Upon:
i. Solubility of drug
ii. Particle size
iii. Spreading capacity
iv. Excipient viscosity at rectal temperature
v. Retention of active principles by excipients
Third Step of Absorption Depends upon:
i. pKa of drug
ii. pH induced to rectal fluid
iii. presence of buffers
iv. additive affects on membrane permeability
v. partition co-efficient of drug
Factor Affecting Drug Absorption From Rectal
Suppository:
1. Physiologic Factor:
• The human rectum is approximately 15-20 cm in the length, when
empty of fecal material; it contains 2-3 ml of inert mucous fluid.
• In resting state, the rectum is non motile.
• There is no villa or microvillus on rectal mucosa.
Physiological factors include:
1) Colonic Content
2) Circulation
3) pH and lack of buffering capacity of the rectal fluid
2. Physiochemical Characteristics of the Drug:
i. Lipid water solubility of a drug (partition coefficient):
• The lipid water partition coefficient of a drug is important in selecting
the suppository base and in anticipating drug release from that base
• Lipophilic drug, in other word, distributed in a fatty suppository base
has fewer tendencies to escape to the surrounding queues fluids
• Thus water-soluble salt are preferred in fatty base suppository. water-
soluble base e.g. PEG, which dissolve in the rectal fluids, release both
water-soluble and oil-soluble drugs.
ii. Degree of Ionization:
The barrier separating colon lumen from the blood is preferentially
permeable to the unionized forms of drugs, thus absorption of drug
would be enhanced by increase the proportion of unionized drugs
iii. Concentration of a Drug in a Base:
• The more drugs in a base, the more drug will be available for
absorption.
• If the concentration of the drug in the intestinal lumen is above a
particular amount, the rate of absorption is not change by further
increase in concentration of drug.
3. Physiochemical Characteristics of the Base and Adjuvant:
i. Nature of the Base:
• Suppository base capable of melting, softening or dissolving to release the
drug for absorption.
• If the base irritating the colon, it will promote colonic response, lead to
increase bowl movement and decrease absorption.
ii. Presence of Adjuvant in Base:
• Adjuvant in a formula may affect drug absorption, change the
rheological properties of the base at body temperature, or affected
the dissolution of the drug.
SUPPOSITORY BASES
• Introduction:
• Base is an inert medium in which drug is incorporated to dissolve, suspend or
emulsify for a particular period of time.
• Suppository bases play an important role in the release of the medicaments
which they hold and therefore in the availability of the drug for absorption or
systemic effects for localized action.
• Bases alone used as emollient or lubricating effects or as vehicles in the
preparation of medicated suppositories.
Characteristics of an Ideal Suppository Base
(water and fatty base):
• It should be good in appearance.
• It should melt at body temperature (37oC).
• It should be non-toxic and non-irritating.
• It should be compatible with a broad variety of drugs.
• It should shrink (congealing) sufficiently on cooling to release from the mould.
• It should be non-sensitizing.
• It should have melting and emulsifying property.
• It should be stable on storage.
• It can be manufactured by molding either by hand, machine or compression.
• It should be stable if heated above its melting point.
• It should keep its shape while handling.
• It should release the medicament easily.
• It should have good water number.
Additional Characteristics for Fatty Bases:
If the base is fatty it has following requirements.
1. Acid value is below 0.2.
• It is also called as neutralization value.
• It is the mass of KOH (Potassium hydroxide) in mg that is required to
neutralize one gram of chemical substance.
2. SaponificationValuerangesfrom200-245.
• It is the no. of mg of KOH required to neutralize the free acids and saponify
the esters contained in 1gm of a fat.
3. Iodine Value is less than 1.
It is the no. of gm of iodine that reacts with 100g of fat or other unsaturated
material.
Classification of Suppository Bases:
• Suppository bases are classified into two main categories according to
their physical characteristics and a third miscellaneous group.
1. Fatty or oleaginous bases
• Cocoa Butter (Theobroma Oil)
• Hydrogenated Oil
2. The water soluble or water miscible bases
• Glycerogelatin Base
• Base of Polyethylene glycol
3. Miscellaneousbases
• Generally a combination of hydrophilic and hydrophobic substances
FATTY OR OLEAGINOUS BASES
A. Cocoa Butter (Theobroma Oil):
• It is the number of this group of the substances.
• Cocoa butter NF is defined as, « the fat obtained from the roasted
seeds of Theobroma cacao »
The Particular Characteristics of Cocoa Butter:
• Chemically it is triglyceride that is combination of glycerin with one or more
fatty acids.
• It is yellowish white solid, brittle fat which smells and taste like chocolate.
• Its melting point is between 300C to 350C.
• Its iodine value is ranges from 34 to 38.
• Its acid value is not higher than 4.
Different Crystalline Forms of Cocoa Butter:
Cocoa butter exhibits in four states.
i. α-form:
The α-form melts at 240C and it is obtained by suddenly cooling the melted
cocoa butter to 00C.
ii. β-form:
It crystallizes out from the liquefied cocoa butter with stirring at 18-230C. Its
melting point ranges from 28 to 310C.
iii. β’-form:
β’-form changes slowly into the stable form which melts between 34 to 350C
and this change is accompanied by a volume contraction.
iv. γ-form:
It melts at 180C and it is obtained by pouring a cool cocoa butter before it
solidifies into a container which is cooled at deep freeze temperature.
Methods to Prevent the Unstable Crystalline Forms:
Problems Associated with Volatile Drugs and the Cocoa Butter:
• Advantages Cocoa Butter: Non reactive, Melt at body temp,
Solidification point lies 12-13° C below melting point, viscocity hepls
in easy drug corporation.
• Disadvantages Cocoa Butter: Rancidity, Melt, Liquefy, metastable
form, Low contractility during solidification, Water number is low (20-
30), Leakage from the body.
B. Hydrogenated Oil (Cocoa Butter Substitutes)
Topical Treatment of Vegetable Oils to produce Suppository
Bases:
 The fat type suppository bases are produce from a variety of material
either synthetic or natural in origin e.g. vegetable oils including:
oCoconut Oil
oCotton Seed Oil
oPalmitic Oil
• These are modified by Esterification, hydrogenation or fractionation
at different melting range to obtain the desired product.
WATER SOLUBLE / MISCIBLE BASES:
• The main members of this group are:
• o Glycerogelatin Bases
o Polyethylene glycol
i. Glycerogelatin Bases
• Glycerogelatin bases may be prepared by dissolving gelatin 20%,
glycerin (70%), and adding solution or suspension of medicament
(10%).
Glycerogelatin Base in Vaginal Suppositories:
• Glycerogelatin base is not frequently used in preparation of vaginal
suppositories where prolong localized action of medicinal agent is
usually desired.
• It is slower to soften and mix with physiological fluids. It provides a
more prolonged release.
• They have a tendency to absorb the moisture due to hygroscopic
nature of glycerin.
• Therefore they must be protected from atmospheric moisture in
order to maintain their shape and consistency.
• Due to hygroscopicity of the glycerin, these suppositories may have a
dehydrated effect and be irritating to tissue upon insertion.
• The water present in formula for suppositories minimizes with water
to reduce the initial tendency of base to draw the water from mucus
membrane which irritate the tissue.
Glycerogelatin Base in Urethral Suppositories:
• TheurethralsuppositoriesmaybepreparedfromtheGlycerogelatinbase.
• For urethral suppositories the gelatin constitutes about 60% of the
weight of formula, glycerin about 20% and the medicated aqueous
portion 20%.
• Urethral suppositories of glycerogelatin are more easily inserted then
suppositories with cocoa butter base, because of brittleness of cocoa
butter and its rapid softening at body temperature.
ii. Polyethylene Glycol Bases (Carbowax)
• Polyethylene glycol is polymers of ethylene oxide and water prepare
to various chain length, molecular weights and physical states.
• These are available in a number of molecular weight ranges.
• The more commonly used polyethylene glycol bases are PEG 200,
400, 600, 800, 1500, 1540, 3350, 4000, 6000 and 8000.
• These numerical designations refer to the average molecular weight
of the polymers.
• PEG having average molecular weight of 200, 400 and 600 are clear
colorless liquids and those which have average molecular weight of
greater than 1000 are wax-like solids with hardness increasing with an
increase in molecular weight.
• Various combinations of these PEG may be combined by fusion, using
two or more of various types to achieve a suppository base of desired
consistency and characteristics.
• PEG suppositories don’t melt at body temperature and dissolve slowly
in body fluids.
• It is possible to prepare suppositories from PEG mixture having
melting point higher than that of body temperature.
• Advantages:
• It permits the slow release of medicament from base.
• Convenient storage of these suppositories without need of refrigerator and
• without danger of softening in warm weather.
• They’re chemically stable.
• Inert,andnon-irritating
• Itdoesn’tallowbacterialgrowth.
• Physical properties changes according to molecular weight.
• Itprovidesprolongedaction.
• Itdoesn’tsticktomold.
• Suppositoriesarecleanandsmoothinappearance.
Disadvantages:
i. If PEG suppository doesn’t contain atleast 20% of water they can
cause irritation to mucous membrane after insertion. In such case
they are dipped in water just prior to use. This procedure prevents
the moisture which is being drawn from tissue after insertion and
produces the ―stinging‖ sensation.
ii. In the miscellaneous group of bases are included those which are
mixtures of the oleaginous and water soluble or water miscible
materials.
iii. These materials may be physical or chemical mixtures.
iv. Some materials are preformed emulsions generally w/o type or
they may be dispersing in aqueous fluids.
v. One of these substances is polyoxyl 40 sterate.
Characteristics of Polyoxyl 40 Sterate:
i. It is a surface active agent that is employed in a no. of commercial
suppositories bases.
ii. This substance is waxy white solid that is water soluble.
iii. Its melting point is 39 – 400C.
iv. Mixtures of many fatty bases including cocoa butter with
emulsifying agent capable of forming w/o emulsions.
v. These bases have ability to hold water or aqueous solutions and
sometimes refer to as hydrophilic suppositories bases.
METHODS OF PREPARATION OF SUPPOSITORIES
Suppositories are prepared by three methods:
a. Molding from a melt (fusion)
b. Compression (Cold Compression)
c. Hand Rolling and Shaping
a. Preparation of Suppositories by molding (fusion):
 This method is most frequently employed both on a small
scale and on an industrial scale.
Bases Used:
•Cocoa butter
•Glycerinated gelatin
•Polyethylene glycol
• Suppository Molds:
• Molds in common use today are made from stainless steel,
aluminum, brass, or plastic.
• They’re reusable and disposable.
• Commercially available molds available for preparation of rectal,
vaginal, and urethral suppositories can produce individual or large
numbers of suppositories of various shapes and sizes.
i. Lubrication of the Mold
ii. Calibration of the Mold
iii. Preparing and Pouring the Melt
iv. Allowing the melt to cool and Congeal into Suppositories
v. Removing the formed suppositories from the mold
Advantages:
• It is a simple method.
• It gives suppositories that are more elegant than hand mould
suppositories.
• Sedimentation of solids in base is prevented.
• It is suitable for heat labile medicaments.
Disadvantages:
• Air entrapment may take place.
• This air may cause weight variation.
• The drug or base may be oxidized in air.
b. Preparation of Suppositories by Cold-Compression (Fusion)
Advantages:
• This technique is time saving.
• It gives suppositories that are more elegant than hand mould suppositories.
• Suitable for heat labile medicinal substances.
• No mold preparation
• No heating is required.
Disadvantages:
• The disadvantage to compression is that the special suppository machine is
required and there is some limitation as to the shapes of suppositories that
can be made.
• Manipulation requires considerable skills.
• Appearance is not elegant.
c. Hand Rolling Method
Advantage:
• It has the advantage of avoiding the necessity of heating the coca butter.
• No equipment required
• No special calculations are to be done
Disadvantages:
• Difficult to manufacture
• Not pretty in appearance
d. Automatic Molding
• The molding operations (pouring, cooling and removal) can be
performed by machine.
• All filling, ejecting and mold-cleaning operations are fully automated.
• The output of a typical rotary machine ranges from 3500 to 6000
suppositories an hour.
• Firstly, the prepared mass is filled into filling hopper where it is
continuously mixed and maintained at constant temperature.
• The suppository mould is lubricated by brushing or spraying.
• The cooling cycle is adjusted as required by individual suppository
mass by adjusting the speed of rotatory cooling turn table.
• After mass solidifies, the excess of material is scraped off and
collected for reuse.
• The solidified suppositories are moved to ejecting station, where the
mould is opened and suppositories are pushed out.
COMMERCIAL SUPPOSITORY PRODUCTION
• Automated filling of molds by volumetric dosing pumps
• Strips of perforated shells pass beneath dosing pumps & filled
successively
• Passed through cooling chambers for solidification.....sealed and then
• packaged
• Quality control procedures i.e. weight, volume, leakage are conducted
Injection Molding:
• Alternative to melt and pour molding
• Described by Snipes
• Use of injection molding technique developed for fabrication of plastics
• Excipients of choice are polyethylene glycol
• Povidone or silicon dioxide are added for viscosity or plasticity adjustment
CLASSIFICATION OF SUPPOSITORIES:
• Suppositories are classified into following types:
i. Rectal suppositories
ii. Vaginal suppositories or Pesseries
iii. Urethral suppositories or Bougies
iv. Nasal suppositories or Bouginaria
v. Ear suppositories
vi. Oral suppositories (Not used anymore)
i. Rectal Suppositories:
1. These are conical or cylindrical in shape.
2. These have flat base and tapered at the other end for easy insertion into
rectum.
3. Its length is usually 32mm and has a bullet shape e.g.Bisacodyl suppositories,
USP (10mg).
4. USP-NF states that adult rectal suppository should weight about 2 gram, when
cocoa butter is employed as the suppository base.
5. Rectal suppositories are used by infants or children are about half the weight
and size of the adult suppository and assume more pencil like shape.
6. Rectal suppositories are used for local, systemic or mechanical effect.
a. Local effect e.g. in hemorrhoids infection
b. Systemic effect e.g. infection away from rectum
c. Mechanical effect e.g. in evacuation of bowel in constipation
ii. Urethral Suppositories (Bougies):
• These are long, thin and pencil shaped.
• These are rounded from both sides.
• Their diameter is 5mm.
• Their length for male is 25mm and for female is 50 mm.
• Their weight for female is 2g and for male is 4g.
• These are rarely prescribed.
• For their formulation base is composed of glyceryl monosterate and
• polyoxyethylene.
• E.g. Furacin Urethral Inserts (Anti-septic)
iii. Nasal Suppositories (Bouginaria):
• These are pencil shaped similar to urethral suppositories.
• These are shorter in length i.e. about 32mm.
• Base for their formulation is usually glycerogelatin base.
iv.
v.
SPECIFIC PROBLEMS IN FORMULATING
SUPPOSITORIES:
1. Water in Suppositories:
Use of water as a solvent for drug should be avoided for the following.
Reasons:
• Water accelerates oxidation of fats.
• If water evaporates, the dissolved substance crystallizes out.
• Unless H2O is present at level than that requires for dissolving the drug, the
water has little value in facilitating drug absorption. Absorption from water
containing suppository enhance only if an oil in water emulsion exist with more
than 50% of the water in the external phase .
• Reaction between ingredients (in suppository) are more likely to occur in the
presence of water.
• The incorporation of water or other substances that might be contaminate with
bacteria or fungi necessitates the addition of bacteriostatic agents (as parabens)
2- Hygroscopicity:
• Glycerinated gelatin suppositories lost moisture by evaporation in dry
climates and absorbed moisture under conditions of high humidity
• PEG bases are also hygroscopic
3. Incompatibilities:
•PEG bases are incompatible with silver salt, tannic acid, aminopyrine ,
quinine , icthammol, asprine , benzoc.aine & sulphonamides .
•Many chemicals have a tendency to crystallize out of PEG, e.g.: sodium
sarbital, salicylic acid & camphor.
•Higher concentration of salicylic acid softens PEG to an ointment-like
consistency, d- Aspirin complexes with PEG.
•Penicillin G, although stable in cocoa butter and other fatty bases, was
found to decompose in PEG bases .
•Fatty bases with significant hydroxyl values may react with acidic
ingredients.
4- Viscosity:
•The viscosity of the melted suppository base is important in the manufacture
of the suppository and to its behavior in the rectum after melting.
•Melted cocoa butter have low viscosity than glycerinated gelatin and PEG
type base in low viscosity bases, extra
•Care must be exercised to avoid sedimentation of suspended particles.
•To overcome the problems caused by use of low viscosity bases:
o Use base with a narrower melting rang that is closer to body temperature.
o The inclusion of approximately 2% aluminum monostearate not only
increases the viscosity of the fat base but to maintain homogenous suspension
of insoluble material.
o Cetyl, stearyl or myristyl alcohols or stearic acid are added to improve the
consistency of suppositories.
5- Brittleness:
• Suppositories made from cocoa butter are elastic and don't fracture
readily.
• Synthetic fat base with high degree of hydrogenation and high
stearate content and higher solids content at room temperature are
usually more brittle.
• To overcome
o The temperature difference between the melted base & the mold
should be minimal.
o Addition of small amount of Tween 80, castor oil, glycerin imparts
plasticity to a fat
6- Volume contraction:
Occurs in many melted suppository base after cooling the mold, result in:
o Good mold release (contraction facilitate the removal of the suppository
from the mold , eliminating the need for mold release agents).
o Contraction hole formation at the open end of the mold, this will lowered
suppository . The contraction can be eliminated by pouring a mass slightly
above its congealing temperature into a mold warmed at about the same
temperature or the mold is overfilled so that the excess mass containing the
contraction hole can be scraped off.
Lubricant or mold releasing agent:
o Cocoa butter adheres to suppository molds because of its low volume
contraction. A various mold lubricants or release agents must be used to
overcome this difficulty (mineral oil, aqueous solution of sodium lauryl
sulfate , alcohol , silicones , soap).
o The release of suppository from damaged mold was improved by coating
the cavities with polytetrofluoroethylene (Teflone).
7- Rancidity and Antioxidant:
Rancidity results from the autoxidation and subsequent decomposition
of unsaturated fats into low & medium molecular weight saturated &
unsaturated aldehydes , ketones and acids , which have strong
unpleasant odor. Examples of effective antioxidant are phenols such as
―hydroquinone or B-naphtholquinone.
QUALITY CONTROL OF SUPPOSITORIES:
1. Surface Appearance and Shape:
2. Melting Test Range:
3. Liquefaction or Softening Time Tests of Rectal Suppositories:
4. Breaking Test:
5. Mechanical Strength:
6. Melting & Solidification:
7. Dissolution Testing:
DISPLACEMENT VALUES:
• The displacement value of a medicament is the no. of parts by weight
of a medicament that will displace one part of suppository base
(normally Theobroma oil).
• Displacement values for various medicaments are given in B.P.C.
(British Pharmaceutical Codex).
• It is the amount of drug that will displace one part of base. OR
• It is the amount of the base which is displaced by certain amount of
drug.
Problem # 1:
• Calculate the quantities required to make 10 theobroma oil
suppositories (2g mould) each containing 400mg of zinc oxide
(displacement value = 4.7).
Solution:
• Total wt. of zinc oxide required = 400 mg × 10 = 4000 mg = 4 g
• Wt. of base required for un-medicated suppositories = 2g × 10 = 20 g
• As the displacement value of ZnO = 4.7
And,
• 4.7 g of ZnO displace theobroma oil = 1 g
• 1 g of ZnO displace theobroma oil = 1/4.7
• 4 g of ZnO displace theobroma oil = 1/4.7 * 4 = 0.85
So,
Wt. of suppository base required to make medicated suppositories =
20 – 0.85 = 19.15 gm
PACKAGING AND STORAGE:
• Suppositories are often packaged in partitioned boxes that hold the
suppositories upright.
• Glycerine and glycerinated derivatives are often packed in screw-
capped glass containers.
• Many other suppositories are wrapped individually in tin, aluminum
foil, paper, plastic or PVC-polyethylene.
• Poorly packed suppositories may give rise to staining, breakage or
deformation by melting.
• Strip packaging is common place.
• Alternatively, suppositories may be molded directly into their
packages and then store below 300C to gain a specific shape.
• All suppositories particularly Theobroma oil suppositories and
glycerogelat in suppositories should be refrigerated.
• Polyethylene glycol suppositories are stored at usual room
temperature without requirement of refrigerator.
VAGINAL AND RECTAL SOLUTIONS
Vaginal Douches:
1. These powders are used to prepare solutions for vaginal douche, for
irrigating and cleansing of vagina.
2. These powders may be prepared and packed in bulk or as a unit
packages.
3. Unit package is designed to contain the appropriate amount of
powder to prepare the specified volume of douche solution.
4. The bulk powders are used by tea spoonfull(5ml) or table
spoonfull(15ml) in preparation of desired solution.
Components of Douche Solution:
1. Boric acid (sodium borate)
2. Astringente.g.Potassiumorzincsulphate
3. Anti-microbial agent e.g. iodine
4. Surfactant or detergents (sodium Lauryl sulphate)
5. Salts (Sod. Citrate or sodium chloride)
6. Quaternary ammonium compounds e.g. benzethonium chloride
7. Oxidizing agents e.g. sodium perborate
8. Aromatics, e.g. menthol, thymol, and phenol etc.
Use:
The douche powders are used for hygiene effect.
Rectal Douches (Enemas)
• An enema is an introduction of fluid into the lower bowel through the
rectum for the purpose of cleansing or to introduce medication or
nourishment
1. Retention enemas
• Stimulant Enemas
• Nutrient Enemas
• Emollient Enemas
• Sedative Enemas
• Anesthetic Enemas
2 Evacuation enemas
• Simple Evacuant Enemas
• MedicatedEvacuantEnemas
• ColdEvacuantEnemas
3. Medicated Evacuant Enemas:
• Oil Enemas
• Purgative Enemas
• AstringentEnemas
• Anthelmintic Enemas
• Carminative Enemas
Purpose of Enemas:
• To stimulate defecation & to treat constipation ex: simple evacuant enema
• To soften hard faecal matter ex: oil enema
• To administer medication ex: sedative enema
• To protect and soothe the mucus membrane of intestine & to check
diarrhoea ex : emollient enema
• To destroy intestinal parasites ex : anthelminitic enema
• To relieve the gaseous distention ex : carminative enema
• To administer the fluid and nutrients ex: nutritive enema
• To relieve inflammation ex : astringent enema
• To induce peristalsis ex : purgative enema
• To stimulate a person in shock and collapse ex: stimulant enema
• To reduce the temperature ex : cold enema or ice enema
• To clean the bowels prior to x-ray studies, visualization of the bowel ,
surgery on the bowel or delivery of a baby ex : saline enema
• To make diagnosis ex: barium enema
• To establish regular bowel functions during a bowel training
programme
• To induce anesthesia ex : anesthetic enema
RETENTION ENEMAS:
1. A no. of solutions administered rectally for local effect e.g.
hydrocortisone or for systemic absorption e.g. aminophylline.
2. In case of aminophylline rectal administration minimizes the
undesirable gastrointestinal reaction associated with oral therapy.
3. Corticosteroids are administered as retention enemas for the
treatment of patients for ulcerative colitis.
Stimulant Enema:
• A stimulant enema is given in the treatment of shock and collapse
• It is also sometimes given in case of poisoning e.g. coffee enema is
given in case of opium poisoning
Solutions:
• Black coffee : 1 table spoon coffee powder to 300 ml of water
• Brandy : 15 ml of brandy added to 120 to 180 ml of glucose saline
• Amount of solution: 180 to 240 ml
• Temp of solution: 108 to 110 degree Fahrenheit
• Sedative enema:
• It is retention enema containing a sedative drug given to induce sleep
• Drugs used:
o Paraldehyde
o Chloral hydrate
o Potassium bromide
Dose: As ordered by the doctor
• Anesthetic Enema:
• It is a retention enema containing an anesthetic drug to produce anesthesia in client
Drugs used: Avertin
Dose: 150 to 300 mg per kg of body weight
• Emollient Enema:
• This is an introduction of bland solution into the rectum for the purpose of
checking diarrhea or soothing & relieving irritation on an inflamed mucus
membrane
Solution used:
o Starch & opium : opium 1 to 2ml is added to 120 to 180 ml of starch
mucilage or rice water
o Starch mucilage alone
• Amount of solution: 120 to 180 ml
• Temp of solution: 100 to 105 degree Fahrenheit (37.8 to 40.5 degree
centigrade )
Nutrient Enema:
• It is a retention enema to supply food & fluids to the body.
• Selection of the fluids depends upon the ability of the colon to absorb it.
• Nutrient enema is particularly useful in conditions like haemophilia which
makes I.V. infusion difficult or undesirable
Solutions :
o Normal saline
o Glucose 2 to 5%
o Peptonized milk 120 ml
• Amount of solution: 1100 to 1700 ml in 24 hour or 180 to 270 ml at 4
hourly interval
• Temperature of solution: 100 degree Fahrenheit (37.8 degree Fahrenheit )
EVACUATION ENEMAS:
• The rectal enemas are used to cleanse the bowel.
• Many enemas are available in disposable plastic squeeze bottles
containing premeasured amount of enemas solution.
• The active agents are solutions of:
a. Sodium phosphate
b. Sodium biphosphate
c. Glycerine
d. Light Mineral Oil
Simple Evacuant Enema:
• Purpose :
To stimulate defecation & to treat constipation
To relieve the gaseous distention by stimulating the peristalsis
To relieve the retention of urine by reflex stimulation of the bladder
To stimulate uterine contraction & to hasten the child birth
To cleanse the bowel prior to x-ray studies, visualization of the bowels (ex:
sigmoidoscopy), surgery & retention enemas
• Solutions Used:
i. Soap & water: soap jelly 50ml to 1 liter of water
ii. Normal saline: sodium chloride 1 teaspoon of half liter of water
iii. Tap water
• Amount of solutions to be used:
o Adults:500to1000ml(1to2pint)
o Children's: 250 to 500 ml ( 0.5 to 1 pint ) o Infants: 250 ml or less
• Temp of solution:
o Adults : 105 to 110 degree Fahrenheit
o Children : 100 degree Fahrenheit
Oil Enema:
• These are given to soften fecal matter in case of severe constipation.
• Before the 1st bowel movement after operation on the rectum or
perineum.
• To avoid straining & injury to the sutures & wounds.
• It should be retained for half an hour to 1 hour to soften the faeces.
• It should then be followed by a soap & water enema to open the bowels.
Solutions used:
o Olive oil
o Gingerly oil or sweet oil
o Castor oil & olive oil (1:2)
Amount of solution to be used: 115 to 175 ml
Temperature of the solutions: 100 degree Fahrenheit
Purgative Enema:
• These are given to cause the bowel to contrast actively & to evacuate its contents.
• Its acts by their irritating effect on the mucus lining , stimulate peristalsis & cause the
evacuation of bowel.
• The stretching of the intestine due to this inflow of fluid causes the intestine to
contract & leads to the evacuation of bowel.
Solutions used:
o Pure glycerin – 15 to 30 ml
o Glycerin & water – 1:2
o Glycerin & caster oil – 1:1
o Magnesium sulphate : 60 to 120 ml with sufficient amount of water to
dissolve it
o 1-2-3 enema : magnesium sulphate 30 ml, glycerin 60 ml, & water 90 ml
Amount & temp of solution is that of oil enema
Carminative Enema (Anti spasmodic):
• These are given to relieve gaseous distention of the abdomen by
causing peristalsis & expulsion of flatus & faeces
• It is given as simple evacuant enema.
Solution:
• Turpentine : 8 to 16 ml of turpentine mixed thoroughly with 600 to
1200 ml of soap solution
• Milk and molasses (granular sugar ) : 90 to 230 ml of molasses well
mixed with equal quantity of warm milk
Anthelmintic Enema:
• This is given to destroy & expel the worms from the intestines.
• Before the treatment is given the bowel should be cleansed by a soap
water enema so that the drug may come in direct contact with the
worms & the lining of the intestine.
• The treatment is given until the worms are destroyed.
Solution :
o Infusion of quassia : 15gms of chips to 600 ml of water
o Hypertonic saline solution : sodium chloride 60 ml with 600 ml of
water
Amount of the solution: 250 ml
Astringent Enema:
• It contracts the tissues & the blood vessels, checks bleeding &
inflammation, lessens the amount of mucus discharge & gives a temporary
relief in the inflamed area.
• It is usually given in colitis & dysentery.
• They are usually given in the form of rectal or colonic irrigations.
• The solution is allowed to run in slowly & return quickly to avoid
distension, pain & irritation of the inflamed wall.
• Solutions:
o Tannic acid : 2 gms to 600ml of water
o Alum : 30 gms to 600ml of water
o Silver nitrate 2% : (silver nitrate is dissolved in distilled water )
• Temperature of the solution: It is given as hot as the client can stand
Cold Enema (Ice Enema):
• This is given to decrease the body temperature in hyperpyrexia and
heat stroke.
• It is given in the form of colonic irrigation.
Complications :
o Hypothemia
o Abdominal cramps

More Related Content

What's hot

Surface and Interfacial tension [Part-6] ( Solubilization, Detergency, Adsorp...
Surface and Interfacial tension [Part-6]( Solubilization, Detergency, Adsorp...Surface and Interfacial tension [Part-6]( Solubilization, Detergency, Adsorp...
Surface and Interfacial tension [Part-6] ( Solubilization, Detergency, Adsorp...
Ms. Pooja Bhandare
 
Pharmaceutical solutions
Pharmaceutical solutionsPharmaceutical solutions
Pharmaceutical solutions
MuhammadUmair674
 
Stability of suspensions
Stability of suspensionsStability of suspensions
Stability of suspensions
Abdelrhman abooda
 
Pharmaceutical Dosage Forms - Classification
Pharmaceutical Dosage Forms - ClassificationPharmaceutical Dosage Forms - Classification
Pharmaceutical Dosage Forms - Classification
Md Altamash Ahmad
 
Vaginal route of administration
Vaginal route of administrationVaginal route of administration
Vaginal route of administration
SANDEEP MEWADA
 
Ointment
OintmentOintment
Pharmaceutical Emulsion
Pharmaceutical EmulsionPharmaceutical Emulsion
Pharmaceutical Emulsion
Mirza Salman Baig
 
Dosage forms and routes of drug administration
Dosage forms and routes of drug administrationDosage forms and routes of drug administration
Dosage forms and routes of drug administration
FatenAlsadek
 
Suspensions
SuspensionsSuspensions
Suspensions
Saif Khan
 
Pharmaceutical Suspension
Pharmaceutical SuspensionPharmaceutical Suspension
Pharmaceutical Suspension
Parag Jain
 
Pharmaceutical dosage forms
Pharmaceutical dosage formsPharmaceutical dosage forms
Pharmaceutical dosage forms
Harishankar Sahu
 
Pharmaceutical Elixirs
Pharmaceutical ElixirsPharmaceutical Elixirs
Pharmaceutical Elixirs
Mohammad Zain Idrees
 
Pastes
PastesPastes
Syrups and elixirs
Syrups and elixirsSyrups and elixirs
Syrups and elixirs
Medical Knowledge
 
Disperse system--------(Pharmaceutics)
Disperse system--------(Pharmaceutics)Disperse system--------(Pharmaceutics)
Disperse system--------(Pharmaceutics)
Soft-Learners
 
emulsion
 emulsion emulsion
emulsion
Ravikumar Patil
 
Mechanism of solute solvent interaction
Mechanism of solute solvent interactionMechanism of solute solvent interaction
Mechanism of solute solvent interaction
VickyLone1
 
Surfactant
SurfactantSurfactant
Surfactant
Sagar Savale
 
Syrups and elixirs
Syrups and elixirsSyrups and elixirs
Syrups and elixirs
M ArsaLan ChisHti
 

What's hot (20)

Powders
PowdersPowders
Powders
 
Surface and Interfacial tension [Part-6] ( Solubilization, Detergency, Adsorp...
Surface and Interfacial tension [Part-6]( Solubilization, Detergency, Adsorp...Surface and Interfacial tension [Part-6]( Solubilization, Detergency, Adsorp...
Surface and Interfacial tension [Part-6] ( Solubilization, Detergency, Adsorp...
 
Pharmaceutical solutions
Pharmaceutical solutionsPharmaceutical solutions
Pharmaceutical solutions
 
Stability of suspensions
Stability of suspensionsStability of suspensions
Stability of suspensions
 
Pharmaceutical Dosage Forms - Classification
Pharmaceutical Dosage Forms - ClassificationPharmaceutical Dosage Forms - Classification
Pharmaceutical Dosage Forms - Classification
 
Vaginal route of administration
Vaginal route of administrationVaginal route of administration
Vaginal route of administration
 
Ointment
OintmentOintment
Ointment
 
Pharmaceutical Emulsion
Pharmaceutical EmulsionPharmaceutical Emulsion
Pharmaceutical Emulsion
 
Dosage forms and routes of drug administration
Dosage forms and routes of drug administrationDosage forms and routes of drug administration
Dosage forms and routes of drug administration
 
Suspensions
SuspensionsSuspensions
Suspensions
 
Pharmaceutical Suspension
Pharmaceutical SuspensionPharmaceutical Suspension
Pharmaceutical Suspension
 
Pharmaceutical dosage forms
Pharmaceutical dosage formsPharmaceutical dosage forms
Pharmaceutical dosage forms
 
Pharmaceutical Elixirs
Pharmaceutical ElixirsPharmaceutical Elixirs
Pharmaceutical Elixirs
 
Pastes
PastesPastes
Pastes
 
Syrups and elixirs
Syrups and elixirsSyrups and elixirs
Syrups and elixirs
 
Disperse system--------(Pharmaceutics)
Disperse system--------(Pharmaceutics)Disperse system--------(Pharmaceutics)
Disperse system--------(Pharmaceutics)
 
emulsion
 emulsion emulsion
emulsion
 
Mechanism of solute solvent interaction
Mechanism of solute solvent interactionMechanism of solute solvent interaction
Mechanism of solute solvent interaction
 
Surfactant
SurfactantSurfactant
Surfactant
 
Syrups and elixirs
Syrups and elixirsSyrups and elixirs
Syrups and elixirs
 

Similar to suppositories Dr.pptx

Suppositories SB 2020
Suppositories SB 2020Suppositories SB 2020
Suppositories SB 2020
Mirza Salman Baig
 
Fundamentals of LA Administration
Fundamentals of LA AdministrationFundamentals of LA Administration
Fundamentals of LA Administration
letsgogaga
 
Suppositories sb
Suppositories sbSuppositories sb
Suppositories sb
Mirza Salman Baig
 
Suppository - Types & Formulation
Suppository - Types & FormulationSuppository - Types & Formulation
Suppository - Types & Formulation
Zobayer Hossain
 
SUPPOSITORIES.pdf
SUPPOSITORIES.pdfSUPPOSITORIES.pdf
SUPPOSITORIES.pdf
TridevSastri1
 
Suppositories and pessaries
Suppositories and pessariesSuppositories and pessaries
Suppositories and pessaries
Nabina Paudel
 
Solutions
SolutionsSolutions
Solutions
NoumanAziz13
 
Parenteral products
Parenteral productsParenteral products
Parenteral products
Abd Rhman Gamil gamil
 
SUPPOSITORIES & PESSARIES Pharmaceutics .ppt
SUPPOSITORIES & PESSARIES Pharmaceutics .pptSUPPOSITORIES & PESSARIES Pharmaceutics .ppt
SUPPOSITORIES & PESSARIES Pharmaceutics .ppt
nsppharmacist
 
Pharmacology
PharmacologyPharmacology
Pharmacology
sallamahmed1
 
chapter 2.pptx
chapter 2.pptxchapter 2.pptx
chapter 2.pptx
MohammedAbdela7
 
Pharmacokinetics.pptx
Pharmacokinetics.pptxPharmacokinetics.pptx
Pharmacokinetics.pptx
DeeptiBhagchandani
 
Forms of topical medicines
Forms of topical medicinesForms of topical medicines
Forms of topical medicinesbelton Mybelton
 
Rectal & vaginal
Rectal & vaginalRectal & vaginal
Rectal & vaginal
Abd Rhman Gamil gamil
 
Oral Solutions Dr.pptx
Oral Solutions Dr.pptxOral Solutions Dr.pptx
Oral Solutions Dr.pptx
Dr. Samia
 
Leture 1 slides.pptx
Leture 1 slides.pptxLeture 1 slides.pptx
Leture 1 slides.pptx
SarahAlaa31
 
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
wakogeleta
 
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
gopu vijaya sindhuri
 
Absorption of drugs
Absorption of drugsAbsorption of drugs
Absorption of drugs
Harsha Negi
 
biopharmaceutical factors affecting drug bioavailability.pptx
biopharmaceutical factors affecting drug bioavailability.pptxbiopharmaceutical factors affecting drug bioavailability.pptx
biopharmaceutical factors affecting drug bioavailability.pptx
anumalagundam sreekanth
 

Similar to suppositories Dr.pptx (20)

Suppositories SB 2020
Suppositories SB 2020Suppositories SB 2020
Suppositories SB 2020
 
Fundamentals of LA Administration
Fundamentals of LA AdministrationFundamentals of LA Administration
Fundamentals of LA Administration
 
Suppositories sb
Suppositories sbSuppositories sb
Suppositories sb
 
Suppository - Types & Formulation
Suppository - Types & FormulationSuppository - Types & Formulation
Suppository - Types & Formulation
 
SUPPOSITORIES.pdf
SUPPOSITORIES.pdfSUPPOSITORIES.pdf
SUPPOSITORIES.pdf
 
Suppositories and pessaries
Suppositories and pessariesSuppositories and pessaries
Suppositories and pessaries
 
Solutions
SolutionsSolutions
Solutions
 
Parenteral products
Parenteral productsParenteral products
Parenteral products
 
SUPPOSITORIES & PESSARIES Pharmaceutics .ppt
SUPPOSITORIES & PESSARIES Pharmaceutics .pptSUPPOSITORIES & PESSARIES Pharmaceutics .ppt
SUPPOSITORIES & PESSARIES Pharmaceutics .ppt
 
Pharmacology
PharmacologyPharmacology
Pharmacology
 
chapter 2.pptx
chapter 2.pptxchapter 2.pptx
chapter 2.pptx
 
Pharmacokinetics.pptx
Pharmacokinetics.pptxPharmacokinetics.pptx
Pharmacokinetics.pptx
 
Forms of topical medicines
Forms of topical medicinesForms of topical medicines
Forms of topical medicines
 
Rectal & vaginal
Rectal & vaginalRectal & vaginal
Rectal & vaginal
 
Oral Solutions Dr.pptx
Oral Solutions Dr.pptxOral Solutions Dr.pptx
Oral Solutions Dr.pptx
 
Leture 1 slides.pptx
Leture 1 slides.pptxLeture 1 slides.pptx
Leture 1 slides.pptx
 
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
1_Midwifery_introduction_to_pharmacology_and_pharmacokinetics_2015.pptx
 
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
Suppositories by G VIJAYA SINDHURI(Ph.D) Department of pharmaceutics
 
Absorption of drugs
Absorption of drugsAbsorption of drugs
Absorption of drugs
 
biopharmaceutical factors affecting drug bioavailability.pptx
biopharmaceutical factors affecting drug bioavailability.pptxbiopharmaceutical factors affecting drug bioavailability.pptx
biopharmaceutical factors affecting drug bioavailability.pptx
 

More from Dr. Samia

evaporationanddistillation.pptx
evaporationanddistillation.pptxevaporationanddistillation.pptx
evaporationanddistillation.pptx
Dr. Samia
 
Otic preps Dr.pptx
Otic preps Dr.pptxOtic preps Dr.pptx
Otic preps Dr.pptx
Dr. Samia
 
Opthalmic Dr.pptx
Opthalmic Dr.pptxOpthalmic Dr.pptx
Opthalmic Dr.pptx
Dr. Samia
 
galenicals DR.pptx
galenicals DR.pptxgalenicals DR.pptx
galenicals DR.pptx
Dr. Samia
 
solvents used in pharma prep DR.pptx
solvents used in pharma prep DR.pptxsolvents used in pharma prep DR.pptx
solvents used in pharma prep DR.pptx
Dr. Samia
 
ORS, OCLS.ppt
ORS, OCLS.pptORS, OCLS.ppt
ORS, OCLS.ppt
Dr. Samia
 
Aerosols Dr.ppt
Aerosols Dr.pptAerosols Dr.ppt
Aerosols Dr.ppt
Dr. Samia
 
aromatic waters Dr.pptx
aromatic waters Dr.pptxaromatic waters Dr.pptx
aromatic waters Dr.pptx
Dr. Samia
 
Emulsions Dr.pptx
Emulsions Dr.pptxEmulsions Dr.pptx
Emulsions Dr.pptx
Dr. Samia
 
TDDS Dr.pdf
TDDS Dr.pdfTDDS Dr.pdf
TDDS Dr.pdf
Dr. Samia
 
suspensions Dr.pptx
suspensions Dr.pptxsuspensions Dr.pptx
suspensions Dr.pptx
Dr. Samia
 
emulsions Dr Samia.pdf
emulsions Dr Samia.pdfemulsions Dr Samia.pdf
emulsions Dr Samia.pdf
Dr. Samia
 
Introduction.pdf
Introduction.pdfIntroduction.pdf
Introduction.pdf
Dr. Samia
 
powders, granules, tablets, capsules Dr.pptx
powders, granules, tablets, capsules Dr.pptxpowders, granules, tablets, capsules Dr.pptx
powders, granules, tablets, capsules Dr.pptx
Dr. Samia
 
Magmas and Gels Dr.pptx
Magmas and Gels Dr.pptxMagmas and Gels Dr.pptx
Magmas and Gels Dr.pptx
Dr. Samia
 
Pesticides 2nd yr cognosy
Pesticides 2nd yr cognosyPesticides 2nd yr cognosy
Pesticides 2nd yr cognosy
Dr. Samia
 
Industrial hazards 4rth yr
Industrial hazards 4rth yrIndustrial hazards 4rth yr
Industrial hazards 4rth yr
Dr. Samia
 
Sterile products manufacturing
Sterile products manufacturingSterile products manufacturing
Sterile products manufacturing
Dr. Samia
 
Sterelization 08 04-2021
Sterelization 08 04-2021Sterelization 08 04-2021
Sterelization 08 04-2021
Dr. Samia
 
Drying 4rth prof
Drying 4rth profDrying 4rth prof
Drying 4rth prof
Dr. Samia
 

More from Dr. Samia (20)

evaporationanddistillation.pptx
evaporationanddistillation.pptxevaporationanddistillation.pptx
evaporationanddistillation.pptx
 
Otic preps Dr.pptx
Otic preps Dr.pptxOtic preps Dr.pptx
Otic preps Dr.pptx
 
Opthalmic Dr.pptx
Opthalmic Dr.pptxOpthalmic Dr.pptx
Opthalmic Dr.pptx
 
galenicals DR.pptx
galenicals DR.pptxgalenicals DR.pptx
galenicals DR.pptx
 
solvents used in pharma prep DR.pptx
solvents used in pharma prep DR.pptxsolvents used in pharma prep DR.pptx
solvents used in pharma prep DR.pptx
 
ORS, OCLS.ppt
ORS, OCLS.pptORS, OCLS.ppt
ORS, OCLS.ppt
 
Aerosols Dr.ppt
Aerosols Dr.pptAerosols Dr.ppt
Aerosols Dr.ppt
 
aromatic waters Dr.pptx
aromatic waters Dr.pptxaromatic waters Dr.pptx
aromatic waters Dr.pptx
 
Emulsions Dr.pptx
Emulsions Dr.pptxEmulsions Dr.pptx
Emulsions Dr.pptx
 
TDDS Dr.pdf
TDDS Dr.pdfTDDS Dr.pdf
TDDS Dr.pdf
 
suspensions Dr.pptx
suspensions Dr.pptxsuspensions Dr.pptx
suspensions Dr.pptx
 
emulsions Dr Samia.pdf
emulsions Dr Samia.pdfemulsions Dr Samia.pdf
emulsions Dr Samia.pdf
 
Introduction.pdf
Introduction.pdfIntroduction.pdf
Introduction.pdf
 
powders, granules, tablets, capsules Dr.pptx
powders, granules, tablets, capsules Dr.pptxpowders, granules, tablets, capsules Dr.pptx
powders, granules, tablets, capsules Dr.pptx
 
Magmas and Gels Dr.pptx
Magmas and Gels Dr.pptxMagmas and Gels Dr.pptx
Magmas and Gels Dr.pptx
 
Pesticides 2nd yr cognosy
Pesticides 2nd yr cognosyPesticides 2nd yr cognosy
Pesticides 2nd yr cognosy
 
Industrial hazards 4rth yr
Industrial hazards 4rth yrIndustrial hazards 4rth yr
Industrial hazards 4rth yr
 
Sterile products manufacturing
Sterile products manufacturingSterile products manufacturing
Sterile products manufacturing
 
Sterelization 08 04-2021
Sterelization 08 04-2021Sterelization 08 04-2021
Sterelization 08 04-2021
 
Drying 4rth prof
Drying 4rth profDrying 4rth prof
Drying 4rth prof
 

Recently uploaded

The Art Pastor's Guide to Sabbath | Steve Thomason
The Art Pastor's Guide to Sabbath | Steve ThomasonThe Art Pastor's Guide to Sabbath | Steve Thomason
The Art Pastor's Guide to Sabbath | Steve Thomason
Steve Thomason
 
How to Create Map Views in the Odoo 17 ERP
How to Create Map Views in the Odoo 17 ERPHow to Create Map Views in the Odoo 17 ERP
How to Create Map Views in the Odoo 17 ERP
Celine George
 
The Roman Empire A Historical Colossus.pdf
The Roman Empire A Historical Colossus.pdfThe Roman Empire A Historical Colossus.pdf
The Roman Empire A Historical Colossus.pdf
kaushalkr1407
 
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
siemaillard
 
TESDA TM1 REVIEWER FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
TESDA TM1 REVIEWER  FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...TESDA TM1 REVIEWER  FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
TESDA TM1 REVIEWER FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
EugeneSaldivar
 
Fish and Chips - have they had their chips
Fish and Chips - have they had their chipsFish and Chips - have they had their chips
Fish and Chips - have they had their chips
GeoBlogs
 
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCECLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
BhavyaRajput3
 
Basic phrases for greeting and assisting costumers
Basic phrases for greeting and assisting costumersBasic phrases for greeting and assisting costumers
Basic phrases for greeting and assisting costumers
PedroFerreira53928
 
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptxStudents, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
EduSkills OECD
 
special B.ed 2nd year old paper_20240531.pdf
special B.ed 2nd year old paper_20240531.pdfspecial B.ed 2nd year old paper_20240531.pdf
special B.ed 2nd year old paper_20240531.pdf
Special education needs
 
Additional Benefits for Employee Website.pdf
Additional Benefits for Employee Website.pdfAdditional Benefits for Employee Website.pdf
Additional Benefits for Employee Website.pdf
joachimlavalley1
 
Unit 2- Research Aptitude (UGC NET Paper I).pdf
Unit 2- Research Aptitude (UGC NET Paper I).pdfUnit 2- Research Aptitude (UGC NET Paper I).pdf
Unit 2- Research Aptitude (UGC NET Paper I).pdf
Thiyagu K
 
How to Make a Field invisible in Odoo 17
How to Make a Field invisible in Odoo 17How to Make a Field invisible in Odoo 17
How to Make a Field invisible in Odoo 17
Celine George
 
Introduction to Quality Improvement Essentials
Introduction to Quality Improvement EssentialsIntroduction to Quality Improvement Essentials
Introduction to Quality Improvement Essentials
Excellence Foundation for South Sudan
 
Polish students' mobility in the Czech Republic
Polish students' mobility in the Czech RepublicPolish students' mobility in the Czech Republic
Polish students' mobility in the Czech Republic
Anna Sz.
 
Thesis Statement for students diagnonsed withADHD.ppt
Thesis Statement for students diagnonsed withADHD.pptThesis Statement for students diagnonsed withADHD.ppt
Thesis Statement for students diagnonsed withADHD.ppt
EverAndrsGuerraGuerr
 
Palestine last event orientationfvgnh .pptx
Palestine last event orientationfvgnh .pptxPalestine last event orientationfvgnh .pptx
Palestine last event orientationfvgnh .pptx
RaedMohamed3
 
Sectors of the Indian Economy - Class 10 Study Notes pdf
Sectors of the Indian Economy - Class 10 Study Notes pdfSectors of the Indian Economy - Class 10 Study Notes pdf
Sectors of the Indian Economy - Class 10 Study Notes pdf
Vivekanand Anglo Vedic Academy
 
Synthetic Fiber Construction in lab .pptx
Synthetic Fiber Construction in lab .pptxSynthetic Fiber Construction in lab .pptx
Synthetic Fiber Construction in lab .pptx
Pavel ( NSTU)
 
Ethnobotany and Ethnopharmacology ......
Ethnobotany and Ethnopharmacology ......Ethnobotany and Ethnopharmacology ......
Ethnobotany and Ethnopharmacology ......
Ashokrao Mane college of Pharmacy Peth-Vadgaon
 

Recently uploaded (20)

The Art Pastor's Guide to Sabbath | Steve Thomason
The Art Pastor's Guide to Sabbath | Steve ThomasonThe Art Pastor's Guide to Sabbath | Steve Thomason
The Art Pastor's Guide to Sabbath | Steve Thomason
 
How to Create Map Views in the Odoo 17 ERP
How to Create Map Views in the Odoo 17 ERPHow to Create Map Views in the Odoo 17 ERP
How to Create Map Views in the Odoo 17 ERP
 
The Roman Empire A Historical Colossus.pdf
The Roman Empire A Historical Colossus.pdfThe Roman Empire A Historical Colossus.pdf
The Roman Empire A Historical Colossus.pdf
 
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
aaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaaa
 
TESDA TM1 REVIEWER FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
TESDA TM1 REVIEWER  FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...TESDA TM1 REVIEWER  FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
TESDA TM1 REVIEWER FOR NATIONAL ASSESSMENT WRITTEN AND ORAL QUESTIONS WITH A...
 
Fish and Chips - have they had their chips
Fish and Chips - have they had their chipsFish and Chips - have they had their chips
Fish and Chips - have they had their chips
 
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCECLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
CLASS 11 CBSE B.St Project AIDS TO TRADE - INSURANCE
 
Basic phrases for greeting and assisting costumers
Basic phrases for greeting and assisting costumersBasic phrases for greeting and assisting costumers
Basic phrases for greeting and assisting costumers
 
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptxStudents, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptx
 
special B.ed 2nd year old paper_20240531.pdf
special B.ed 2nd year old paper_20240531.pdfspecial B.ed 2nd year old paper_20240531.pdf
special B.ed 2nd year old paper_20240531.pdf
 
Additional Benefits for Employee Website.pdf
Additional Benefits for Employee Website.pdfAdditional Benefits for Employee Website.pdf
Additional Benefits for Employee Website.pdf
 
Unit 2- Research Aptitude (UGC NET Paper I).pdf
Unit 2- Research Aptitude (UGC NET Paper I).pdfUnit 2- Research Aptitude (UGC NET Paper I).pdf
Unit 2- Research Aptitude (UGC NET Paper I).pdf
 
How to Make a Field invisible in Odoo 17
How to Make a Field invisible in Odoo 17How to Make a Field invisible in Odoo 17
How to Make a Field invisible in Odoo 17
 
Introduction to Quality Improvement Essentials
Introduction to Quality Improvement EssentialsIntroduction to Quality Improvement Essentials
Introduction to Quality Improvement Essentials
 
Polish students' mobility in the Czech Republic
Polish students' mobility in the Czech RepublicPolish students' mobility in the Czech Republic
Polish students' mobility in the Czech Republic
 
Thesis Statement for students diagnonsed withADHD.ppt
Thesis Statement for students diagnonsed withADHD.pptThesis Statement for students diagnonsed withADHD.ppt
Thesis Statement for students diagnonsed withADHD.ppt
 
Palestine last event orientationfvgnh .pptx
Palestine last event orientationfvgnh .pptxPalestine last event orientationfvgnh .pptx
Palestine last event orientationfvgnh .pptx
 
Sectors of the Indian Economy - Class 10 Study Notes pdf
Sectors of the Indian Economy - Class 10 Study Notes pdfSectors of the Indian Economy - Class 10 Study Notes pdf
Sectors of the Indian Economy - Class 10 Study Notes pdf
 
Synthetic Fiber Construction in lab .pptx
Synthetic Fiber Construction in lab .pptxSynthetic Fiber Construction in lab .pptx
Synthetic Fiber Construction in lab .pptx
 
Ethnobotany and Ethnopharmacology ......
Ethnobotany and Ethnopharmacology ......Ethnobotany and Ethnopharmacology ......
Ethnobotany and Ethnopharmacology ......
 

suppositories Dr.pptx

  • 1. SUPPOSITORIES and ENEMAS Dr. Samia Ghani M. Phil Pharmaceutics
  • 2. •The word suppository is derived from Latin word « suppositorium » which means « to place under »
  • 3. Definition • Suppositories are solid or semi-solid dosage forms intended for insertion into the body cavities e.g. rectum, vaginal cavity, occasionally into the urethral tract where these suppositories melt or soften or dissolve in the cavity fluid and exert a localized or systemic effects. • The derivation of the word suppository is from the Latin supponere, meaning “to place under,” as derived from sub (under) and ponere (to place). Thus, suppositories are meant both linguistically and therapeutically to be placed under the body, as into the rectum
  • 4. • Suppositories are commonly employed rectally and vaginally, occasionally they’re used uretharlly and rarely they are also used nasally or orally. • They have various shapes, sizes and weights. • These are employed when a drug cannot tolerate orally or patient cannot swallow a drug easily. • The shape and size of suppository must be such that it is capable of being easily inserted into the intended body cavity and once it is intended it must be retained for an appropriate period of time. • Suppository generally have been employed for three reasons to: o Promote defecation o Introduce drugs into body o Treat anorectal diseases
  • 5. THE THERAPEUTIC USES OF SUPPOSITORIES 1. The drugs may be administered in the suppository dosage form for local or systemic effect. 2. Such health action depends on: • Nature of drug • Concentration of drug • Rate of drug absorption which depends upon the blood supply and • solubilities of the drugs 3. The lipid soluble or un-dissociated drugs are readily dissolved after release from the base and fat.
  • 6. Local Action: 1. The emollient (substances that soften the skin), the astringents (chemical substances that constrict the body tissues to stop bleeding or to make skin less oily – also called as protein precipitant), anti-bacterial agents, hormones, steroids and local anesthetics are dispersed in the suppositories for the treatment of local conditions of either vagina or urethra. 2. The rectal suppositories are primarily intended for the localized action and these are most frequently used or employed to relieve the constipation, pain, irritation, itching and inflammation associated with hemorrhoids (swollen or painful condition in which bleeding can occur).
  • 7. 3. Anti-hemorrhoidalsuppositories frequently contain a number of components including: 1.Local anesthetics 2.Astringents 3.Soothing agents v. Vasoconstrictors vi. Analgesics vii. Emollients iv. Protective E.g. glycerin suppository as a laxative (increase bowel movement) 4.Vaginal suppositories are used for the local action e.g. antiseptics, contraceptives (to stop child birth) etc. 5.Urethral suppositories may be used as anti-bacterial and as local anesthetics.
  • 8. Systemic Action: 1. For systemic action, the mucous membrane of the rectum and vagina permit the absorption of many soluble drugs. 2. Awiderangeofdrugsareemployedforsystemicactione.g. o Analgesics o Anti-spasmodic (to treat spasm - Biscopan) o Sedatives (induce sleep) o Tranquilizers o Anti-bacterial agents
  • 9. Advantages of Suppositories over Oral Therapy: 1. Some drugs are destroyed by the GIT enzymes (or by the pH of GIT). Such drugs are administered in suppository form. 2. Drugs which cause gastric irritation may be given rectally in the form of suppository. 3. To bypass the first pass action (drugs destroyed by portal circulation may bypass the liver after rectal absorption) e.g. • Propranolol (Anti-hypersensitive) • Glycerol trinitrate (used in angina attack–placed under tongue or given as suppository)
  • 10. 4. The route of administrations are also convenient for: • Adult patients • Unconscious persons • Mental retarded person • For infants who may unable to swallow the medicines 5. In vaginal cavity, for local antiseptics and anti-bacterial action. 6. This route has ability to administer some what larger doses of drugs than using oral administration. 7. This route ensures a rapid drug effect systematically (as an alternate to injections). 8. This route avoids bad taste or odour of drug.
  • 11. Disadvantages of Suppository: • 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.
  • 12. • A perceived lack of flexibility regarding dosage of commercially available suppository resulting in underuse and a lack of availability. • They’re expensive if made on demand. • Different formulations of a drug with a narrow therapeutic margin, such as aminophylline, cannot be interchanged without risk of toxicity. • Defecation may interrupt the absorption process of the drug, if drug is irritating. • There is possibility of degeneration of some drugs by the micro-flora present in the rectum.
  • 13. Examples of Drugs: • Prochlorperazine (for nausea and vomiting) • Chlorpromazine (as a tranquillizer) • Oxymorphine HCl (narcotic analgesic) • Indomethacin (NSAID analgesic and anti-pyretic) • Ergotamine tartarate (relief of migraine)
  • 14. Drugs Dispensing in Suppositories: • Hormones • Steroids • Emollients • Astringents • Antibiotics • Local anesthetics • Local analgesics
  • 15. FACTORS AFFECTING THE ACTION OF SUPPOSITORIES First Step of Dissolution Depends Upon: i. Melting point of base used ii. Liquefaction of base used Second Step of Diffusion Depends Upon: i. Solubility of drug ii. Particle size iii. Spreading capacity iv. Excipient viscosity at rectal temperature v. Retention of active principles by excipients
  • 16. Third Step of Absorption Depends upon: i. pKa of drug ii. pH induced to rectal fluid iii. presence of buffers iv. additive affects on membrane permeability v. partition co-efficient of drug
  • 17. Factor Affecting Drug Absorption From Rectal Suppository: 1. Physiologic Factor: • The human rectum is approximately 15-20 cm in the length, when empty of fecal material; it contains 2-3 ml of inert mucous fluid. • In resting state, the rectum is non motile. • There is no villa or microvillus on rectal mucosa. Physiological factors include: 1) Colonic Content 2) Circulation 3) pH and lack of buffering capacity of the rectal fluid
  • 18. 2. Physiochemical Characteristics of the Drug: i. Lipid water solubility of a drug (partition coefficient): • The lipid water partition coefficient of a drug is important in selecting the suppository base and in anticipating drug release from that base • Lipophilic drug, in other word, distributed in a fatty suppository base has fewer tendencies to escape to the surrounding queues fluids • Thus water-soluble salt are preferred in fatty base suppository. water- soluble base e.g. PEG, which dissolve in the rectal fluids, release both water-soluble and oil-soluble drugs.
  • 19. ii. Degree of Ionization: The barrier separating colon lumen from the blood is preferentially permeable to the unionized forms of drugs, thus absorption of drug would be enhanced by increase the proportion of unionized drugs iii. Concentration of a Drug in a Base: • The more drugs in a base, the more drug will be available for absorption. • If the concentration of the drug in the intestinal lumen is above a particular amount, the rate of absorption is not change by further increase in concentration of drug.
  • 20. 3. Physiochemical Characteristics of the Base and Adjuvant: i. Nature of the Base: • Suppository base capable of melting, softening or dissolving to release the drug for absorption. • If the base irritating the colon, it will promote colonic response, lead to increase bowl movement and decrease absorption. ii. Presence of Adjuvant in Base: • Adjuvant in a formula may affect drug absorption, change the rheological properties of the base at body temperature, or affected the dissolution of the drug.
  • 21. SUPPOSITORY BASES • Introduction: • Base is an inert medium in which drug is incorporated to dissolve, suspend or emulsify for a particular period of time. • Suppository bases play an important role in the release of the medicaments which they hold and therefore in the availability of the drug for absorption or systemic effects for localized action. • Bases alone used as emollient or lubricating effects or as vehicles in the preparation of medicated suppositories.
  • 22. Characteristics of an Ideal Suppository Base (water and fatty base): • It should be good in appearance. • It should melt at body temperature (37oC). • It should be non-toxic and non-irritating. • It should be compatible with a broad variety of drugs. • It should shrink (congealing) sufficiently on cooling to release from the mould. • It should be non-sensitizing. • It should have melting and emulsifying property. • It should be stable on storage. • It can be manufactured by molding either by hand, machine or compression. • It should be stable if heated above its melting point. • It should keep its shape while handling. • It should release the medicament easily. • It should have good water number.
  • 23. Additional Characteristics for Fatty Bases: If the base is fatty it has following requirements. 1. Acid value is below 0.2. • It is also called as neutralization value. • It is the mass of KOH (Potassium hydroxide) in mg that is required to neutralize one gram of chemical substance. 2. SaponificationValuerangesfrom200-245. • It is the no. of mg of KOH required to neutralize the free acids and saponify the esters contained in 1gm of a fat. 3. Iodine Value is less than 1. It is the no. of gm of iodine that reacts with 100g of fat or other unsaturated material.
  • 24. Classification of Suppository Bases: • Suppository bases are classified into two main categories according to their physical characteristics and a third miscellaneous group. 1. Fatty or oleaginous bases • Cocoa Butter (Theobroma Oil) • Hydrogenated Oil 2. The water soluble or water miscible bases • Glycerogelatin Base • Base of Polyethylene glycol 3. Miscellaneousbases • Generally a combination of hydrophilic and hydrophobic substances
  • 25. FATTY OR OLEAGINOUS BASES A. Cocoa Butter (Theobroma Oil): • It is the number of this group of the substances. • Cocoa butter NF is defined as, « the fat obtained from the roasted seeds of Theobroma cacao » The Particular Characteristics of Cocoa Butter: • Chemically it is triglyceride that is combination of glycerin with one or more fatty acids. • It is yellowish white solid, brittle fat which smells and taste like chocolate. • Its melting point is between 300C to 350C. • Its iodine value is ranges from 34 to 38. • Its acid value is not higher than 4.
  • 26. Different Crystalline Forms of Cocoa Butter: Cocoa butter exhibits in four states. i. α-form: The α-form melts at 240C and it is obtained by suddenly cooling the melted cocoa butter to 00C. ii. β-form: It crystallizes out from the liquefied cocoa butter with stirring at 18-230C. Its melting point ranges from 28 to 310C. iii. β’-form: β’-form changes slowly into the stable form which melts between 34 to 350C and this change is accompanied by a volume contraction. iv. γ-form: It melts at 180C and it is obtained by pouring a cool cocoa butter before it solidifies into a container which is cooled at deep freeze temperature.
  • 27. Methods to Prevent the Unstable Crystalline Forms: Problems Associated with Volatile Drugs and the Cocoa Butter: • Advantages Cocoa Butter: Non reactive, Melt at body temp, Solidification point lies 12-13° C below melting point, viscocity hepls in easy drug corporation. • Disadvantages Cocoa Butter: Rancidity, Melt, Liquefy, metastable form, Low contractility during solidification, Water number is low (20- 30), Leakage from the body.
  • 28. B. Hydrogenated Oil (Cocoa Butter Substitutes) Topical Treatment of Vegetable Oils to produce Suppository Bases:  The fat type suppository bases are produce from a variety of material either synthetic or natural in origin e.g. vegetable oils including: oCoconut Oil oCotton Seed Oil oPalmitic Oil
  • 29. • These are modified by Esterification, hydrogenation or fractionation at different melting range to obtain the desired product.
  • 30. WATER SOLUBLE / MISCIBLE BASES: • The main members of this group are: • o Glycerogelatin Bases o Polyethylene glycol
  • 31. i. Glycerogelatin Bases • Glycerogelatin bases may be prepared by dissolving gelatin 20%, glycerin (70%), and adding solution or suspension of medicament (10%). Glycerogelatin Base in Vaginal Suppositories: • Glycerogelatin base is not frequently used in preparation of vaginal suppositories where prolong localized action of medicinal agent is usually desired. • It is slower to soften and mix with physiological fluids. It provides a more prolonged release. • They have a tendency to absorb the moisture due to hygroscopic nature of glycerin.
  • 32. • Therefore they must be protected from atmospheric moisture in order to maintain their shape and consistency. • Due to hygroscopicity of the glycerin, these suppositories may have a dehydrated effect and be irritating to tissue upon insertion. • The water present in formula for suppositories minimizes with water to reduce the initial tendency of base to draw the water from mucus membrane which irritate the tissue.
  • 33. Glycerogelatin Base in Urethral Suppositories: • TheurethralsuppositoriesmaybepreparedfromtheGlycerogelatinbase. • For urethral suppositories the gelatin constitutes about 60% of the weight of formula, glycerin about 20% and the medicated aqueous portion 20%. • Urethral suppositories of glycerogelatin are more easily inserted then suppositories with cocoa butter base, because of brittleness of cocoa butter and its rapid softening at body temperature.
  • 34. ii. Polyethylene Glycol Bases (Carbowax) • Polyethylene glycol is polymers of ethylene oxide and water prepare to various chain length, molecular weights and physical states. • These are available in a number of molecular weight ranges. • The more commonly used polyethylene glycol bases are PEG 200, 400, 600, 800, 1500, 1540, 3350, 4000, 6000 and 8000. • These numerical designations refer to the average molecular weight of the polymers.
  • 35. • PEG having average molecular weight of 200, 400 and 600 are clear colorless liquids and those which have average molecular weight of greater than 1000 are wax-like solids with hardness increasing with an increase in molecular weight. • Various combinations of these PEG may be combined by fusion, using two or more of various types to achieve a suppository base of desired consistency and characteristics. • PEG suppositories don’t melt at body temperature and dissolve slowly in body fluids. • It is possible to prepare suppositories from PEG mixture having melting point higher than that of body temperature.
  • 36. • Advantages: • It permits the slow release of medicament from base. • Convenient storage of these suppositories without need of refrigerator and • without danger of softening in warm weather. • They’re chemically stable. • Inert,andnon-irritating • Itdoesn’tallowbacterialgrowth. • Physical properties changes according to molecular weight. • Itprovidesprolongedaction. • Itdoesn’tsticktomold. • Suppositoriesarecleanandsmoothinappearance.
  • 37. Disadvantages: i. If PEG suppository doesn’t contain atleast 20% of water they can cause irritation to mucous membrane after insertion. In such case they are dipped in water just prior to use. This procedure prevents the moisture which is being drawn from tissue after insertion and produces the ―stinging‖ sensation. ii. In the miscellaneous group of bases are included those which are mixtures of the oleaginous and water soluble or water miscible materials. iii. These materials may be physical or chemical mixtures. iv. Some materials are preformed emulsions generally w/o type or they may be dispersing in aqueous fluids. v. One of these substances is polyoxyl 40 sterate.
  • 38. Characteristics of Polyoxyl 40 Sterate: i. It is a surface active agent that is employed in a no. of commercial suppositories bases. ii. This substance is waxy white solid that is water soluble. iii. Its melting point is 39 – 400C. iv. Mixtures of many fatty bases including cocoa butter with emulsifying agent capable of forming w/o emulsions. v. These bases have ability to hold water or aqueous solutions and sometimes refer to as hydrophilic suppositories bases.
  • 39. METHODS OF PREPARATION OF SUPPOSITORIES Suppositories are prepared by three methods: a. Molding from a melt (fusion) b. Compression (Cold Compression) c. Hand Rolling and Shaping
  • 40. a. Preparation of Suppositories by molding (fusion):  This method is most frequently employed both on a small scale and on an industrial scale. Bases Used: •Cocoa butter •Glycerinated gelatin •Polyethylene glycol
  • 41. • Suppository Molds: • Molds in common use today are made from stainless steel, aluminum, brass, or plastic. • They’re reusable and disposable. • Commercially available molds available for preparation of rectal, vaginal, and urethral suppositories can produce individual or large numbers of suppositories of various shapes and sizes. i. Lubrication of the Mold ii. Calibration of the Mold iii. Preparing and Pouring the Melt iv. Allowing the melt to cool and Congeal into Suppositories v. Removing the formed suppositories from the mold
  • 42. Advantages: • It is a simple method. • It gives suppositories that are more elegant than hand mould suppositories. • Sedimentation of solids in base is prevented. • It is suitable for heat labile medicaments. Disadvantages: • Air entrapment may take place. • This air may cause weight variation. • The drug or base may be oxidized in air.
  • 43. b. Preparation of Suppositories by Cold-Compression (Fusion)
  • 44. Advantages: • This technique is time saving. • It gives suppositories that are more elegant than hand mould suppositories. • Suitable for heat labile medicinal substances. • No mold preparation • No heating is required. Disadvantages: • The disadvantage to compression is that the special suppository machine is required and there is some limitation as to the shapes of suppositories that can be made. • Manipulation requires considerable skills. • Appearance is not elegant.
  • 45. c. Hand Rolling Method
  • 46. Advantage: • It has the advantage of avoiding the necessity of heating the coca butter. • No equipment required • No special calculations are to be done Disadvantages: • Difficult to manufacture • Not pretty in appearance
  • 47. d. Automatic Molding • The molding operations (pouring, cooling and removal) can be performed by machine. • All filling, ejecting and mold-cleaning operations are fully automated. • The output of a typical rotary machine ranges from 3500 to 6000 suppositories an hour.
  • 48. • Firstly, the prepared mass is filled into filling hopper where it is continuously mixed and maintained at constant temperature. • The suppository mould is lubricated by brushing or spraying. • The cooling cycle is adjusted as required by individual suppository mass by adjusting the speed of rotatory cooling turn table. • After mass solidifies, the excess of material is scraped off and collected for reuse. • The solidified suppositories are moved to ejecting station, where the mould is opened and suppositories are pushed out.
  • 49. COMMERCIAL SUPPOSITORY PRODUCTION • Automated filling of molds by volumetric dosing pumps • Strips of perforated shells pass beneath dosing pumps & filled successively • Passed through cooling chambers for solidification.....sealed and then • packaged • Quality control procedures i.e. weight, volume, leakage are conducted Injection Molding: • Alternative to melt and pour molding • Described by Snipes • Use of injection molding technique developed for fabrication of plastics • Excipients of choice are polyethylene glycol • Povidone or silicon dioxide are added for viscosity or plasticity adjustment
  • 50. CLASSIFICATION OF SUPPOSITORIES: • Suppositories are classified into following types: i. Rectal suppositories ii. Vaginal suppositories or Pesseries iii. Urethral suppositories or Bougies iv. Nasal suppositories or Bouginaria v. Ear suppositories vi. Oral suppositories (Not used anymore)
  • 51. i. Rectal Suppositories: 1. These are conical or cylindrical in shape. 2. These have flat base and tapered at the other end for easy insertion into rectum. 3. Its length is usually 32mm and has a bullet shape e.g.Bisacodyl suppositories, USP (10mg). 4. USP-NF states that adult rectal suppository should weight about 2 gram, when cocoa butter is employed as the suppository base. 5. Rectal suppositories are used by infants or children are about half the weight and size of the adult suppository and assume more pencil like shape. 6. Rectal suppositories are used for local, systemic or mechanical effect. a. Local effect e.g. in hemorrhoids infection b. Systemic effect e.g. infection away from rectum c. Mechanical effect e.g. in evacuation of bowel in constipation
  • 52.
  • 53.
  • 54.
  • 55. ii. Urethral Suppositories (Bougies): • These are long, thin and pencil shaped. • These are rounded from both sides. • Their diameter is 5mm. • Their length for male is 25mm and for female is 50 mm. • Their weight for female is 2g and for male is 4g. • These are rarely prescribed. • For their formulation base is composed of glyceryl monosterate and • polyoxyethylene. • E.g. Furacin Urethral Inserts (Anti-septic)
  • 56. iii. Nasal Suppositories (Bouginaria): • These are pencil shaped similar to urethral suppositories. • These are shorter in length i.e. about 32mm. • Base for their formulation is usually glycerogelatin base.
  • 57. iv.
  • 58. v.
  • 59. SPECIFIC PROBLEMS IN FORMULATING SUPPOSITORIES: 1. Water in Suppositories: Use of water as a solvent for drug should be avoided for the following. Reasons: • Water accelerates oxidation of fats. • If water evaporates, the dissolved substance crystallizes out. • Unless H2O is present at level than that requires for dissolving the drug, the water has little value in facilitating drug absorption. Absorption from water containing suppository enhance only if an oil in water emulsion exist with more than 50% of the water in the external phase . • Reaction between ingredients (in suppository) are more likely to occur in the presence of water. • The incorporation of water or other substances that might be contaminate with bacteria or fungi necessitates the addition of bacteriostatic agents (as parabens)
  • 60. 2- Hygroscopicity: • Glycerinated gelatin suppositories lost moisture by evaporation in dry climates and absorbed moisture under conditions of high humidity • PEG bases are also hygroscopic
  • 61. 3. Incompatibilities: •PEG bases are incompatible with silver salt, tannic acid, aminopyrine , quinine , icthammol, asprine , benzoc.aine & sulphonamides . •Many chemicals have a tendency to crystallize out of PEG, e.g.: sodium sarbital, salicylic acid & camphor. •Higher concentration of salicylic acid softens PEG to an ointment-like consistency, d- Aspirin complexes with PEG. •Penicillin G, although stable in cocoa butter and other fatty bases, was found to decompose in PEG bases . •Fatty bases with significant hydroxyl values may react with acidic ingredients.
  • 62. 4- Viscosity: •The viscosity of the melted suppository base is important in the manufacture of the suppository and to its behavior in the rectum after melting. •Melted cocoa butter have low viscosity than glycerinated gelatin and PEG type base in low viscosity bases, extra •Care must be exercised to avoid sedimentation of suspended particles. •To overcome the problems caused by use of low viscosity bases: o Use base with a narrower melting rang that is closer to body temperature. o The inclusion of approximately 2% aluminum monostearate not only increases the viscosity of the fat base but to maintain homogenous suspension of insoluble material. o Cetyl, stearyl or myristyl alcohols or stearic acid are added to improve the consistency of suppositories.
  • 63. 5- Brittleness: • Suppositories made from cocoa butter are elastic and don't fracture readily. • Synthetic fat base with high degree of hydrogenation and high stearate content and higher solids content at room temperature are usually more brittle. • To overcome o The temperature difference between the melted base & the mold should be minimal. o Addition of small amount of Tween 80, castor oil, glycerin imparts plasticity to a fat
  • 64. 6- Volume contraction: Occurs in many melted suppository base after cooling the mold, result in: o Good mold release (contraction facilitate the removal of the suppository from the mold , eliminating the need for mold release agents). o Contraction hole formation at the open end of the mold, this will lowered suppository . The contraction can be eliminated by pouring a mass slightly above its congealing temperature into a mold warmed at about the same temperature or the mold is overfilled so that the excess mass containing the contraction hole can be scraped off. Lubricant or mold releasing agent: o Cocoa butter adheres to suppository molds because of its low volume contraction. A various mold lubricants or release agents must be used to overcome this difficulty (mineral oil, aqueous solution of sodium lauryl sulfate , alcohol , silicones , soap). o The release of suppository from damaged mold was improved by coating the cavities with polytetrofluoroethylene (Teflone).
  • 65. 7- Rancidity and Antioxidant: Rancidity results from the autoxidation and subsequent decomposition of unsaturated fats into low & medium molecular weight saturated & unsaturated aldehydes , ketones and acids , which have strong unpleasant odor. Examples of effective antioxidant are phenols such as ―hydroquinone or B-naphtholquinone.
  • 66. QUALITY CONTROL OF SUPPOSITORIES: 1. Surface Appearance and Shape: 2. Melting Test Range: 3. Liquefaction or Softening Time Tests of Rectal Suppositories: 4. Breaking Test: 5. Mechanical Strength: 6. Melting & Solidification: 7. Dissolution Testing:
  • 67. DISPLACEMENT VALUES: • The displacement value of a medicament is the no. of parts by weight of a medicament that will displace one part of suppository base (normally Theobroma oil). • Displacement values for various medicaments are given in B.P.C. (British Pharmaceutical Codex). • It is the amount of drug that will displace one part of base. OR • It is the amount of the base which is displaced by certain amount of drug.
  • 68.
  • 69. Problem # 1: • Calculate the quantities required to make 10 theobroma oil suppositories (2g mould) each containing 400mg of zinc oxide (displacement value = 4.7). Solution: • Total wt. of zinc oxide required = 400 mg × 10 = 4000 mg = 4 g • Wt. of base required for un-medicated suppositories = 2g × 10 = 20 g • As the displacement value of ZnO = 4.7
  • 70. And, • 4.7 g of ZnO displace theobroma oil = 1 g • 1 g of ZnO displace theobroma oil = 1/4.7 • 4 g of ZnO displace theobroma oil = 1/4.7 * 4 = 0.85 So, Wt. of suppository base required to make medicated suppositories = 20 – 0.85 = 19.15 gm
  • 71.
  • 72. PACKAGING AND STORAGE: • Suppositories are often packaged in partitioned boxes that hold the suppositories upright. • Glycerine and glycerinated derivatives are often packed in screw- capped glass containers. • Many other suppositories are wrapped individually in tin, aluminum foil, paper, plastic or PVC-polyethylene. • Poorly packed suppositories may give rise to staining, breakage or deformation by melting. • Strip packaging is common place.
  • 73. • Alternatively, suppositories may be molded directly into their packages and then store below 300C to gain a specific shape. • All suppositories particularly Theobroma oil suppositories and glycerogelat in suppositories should be refrigerated. • Polyethylene glycol suppositories are stored at usual room temperature without requirement of refrigerator.
  • 74.
  • 75. VAGINAL AND RECTAL SOLUTIONS Vaginal Douches: 1. These powders are used to prepare solutions for vaginal douche, for irrigating and cleansing of vagina. 2. These powders may be prepared and packed in bulk or as a unit packages. 3. Unit package is designed to contain the appropriate amount of powder to prepare the specified volume of douche solution. 4. The bulk powders are used by tea spoonfull(5ml) or table spoonfull(15ml) in preparation of desired solution.
  • 76. Components of Douche Solution: 1. Boric acid (sodium borate) 2. Astringente.g.Potassiumorzincsulphate 3. Anti-microbial agent e.g. iodine 4. Surfactant or detergents (sodium Lauryl sulphate) 5. Salts (Sod. Citrate or sodium chloride) 6. Quaternary ammonium compounds e.g. benzethonium chloride 7. Oxidizing agents e.g. sodium perborate 8. Aromatics, e.g. menthol, thymol, and phenol etc. Use: The douche powders are used for hygiene effect.
  • 77. Rectal Douches (Enemas) • An enema is an introduction of fluid into the lower bowel through the rectum for the purpose of cleansing or to introduce medication or nourishment 1. Retention enemas • Stimulant Enemas • Nutrient Enemas • Emollient Enemas • Sedative Enemas • Anesthetic Enemas
  • 78. 2 Evacuation enemas • Simple Evacuant Enemas • MedicatedEvacuantEnemas • ColdEvacuantEnemas 3. Medicated Evacuant Enemas: • Oil Enemas • Purgative Enemas • AstringentEnemas • Anthelmintic Enemas • Carminative Enemas
  • 79. Purpose of Enemas: • To stimulate defecation & to treat constipation ex: simple evacuant enema • To soften hard faecal matter ex: oil enema • To administer medication ex: sedative enema • To protect and soothe the mucus membrane of intestine & to check diarrhoea ex : emollient enema • To destroy intestinal parasites ex : anthelminitic enema • To relieve the gaseous distention ex : carminative enema • To administer the fluid and nutrients ex: nutritive enema • To relieve inflammation ex : astringent enema
  • 80. • To induce peristalsis ex : purgative enema • To stimulate a person in shock and collapse ex: stimulant enema • To reduce the temperature ex : cold enema or ice enema • To clean the bowels prior to x-ray studies, visualization of the bowel , surgery on the bowel or delivery of a baby ex : saline enema • To make diagnosis ex: barium enema • To establish regular bowel functions during a bowel training programme • To induce anesthesia ex : anesthetic enema
  • 81. RETENTION ENEMAS: 1. A no. of solutions administered rectally for local effect e.g. hydrocortisone or for systemic absorption e.g. aminophylline. 2. In case of aminophylline rectal administration minimizes the undesirable gastrointestinal reaction associated with oral therapy. 3. Corticosteroids are administered as retention enemas for the treatment of patients for ulcerative colitis.
  • 82. Stimulant Enema: • A stimulant enema is given in the treatment of shock and collapse • It is also sometimes given in case of poisoning e.g. coffee enema is given in case of opium poisoning Solutions: • Black coffee : 1 table spoon coffee powder to 300 ml of water • Brandy : 15 ml of brandy added to 120 to 180 ml of glucose saline • Amount of solution: 180 to 240 ml • Temp of solution: 108 to 110 degree Fahrenheit
  • 83. • Sedative enema: • It is retention enema containing a sedative drug given to induce sleep • Drugs used: o Paraldehyde o Chloral hydrate o Potassium bromide Dose: As ordered by the doctor • Anesthetic Enema: • It is a retention enema containing an anesthetic drug to produce anesthesia in client Drugs used: Avertin Dose: 150 to 300 mg per kg of body weight
  • 84. • Emollient Enema: • This is an introduction of bland solution into the rectum for the purpose of checking diarrhea or soothing & relieving irritation on an inflamed mucus membrane Solution used: o Starch & opium : opium 1 to 2ml is added to 120 to 180 ml of starch mucilage or rice water o Starch mucilage alone • Amount of solution: 120 to 180 ml • Temp of solution: 100 to 105 degree Fahrenheit (37.8 to 40.5 degree centigrade )
  • 85. Nutrient Enema: • It is a retention enema to supply food & fluids to the body. • Selection of the fluids depends upon the ability of the colon to absorb it. • Nutrient enema is particularly useful in conditions like haemophilia which makes I.V. infusion difficult or undesirable Solutions : o Normal saline o Glucose 2 to 5% o Peptonized milk 120 ml • Amount of solution: 1100 to 1700 ml in 24 hour or 180 to 270 ml at 4 hourly interval • Temperature of solution: 100 degree Fahrenheit (37.8 degree Fahrenheit )
  • 86. EVACUATION ENEMAS: • The rectal enemas are used to cleanse the bowel. • Many enemas are available in disposable plastic squeeze bottles containing premeasured amount of enemas solution. • The active agents are solutions of: a. Sodium phosphate b. Sodium biphosphate c. Glycerine d. Light Mineral Oil
  • 87. Simple Evacuant Enema: • Purpose : To stimulate defecation & to treat constipation To relieve the gaseous distention by stimulating the peristalsis To relieve the retention of urine by reflex stimulation of the bladder To stimulate uterine contraction & to hasten the child birth To cleanse the bowel prior to x-ray studies, visualization of the bowels (ex: sigmoidoscopy), surgery & retention enemas • Solutions Used: i. Soap & water: soap jelly 50ml to 1 liter of water ii. Normal saline: sodium chloride 1 teaspoon of half liter of water iii. Tap water
  • 88. • Amount of solutions to be used: o Adults:500to1000ml(1to2pint) o Children's: 250 to 500 ml ( 0.5 to 1 pint ) o Infants: 250 ml or less • Temp of solution: o Adults : 105 to 110 degree Fahrenheit o Children : 100 degree Fahrenheit
  • 89. Oil Enema: • These are given to soften fecal matter in case of severe constipation. • Before the 1st bowel movement after operation on the rectum or perineum. • To avoid straining & injury to the sutures & wounds. • It should be retained for half an hour to 1 hour to soften the faeces. • It should then be followed by a soap & water enema to open the bowels. Solutions used: o Olive oil o Gingerly oil or sweet oil o Castor oil & olive oil (1:2) Amount of solution to be used: 115 to 175 ml Temperature of the solutions: 100 degree Fahrenheit
  • 90. Purgative Enema: • These are given to cause the bowel to contrast actively & to evacuate its contents. • Its acts by their irritating effect on the mucus lining , stimulate peristalsis & cause the evacuation of bowel. • The stretching of the intestine due to this inflow of fluid causes the intestine to contract & leads to the evacuation of bowel. Solutions used: o Pure glycerin – 15 to 30 ml o Glycerin & water – 1:2 o Glycerin & caster oil – 1:1 o Magnesium sulphate : 60 to 120 ml with sufficient amount of water to dissolve it o 1-2-3 enema : magnesium sulphate 30 ml, glycerin 60 ml, & water 90 ml Amount & temp of solution is that of oil enema
  • 91. Carminative Enema (Anti spasmodic): • These are given to relieve gaseous distention of the abdomen by causing peristalsis & expulsion of flatus & faeces • It is given as simple evacuant enema. Solution: • Turpentine : 8 to 16 ml of turpentine mixed thoroughly with 600 to 1200 ml of soap solution • Milk and molasses (granular sugar ) : 90 to 230 ml of molasses well mixed with equal quantity of warm milk
  • 92. Anthelmintic Enema: • This is given to destroy & expel the worms from the intestines. • Before the treatment is given the bowel should be cleansed by a soap water enema so that the drug may come in direct contact with the worms & the lining of the intestine. • The treatment is given until the worms are destroyed. Solution : o Infusion of quassia : 15gms of chips to 600 ml of water o Hypertonic saline solution : sodium chloride 60 ml with 600 ml of water Amount of the solution: 250 ml
  • 93. Astringent Enema: • It contracts the tissues & the blood vessels, checks bleeding & inflammation, lessens the amount of mucus discharge & gives a temporary relief in the inflamed area. • It is usually given in colitis & dysentery. • They are usually given in the form of rectal or colonic irrigations. • The solution is allowed to run in slowly & return quickly to avoid distension, pain & irritation of the inflamed wall. • Solutions: o Tannic acid : 2 gms to 600ml of water o Alum : 30 gms to 600ml of water o Silver nitrate 2% : (silver nitrate is dissolved in distilled water ) • Temperature of the solution: It is given as hot as the client can stand
  • 94. Cold Enema (Ice Enema): • This is given to decrease the body temperature in hyperpyrexia and heat stroke. • It is given in the form of colonic irrigation. Complications : o Hypothemia o Abdominal cramps