Suppositories are solid or semi-solid dosage forms intended for insertion into body cavities like the rectum or vagina. They melt or dissolve in the cavity fluid and exert local or systemic effects. Suppository bases include fatty bases like cocoa butter and hydrogenated oils, water-soluble bases like glycerogelatin and polyethylene glycol, and combinations. Factors affecting drug absorption from suppositories include physiological factors, drug properties, and base properties. Suppositories are used to deliver drugs locally or systemically and have advantages over oral drugs in certain situations.
Dosage forms and routes of drug administrationFatenAlsadek
this presentation give an over review about Routes of drug administrations and dosage forms
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
Hydrophilic- Water loving / Oil hating
Hydrophobic- Water hating / Oil loving
Surfactants are amphiphilic molecules composed of a hydrophilic or polar moiety known as head and a hydrophobic or nonpolar moiety known as tail.
The nature and number of polar and nonpolar groups – Hydrophilic, Lipophillic or somewhere in between.
Example - Alcohols, Amines and Acids Changes from hydrophilic to Lipophillic as carbons atoms increasing in their alkyl chain.
Dosage forms and routes of drug administrationFatenAlsadek
this presentation give an over review about Routes of drug administrations and dosage forms
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
Hydrophilic- Water loving / Oil hating
Hydrophobic- Water hating / Oil loving
Surfactants are amphiphilic molecules composed of a hydrophilic or polar moiety known as head and a hydrophobic or nonpolar moiety known as tail.
The nature and number of polar and nonpolar groups – Hydrophilic, Lipophillic or somewhere in between.
Example - Alcohols, Amines and Acids Changes from hydrophilic to Lipophillic as carbons atoms increasing in their alkyl chain.
To prepare relatively stable and homogeneous mixtures of two immiscible liquids.
Permits administration of a liquid drug in the form of minute globules rather than in bulk.
Palatable administration of an otherwise distasteful oil by dispersing it in a sweetened, flavored aqueous vehicle.
Biphasic system
emulsions
Classification of emulsion
Theories of emulsification
The HLB system
Stability of Emulsion
Emulsion Manufacturing
Test for emulsions
Pharmaceutical applications of emulsions
Packaging of emulsions
Notes made by PU student:
INTRODUCTION TO DRUG AND DIFFERENT DOSAGE FORMS
Drug
Pharmaceutical Preparations Manufactured by Pharmaceutical Industry
Pharmaceutical Preparations Compounded Individually
SOLID DOSAGE FORMS
LIQUID DOSAGE FORMS
SEMI-SOLID DOSAGE FORM
NEW DRUG DELIVERY SYSTEMS
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Culturally, the Romans were eclectic, absorbing and adapting elements from the civilizations they encountered, particularly the Greeks. Roman art, literature, and philosophy reflected this synthesis, creating a rich cultural tapestry. Latin, the Roman language, became the lingua franca of the Western world, influencing numerous modern languages.
Roman architecture and engineering achievements were monumental. They perfected the arch, vault, and dome, constructing enduring structures like the Colosseum, Pantheon, and aqueducts. These engineering marvels not only showcased Roman ingenuity but also served practical purposes, from public entertainment to water supply.
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Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
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Reverse Pharmacology.
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.
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.
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.
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
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