Suppositories Presented by Adilla Vaishnavi 23T21T0002 Pharm.D 1st Year Under the Guidence of M. Swetha Assistant Professor, Department of Pharmaceutics CMR College of PHARMACY
INTRODUCTION Suppositories are semisolid dosage forms of medicament for insertion into body orifices other than mouth They are inserted into rectum, vagina, ear, urethral, nasal cavity. Suppositories are in different shapes, sizes and weights.
Advantages Melts at body temperature. Both localized and systemic action. Eas y t o use for pediatri c a nd geriatric patients. Administered to unconscious patient. Suppositories are unit dosage form of drugs The drugs in suppositories are slowly absorbed giving sustained action.
Disadvantages Irritant drug cant be administered. Embarrassment to patients. Need to store at low temp. Cannot be prepared easily Cost-expensive. Fluid content of the rectum is much less than that of the small intestine; this may effect dissolution rate, etc. Some drug may be degraded by the microbial flora present in the rectum.
Rectal Suppositories These are meant for introduction into the rectum for their systemic effect. These are generally made from theo - broma oil. The weight of Rectal suppositories are about 1-2 g. They are either cone or torpedo shaped
EXAMPLES: DULCOLAX CANASA NUMORPHAN
Vaginal Suppositories These are meant for introduction into the vagina. These suppositories are also known as pessaries They are larger than rectal suppositories. The vaginal suppositories are biconical, rod-shaped or wedge shaped The weight is about 4-8 g.
These are generally used to combat infections occurring in the female genitourinary area, to restore the vaginal mucosa to its normal state and for contraception. EXAMPLES: clotrimazole miconazole
Urethral Suppositories These are meant for introduction into the urethra. These are also known as urethral bougies. These are thin, long and cylindrical forms rounded at one end to facilitate insertion. The weight varies from 2 to 4 g.
EXAMPLE: ANUSOL
Nasal Suppositories These are meant for introduction into the nasal cavity These are also known as nasal bougies. These are thin and cylindrical in shape These are always prepared with glycero -gelatin base. Nasal suppositories are about9-10 cm long and weigh about 1.0 g.
EXAMPLE: Livostin Nasonex Nascobal
Ear Cones These are meant for introduction into the ear These are also known as aurinaria . These suppositories are thin, long and cylindrical in shape and weigh about 1 gram. Ear cones are usually prepared with theobroma oil.
EXAMPLE: Otosan Benexe
New Trends of Suppositories Tablet Suppositories Layered Suppositories Capsule Suppositories Coated Suppositories Disposable mould
SUPPOSITORY BASES The various types of suppositories bases are used to prepare suppositories, so that they can retain its shape, and firmness during storage and administration.
Ideal properties: It must retain the shape and size on storage. It should melt at body temperature after insertion. It should be non-irritant. It should shrink sufficiently to remove from mould . It should not interfere in release or absorption of drug. It should permit incorporation of drug. It should be compatible with variety of drugs. It should not be soften or harden on storage.
1.Fatty bases i ) Theobroma oil: It is yellowish white solid obtained from crushed and roasted seeds of Theobormococoa . It is also known as cocoa butter. It has butter like consistency having melting point of 30°C-35°C. It is a mixture of glyceryl esters of stearic, oleic, palmitic and other fatty acids.
ii) Emulsified Theobroma oil: This may be used as a base when quantities of aqueous solutions are to be incorporated. The use of 5% glyceryl monsterate , 10% lenette wax, 2-3% cetyl alcohol, 4% beeswax and 12% spermaceti is recommended to prepare emulsified theobroma oil suppositories.
(iii) Hydrogenated oils: These can be obtained by hydrogenation of various vegetable oil, such as arachis oil, cottonseed oil, coconut oil, palm oil, etc. It is used as a substitute for theobroma oil because it has a number of advantages over theobroma oil
2. Water soluble and miscible bases: ( i ) Glycero -gelatin base: It is a mixture of glycerin and water which is made stiff by the addition of gelatin. The base may be used for preparing all type of suppositories but it is particularly used for making pessaries. (ii) Soap-glycerin suppositories: In glycero -gelatin base, the gelatin is replaced with either curd soap or sodium sterate which makes the base sufficiently hard to prepare good quality of suppositories. (iii) Polyethylene glycols: PEG polymers are commonly known as carbowaxes or polyglycols or macrogols.
3. Emulsifying bases ( i ) Witepsol : They consist of triglycerides of saturated vegetable fatty acid with varying percentage of partial esters. (ii) Massa estarinum : It is a mixture of mono, di- and triglycerides of saturated fatty acids. This is also known as adeps solidus. (iii) Massuppol : It consists of glyceryl esters mainly of lauric acid to which small amount of glyceryl monsterate has been added to improve its water absorbing capacity.
PREPARATION OF SUPPOSITORIES Suppositories are prepared by the following methods: 1. Hand Rolling method 2. Hot process or Fusion method. 3. Cold compression method
Hand Rolling method It is an ancient method. The suppository base s rolled and then desired shape is given with he hand. Not used now a days.
Hot process or Fusion method It is the common method which involves melting of suppository base, incorporation of medicament, filling into lubricated mould and cooling the mould .
Cold compression method This method is useful for thermolabile and insoluble drugs as it does not involves heating and stirring of the base. The method is not suitable for suppositories in which glycero gelatin base or any other base which involves melting. Use of Hand or power operated compression machines.