Pharmaceutics-III Solid Dosage Forms Lecture 1 Suppositories PDF

Pharmaceutics-iii Solid dosage forms Lecture 1 Suppositories Today you will learn the following: Definition of suppositories Advantages & disadvantages Indications &contraindications Types of suppositories Preparation of suppositories Definition of suppositories: solid dosage...

Pharmaceutics-iii Solid dosage forms Lecture 1 Suppositories Today you will learn the following: Definition of suppositories Advantages & disadvantages Indications &contraindications Types of suppositories Preparation of suppositories Definition of suppositories: solid dosage form intended for insertion into body orifices ( Rectum, Vagina, Urethra ) They melt, soften, or dissolve in the body orifices and exert a local or systemic effect Advantages of Suppositories Advantages Avoid first- pass metabolism  Advantages of Suppositories 1) It is the alternated dosage form for drugs that have less bioavailability when it is taken orally. 2) It is suitable for the drugs that are destroyed by portal circulation as It avoids the first-pass effect. 3) Suitable in case of nausea and vomiting 4) Drugs having bad odour and taste can be used in suppository form. 5) Used for systemic distribution as It is more suitable for unconscious patients who can not take drugs orally. 6) It is suitable for drugs that produce irritating effect in stomach. 7) Suitable for administration of drugs not tolerated orally. E.g. medications that are sensitive to gastric pH and enzymes Advantages of Suppositories 8) Suppositories have faster onset of action than oral route as drug is directly absorbed from mucosa into venous circulation. 9) Useful for rapid and direct local effect When local effect is desired such in case of rectal , vaginal and urethral diseases. 10) They are accurate dosage forms 11) It is suitable pediatric and geriatric patients who find difficulty in swallowing of drugs.  disadvantages of Suppositories 1) Patient acceptance as it is embarrassing to patients 2) fluid content of the rectum is less than that of the small intestine; this may affect dissolution rate, etc. 3) Not suitable in case of diarrhea 4) Need to store at low temp. 5) In some cases the total amount of the drug that must be given will be either too irritating or in greater amount than reasonably can be placed into a suppository. 6) Incomplete absorption may be obtained because the suppository usually promotes evacuation of the bowel. 7) Some drugs may be degraded by the microbial flora present in the rectum. Indications of Suppositories: 1) Local Relief: 1. Hemorrhoids 2. Acute Constipation 3. Rectal inflammation or ulcers 2) systemic Absorption: Nausea and vomiting Fever and pain Hormonal therapy 3) Before endoscopic examination 4) To empty the bowel; before certain surgery Contraindications of Suppositories: 1.Severe Rectal Conditions eg: Rectal bleeding or severe hemorrhoids 2.Known Hypersensitivity or Allergy 3.Rectal Surgery 4.Obstruction or Severe Stricture 5.Diarrhea 6. Chronic constipation because it needs repetitive use 7. Paralytic ileus  VARIOUS SHAPES OF SUPPOSITORY ❑the shape and size of a suppository must be such that: a. It can be easily inserted into the intended orifice b. Once inserted, it must be retained for the appropriate period. Page 1. Rectal suppositories. 2. Vaginal suppositories. 3. Urethral suppositories. 4. Nasal suppositories. 5. Ear cones. ( According to Route of administration ) (A)RECTAL SUPPOSITORY- It is inserted in the rectum. The weight of suppository used in children is about 1g and in adult about 2g. The shape of the suppository used in the rectum is a torpedo shape. The length is about 3 cm  COMMON O L TAM R E N AC E LTA SUPPOSITORY PA R VO MEDICATIONS  (B) URETHRAL SUPPOSITORY ❖ The weight of this type suppository is about 2g and 60-75 mm long in Females. ❖ Those intended for males weigh 4 gm each and are 100-150 mm long. ❖ It is available in pencil shape. (C) VAGINAL SUPPOSITORY It is in oviform shape. It is about 3-5g in weight. It contains drugs that are used in treatment of the infections of female genitourinary tract and for contraception. It contains the combination of polyethylene glycol of different molecular weights as suppository bases. Page  (D) NASAL SUPPOSITORY ❖These suppository are meant for introduction into nasal cavity. ❖It is about 1g in weight. ❖The glycero- gelatin is used as suppository bases. (E) EAR CONE ❖It is also known as AURINARIES. ❖Rarely used ❖These are meant for introduction into the ear. ❖It is cylindrical in shape. ❖It is about 1g in weight. Page ⦁ Tablet Suppositories ⦁ Layered Suppositories ⦁ Coated Suppositories ⦁ Capsule Suppositories ⦁ This type of tablet is prepared by compression like tablets. ⦁ Such type of suppositories used for rectal & vaginal purposes. ⦁ Pessaries tablet suppositories are present in almond-like shape. ⦁ Rectal tablets covered with thin layers of materials such as polyethylene glycol for protection.  ⦁ In that type of suppositories contain different drugs in different layers. ⦁ So that, incompatibility drugs can be separated from each other. ⦁ In that type of suppositories contains polyethylene glycol, cetyl alcohol etc. ⦁ Those materials control their disintegration rate, to provide lubricant properties & protection action during storage. ⦁ Soft gelatin capsules of different shapes & sizes are prepared in that type of suppositories. ⦁ In that type of capsule suppositories are filled with liquids, semisolids, or solids. ⦁ These type of capsules are increasing in popularity.  Hand rolling. Method of Suppositories Fusion method. preparation Cold compression.  Hand Rolling It is the oldest and simplest method of suppository preparation when only a few suppositories are to be prepared in a cocoa butter base. It has the advantage of avoiding the necessity of heating the cocoa butter. A paste-like mass is prepared by triturating grated cocoa butter and active ingredients in a mortar. The mass is formed into a ball in the palm of the hands, then rolled into a uniform cylinder. The cylinder is then cut into the appropriate number of pieces which are rolled on one end to produce a conical shape. Effective hand rolling requires considerable practice and skill.  Fusion Method 1. Melting the suppository base 2. Dispersing or dissolving the drug in the melted base. 3. The mixture is removed from the heat and poured into a suppository mould. 4. Allowing the melt to congeal 5. Removing the formed suppositories from the mold. The fusion method can be used with all types of suppositories and must be used with most of them. Fusion Method Small scale molds are capable of producing 6 or 12 suppositories in a single operation. Industrial molds produce hundreds of suppositories from a single molding.  Cold Compression moulding The grated suppository base, drug, and the other ingredients are combined through mixing. Compression moulding is a method of preparing suppositories from a mixed mass of base and medicaments which is forced into a special compression mould using suppository making machines.  **Advantages: 1. It is a simple method. 2. It produces suppositories that are more elegant than hand moulded suppositories. 3. Suitable for heat labile medicaments. **Disadvantages: 1. Air entrapment may take place. 2. This air may cause weight variation. 3.The drug and/or the base may be oxidized by this air.  Lubricating the cavities of the mould helps produce elegant suppositories and free from surface depression. - The lubricant must be different in nature from the suppository base, otherwise it will become absorbed and will fail to provide a buffer film between the mass &the metal. - The water-soluble lubricant is useful for fatty bases while the oily lubricant is useful for water-soluble bases. - The lubricant should be applied with gauze or with fairly stiff brush. LUBRICANTS FOR USE WITH SUPPOSITORY BASES: No lubricant Base Lubricant required Theobroma Soap spirit Synthetic oil liquid fats Glycerol- paraffin Macrogols gelatin base Infrastructure Deterioration Models 29