Drug formulations for BPH

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1. Drug Formulations For BPH 1 st Year Dr. Pravin Prasad 2 nd Year Resident, MD Clinical Pharmacology Maharajgunj Medical Campus 15 th December, 2016 ( Mangsir 30, 2073), Thursday

2. Drug Formulations: Introduction Are the means by which drug molecules are delivered to sites of action within the body Contains Active Pharmaceutical Ingredient (API) and Excipients

3. Problems with direct use of API Difficult to handle, accurate dosing & administration Inherent chemical instability Degradation at the site of administration May cause local irritations/injury Can have unpleasant qualities

4. Dosage forms: Types Route of Administration Formulation Solid Liquid Gases Enteral Tablets, Capsules, Lozenges, Granules, Suppositories Solutions, Dispersions, Enemas Parenteral Implants Injections, Infusions Inhalational Solutions (Nebulizer, Atomizer) Inhalers Topical (Skin/Hair) Powder, Cream, Ointment, Gel, Lotion, Paint, Pastes, Plaster, Liniments Ophthalmic & ENT Ointments Drops Local (female genital tract) Pessary, Rings, IUCD Douche Aerosols

5. Oral Solid Dosage forms: Tablets Hard compressed medication Conventional vs Coated Easy to use, convenient, economical Cannot be used in Emergency condition, unconscious patients, uncompliant patients Other forms of tablets: effervescent forms, chewable, sub-lingual, buccal

6. Tablets: other forms Effervescent Tablets Should be dissolved or dispersed in water before use Rapid onset of action Palatable Avoids local irritation Examples: Fexofenadine, Ranitidine, Paracetamol, Vitamins, Chlorine

7. Tablets: other forms Chewable tablet Chewed prior to swallowing Designed for administration to children e.g. Vitamin products, Antacids Sublingual and buccal tablets Dissolve rapidly  thru’ mucous membranes  bloodstream Avoids acidic gastric environment & first pass metabolism e.g. Vasodilators, Steroidal hormones

8. Oral Solid Dosage Forms: Capsules Medication in a water soluble, hygroscopic gelatin container Advantage- Masks the unpleasant taste of its contents Not to be divided

9. Oral Solid Dosage forms: Lozenges Consisting of one or more medicaments along with sugar and gum Intended to dissolve or disintegrate slowly in the mouth Mostly for treatment of local irritation/infections of the mouth or throat, cough remedies, indigestion

10. Oral Solid Dosage Forms: Granules Solid, dry aggregates of powder particles often supplied in single-dose sachets Some placed on the tongue and swallowed with water Some intended to be dissolved in water before taking Effervescent granules evolve carbon dioxide when added to water

11. Oral Solid Dosage forms: Powders Usually dispersed/dissolved in water before taking Marketed as: Bulk Powders Multi-dose preparations Usually contain non-potent medicaments e.g. antacids Divided Powders Single-dose presentations (e.g. a small sachet)

12. Rectal Solid Dosage Forms Suppositories Non-irritating, chemically stable and inert Advantages: Can avoid first pass metabolism Alternative to oral route No local (gastric) adverse reactions Disadvantages Poor compliance Some API can cause local irritation of rectal mucosa May melt at high temperature Tablets, Capsules

13. Oral Liquid Dosage Forms: Solutions Solutions Clear liquid preparations for oral and other use One or more active ingredients dissolved in a suitable vehicle Examples: Syrups, elixirs, linctus, gargles/mouthwash, tincture, oral drops Dispersions Dispersions Ingredients are not dissolved Emulsion Stabilized dispersions Suspension API suspended in a suitable vehicle

14. Solution Types Syrups Concentrated aqueous solution of a sugar, usually sucrose 66 % Flavored syrups (mask disagreeable tastes) E.g. cough syrup, ipecac syrup Elixirs Pleasantly flavored clear hydroalcoholic solutions (≤ 20 % alcohol) Used mostly for potent or nauseous drugs E.g. Codeine elixirs, Phenobarbital elixirs

15. Solution: Types Linctuses Viscous preparations Small dose (5ml) Taken undiluted (longer demulcent action) E.g. Codeine cough linctus Oral drops Administered in small volumes Tincture Alcoholic or hydroalcoholic solutions of plant extracts E.g. Tincture iodine, Belladona tincture Gargles, Mouthwashes

16. Oral Liquid Dosage forms: Dispersions Dispersions Ingredients are not dissolved, simply distributed throughout the vehicle Emulsion Stabilized dispersions (2 immiscible liquids) Suspension Active ingredient(s) suspended in a suitable vehicle (solid in a liquid) Settles slowly, may show a sediment readily dispersed uniformly on shaking Oral, topical, injectable E.g. Antacids, Insulin, Antifungal

17. Rectal Liquid Dosage Forms: Enemas Evacuant enema Bowel stimulant to treat constipation. E.g. soft soap enema Pre-eclampsia/ Eclampsia- MgSO4 enema Retention Enema Local effect- barium enema Systemic effect- anti-emetics, nutrients, paracetamol Enemas: Procedure of introducing liquids into rectum and colon via anus