Drug Formulations Oral Formulations: Tablet, Capsule, Solution, Suspension, etc. Parenterals: Injections, Ophthalmics Inhalations Topicals.

Apresentação em tema: "Drug Formulations Oral Formulations: Tablet, Capsule, Solution, Suspension, etc. Parenterals: Injections, Ophthalmics Inhalations Topicals."— Transcrição da apresentação:

1 Drug Formulations Oral Formulations: Tablet, Capsule, Solution, Suspension, etc. Parenterals: Injections, Ophthalmics Inhalations Topicals

2 Dosage Forms Containing Solid API Tablet Capsule Ointment Suppository Suspension Oral Injection Inhalation Ophthalmic

3 Tablet Disintegration Dissolution Absorption

4 Particle Size Crystal Form Dissolution Tableting Properties Physical and Chemical Stability Solubility Important Solid-State Properties

5 Problems in Dosage forms Resulting from Use of the Wrong Polymorph Suspension (Aqueous vehicle) - Crystal growth leading to undesirableparticle size distribution, particularly, in parenteral suspensions, or caking Cream - Crystal growth, yielding gritty, cosmetically unacceptable creams ore uneven distribution of active ingredient Solution - Precipitation due to crystal growth Suppositories - Melting point changes of vehicles resulting in softening of product or hindrance in release of active ingredient

6 Chemical Stability Summary of the reactives of the α, β and γcrystalline forms of ethoxycinnamic acid exposure to ultraviolet light

7 Bioavailability Comparison of mean blood serum levels obtained with choramphenical palmitate suspension containing varying ratios of A and B polymorphs (per cent of Form B in the suspension: M, 0%; N 25%; O, 50%, P; 75%; L, 100%)

8 Tablet Friability: 30 tabs, wt loss < 1% Disintegration Dissolution Rate or Dissolution Profile Uniformity of Dosage Unit Weight Variation: 10 units Content Uniformity: 10 units Quality Control of Tablets

9 Tablet Formulation Filler: Starch, Lactose, Mannitol Microcrystalline Cellulose (Avecil) Binder: Starch, Acacia, Gelatin, Simple Syrup Lubricant: Mg Stearate, Ca Stearate, Talc Disintegrant: Starch, Avecil Flavor Colorant: D&C Misc. : Stabilizer

10 Pediatric Chewable Aspirin Tablet (wet granulation) Aspirin Mannitol Saccharin sodium Acacia Starch Stearic acid Talc Dry Flavor 100.0 115.0 1.0 4.0 20.0 0.5 8.0 1.5 250 mg/tab

11 Tablet Manufacturing (Wet Granulation) Binder Preparation (10% Acacia) Sieving (Mannitol & Saccharin sodium) Mixing & Granulation Sieving (Aspirin, starch, Stearic acid, Talc, dry flavor) Mixing Drying Compression

12 Sustained Release Tablets Therapeutic Range Minimum Effective Level Time Toxic level Drug Concentration (units mL-1) “Ideal” sustained blood or tissue drug level versus time profile

13 Toxic level Minimum Effective Level Drug Concentration (units mL-1) Time Repetitive release approach to sustained-release.

14 Pores produces by soluble portion of polymer membrane Membrane Reservoir Mechanism of Sustained Release : Diffusion Diffusion control of drug release by a water-insoluble polymer (left) Diffusion control of drug release by a Partially water-soluble polymer (right)

15 Mechanism of Sustained release: Dissolution

16 Mechanism of Sustained Release : Osmosis