Formulation development of Drugs Used in CNS Disorders

Abstract

The aim of the present work was to prepare immediate release (IR) tablet of Temazepam - a BCS class II drug used in treatment of Insomnia for better therapeutics. Direct compression and wet granulation were explored to formulate IR tablets, however direct compression method exhibited higher weight variation and hence further trials were conducted using wet granulation technique. Lactose granulac 200, povidone, maize starch, aerosil, magnesium stearate were used as excipients. The preformulation studies like bulk density, tapped density; moisture content and compatibility of all excipients with API were carried out. Wet granulation was carried out in rapid mixer granulator, followed by drying in fluid bed dryer, and blending in V-cone blender, followed by compression. Formulation showed acceptable hardness, disintegration, diameter, thickness and invitro drug release. Blend had excellent flow property which resulted in better compliance for blend and content uniformity. The formulations were evaluated and optimized by comparing it with generic formulation to attain comparable drug release pattern as that of innovator product. The stability testing of optimized formulation was carried out at different condition for 1 month as per ICH guidelines. Optimized formulation is expected to be bioequivalent to innovator product. Simultaneously, the minor project carried out at institute with the aim to explore various excipients and prepare formulation of Olanzapine - a BCS class II drug (antipsychotic agent). Tablets were prepared by direct compression utilizing microcrystalline cellulose, lactose monohydrate, crospovidone, Ac-Di-Sol, sodium starch glycolate, aerosil, L-HPC and magnesium stearate as lubricant in different ratios using rotary tablet press. Prepared tablet showed invitro drug release as comparable with that of reference product.