DEVELOPMENT AND EVALUATION OF LOW DOSE SOLID ORAL FORMULATION OF ESZOPICLONE TABLETS 1mg, 2 mg AND 3 mg

The content uniformity of the blend and tablet formulation is critical property that needs to be well controlled in order to produce acceptable pharmaceutical product. The main objective of the present study was to develop a stable and bioequivalent oral formulation of Eszopiclone tablets having low dose with three different strengths 1mg, 2mg & 3mg. Eszopiclone is a nonbenzodiazepine hypnotic agent that is a pyrrolopyrazine derivative of the cyclopyrrolone class, used for the treatment of insomnia. Due to its low dose main emphasis was given to content uniformity of blend and maintaining it throughout the manufacturing process. Initial trials were taken on 2 mg strength with different excipients with different grades. Batches were exposed to stress condition at 55 0C for 15 days showed increase in related substance. Then preformulation study was conducted and it was observed that Dicalcium Phosphate and Colloidal Silicon Dioxide were incompatible with Eszopiclone. New batches were taken without Dicalcium Phosphate and Colloidal silicon-di-oxide. All physical and chemical parameters like dissolution, assay, and related substance were found satisfactory during stability for 3 Month at 40°C/75% RH. On the basis of final formulation of 2 mg strength, look alike formula for Eszopiclone 1mg and 3mg were developed and evaluated. Blend uniformity was evaluated at every step of formulation and found within limits. Stratified sampling was done at regular interval to evaluate content uniformity. Bioequivalence study with innovator was also performed and test sample was found to be bioequivalent with innovator.