Abstract

The aim of present study were to arrest the problem of content uniformity without the use of harmful organic solvent and to improve ex vivo permeability of captopril, a low dose class III drug as per biological classification system. Eutectic mixture of camphor and menthol was innovatively used in the work. Captopril solution in eutectic mixture was blended with Avicel PH 102 and then the mixture was blended with mannitol in different ratios. Formulated batches were characterized for angle of repose and Carr's index. A selected batch was filled in hard gelatin capsule. Tablet dosage form was also developed. Capsules and tablets were characterized for in vitro drug release in 0.1N HCl. Additionally, the captopril tablets were analyzed for content uniformity and ex vivo drug permeation study using rat ileum in modified apparatus. The measurement of angle of repose and Carr's index revealed that the powder blend exhibited good flow property and compressibility. The captopril capsules and tablets exhibited immediate drug release in 0.1 N HCl. The captopril tablets passed content uniformity test as per IP 1996. Ex vivo permeation of captopril, formulated with eutectic mixture, was faster than control. The permeation was increased by 15% at the end of 3 h. Tablets and capsule exhibited reasonable short term stability with no considerable change in performance characteristics.

Highlights

  • The aim of present study were to arrest the problem of content uniformity without the use of harmful organic solvent and to improve ex vivo permeability of captopril, a low dose class III drug as per biological classification system

  • Eutectic mixture of camphor and menthol was used as a solvent for captopril

  • The solution was adsorbed on Avicel PH 102 to overcome the problem of content uniformity and improve permeability of Biopharmaceutical Classification System (BCS) class III low dose drug without infringing existing patents

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Summary

Introduction

The aim of present study were to arrest the problem of content uniformity without the use of harmful organic solvent and to improve ex vivo permeability of captopril, a low dose class III drug as per biological classification system. Eutectic mixture of camphor and menthol was used as a solvent for captopril. Presence of traces of eutectic mixture of camphor and menthol can significantly improve the bioavailability of Biological Classification System (BCS) class III drugs.

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