Formulation and Assessment of Celecoxib Floating Beads in Capsule using 2^3 Full Factorial Design

Document Type : Original Article

Authors

1 Pharmaceutics Department, Faculty of Pharmacy, Assiut University, Assiut, Egypt.

2 Dept. of Pharmaceutics, Faculty of Pharmacy Assiut University

Abstract

Floating beads have been formed to create a prolonged drug release in the stomach and to reduce the number of frequencies, thereby overcoming its side effects. The current study is concerned with the design and evaluation of stomach-specific oil embedded floating beads of celecoxib in a capsule. Hard gelatin capsules (size 1) were filled with celecoxib oil entrapped beads. A 2³ factorial design was used to investigate the effects of different weight masses of HPMC K4M, Sodium alginate, and maize starch on drug encapsulation efficiency (EE) of beads and percent of cumulative drug release at 6 hours (R6h) from capsules. The optimization results show an increase in EE in the oil entrapped beads and a decrease in R6h from capsules with increases in the weights of HPMC K4M, Sodium alginate, and maize starch. The optimized formulation (F6) had EE of 91.80±0.20% and R6h of 37.88±1.39%. The capsules floated over 6 h and released the drug in gastric pH (1.2) during the first two hours then in phosphate buffer pH (6.8) for another four hours. An X-ray imaging in vivo study of optimized capsules containing CXB oil embedded floating beads in rabbits indicated stomach-specific gastro retention throughout a long time. An in vivo anti-inflammatory efficacy of optimized CXB floating beads showed sustained drug release and better inhibition of rats’ hind paw edema.

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