Colonic luminal surface retention of meloxicam microsponges delivered by erosion based colon-targeted matrix tablet

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• 作者：Rishabh Srivastava^a ; Deepesh Kumar^b ; Kamla Pathak^a ; ^{kamla_rap@yahoo.co.in}
• 关键词：Meloxicam ; Microsponges ; Calcium pectinate matrix ; Colon targeting ; Lumenal retention
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：10 May, 2012
• 卷：427
• 期：2
• 页码：153-162
• 文件大小：1444 K

摘要

The work was aimed at developing calcium-pectinate matrix tablet for colon-targeted delivery of meloxicam (MLX) microsponges. Modified quassi-emulsion solvent diffusion method was used to formulate microsponges (MS), based on 3² full factorial design. The effects of volume of dichloromethane and EudragitRS100 content (independent variables) were determined on the particle size, entrapment efficiency and%cumulative drug release of MS1-MS9. The optimized formulation, MS5 (d_mean = 44.47 渭m,%EE = 98.73,%CDR = 97.32 and followed zero order release) was developed into colon-targeted matrix tablet using calcium pectinate as the matrix. The optimized colon-targeted tablet (MS5T2) shielded MLX loaded microsponges in gastrointestinal region and selectively delivered them to colon, as vizualized by vivo fluoroscopy in rabbits. The pharmacokinetic evaluation of MS5T2 in rabbits, revealed appearance of drug appeared in plasma after a lag time of 7 h; a t_max of 30 h with Fr = 61.047%, thus presenting a formulation suitable for targeted colonic delivery. CLSM studies provided an evidence for colonic luminal retentive ability of microsponges at the end of 8 h upon oral administration of MS5T2. Thus calcium pectinate matrix tablet loaded with MLX microsponges was developed as a promising system for the colon-specific delivery that has potential for use as an adjuvant therapy for colorectal cancer.