Design, optimization and evaluation of mesalamine matrix tablet for colon drug delivery system

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• 作者：Pravin Kondiba Pawar ; Chinanshu Gautam
• 关键词：Mesalamine ; Eudragit RLPO ; Eudragit RSPO ; Eudragit S ; 100
• 刊名：Journal of Pharmaceutical Investigation
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：46
• 期：1
• 页码：67-78
• 全文大小：1,450 KB
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• 作者单位：Pravin Kondiba Pawar (1)
  Chinanshu Gautam (2)
  
  1. Gourishankar Institute of Pharmaceutical Education & Reseach, Satara, Maharashtra, India
  2. Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab, 140401, India
  
• 刊物主题：Biomedicine general;
• 出版者：Springer Netherlands
• ISSN：2093-6214

文摘

The aim of the present investigation was to develop and evaluate matrix tablet of mesalamine for colonic delivery by using Eudragit RSPO, RLPO and combination of both. The tablets were further coated with different concentration of pH-dependent methacrylic acid copolymers (Eudragit S100), by dip immerse method. The physicochemical parameters of all the formulations were found to be in compliance with the pharmacopoeial standards. The in vitro drug release study was conducted using sequential dissolution technique at pH 1.2 (0.1N) HCl, phosphate buffers pH 6.8 and 7.4, with or without rat cecal content mimicking different regions of gastro intestinal tract. The result demonstrated that the tablet containing Eudragit RLPO coated with Eudragit S100 (1 %) showed a release of 94.91 % for 24 h whereas in the presence of rat cecal content the drug release increases to about 98.55 % for 24 h. The uncoated tablets released the drug within 6 h. The in vitro release of selected formulation was compared with marketed formulation (Octasa MR). In vitro dissolution kinetics followed the Higuchi model via non-Fickian diffusion controlled release mechanism. The stability studies of tablets showed less degradation during accelerated and room temperature storage conditions. The enteric coated Eudragit S100 coated matrix of mesalamine showing promising site specific drug delivery in the colon region. Keywords Mesalamine Eudragit RLPO Eudragit RSPO Eudragit S-100