用于结肠靶向的壳聚糖压制片的制备及体外研究
Preparation and In vitro Investigation of Chitosan Compressed Tablets for Colon Targeting.
作者信息
Bashardoust Negar, Jenita Josephine Leno, Zakeri-Milani Parvin
机构信息
Department of Pharmaceutics, Dayananda Sagar College of Pharmacy, Kumaraswamy Layout, Bangalore - 560078, Karnataka,India ; Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Adv Pharm Bull. 2011;1(2):87-92. doi: 10.5681/apb.2011.013. Epub 2011 Dec 15.
PURPOSE
The aim of the present study was minimizing the drug release in upper gastro intestinal tract and targeting to colon by using the principles of compression coat.
METHODS
Compression coated tablets of Ibuprofen were prepared by direct compression method using chitosan (300, 250, 200 & 175 mg). Tablets were evaluated for their physicochemical properties and in vitro drug release studies. In vitro drug release studies were performed with and without rat caecal contents.
RESULTS
In the rat caecal contents tablets showed enhanced drug release due to degradation of chitosan coat by colonic colonic enzymes. The in vitro release studies in pH-6.8 phosphate buffer containing 2% w/v of rat caecal contents showed the cumulative percentage release of Ibuprofen after 26h as 31.94% ±0.59, 67.89% ± 0.45 and 55.87 % ± 0.45 and 82.52 % ± 0.92 respectively. Coat thickness and amount of chitosan controls the release rate. Formulations are best fitted with Korsmeyer-Peppas kinetics and mechanism of drug release was non-Fickian. FTIR studies reveals there is no drug-polysaccharide interaction. F1 formulation was a promising system for drug targeting to colon.
CONCLUSION
Based on the obtained results chitosan as a press coat could target ibuprofen to the colon.
目的
本研究的目的是利用压制包衣原理，减少药物在上消化道的释放，并使其靶向结肠。
方法
采用壳聚糖（300、250、200和175毫克）通过直接压片法制备布洛芬压制包衣片。对片剂进行了理化性质和体外药物释放研究。在有和没有大鼠盲肠内容物的情况下进行体外药物释放研究。
结果
在大鼠盲肠内容物中，由于结肠酶对壳聚糖包衣的降解，片剂显示出增强的药物释放。在含有2%（w/v）大鼠盲肠内容物的pH-6.8磷酸盐缓冲液中的体外释放研究表明，布洛芬在26小时后的累积释放百分比分别为31.94%±0.59、67.89%±0.45、55.87%±0.45和82.52%±0.92。包衣厚度和壳聚糖用量控制释放速率。制剂最符合Korsmeyer-Peppas动力学，药物释放机制为非Fickian。傅里叶变换红外光谱研究表明不存在药物-多糖相互作用。F1制剂是一种有前景的结肠靶向给药系统。
结论
基于所得结果，壳聚糖作为压制包衣可将布洛芬靶向结肠。
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