水飞蓟素胃内滞留漂浮片的制备与评价

Preparation and evaluation of gastroretentive floating tablets of Silymarin.

作者信息

Garg Rajeev, Gupta Ghanshyam Das

机构信息

Department of Pharmaceutics, ASBASJSM College of Pharmacy, Bela, Ropar-140111, India.

出版信息

Chem Pharm Bull (Tokyo). 2009 Jun;57(6):545-9. doi: 10.1248/cpb.57.545.

Abstract

The present study performed by preparation and evaluation of floating tablets of Silymarin as model drug for prolongation of gastric residence time. Floating effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose (HPMC) K 4M, K 15M, psyllium husk, swelling agent as crospovidone and microcrystalline cellulose and gas generating agent like sodium bicarbonate and citric acid and evaluated for floating properties, swelling characteristics and in vitro drug release studies. Floating noneffervescent tablets were prepared by polypropylene foam powder and different matrix forming polymers like HPMC K 4M, Carbopol 934P, xanthan gum and sodium alginate. In vitro drug release studies were performed and drug release kinetics evaluated using the linear regression method was found to follow both the Higuchi and the Korsemeyer and Peppas equation. The drug release mechanism was found fickian type in most of the formulations. The developed floating tablets of Silymarin may be used in clinic for prolonged drug release for at least 24 h, thereby improving the bioavailability and patient compliance.

摘要

本研究通过制备和评价水飞蓟素漂浮片作为模型药物来延长胃滞留时间。采用多种材料制备了漂浮泡腾片,如羟丙基甲基纤维素(HPMC)K4M、K15M、车前子壳、作为膨胀剂的交联聚维酮和微晶纤维素以及作为产气剂的碳酸氢钠和柠檬酸,并对其漂浮性能、膨胀特性和体外药物释放研究进行了评价。通过聚丙烯泡沫粉和不同的基质形成聚合物如HPMC K4M、卡波姆934P、黄原胶和海藻酸钠制备了非泡腾漂浮片。进行了体外药物释放研究,并使用线性回归方法评估药物释放动力学,发现其遵循Higuchi方程以及Korsemeyer和Peppas方程。在大多数制剂中发现药物释放机制为菲克型。所研制的水飞蓟素漂浮片可用于临床,实现至少24小时的药物缓释,从而提高生物利用度和患者顺应性。

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