Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin
Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin
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DOI：
10.1016/j.ijpharm.2006.02.038
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发表时间：
2006-06-19
影响因子：
5.8
通讯作者：
Vavia, Pradeep R.
中科院分区：
文献类型：
--
作者：
Chavanpatil, Mahesh D.;Jain, Paras;Vavia, Pradeep R.
口服缓释胃滞留剂型为具有从上胃肠道吸收的药物提供了许多优点，并改善了以窄吸收窗为特征的药物的生物利用度。研制了一种具有漂浮、溶胀和生物粘附特性的胃滞留型缓释系统。所有这些性能都进行了优化和评估。尝试并优化了各种缓释聚合物如车前壳、HPMC K100M和溶胀剂、交联聚维酮的组合，以获得24 h的释放曲线。评价制剂的体外药物释放特性、溶胀特性和体外生物粘附特性。体外释药遵循Higuchi动力学，释药机制为反常或非Fickian型。对于开发的制剂，发现n值为0.5766，而对于市售制剂，n值为0.5718，表明存在异常转运。高吸水率导致片剂的更高溶胀支持氧氟沙星的异常释放机制。发现开发制剂的相似因子f2为91.12，表明释放与市售制剂（扎诺星OD）相似。溶胀性能随着交联聚维酮浓度的增加而增加，并显著促进了药物从片剂基质中的释放。与单独的HPMC K100M和车前子壳相比，发现开发的制剂的生物粘附特性在组合中是显著的（P < 0.005）。(c)2006 Elsevier B.V.保留所有权利。
Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window. A new gastroretentive sustained release delivery system was developed with floating, swellable and bioadhesive properties. All these properties were optimized and evaluated. Various release retarding polymers like psyllium husk, HPMC K100M and a swelling agent, crosspovidone in combinations were tried and optimized to get the release profile for 24 h. Formulations were evaluated for in vitro drug release profile, swelling characteristics and in vitro bioadhesion property. The in vitro drug release followed Higuchi kinetics and the drug release mechanism was found to be of anomalous or non-Fickian type. For the developed formulation, the value of n was found to be 0.5766 while for the marketed formulation the value was 0.5718 indicating the anomalous transport. The high water uptake leading to higher swelling of the tablet supported the anomalous release mechanism of ofloxacin. The similarity factor f2 was found to be 91.12 for the developed formulation indicating the release was similar to that of the marketed formulation (Zanocin OD). The swelling properties were increased with increasing crosspovidone concentration and contributed significantly in drug release from the tablet matrix. The bioadhesive property of the developed formulation was found to be significant (P < 0.005) in combination as compared to HPMC K100M and psyllium husk alone. (c) 2006 Elsevier B.V. All rights reserved.