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用于氧氟沙星的新型缓释、可膨胀且生物黏附的胃滞留药物递送系统。

Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin.

作者信息

Chavanpatil Mahesh D, Jain Paras, Chaudhari Sachin, Shear Rajesh, Vavia Pradeep R

机构信息

Mumbai University Institute of Chemical Technology, Pharmaceutical Sciences Division, Near Nathalal Parikh Marg, Matunga, Mumbai 400019, India.

出版信息

Int J Pharm. 2006 Jun 19;316(1-2):86-92. doi: 10.1016/j.ijpharm.2006.02.038. Epub 2006 Mar 29.

Abstract

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.

摘要

口服胃滞留缓释剂型为从胃肠道上部吸收的药物提供了许多优势,并提高了具有狭窄吸收窗的药物的生物利用度。开发了一种具有漂浮、溶胀和生物粘附特性的新型胃滞留缓释给药系统。对所有这些特性进行了优化和评估。尝试并优化了各种缓释聚合物,如车前子壳、羟丙甲纤维素K100M和一种溶胀剂交联聚维酮的组合,以获得24小时的释放曲线。对制剂进行了体外药物释放曲线、溶胀特性和体外生物粘附性能的评估。体外药物释放遵循Higuchi动力学,发现药物释放机制为非菲克型或异常型。对于所开发的制剂,n值为0.5766,而市售制剂的值为0.5718,表明存在异常转运。高吸水率导致片剂更高的溶胀,支持了氧氟沙星的异常释放机制。所开发制剂的相似性因子f2为91.12,表明其释放与市售制剂(Zanocin OD)相似。溶胀性能随交联聚维酮浓度的增加而增强,并对片剂基质中的药物释放有显著贡献。与单独的羟丙甲纤维素K100M和车前子壳相比,所开发制剂的生物粘附性能在组合时具有显著性(P < 0.005)。

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