抗高脂血药胃留置浮片的研制与评价

Raghunandan, V. Pai, Lakshmi Crs, D. V. Gowda, M. S. Khan, S. Bhat
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引用次数: 0

摘要

以不同药聚合物比的HPMC K4M、HPMC K15M、HPMC K100M为原料,采用直接加压法制备含辛伐他汀20 mg的保胃泡腾浮片。对其物理特性进行了评价,即硬度、脆性、药物含量和漂浮性。研究了该片剂12 h的体外释药特性。所制片剂具有控释、缓释、硬度最佳、重量均匀、易碎性低等特点。以F2 (HPMC - K100M 1:3)配制的制剂在12 h时释药率为85.83%,具有最佳的漂浮滞后时间。随着聚合物比例的增加和聚合物(HPMC)粘度等级的增加,药物的释放率降低。泡腾漂浮基质片药物释放持续12 h以上,具有浮力特性。DSC研究显示没有药物与赋形剂的相互作用。在释放动力学方面,各剂型均符合Higuchi、一阶模型和非菲克模型。根据相似因子(f2)(71.32)选择最佳配方(F9),加入BaSO4体外溶出用于放射学研究。人体志愿者体内x线研究显示,平均胃停留时间为5.4±0.32 h。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and evaluation of gastro retentive floating tablets of anti hyperlipidemic drug
The aim of the present study was to develop Gastro retentive effervescent floating tablets (GREFT) containing 20 mg of simvastatin were developed by direct compression method using HPMC K4M, HPMC K15M, HPMC K100M with different drug to polymer ratio. Tablets were evaluated for their physical characteristics, viz ., hardness, friability, drug content and floating properties. Further, tablets were studied for in vitro drug release characteristics for 12 h. The tablets exhibited controlled and prolonged drug release, with optimum hardness, consistent uniformity in weight and low friability. The formulation with F2 (HPMC K100M 1:3 ratio) showed 85.83 % drug release at the end of 12 h and exhibited optimum floating lag time. A decrease in release rate of the drug was observed on increasing polymer ratio and also by increasing viscosity grades of the polymer (HPMC). Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor ( f 2) (71.32) and invitro dissolution was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 5.4 ± 0.32 h.
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