每日一次琥珀酸美托洛尔缓释基质片

D. Nagendrakumar, S. A. Rudani, S. Shirsand, Para
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引用次数: 1

摘要

本研究旨在设计并评价直接压缩法琥珀酸美托洛尔每日一次缓释片,以克服其副作用,提高其生物利用度,减少给药频率,提高患者依从性。以羟丙基甲基纤维素(HPMC) K4M和K10M(人工合成)、瓜尔胶和黄原胶(天然)、卡波醇934p和乌龙木L-100乳糖为通道剂制备片剂。对制备的基质片进行硬度、厚度、重量变化、脆度、药物含量等参数的评价。片剂制剂按照USP指南进行体外药物释放研究。所有制剂均表现一级释放动力学,具有基质扩散释药机制。药物:黄原胶比例为1:3:1,卡波波尔934p为1:3:1的f12制剂符合美国药典规定的释药官方限量,在15个制剂中被选为有前景的制剂。缓释聚合物与缓释调节剂联合使用可有效控制自由水溶性药物在24 h内的缓释,对于每日一次的缓释基质片剂剂型是今后患者各方面依从性的剂型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Once-Daily Sustained Release Matrix Tablets of Metoprolol Succinate
The purpose of the present study was to design and evaluate once-daily sustained release matrix tablets of metoprolol succinate by direct compression method, to overcome its side effects, to increase its bioavailability, to reduce the dosing frequency and improve the patient compliance. The tablets were prepared using hydroxypropyl methylcellulose (HPMC) K4M and K10M (synthetic), guar gum and xanthan gum (natural) carbopol 934p and Eudragit L-100 lactose as a channeling agent. Prepared matrix tablets were evaluated for various parameters like hardness, thickness, weight variation, friability and percent drug content. Tablet formulations were subjected to in-vitro drug release studies as per USP guidelines. All the prepared formulations showed fi rst-order release kinetics with matrix diffusion mechanism of drug release. The formulation F 12 containing drug: xanthan gum ratio of 1:3:1, carbopol 934p 1:3:1 offered the required in-vitro drug release rate according to the offi cial limits of drug release as per USP and selected as a promising formulation among the fi fteen formulations. The combination of release retarding polymer and release modifying agent can effectively control the drug release for freely watersoluble drugs over a period of 24 h in case of once-daily sustained release matrix tablet formulations which are the upcoming dosage forms for patient compliance in all aspects.
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