Development and characterization of gastroretentive mucoadhesive tablets of venlafaxine hydrochloride

S. U. Zate, P. Kothawade, Mohan N. Rathi, Mohan H. Shitole, Chetan Yewale, Vinayak S. Gawande
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引用次数: 8

Abstract

The present study was undertaken with an aim to formulation development and evaluation of gastroretentive mucoadhesive sustained release tablet of Venlafaxine hydrochloride which releases the drug in a sustained manner over a period of 12 hours, by using Carbopol 971P in combination with eudragit RS-PO and ethyl cellulose as a mucoadhesive and release retardant respectively. Preformulation study was done initially and results directed for the further course of formulation. Based on Preformulation studies different batches of Venlafaxine hydrochloride were prepared using Carbopol 971P, Eudragit RS-PO and ethyl cellulose chosen for their different hydrophilic properties to calculate the sustained release properties. Sustained release tablets were prepared by direct compression and were evaluated for bioadhesion time, swelling index and matrix erosion, and in vitro drug release. The tablets of batch F3 and F6 had high swelling behaviors but release of drug is very less. And batch F2 having considerable swelling index and in vitro drug release (99.85%). Batch F2 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hour release as it fulfills all the requirements for sustained release tablet. From the discussion it is concluded that use of carbopol as a release retardant and adhesive polymer is very effective; and also it act as strong release retardant in combination with hydrophobic polymers. Keywords: Gastroretentive; Mucoadhesive; Venlafaxine hydrochloride; Tablet.
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盐酸文拉法辛胃保留黏粘片的研制与表征
本研究以卡波波尔971P与乌龙油RS-PO和乙基纤维素分别作为黏附剂和缓释剂,对盐酸文拉法辛胃保留黏附缓释片进行配方开发和评价,该缓释片的缓释时间为12小时。初步进行了制剂前研究,其结果将指导进一步的制剂过程。在预处方研究的基础上,选择亲水性不同的卡波波尔971P、乌龙木RS-PO和乙基纤维素制备不同批号的盐酸文拉法辛,计算其缓释性能。采用直接压片法制备缓释片,并对其生物黏附时间、溶胀指数、基质侵蚀、体外释放度进行评价。F3、F6批片剂具有较高的溶胀行为,但释药量极少。F2批具有较好的溶胀指数和体外释药率(99.85%)。F2批符合缓释片的各项要求,可作为12小时缓释片的理想或优化制剂。结果表明,卡波波尔是一种有效的缓粘剂;与疏水聚合物结合,也可作为强释放阻燃剂。关键词:Gastroretentive;Mucoadhesive;盐酸文拉法辛;平板电脑。
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