Development and evaluation of gastroretentive floating tablets of an antihypertensive drug using hydrogenated cottonseed oil.

Harshal Ashok Pawar, Pooja Ramchandra Gharat, Rachana Vivek Dhavale, Pooja Rasiklal Joshi, Pushpita Pankajkumar Rakshit
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引用次数: 28

Abstract

The aim of the present work was to develop a gastroretentive floating tablet of Atenolol and investigate the effects of both hydrophilic and hydrophobic retardant on in vitro release. Atenolol is an antihypertensive drug with an oral bioavailability of only 50% because of its poor absorption from lower gastrointestinal tract. The floating tablets of Atenolol were prepared to increase the gastric retention, to extend the drug release, and to improve the bioavailability of the drug. The floating tablets were formulated using hydrophilic polymers as Hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M), hydrophobic retardant as a hydrogenated cottonseed oil (HCSO), and sodium bicarbonate as a gas generating agent to reduce floating lag time. The formulated tablets were evaluated for the quality control tests such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. The in vitro release study of the tablets was performed in 0.1 N HCl as a dissolution media. The results of the present study clearly indicates the promising potential of Atenolol floating system as an alternative to the conventional dosage and other sustained release formulations. The study also revealed the effectiveness of HCSO as retardant in combination with HPMC.

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氢化棉籽油降压药胃保留浮片的研制与评价。
本研究的目的是研制一种胃保留型阿替洛尔漂浮片,并考察亲疏水性阻燃剂对阿替洛尔体外释放的影响。阿替洛尔是一种抗高血压药物,口服生物利用度仅为50%,因为它不易被下胃肠道吸收。制备阿替洛尔漂浮片,增加胃潴留,延长药物释放时间,提高药物的生物利用度。以亲水聚合物羟丙基甲基纤维素(HPMC K4M和HPMC K15M)、疏水阻燃剂氢化棉籽油(HCSO)和碳酸氢钠为生气剂配制漂浮片剂,以减少漂浮滞后时间。对配制的片剂进行重量变化、硬度、脆性、溶胀指数、漂浮滞后时间、总漂浮时间等质量控制指标的评价。以0.1盐酸为溶出介质进行体外释放研究。本研究的结果清楚地表明阿替洛尔漂浮体系作为常规剂量和其他缓释制剂的替代方案具有良好的潜力。研究还揭示了HCSO与HPMC复合作为阻燃剂的有效性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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