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Formulation and in vitro evaluation of Hydrodynamically balanced system for theophylline delivery

机译:茶碱输送液动力平衡系统的制定与体外评价

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摘要

The objective of the present study was to formulate hydrodynamically balanced systems (HBSs) of theophylline as single unit capsules. They were formulated by physical blending of theophylline with hydroxypropyl methyl cellulose, polyethylene oxide, polyvinyl pyrrolidone, ethyl cellulose, liquid paraffin, and lactose in different ratios. These theophylline HBS capsules were evaluated for weight uniformity, drug content uniformity, in vitro floating behavior and drug release in simulated gastric fluids (pH 1.2). All these formulated HBS capsules containing theophylline were floated well over 6 hours with no floating lag time, and also showed sustained in vitro drug release in simulated gastric fluid over 6 hours. The theophylline release from these capsules was more sustained with the addition of release modifiers (ethyl cellulose and liquid paraffin). The drug release pattern from these capsules was correlated well with first order model (F-1 to F-5) and Korsmeyer-Peppas model (F-6 and F-7) with the non-Fickian (anomalous) diffusion mechanism. These experimental results clearly indicated that these theophylline HBS capsules were able to remain buoyant in the gastric juice for longer period, which may improve oral bioavailability of theophylline
机译:本研究的目的是将茶碱的水动力平衡系统(HBS)配制为单个单位胶囊。它们是通过将茶碱与羟丙基甲基纤维素,聚环氧乙烷,聚乙烯吡咯烷酮,乙基纤维素,液体石蜡和乳糖以不同比例物理混合而成。对这些茶碱HBS胶囊的重量均匀性,药物含量均匀性,体外漂浮行为和在模拟胃液(pH 1.2)中的药物释放进行了评估。所有这些含有茶碱的HBS配制胶囊均在6小时内漂浮良好,没有漂浮滞后时间,并且还显示在6小时内在模拟胃液中持续释放体外药物。添加释放调节剂(乙基纤维素和液体石蜡)可使茶碱从这些胶囊中的释放更加持久。这些胶囊的药物释放模式与一阶模型(F-1至F-5)和Korsmeyer-Peppas模型(F-6和F-7)与非Fickian(异常)扩散机制密切相关。这些实验结果清楚地表明,这些茶碱HBS胶囊能够在胃液中长期保持漂浮状态,这可能会提高茶碱的口服生物利用度。

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