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Formulation and Evaluation of Swellable and Floating Gastroretentive Ciprofloxacin Hydrochloride Tablets

机译:溶胀性和漂浮性胃滞留盐酸环丙沙​​星片的配制与评价

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摘要

Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Swellable, floating, and sustained release tablets are developed by using a combination of hydrophilic polymer (hydroxypropyl methylcellulose), swelling agents (crospovidone, sodium starch glycolate, and croscarmelose sodium) and effervescent substance (sodium bicarbonate). Formulations are evaluated for percentage swelling, in vitro drug release, floating lag time, total duration of floating, and mean residence time (MRT) in the stomach. The drug release of optimized formulation follows the Higuchi kinetic model, and the mechanism is found to be non-Fickian/anomalous according to Krosmeyer–Peppas (n value is 0.68). The similarity factor (f2) is found to be 26.17 for the optimized formulation, which the release is not similar to that of marketed produced (CIFRAN OD®). In vivo nature of the tablet at different time intervals is observed in the radiographic pictures of the healthy volunteers and MRT in the stomach is found to be 320 ± 48.99 min (n = 6). A combination of HPMC K100M, crospovidone, and sodium carbonate shows the good swelling, drug release, and floating characters than the CIFRAN OD®.
机译:胃肠道(GIT)吸收窗口狭窄的药物吸收不良。对于这些药物,胃滞留药物递送系统具有延长胃排空时间的优点。通过使用亲水性聚合物(羟丙基甲基纤维素),膨胀剂(交聚维酮,淀粉羟乙酸钠和交联羧甲基蜜糖钠)和泡腾物质(碳酸氢钠)的组合来开发可溶,漂浮和持续释放的片剂。评价制剂的溶胀百分比,体外药物释放,漂浮滞后时间,漂浮的总持续时间以及在胃中的平均停留时间(MRT)。优化制剂的药物释放遵循Higuchi动力学模型,根据Krosmeyer-Peppas(n值为0.68),发现该机理是非菲克/异常的。对于优化的配方,发现相似系数(f2)为26.17,其释放与市售产品(CIFRANOD®)的释放不同。在健康志愿者的放射照片中观察到片剂在不同时间间隔的体内性质,发现胃中的MRT为320±48.99分钟(n = 6)。 HPMC K100M,交聚维酮和碳酸钠的组合显示出比CIFRANOD®更好的溶胀,药物释放和漂浮特性。

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