氧氟沙星胃保留剂型的研制与评价

P. R. Veerareddy, S. Bajjuri, Krishna Sanka, Raju Jukanti, S. Bandari, Rk Ajmeru, A. Potu
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引用次数: 9

摘要

本研究旨在研究以HPMC K4M、HPMC K15M、聚氧聚乙烯WSR 303、卡波波尔971P、黄原胶等不同配比聚合物配制氧氟沙星胃保留给药片,并对其在胃内局部根除幽门螺杆菌感染的作用进行评价。采用湿法造粒法制备GRDDTs,并对其硬度、厚度、脆性、药物含量、漂浮性能等物理特性进行了评价。优化后的配方F4具有较好的缓释效果和较好的漂浮性能,最符合Korsmeyer-Peppas模型,r2值为0.9848。由于Korsmeyer- Peppas模型的n值小于0.45,它遵循菲克式扩散机制。傅里叶变换红外光谱(FT-IR)结果表明,药物与赋形剂无相互作用。用载BaSO4片进行体内放射线研究,以检验制备的片剂对胃停留时间的增加。研究显示,片剂在胃内停留时间为300±10min,表明氧氟沙星治疗幽门螺杆菌性消化性溃疡有效局部作用的胃停留时间增加。关键词:氧氟沙星;幽门螺杆菌;胃停留时间;胃保留性给药系统。DOI: http://dx.doi.org/10.3329/sjps.v4i1.8861 SJPS 2011;4(1): 9到18
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Formulation and Evaluation of Gastroretentive Dosage Form of Ofloxacin
The aim of the present investigation was to develop and evaluate gastroretentive drug delivery tablets (GRDDTs) of ofloxacin using different polymers such as HPMC K4M, HPMC K15M, Polyethylene oxide WSR 303, Carbopol 971P, Xanthan Gum in different ratios for local action in gastric region to eradicate Helicobacter pylori infection. The GRDDTs were prepared by wet granulation method and evaluated for physical characteristics such as hardness, thickness, friability, drug content and floating properties. The optimized formula F4 showed better sustained drug release and which also had good floating properties and fitted best to be Korsmeyer-Peppas model with R 2 value of 0.9848. As the n value for the Korsmeyer- Peppas model was found be less than 0.45 it follows Fickian diffusion mechanism. FT-IR result showed that there is no drug excipient interaction. In vivo radiographic studies were conducted with BaSO4 loaded tablets to examine the increased gastric residence time of the prepared tablets. The study revealed that the tablet remained in the stomach for 300±10min which indicates the increase in the gastric residence time for the effective localized action of the ofloxacin in the treatment of Helicobacter pylori caused peptic ulcer. Key words : Ofloxacin; Helicobacter pylori; gastric residence time; gastroretentive drug delivery system. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8861 SJPS 2011; 4(1): 9-18
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