酮洛芬胃保留原位胶凝系统的研制与评价

AR. Shabaraya, T. T Ashwini, K. Vineetha
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引用次数: 0

摘要

实现长期药物释放的革命性概念是胃保留原位胶凝系统。本研究的目的是制定和测试一种胃保留原位凝胶,用于将酮洛芬递送到目标部位,以增加停留和递送时间。酮洛芬胃保留原位凝胶采用阳离子驱动凝胶化方法,使用各种组合和浓度的聚合物,如结冷胶、海藻酸钠和羟丙基甲基纤维素(HPMC) K100M合成。视觉外观、pH、粘度、体外凝胶化、体外浮力、药物含量、密度测量、凝胶强度测量、吸水率和体外药物释放度均进行了评价。总漂浮时间均大于12 h,漂浮滞后时间小于2 min。所得配方pH值为6.89 ~ 7.61,药物含量为82.01% ~ 95.53%。聚合物海藻酸钠浓度较高(1.5%)、结冷胶与HPMC K100M复合(0.175%、0.2%)的F5和F14的累积释药率分别为84.10%和85.49%。体外溶出度实验和稳定性研究均显示药物含量无明显变化。研究结果表明,原位凝胶有助于延长胃停留时间,使药物在胃中释放。
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Formulation and Evaluation of Gastroretentive In Situ Gelling System of Ketoprofen
Abstract A revolutionary concept for achieving long-term medication release is the gastroretentive in situ gelling system. The goal of this research was to formulate and test a gastroretentive in situ gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive in situ gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, in vitro gelation, in vitro buoyancy, drug content, density measurement, gel strength measurement, water uptake, and in vitro drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. In vitro dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated in situ gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.
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来源期刊
European Pharmaceutical Journal
European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
0.60
自引率
0.00%
发文量
16
期刊介绍: European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.
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