Preparation and In-Vitro Dissolution of Ibuprofen: Soluplus Solid Dispersion

A. Salawi, Ahmed Abu Fayyad, Mohammad M. Kamal, Alsayad Al Arabi Sallam, S. Nazzal
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Abstract

Introduction: Ibuprofen is widely used in treatment of mild to moderated pain and fever. However, according to Biopharmaceutical Classification System (BCS) it is classified as Class II compound having high permeability and low solubility, thus the rate limiting step to avoid delaying in analgesic effect is to be available in soluble state. Objective: To prepares and characterize Ibuprofen:Souplus solid dispersion using co-evaporation technique. Methods: Various ration of Soluplus (0, 10, 30, 50, 70, 80, 90, and 100 %) was first dissolved in a common solvent followed by adding the complementing ratio of Ibuprofen. The solvent was removed under fume hood overnight. The thin film formed after evaporation was collected, compressed and tested for in-vitro dissolution at phosphate buffer pH 7.2. The physical appearance of the film also was tested. Results:At 40% Soluplus the dissolution of Ibuprofen was around 25 % at 30 min compared with 15% Soluplus showed around 80% resales at the same time interval. 10% soluplus released 100% at 30 min. Interestingly, after 8-10 hr. The release profile was more sustained until 24 hr. Regardless the % of Soluplus. Conclusion: Sustained release profile of Ibuprofen:Soluplus solid dispersion can be achieved at lower % of Soluplus.
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布洛芬的制备及体外溶出:固相分散体
简介:布洛芬广泛用于治疗轻度至中度疼痛和发烧。然而,根据生物制药分类系统(BCS),它被归类为II类化合物,具有高渗透性和低溶解度,因此为了避免延迟止痛效果,限速步骤是在可溶性状态下可用。目的:用共蒸发技术制备布洛芬汤加固体分散体并对其进行表征。方法:先将不同比例的Soluplus(0、10、30、50、70、80、90、100%)溶于普通溶剂中,再加入布洛芬的补充比例。溶剂在通风柜下被清除了一夜。收集蒸发后形成的薄膜,压缩,在磷酸盐缓冲液pH 7.2下进行体外溶出测试。对胶片的物理外观也进行了测试。结果:加量40%时布洛芬30 min溶出度约为25%,加量15%时布洛芬30 min溶出度约为80%。10%的溶液在30分钟内释放100%。有趣的是,8-10小时后。释放剖面持续到24小时。不管溶液的百分比是多少。结论:布洛芬缓释片的缓释特征为:在较低的固相分散浓度下可实现固相分散。
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