氢氯噻嗪胶囊化自乳化给药系统的开发与评估

E.S. Essien, T.C. Jackson, E. Olorunsola
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引用次数: 0

摘要

背景:配制固体自乳化给药系统(Solid SEDDS)具有提高药物稳定性和增强给药系统的双重优势。研究目的本研究旨在开发和评估氢氯噻嗪固体自乳化给药系统。方法:测定了氢氯噻嗪在一些油类中的溶解度,并构建了最有效的油、水和表面活性剂的假三元体系。根据假三元图,配制了四种液体 SEDDS,其中包含吐温 80/油酸或 PEG 400/油酸(表面活性剂体系)和蓖麻油,三者的比例为 2:8 或 3:7。每种制剂都是在油/表面活性剂体系中加入药物,在持续搅拌下加热至 60 0C,然后冷却至室温。测定每种液体 SEDDS 的粘度;将液体 SEDDS 与微晶纤维素按 1:2 的比例混合后封装,制备固体 SEDDS。研究了固体 SEDDS 与市售产品的药物释放曲线。结果发现体外释放研究显示,配制的 SEDDS 药物释放率为 85.46% - 87.17%,表面活性剂混合比例为 3:7 的 SEDDS 药物释放率更优;每种配方的药物释放率都是市售产品的两倍。结论 制备的氢氯噻嗪固体 SEDDS 具有更好的药物释放特性,因此优于传统的市售产品。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Encapsulated Self-Emulsifying Drug Delivery System of Hydrochlorothiazide
Background: Formulation of solid self-emulsifying drug delivery system (Solid SEDDS) provides a dual benefit of improved drug stability and enhanced delivery system. Objective: This study was aimed at developing and evaluating a solid self-emulsifying drug delivery system of hydrochlorothiazide. Methods: Solubility of hydrochlorothiazide in some oils was determined and pseudo-ternary system of the most effective oil, water and  surfactant system was constructed. Four Liquid SEDDSs were formulated to contain Tween 80/oleic acid or PEG 400/oleic acid (surfactant  systems) and castor oil combined in ratio 2:8 or 3:7 based on the pseudo-ternary plot. Each preparation was made by adding the drug to  the oil/surfactant system and heating up to 60 0C under continuous stirring followed by cooling to room temperature. Viscosity of each  Liquid SEDDS was determined; Solid SEDDS was prepared by mixing the Liquid SEDDS with microcrystalline cellulose in 1:2 proportion  and then encapsulated. Drug release profile of the Solid SEDDSs in comparison with a marketed product was studied. Results: Castor oil was found to be the best solvent for hydrochlorothiazide and the viscosity of the Liquid SEDDSs was in the range of  79.41 and 187.32 mPa.s. The in vitro release studies showed 85.46 – 87.17 % drug release from the formulated SEDDSs with ratio 3:7 of  surfactant mix being superior; and percentage drug release for each formulation was twice that of the marketed product. Conclusion:  The prepared Solid SEDDS of hydrochlorothiazide exhibited improved drug release characteristics, hence superior to the conventional  commercial product. 
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