Microemulsion drug delivery system: for bioavailability enhancement of ampelopsin.

Shailendra Singh Solanki, Brajesh Sarkar, Rakesh Kumar Dhanwani
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引用次数: 44

Abstract

Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.

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微乳给药系统:用于提高蛇葡萄素的生物利用度。
蛇葡萄素是最常见的类黄酮之一,据报道具有许多药理活性,但水溶性较差。本研究旨在通过开发一种新型的给药系统——微乳(ME)来提高葡萄葡萄素的溶出度和生物利用度,并研究微乳(ME)对葡萄葡萄素口服生物利用度的影响。以Cremophor EL为表面活性剂,Transcutol为助表面活性剂,研制了以cammul mcm为基础的葡萄葡萄素口服给药制剂。对优化后的ME进行透明度、粘度、百分比测定等评价。测定了ME系统的增溶能力。将制备的ME与纯药溶液和市售片剂进行体外释药比较。以蛇葡萄素、Capmul MCM(5.5%)、cremoophor EL(25%)、Transcutol P(8.5%)和蒸馏水为主要成分的最佳ME制剂体外释放度高于普通药物混悬液和市售片剂混悬液。这些结果证明了代谢能在提高诸如蛇葡萄素等水溶性较差的化合物的生物利用度方面的潜在用途。
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