Wang Dong Kai, Shi Zhao Hui, Liu Lai, Wang Xiao Yan, Zhang Cui Xia, Zhao Peng
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
PDA J Pharm Sci Technol. 2006 Nov-Dec;60(6):343-9.
A self-microemulsifying drug delivery system (SMEDDS) for enhancement of oral absorption of a poor water-soluble drug, alpha-Asarone (ARE), is reported. Solubility of ARE was determined in various vehicles. SMEDDS consisted of a mixture of oils, surfactants, and cosurfactants that were emulsified in an aqueous medium under the gentle agitation and digestive motility. Pseudo-ternary phase diagrams were used to identify the efficient self-emulsification regions. The particle size distribution of the resulting microemulsions was determined using a laser scatter particle size analyzer (LSPSA). The optimized SMEDDS formulations containing Ethyl oleate (20%), Tween 80 (60%), and PEG 400 (20%) were tested for in vitro dissolution. The percentage of ARE released from the SMEDDS was significantly higher than that from the conventional tablets. Oral bioavailability of ARE in the SMEDDS via the hard capsules and the conventional tablets was evaluated in fasted beagle dogs. The bioavailability of ARE formulated in SMEDDS showed approximately 4.8-fold higher bioavailability than that in the conventional tablets. The results indicated that SMEDDS is potentially a good drug delivery system for oral delivery of the hydrophobic compound ARE.
据报道，一种用于提高难溶性药物α-细辛醚（ARE）口服吸收的自微乳化药物递送系统（SMEDDS）。测定了ARE在各种载体中的溶解度。SMEDDS由油、表面活性剂和助表面活性剂的混合物组成，在温和搅拌和消化蠕动下于水介质中乳化。使用伪三元相图来确定有效的自乳化区域。使用激光散射粒度分析仪（LSPSA）测定所得微乳液的粒度分布。对含有油酸乙酯（20%）、吐温80（60%）和聚乙二醇400（20%）的优化SMEDDS制剂进行体外溶出度测试。ARE从SMEDDS中的释放百分比显著高于传统片剂。通过硬胶囊和传统片剂对禁食比格犬体内SMEDDS中ARE的口服生物利用度进行了评估。以SMEDDS制剂形式存在的ARE的生物利用度比传统片剂中的生物利用度高约4.8倍。结果表明，SMEDDS可能是一种用于口服递送疏水性化合物ARE的良好药物递送系统。
