Woo Jong Soo, Kim Tae-Seo, Park Jae-Hyun, Chi Sang-Cheol
Pharmaceutical Research Lab. Hanmi Pharm. Co., Hwaseong 445-913, Korea.
Arch Pharm Res. 2007 Jan;30(1):82-9. doi: 10.1007/BF02977782.
Silymarin has been used to treat hepatobiliary diseases. However, it has a low bioavailability after being administered orally on account of its low solubility in water. In order to improve the dissolution rate, silymarin was formulated in the form of a self-microemulsifying drug delivery system (SMEDDS). The optimum formulation of SMEDDS containing silymarin was obtained based on the study of pseudo-ternary phase diagram. The SMEDDS consisted of 15% silymarin, 10% glyceryl monooleate as the oil phase, a mixture of polysorbate 20 and HCO-50 (1:1) as the surfactant, Transcutol as the cosurfactant with a surfactant/cosurfactant ratio of 1. The mean droplet size of the oil phase in the microemulsion formed from the SMEDDS was 67 nm. The % release of silybin from the SMEDDS after 6 hours was 2.5 times higher than that from the reference capsule. After its oral administration to rats, the bioavailability of the drug from the SMEDDS was 3.6 times higher than the reference capsule.
水飞蓟素已被用于治疗肝胆疾病。然而，由于其在水中的溶解度低，口服给药后生物利用度较低。为了提高溶出速率，水飞蓟素被制成自微乳化药物递送系统（SMEDDS）的形式。基于伪三元相图的研究，获得了含水飞蓟素的SMEDDS的最佳配方。该SMEDDS由15%的水飞蓟素、10%的单油酸甘油酯作为油相、聚山梨酯20和HCO-50（1:1）的混合物作为表面活性剂、肉豆蔻酸异丙酯作为助表面活性剂组成，表面活性剂/助表面活性剂比例为1。由SMEDDS形成的微乳液中油相的平均液滴尺寸为67nm。水飞蓟宾从SMEDDS中6小时后的释放率比参比胶囊高2.5倍。大鼠口服给药后，该药物从SMEDDS中的生物利用度比参比胶囊高3.6倍。
