College of Pharmacy, Yeungnam University, Gyongsan, South Korea.
Eur J Pharm Biopharm. 2009 Aug;72(3):539-45. doi: 10.1016/j.ejpb.2009.03.001. Epub 2009 Mar 17.
The main objective of this study was to prepare a solid form of lipid-based self-emulsifying drug delivery system (SEDDS) by spray drying liquid SEDDS with an inert solid carrier Aerosil 200 to improve the oral bioavailability of poorly water-soluble drug dexibuprofen. The liquid SEDDS was a system that consisted of dexibuprofen, Labrasol, Capryol 90 and Labrafil M 1944 CS. The particle size analysis revealed no difference in the z-average particle diameter of the reconstituted emulsion between liquid and solid SEDDS. The solid SEDDS was characterized by SEM, DSC and XRD studies. In vivo results of solid SEDDS and dexibuprofen powder in rats at the dose of 10mg/kg showed that the initial plasma concentrations of drug in solid SEDDS were significantly higher than those of dexibuprofen powder (P<0.05). The solid SEDDS gave significantly higher AUC and Cmax than did dexibuprofen powder (P<0.05). In particular, the AUC of solid SEDDS was about twofold higher than that of dexibuprofen powder. Our results suggested that this solid SEDDS could be used as an effective oral solid dosage form to improve the bioavailability of poorly water-soluble drug dexibuprofen.
本研究的主要目的是通过喷雾干燥含有惰性固体载体 Aerosil 200 的液态自乳化药物传递系统(SEDDS)来制备固态 SEDDS,以提高疏水性差的药物右旋布洛芬的口服生物利用度。液态 SEDDS 由右旋布洛芬、Labrasol、Capryol 90 和 Labrafil M 1944 CS 组成。粒径分析表明,重构乳液的 z 均粒径在液态和固态 SEDDS 之间没有差异。固态 SEDDS 通过 SEM、DSC 和 XRD 研究进行了表征。在 10mg/kg 剂量下,大鼠体内固态 SEDDS 和右旋布洛芬粉末的结果表明,固态 SEDDS 的药物初始血浆浓度明显高于右旋布洛芬粉末(P<0.05)。固态 SEDDS 比右旋布洛芬粉末具有更高的 AUC 和 Cmax(P<0.05)。特别是,固态 SEDDS 的 AUC 约为右旋布洛芬粉末的两倍。我们的结果表明,这种固态 SEDDS 可作为一种有效的口服固体剂型,以提高疏水性差的药物右旋布洛芬的生物利用度。