School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
Int J Pharm. 2012 May 10;427(2):337-44. doi: 10.1016/j.ijpharm.2012.02.013. Epub 2012 Feb 16.
The present study aims to develop self-microemulsifying drug delivery systems (SMEDDS) in sustained-release pellets of puerarin to enhance the oral bioavailability of puerarin. The performances of puerarin-SMEDDS including oils, emulsifiers, and co-emulsifiers were evaluated. Pseudo-ternary phase diagrams shows that the optimized formulation consisted of castor oil as the oil phase, Cremophor EL as the emulsifier, and 1,2-propanediol as the co-emulsifier. SMEDDS sustained-release pellets were prepared via extrusion-spheronization. The particle size distributions of the formulations were determined using transmission electron microscopy and scanning electronic microscopy. The mean particle size was 50 ± 8 nm. The pharmacokinetics and bioavailability of the puerarin-SMEDDS sustained-release pellets and puerarin tablets were evaluated and compared in beagle dogs. The absolute bioavailability of the puerarin-SMEDDS sustained-release pellets was enhanced by approximately 2.6-fold compared with that of the puerarin tablet. The relative bioavailability (F(rel)) of the SMEDDS pellets was 259.7% compared with the tablet group. The results demonstrated that the puerarin-SMEDDS sustained-release pellets had a sustained-release effect, and could remarkably improve the oral bioavailability of puerarin.
本研究旨在开发葛根素自微乳给药系统（SMEDDS）的缓释微丸，以提高葛根素的口服生物利用度。评价了葛根素-SMEDDS 的油相、乳化剂和助乳化剂的性能。伪三元相图表明，优化的配方由蓖麻油作为油相、吐温 EL 作为乳化剂和 1,2-丙二醇作为助乳化剂组成。通过挤出-滚圆法制备 SMEDDS 缓释微丸。采用透射电子显微镜和扫描电子显微镜测定制剂的粒径分布。平均粒径为 50±8nm。在比格犬中评价并比较了葛根素-SMEDDS 缓释微丸和葛根素片的药代动力学和生物利用度。与葛根素片相比，葛根素-SMEDDS 缓释微丸的绝对生物利用度提高了约 2.6 倍。与片剂组相比，SMEDDS 微丸的相对生物利用度（F（rel））为 259.7%。结果表明，葛根素-SMEDDS 缓释微丸具有缓释作用，可显著提高葛根素的口服生物利用度。
