葛根素缓释片的制备及犬体内生物利用度的研究

Correlation between in vitro release and in vivo absorption in dogs of Puerarin sustained-release tablets

选用磷脂和聚维酮为载体材料制备葛根素固体分散体后再制成缓释片,并考察其体外释放度和犬体内药动学试验,以Wagner-Nelson法计算体内吸收分数。采用HPLC的方法测定犬血浆中葛根素的浓度,应用3p97程序计算药动学参数和生物利用度。结果表明:葛根素缓释片具有较好的缓释效果,体内外相关性较好(r=0.9875)。与普通片相比,葛根素缓释片的相对生物利用度为253%,可以通过固体分散技术明显提高葛根素生物利用度,并减少给药次数。

The puerarin solid dispersion was prepared using phospholipid and PVP as dispersion carriers and then sustained release tablets were produced with the solid dispersion and proper formulation. The in vitro release and in vivo absorption in dogs of puerarin sustained-release tablets were investigated. The concentration of puerarin in plasma was determined by HPLC. The 3p97 program was applied to calculate the phamcokinetic parameters. The sustained-release tablets had a good correlativity between in vitro release and in vivo absorption （ r = 0. 987 5 ）. The relative bioavailability of puerarin sustained-release tablets to the conventional puerarin tablets was 253%. The rel- ative bioavailability of the sustained release tablets was greatly improved by the solid dispersion technique