厚朴酚磷脂复合物理化性质与大鼠口服生物利用度

目的对制备的厚朴酚磷脂复合物的理化性质进行表征,并与厚朴酚及其磷脂物理混合物进行大鼠口服生物利用度比较。方法分别用差示扫描量热、X-射线粉末衍射和红外光谱分析厚朴酚磷脂复合物与厚朴酚及其磷脂物理混合物理化性质的差异;用实验建立的RP-HPLC法测定大鼠灌胃给药后不同时间血浆中厚朴酚的浓度,通过非房室模型统计矩方法计算药代动力学参数。结果厚朴酚磷脂复合物的理化性质与厚朴酚及其磷脂物理混合物明显不同;大鼠口服给药后厚朴酚磷脂复合物与厚朴酚及其磷脂物理混合物的主要药代动力学参数Tmax,Cmax,t1/2和AUC0-6分别为(1.17±0.26),(0.42±0.13)和(0.46±0.10)h;(0.63±0.06),(0.45±0.09)和(0.67±0.07)mg/L;(1.85±0.34),(1.30±0.32)和(1.52±0.28)h;(1.77±0.15),(0.90±0.17)和(1.38±0.19)mg.h/L。结论厚朴酚磷脂复合物中厚朴酚与磷脂以分子间力结合并以无定型形态分散于磷脂分子中;磷脂复合物显著提高了厚朴酚的大鼠口服生物利用度并表现出了一定的缓释特征。

Physicochemical characterization of magnolol-phospholipid complex and its oral bioavailability in rats

Aim To compare the physicochemical properties and the bioavailability after oral administrations of magnolol phospholipid-complex,magnolol and its phospholipid mixture in rats.Methods Their physicochemical properties including DSC,X-ray powder diffraction,IR were determined;the plasma concentration of magnolol was assayed by RP-HPLC and the pharmacokinetic parameters were computed by non-compartmental model with statistical moment theory.Results The magnolol-phospholipid complex showed different physicochemical properties and the Tmax,Cmax,t1/2andAUC0-6of the above 3 test groups were(1.17±0.26),(0.42±0.13) and(0.46±0.10) h;(0.63±0.06),(0.45±0.09) and(0.67±0.07) mg·L-1;(1.85±0.34),(1.30±0.32) and(1.52±0.28) h;(1.77±0.15),(0.90±0.17) and(1.38±0.19) mg·h·L-1,respectively.Conclusion The magnolol and phospholipid were combined by inter-molecular forces in the complex and its oral bioavailability increased significantly with a manner of sustained release compared to magnolol in rats.