School of Pharmacy, China Medical University , Taichung , Taiwan.
Drug Dev Ind Pharm. 2014 Mar;40(3):330-7. doi: 10.3109/03639045.2012.760580. Epub 2013 Feb 1.
Preparation of magnolol-loaded amorphous solid dispersion was investigated for improving the bioavailability.
A solid dispersion of magnolol was prepared with polyvinylpyrrolidone K-30 (PVP) by melting method, and the physical properties were characterized by using differential scanning calorimetry, powder X-ray diffractometry, Fourier transformation-infrared spectroscopy and scanning electron microscope. In addition, dissolution test was also performed. Subsequently, the bioavailability of magnolol pure compound, its physical mixture and solid dispersion were compared in rabbits. The blood samples withdrawn via marginal ear vein at specific time points were assayed by HPLC method.
Oral administration of the solid dispersion of magnolol with PVP significantly increased the systemic exposures of magnolol and magnolol sulfates/glucuronides by 80.1% and 142.8%, respectively, compared to those given with magnolol pure compound.
Magnolol-loaded amorphous solid dispersion with PVP has demonstrated enhanced bioavailability of magnolol in rabbits.
制备厚朴酚无定形固体分散体以提高其生物利用度。
采用熔融法将厚朴酚与聚乙烯吡咯烷酮 K-30（PVP）制成固体分散体，通过差示扫描量热法、粉末 X 射线衍射法、傅里叶变换红外光谱法和扫描电子显微镜对其物理性质进行表征。此外，还进行了溶出度试验。随后，在兔体内比较了厚朴酚纯化合物、物理混合物和固体分散体的生物利用度。通过高效液相色谱法测定特定时间点从耳缘静脉采集的血样。
与厚朴酚纯化合物相比，PVP 载厚朴酚固体分散体口服给药后，厚朴酚及其硫酸盐/葡萄糖醛酸苷的全身暴露量分别显著增加了 80.1%和 142.8%。
PVP 载厚朴酚无定形固体分散体提高了兔体内厚朴酚的生物利用度。
