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利用聚乙烯吡咯烷酮熔融固体分散体提高兔体内厚朴酚的生物利用度。

Enhancing the bioavailability of magnolol in rabbits using melting solid dispersion with polyvinylpyrrolidone.

机构信息

School of Pharmacy, China Medical University , Taichung , Taiwan.

出版信息

Drug Dev Ind Pharm. 2014 Mar;40(3):330-7. doi: 10.3109/03639045.2012.760580. Epub 2013 Feb 1.

Abstract

OBJECTIVE

Preparation of magnolol-loaded amorphous solid dispersion was investigated for improving the bioavailability.

MATERIALS AND METHODS

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 The blood samples withdrawn via marginal ear vein at specific time points were assayed by HPLC method.

RESULTS

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.

CONCLUSION

Magnolol-loaded amorphous solid dispersion with PVP has demonstrated enhanced bioavailability of magnolol in rabbits.

摘要

目的

制备厚朴酚无定形固体分散体以提高其生物利用度。

材料与方法

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。

结果

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%。

结论

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。

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