Improving the oral absorption of magnolol in New Zealand rabbits by the solid dispersion technique

• Main Authors: Tzu-Yun Liao, 廖慈雲
• Other Authors: 蔡尚元
• Format: Others
• Language: zh-TW
• Published: 2007
• Online Access: http://ndltd.ncl.edu.tw/handle/51888145281352644736

碩士 === 中國醫藥大學 === 藥學系碩士班 === 95 === Magnolol, a water-insoluble polyphenol, were isolated from Magnolia officinalis and reported to possess many beneficial pharmacological activities including anti-oxidation, anti-inflammatory, anti-thrombus, anti-carcinogenic, antibacterial and protecting gastro-intestinal tract. However, its oral absorption is poor and erratic that many offend its efficiency. In this paper, we attempted to enhance the solubility and dissolution of magnolol by the formation of amorphous solid dispersionwith water-solable carrier and thereby could tried to render its utilization in oral absorption more efficient in clinic. Among of the investigated carries, povidone K-30 and HP-β-cyclodextrin were found to have significant solubility enhancing effect on the magnolol. Therefore, the solid dispersions （SD） of magnolol were prepared by comelting or solvent evaporating method with povidone K-30 or HP-β-cyclodextrin and the characterization of the SD were assessed by the differential scanning calorimetry, Fourier transformation infrared spectrophotometry, powder X-ray diffraction and scanning electron microscopy. It was found that the solid dispersion would be an amorphous when the sufficient amount of carrier was used. The SD prepared from the povidone K-30 was found having the best dissolution rate than that of prepared from HP-β-cyclodextrin or the intact drug. The pharmacokinetics of oral absorption of magnolol in rabbits were also significantly enhanced ( 45％ in Cmax or 83％ in AUC, respectively) when the SD was administered to compared with the intact drug. In this study, we had found that the comelting methond was easier to form the amorphous amagnolol solid dispersion than the solvent evaporating method. On the other hand, the former also had the benefits of being feasible, economic, safety and environmental protection. In practice, if the oral solid dosage form of magnolol would be expected to have more efficiency, this proposed method was worthy of paying more attention to refer.