Wu Kai-Rong, Chuo Wen-Ho, Huang Yuh-Tyng
Graduate Institute of Biomedical Science, Chung Hwa University of Medical Technology, Tainan 717302, Taiwan.
Department of Pharmacy, Tajen University, Pingtung 90741, Taiwan.
Pharmaceuticals (Basel). 2022 Nov 19;15(11):1433. doi: 10.3390/ph15111433.
Oleanolic acid (OA) is an active ingredient of the traditional Chinese medicine (TCM) (FLL). Its clinical use is restricted because it is water-insoluble and has limited dosage forms of administration at present. Hence, the FFL dropping pills were prepared by the hot-melt method of solid dispersion technology. A 2 factorial design was used to examine the effects of the materials used to prepare the dropping pills (e.g., different ratios of PEG4000 and PEG6000, FLL extract loading, and percentage of Tween 80) on parameters such as dropping pill roundness, weight variation, and disintegration time. Moreover, 2 full factorial design was utilized to search for the optimal formulation for dissolution experiments. The results showed that the percentage of Tween 80 demonstrated significant effects on dropping pill roundness, weight variation, and disintegration time; FLL extract loading affected roundness and weight variation; and different ratios of PEG4000 and PEG6000 only affected disintegration time. The optimal formulation of the dropping pills released 70% of the drug after 30 min of dissolution release, which was faster than commercially available FLL Chinese medicines. Furthermore, the amount released was higher than that of commercially available formulations. In this study, a solid dispersion technique was used to successfully produce FLL dropping pills. In addition to improving the water insolubility of FLL and increasing the dissolution release percentage of the drug, we increased the application value of FLL and reduced the issues of traditional administration dosage forms.
齐墩果酸（OA）是中药（FLL）的一种活性成分。其临床应用受到限制，因为它不溶于水且目前给药剂型有限。因此，采用固体分散技术的热熔法制备了FLL滴丸。采用二因素析因设计来考察制备滴丸所用材料（如PEG4000与PEG6000的不同比例、FLL提取物载量和吐温80的百分比）对滴丸圆整度、重量差异和崩解时间等参数的影响。此外，利用二全因子设计来寻找用于溶出实验的最佳处方。结果表明，吐温80的百分比对滴丸圆整度、重量差异和崩解时间有显著影响；FLL提取物载量影响圆整度和重量差异；PEG4000与PEG6000的不同比例仅影响崩解时间。滴丸的最佳处方在溶出释放30分钟后释放了70%的药物，这比市售的FLL中药更快。此外，释放量高于市售制剂。在本研究中，采用固体分散技术成功制备了FLL滴丸。除了改善FLL的水不溶性和提高药物的溶出释放百分比外，我们还提高了FLL的应用价值并减少了传统给药剂型的问题。
