The preparation of Garcinia Glycosides solid dispersion and intestinal absorption by rat in situ single pass intestinal perfusion

Ye-jun Chen, L. Shengnan, Ji Jingchao, Cheng Yinghui, Ju Liu, Yang Wang, Hongsheng Liu
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Abstract

Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.
大鼠原位单次肠灌注制备藤黄苷固体分散体及肠吸收
藤黄苷(Garcinia Glycosides)是通过高通量筛选(High Throughput Screening, HTS)对藤黄酸(Gambogic Acid, GA)进行结构修饰获得的一种候选药物。由于藤黄苷是一种有效但不溶性的抗肿瘤药物,本研究的目的是通过溶剂熔融法制得藤黄苷的固体分散体,以提高其溶解度和溶出速度。采用高效液相色谱(HPLC)和红外光谱对其进行了表征,并评价了大鼠原位单次肠灌注对该药物的肠道吸收。结果表明,与其他形式相比,其溶解度、溶出速度和吸收率均有所提高。表明固体分散体可显著提高藤黄苷的体内相对生物利用度。
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