Utilization and Evaluation of Tropical Medicinal Resources

1.泰国传统药材中种子分子的分离(1)葛根(豆科)(泰文名“Kwaw-Keur”)是一种推荐给老年人的民间返老药。通过对其活性成分的再研究，分离得到两个新化合物：脱氧米孕酮和异米孕酮。研究发现，脱氧米雌醇的雌激素活性是米非司酮的10倍，而米洛雌醇被认为是该植物中最有效的成分。有证据表明，米非司酮是脱氧米非司酮的产物。对产于泰国北部的伞房花中的吲哚生物碱进行了研究，分离得到6个吲哚生物碱，分别为：艾尔瓦他明、20-表艾尔瓦他明、伏阿卡宁、伏拉西汀、塔贝那那他宁、德雷加明。难溶药物溶出度的改进研究(1)以水溶性物质为载体的溶出度改进方法：将熊去氧胆酸或氧氟沙星与水溶性载体混合形成固体分散体。以聚乙二醇6000、尿素和甘露醇为载体。利用粉末X射线衍射仪、差示扫描量热仪和红外光谱仪对药物-载体相互作用进行了精确的研究。(2)以多孔材料为载体的溶出度改进方法制备了水不溶性药物与可控孔玻璃的物理混合物。采用差示扫描量热法、压力差示扫描量热法、粉末X射线衍射法和红外光谱仪对所制备的固体分散体的物理化学性质进行了研究。

1. Isolation of seed molecules from Thai traditional medicines(1) Pueraria mirifica (Leguminosae) (Thai name "Kwaw-keur") is known as a rejuvenating folk medicine recommended to aged people. Reinvestigation for the active principle resulted in isolation of two new compounds, deoxymiroestrol and isomiroestrol. Deoxymiroestrol was found to possess 10 fold stronger estrogenic activity over miroestrol which had been reported to be most active principle of the plant. Evidence was obtained to suggest miroestrol is an artefact arising from deoxymiroestrol. Isoflavonoid of the plant was studied for the structures and estrogenic activity.(2) Indole alkaloids of Tabernaemontana corymbosa from northern Thailand was studied and six indole alkaloids, ervatamine, 20-epiervatamine, voacangine, voacristine, tabernaemonatanine, dregamine, were isolated.2. Studies on improved dissolution of poorly soluble drugs(1) Improved dissolution using water soluble substances as carriersUrsodeoxycholic acid or ofloxacin were mixed with water soluble carriers to form solid dispersions. PEG6000, urea, and mannitol were chosen as the carriers. Powder X-ray diffractometry, differential scanning calorimetry, and infrared spectroscopy were used to study drug-carrier interactions precisely.(2) Improved dissolution using porous materials as carriersThe physical mixtures of a water insoluble drug and controlled pore glass were prepared. Physicochemical properties of the test solid dispersions were studied by differential scanning calorimetry, pressure differential scanning calorimetry, powder X-ray diffractometry, and infrared spectrometry.