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Utilization and Evaluation of Tropical Medicinal Resources

热带药用资源的利用与评价

基本信息

批准号：
09045076
负责人：
AIMI Norio
金额：
$ 4.16万
依托单位：
Chiba University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B).
财政年份：
1997
资助国家：
日本
起止时间：
1997 至 1999
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-09045076/
关键词：
Thailand Tropical Medicinal Resources Natural Product Chemistry Pueraria mirifica Estrogenic activity Evaluation of biological activity Pharmaceutical technology Solid dispersion Pueraria mirifica 薬理学分析化学環境化学

项目摘要

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.

1.从泰国传统药物中分离种子分子（1）野葛（Pueraria mirifica）（Legumariae）（泰国名“Kwaw-keur”）被认为是推荐给老年人的一种恢复活力的民间药物。对活性成分的重新研究导致分离出两种新化合物，脱氧雌酚和异雌酚。发现脱氧雌酚的雌激素活性比已报道的植物中最有效的成分雌酚强10倍。获得的证据表明miroestrol是由deoxymiroestrol产生的伪影。对该植物的异黄酮进行了结构和雌激素活性的研究。(2)研究了泰国北方产的伞房塔贝蒙塔纳（Tabernaemontana corymbosa）中的吲哚生物碱，分离得到6种吲哚生物碱，分别为ervatamine、20-epiervatamine、voacangine、voacristine、tabernaemonatanine、dregamine.提高难溶性药物溶出度的研究（1）以水溶性物质为载体提高药物溶出度将熊去氧胆酸或氧氟沙星与水溶性载体混合制成固体分散体。选择PEG 6000、尿素、甘露醇为载体。粉末X射线衍射法，差示扫描量热法和红外光谱法被用来研究药物载体的相互作用，精确。(2)用多孔材料作载体改善溶出度制备了水不溶性药物和可控孔玻璃的物理混合物。通过差示扫描量热法、压力差示扫描量热法、粉末X射线衍射法和红外光谱法研究了测试固体分散体的物理化学性质。