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抗疟药α-(二丁氨甲基)-6,8-二氯-2,-(3′,4′-二氯苯基)-4-喹啉甲醇(Ⅰ)及其盐酸盐(Ⅱ),对耐氯喹疟原虫株在人体及动物上均获良好疗效。但由于溶解度小,不易吸收,口服Ⅱ硬胶囊后大部分药物能从大便中检出,所以生物利用度很低; 只有加大剂量才能达到有效血药浓度。Ⅱ硬胶囊通常要给予250mg、一日三次,连服六天才能显效。过去曾试图制成水溶性大的盐来提高它的有效性,但未获得成功。本文研究了利用油酸作为溶剂,制成软胶囊,提高Ⅰ的生物利用度。Ⅰ在油酸中的溶解量可达到23.5,%(w/w)。而Ⅰ与Ⅱ在水中的溶解度均为1mg/l。同时对Ⅰ油酸软
The antimalarial drug alpha- (dibutylaminomethyl) -6,8-dichloro-2, - (3 ’, 4’- dichlorophenyl) -4quinolinemethanol (I) and its hydrochloride Ⅱ), against chloroquine resistant Plasmodium strains in the human body and animals have a good effect. However, due to the low solubility, not easy to absorb, most of the drugs Ⅱ oral hard capsules can be detected from the stool, so the bioavailability is very low; only to increase the dose to achieve effective plasma concentration. Ⅱ hard capsules usually give 250mg, three times a day, even for six days to be effective. In the past, attempts to make a salt that was water-soluble to increase its effectiveness were unsuccessful. In this paper, the use of oleic acid as a solvent, made of soft capsules, improve the bioavailability of Ⅰ. Ⅰ dissolved in oleic acid up to 23.5% (w / w). The solubility of I and II in water is 1 mg / l. At the same time I oleic acid soft