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抗疟药α-(二正丁氨基甲基)-2,7-二氯-9-对氯苄叉基-4-芴甲醇(下用代号76028)为疟疾治疗药。其结构式为: 此化合物是典型的疏水性药物,在水中易凝聚,溶解度极低(约1μg/ml)。口服本品吸收极少,只得靠增加服用剂量来提高吸收,而造成药物的浪费。由于它在体内的溶解度差,吸收速度缓慢,有效血药浓度出现迟缓,因此,原虫转阴速度也相应地较慢。为了克服76028的凝聚现象和增加药物的吸收表面积,曾研究过它的固态分散体制剂,但未达到预期目的。由于消化管上皮细胞(生物
The antimalarial drug α- (di-n-butylaminomethyl) -2,7-dichloro-9-p-chlorobenzylidene-4-fluorenemethanol (used as reference number 76028) is a malaria drug. Its structure is: This compound is a typical hydrophobic drug, easy to aggregate in water, very low solubility (about 1μg / ml). Oral absorption of this product is minimal, only by increasing the dose to increase absorption, resulting in the waste of drugs. Due to its poor solubility in the body, the absorption rate is slow, effective plasma concentration appears sluggish, therefore, protozoa negative speed is also slower. In order to overcome the coagulation phenomenon of 76028 and increase the absorption surface area of the drug, its solid dispersion preparation has been studied, but its intended purpose has not been achieved. Because of the digestive tract epithelial cells (biology