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由于安体舒通的溶解度小,溶出率低,故口服吸收不完全,为此本文研究用β-环糊精制成包合物,企图提高其人体口服的生物利用度。环糊精包合物相当于分子包囊,药物分子被分离而分散于低聚糖骨架中。由于疏水性药物的晶格在胃肠液中不崩散,而与环糊精包合的亲水晶格溶出很快,为此提高了口服生物利用度。本实验采用三个样品:①安体舒通,②安体舒通和β-环糊精的混合物,③安体舒通β-环糊精(1∶3)包合物。进行了红外、差示扫描量热法及X-线衍射测定。 12个20~35岁健康男女志愿者(无肾
Because spironolactone solubility, low dissolution rate, so the oral absorption is not complete, for this study, β-cyclodextrin made of inclusion complex, in an attempt to improve its bioavailability of oral. Cyclodextrin inclusion complex is equivalent to molecular encapsulation, drug molecules are separated and dispersed in the oligosaccharide backbone. Since the crystal lattice of the hydrophobic drug does not collapse in the gastrointestinal fluids, the hydrophilic crystalline lattice enclosed in the cyclodextrin dissolves rapidly, thereby increasing the oral bioavailability. The experiment used three samples: ① spironolactone, ② spironolactone and β-cyclodextrin mixture, spironolactone β-cyclodextrin (1: 3) inclusion complex. Infrared, differential scanning calorimetry and X-ray diffraction were performed. 12 healthy men and women volunteers aged 20 to 35 (no kidney