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目的:对马尼地平磷脂复合物进行表征,并考察其体外肠吸收特性。方法:采用紫外分光光度法、差示扫描量热分析法、溶解度法和溶出度测定法对马尼地平磷脂复合物性质进行表征;通过离体外翻肠囊模型考察马尼地平在不同肠段的吸收特性。结果:与原药及原药-磷脂物理混合物比较,磷脂复合物的溶解度、溶出度、油/水分配系数、紫外吸收均有不同程度的改变,磷脂复合物在各肠段部位的转运速率Vt和表观渗透系数Papp均大于原药,其中在空肠的吸收均显著强于其他部位(P<0.01)。结论:马尼地平复合磷脂后,其溶解度、溶出度、肠吸收明显改善,马尼地平磷脂复合物将有利于提高药物的生物利用度。
OBJECTIVE: To characterize manidipine phospholipid complex and investigate its intestinal absorption characteristics in vitro. Methods: The properties of Manidipine phospholipid complex were characterized by UV spectrophotometry, differential scanning calorimetry, solubility and dissolution assay. The effects of Manidipine on the different intestinal segments Absorption characteristics. Results: Compared with the original drug and phospholipid physical mixture, the solubility, dissolution, oil / water partition coefficient and ultraviolet absorption of the phospholipid complex all changed to some extent. The transport rate of phospholipid complex in each segment of bowel was Vt And the apparent permeability coefficient Papp were greater than the original drug, which in the jejunum absorption were significantly stronger than other parts (P <0.01). Conclusion: Manidipine complex phospholipid, its solubility, dissolution, intestinal absorption improved significantly, manidipine phospholipid complex will help to improve the bioavailability of drugs.