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伊曲康唑是一种活性很强的抗真菌药,但它是一个弱碱(pKa=3.7),还具有较强的疏水性(pH=8.1时辛醇/水分配系数logP=5.66)。为了开发其静脉注射剂型,尝试了以聚-ε-己酸内酯为载体制备毫微球后,再分散成混悬液的制剂。但该剂型稳定性较差,主要?
Itraconazole is a very active antimycotic but it is a weak base (pKa = 3.7) and has a strong hydrophobicity (octanol / water partition coefficient logP at pH = 8.1 = 5.66). In order to develop its intravenous dosage form, an attempt was made to prepare a nanosphere with poly-ε-caprolactone as a carrier and then disperse into a suspension. However, the stability of the formulation is poor, mainly?