中文名 | HYDROXY ITRACONAZOLE |
英文名 | HYDROXY ITRACONAZOLE |
别名 | 羟基伊曲康唑 依曲康唑杂质 伊曲康唑杂质8 伊曲康唑杂质1 伊曲康唑代谢物 伊曲康唑2-羟基代谢物 羟基伊曲康唑(伊曲康唑代谢物) |
英文别名 | R 63373 HYDROXY ITRACONAZOLE Itraconazole 2-Hydroxy Metabolite Itraconazole metabolite Hydroxy Itraconazole Itraconazole Impurity 8(Hydroxy Itraconazole) 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylMethyl)-1,3-dioxolan-4-yl]Methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(2-hydroxy-1-Methylpropyl)- 3H-1,2,4-Triazol-3-one, 4-4-4-4-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-(2-hydroxy-1-methylpropyl)- 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(2-hydroxy-1-methylpropyl)-3H-1,2,4-triazol-3-one |
CAS | 112559-91-8 |
化学式 | C35H38Cl2N8O5 |
分子量 | 721.63 |
密度 | 1.44±0.1 g/cm3(Predicted) |
熔点 | 76-78°C |
沸点 | 884.7±75.0 °C(Predicted) |
溶解度 | 氯仿 (微溶) 、乙酸乙酯 (微溶) 、甲醇 (微溶) |
酸度系数 | 14.72±0.20(Predicted) |
存储条件 | -20°C Freezer |
外观 | 固体 |
颜色 | White to Pale Beige |
体外研究 | Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ). Although Hydroxy Itraconazole is also reported to have antifungal activity in vitro, its pharmacokinetics in humans has been studied less than that of ITZ. ITZ and Hydroxy Itraconazole have a triazole ring and inhibit CYP3A. Their half-lives can be extended by 26-60% with repeated administration compared to single administration. |
体内研究 | The plasma concentration of Hydroxy Itraconazole is weakly dependent on the dose of ITZ, most likely because the process that forms Hydroxy Itraconazole is saturated. Serum albumin and GFR may alter the pharmacokinetics of ITZ and Hydroxy Itraconazole. Antifungal activity should be discussed while taking into account not only the plasma concentration of ITZ but also that of Hydroxy Itraconazole. However, the pharmacokinetics of Hydroxy Itraconazole is similar to that of ITZ in immunocompromised patients taking an oral solution of ITZ. Since the plasma concentrations of ITZ and Hydroxy Itraconazole are closely correlated, determining the plasma concentration of either should be sufficient from a clinical point of view. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.413 ml | 7.066 ml | 14.131 ml |
5 mM | 0.283 ml | 1.413 ml | 2.826 ml |
10 mM | 0.141 ml | 0.707 ml | 1.413 ml |
5 mM | 0.028 ml | 0.141 ml | 0.283 ml |
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