中文名 | 磷氟康唑 |
英文名 | Fosfluconazole |
别名 | 磷康唑 氟氟康唑 磷氟康唑 福司氟康唑 福斯氟康唑杂质 磷氟康唑(福司氟康唑) 2-(2,4-二氟苯基)-1,3-二(1H-1,2,4-三氮唑-1-基)丙基二氢磷酸酯 |
英文别名 | Prodif Procif CS-969 UK-292,663 Fosfluconazole UNII-3JIJ299EWH Fosfluconazole(INN) Dihydrogen phosphate ester 2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propyl dihydrogen phosphate 2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-yl dihydrogen phosphate PHARMA PRODUCT FLUCONAZOLE USP 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1,2,4-TRIAZOL-1-YL) PROPAN-2-OL 2,4-Difluoro-alpha,alpha-bis(1H-1,2,4-triazol-1-ylmethyl)benzyl alcohol, dihydrogen phosphate (ester) 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-((1H-1,2,4-triazol-1-yl)methyl)ethyl dihydrogen phosphate 1H-1,2,4-Triazole-1-ethanol, α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-ylmethyl)-, 1-(dihydrogen phosphate) |
CAS | 194798-83-9 |
EINECS | 1312995-182-4 |
化学式 | C13H13F2N6O4P |
分子量 | 386.25 |
InChI | InChI=1/C13H13F2N6O4P/c14-10-1-2-11(12(15)3-10)13(25-26(22,23)24,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9H,4-5H2,(H2,22,23,24) |
密度 | 1.70±0.1 g/cm3(Predicted) |
熔点 | 223-224° |
沸点 | 701.5±70.0 °C(Predicted) |
闪点 | 378.1°C |
蒸汽压 | 1.18E-20mmHg at 25°C |
折射率 | 1.683 |
酸度系数 | 1.44±0.10(Predicted) |
存储条件 | 2-8℃ |
体外研究 | To investigate the polarized bioconversion and the Transwell transport of phosphate prodrugs in Caco-2 monolayer, 10 μM Fosfluconazole or Fosphenytoin is dosed either in the apical or basal compartment in Transwell plates. Both prodrugs are efficiently cleaved in the apical compartment after a 2 h incubation. To further investigate the kinetics of ALP-mediated bioconversion, the concentration-dependent ALP-mediated bioconversions are conducted to determine the Michaelis-Menten constant (K m ) of prodrug bioconversion in Caco-2 monolayers. The saturation curves of Fosphenytoin and Fosfluconazole with the concentration increase are found. The estimated K m values of Fosphenytoin and Fosfluconazole are 1160 and 357 μM, respectively. |
体内研究 | The apparent half-life for Fosfluconazole bioconversion in intestinal mucosa scraps is 10 min. Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study are to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ is administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ is detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration is lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations are analyzed using a two-compartment model in which the distribution volume of the peripheral compartment is fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.589 ml | 12.945 ml | 25.89 ml |
5 mM | 0.518 ml | 2.589 ml | 5.178 ml |
10 mM | 0.259 ml | 1.294 ml | 2.589 ml |
5 mM | 0.052 ml | 0.259 ml | 0.518 ml |