Itraconazole CAS 84625-61-6 Uvavanyo 98.5 ~ 101.5%

I-Itraconazole iqulethe ngaphantsi kweepesenti ze-98.5 kwaye ingabi ngaphezu kwe-101.5 ipesenti ye-C35H38Cl2N8O4, ibalwa kwisiseko esomileyo.
Ukupakishwa kunye nokugcinwa-Londoloza kwizikhongozeli eziqinile, ezikwazi ukumelana nokukhanya, kwaye ugcine kwiqondo lokushisa.
Imigangatho yezalathiso ye-USP <11>-
USP Itraconazole RS
USP Miconazole RS
Isazisi-
A: I-Infrared Absorption <197K>.
Ukujikeleza kwe-Angular <781A>: phakathi kwe -0.10 ° kunye +0.10 °, kulinganiswa kwi-20 °
Isisombululo sovavanyo: 100 mg nge-mL, kwi-methylene chloride
Uluhlu olunyibilikayo <741>: phakathi kwe-166 ° kunye ne-170 °
Ilahleko ekumiseni <731> -Yomisa malunga ne-1 g kwi-105 ° kwiiyure ze-4: ilahlekelwa ngaphezu kwe-0.5% yobunzima bayo.
Intsalela ekutshiseni <281>: hayi ngaphezulu kwe-0.1%, inqunywe kwi-1.0 g.
Iikhompawundi ezinxulumene-
Isisombululo A: 0.08 M tetrabutylammonium hydrogen sulfate.
Isisombululo B: i-acetonitrile
I-Diluent-Lungisa umxube we-methanol kunye ne-tetrahydrofuran (1: 1).
Isisombululo esisemgangathweni-Dibanisa isixa esilinganiswe ngokuchanekileyo se-USP Itraconazole RS kwi-Diluent, i-stepwise ukuba iyimfuneko y, ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-0.05 mg nge-mL.
Isisombululo sesisombululo-Dibanisa ubungakanani obufanelekileyo be-USP Itraconazole RS kunye ne-USP Miconazole kwi-RS kwi-Diluent ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-0.05 mg nganye nge-mL.
Isisombululo sovavanyo-Dibanisa isixa esilinganiswe ngokuchanekileyo se-Itraconazole kwi-Diluent ukufumana isisombululo esinoxinzelelo olwaziwayo malunga ne-10 mg nge-mL nganye.
Inkqubo yeChromatographic (jonga i-Chromatography <621>) -I-chromatograph yolwelo ixhotyiswe nge-225-nm detector kunye ne-4.6-mm × 10-cm ikholomu equlethe i-3- μm yokupakisha i-L1.Izinga lokuhamba malunga ne-1.5 mL ngomzuzu.Ubushushu bekholomu bugcinwa kwi-30 °.Ichromatograph icwangciswe ngolu hlobo lulandelayo
Ixesha Isisombululo Isisombululo B
(imizuzu) (%) (%) Elution
0–20 80→50 20→50 umgca wodidi
20–25 50 50 isokhrasi
25–30 80 20 ulungelelwaniso
[QAPHELA-Lungisa ikholamu ubuncinane imizuzu ye-30 kunye ne-acetonitrile kwisantya sokuhamba kwe-1.5 mL ngomzuzu kwaye emva koko ulungelelanise ukubunjwa kwe-eluent yokuqala ubuncinane imizuzu emi-5.]
I-Chromatograph isisombululo seSigqibo, kwaye urekhode iimpendulo eziphezulu njengoko ziqondiswe kwiNkqubo: isisombululo, R, phakathi kwe-miconazole kunye ne-itraconazole ayikho ngaphantsi kwe-2.0.
Inkqubo-Ngokwahlukileyo tofa imithamo elinganayo (malunga ne-10 µL) yeDiluent, isisombululo soMgangatho kunye nesisombululo soVavanyo kwichromatograph kwaye urekhode iichromatogram.Bala ipesenti yokungahlambuluki ngakunye kwisahlulo se-Itraconazole esithathwe ngefomula:
100(CS / CU)(rU / rS)
apho i-CS igxininiso, kwi-mg nge-mL, ye-Itraconazole kwisisombululo esiPhakathi;I-CU yingqwalasela, kwi-mg nge-mL, ye-Itraconazole kwisisombululo soVavanyo;I-rU yindawo encopho yokungcola ngakunye kwisisombululo soVavanyo;kunye ne-rS yindawo ephakamileyo ye-Itraconazole kwisisombululo esiPhakathi: akukho ngaphezu kwe-0.5% yokungcola okuchaziweyo, njengoko kuboniswe kwiThebhile 1, ifunyenwe;kwaye akukho ngaphezu kwe-1.25% yokungcola okupheleleyo kufunyenwe.Ukungahoyi nayiphi na incopho ebonwe kwi-Diluent kunye nayo nayiphi na incopho engaphantsi kwe-0.05%.
Uluhlu loku-1
Umda wamagama aqhelekileyo (%)
I-4-Methoxy derivative1 0.5
4-Triazolyl isomer2 0.5
Ipropyl analog3 0.5
I-analog ye-Isopropyl4 0.5
Epimer5 0.5
n-Butyl isomer6 0.5
Didioxolanyl analog7 0.5
I-1 2-sec-Butyl-4-{4--[4-(4-methoxyphenyl)piperazin-1-yl]phenyl}-2H-1,2,4-triazol-3(4H)-enye.
2 4-(4-{4-[4-({(2RS,4SR))-2-[(4H-1,2,4-Triazol-4-yl)methyl]-2-(2,4-dichlorophenyl) -1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-sec-butyl-2H-1,2,4-triazol-3(4H)-enye.
3 4-(4-{4--[4-({(2RS,4SR))-2-[(1H-1,2,4-Triazol-1-yl)methyl]-2-(2,4-dichlorophenyl) -1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-propyl-2H-1,2,4-triazol-3(4H)-enye.
4 4-(4-{4-[4-({(2RS,4SR))-2-[(1H-1,2,4-Triazol-1-yl)methyl]-2-(2,4-dichlorophenyl) -1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-isopropyl-2H-1,2,4-triazol-3(4H)-enye.
5 4-(4-{4-[4-({(2 chelating agents. RS,4RS)-2-[(1H-1,2,4-Triazol-1-yl)methyl]-2-(2, 4-dichlorophenyl)-1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-sec-butyl-2H-1,2,4-triazol-3(4H)-enye .
6 4-(4-{4-[4-({(2RS,4SR))-2-[(1H-1,2,4-Triazol-1-yl)methyl]-2-(2,4-dichlorophenyl) -1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-butyl-2H-1,2,4-triazol-3(4H)-enye.
7 4-(4-{4-[4-({(2RS,4SR))-2-[(1H-1,2,4-Triazol-1-yl)methyl]-2-(2,4-dichlorophenyl) -1,3-dioxolan-4-yl}methoxy)phenyl]piperazin-1-yl}phenyl)-2-({(2RS,4SR)-2-[(1H-1,2,4-triazol-1-) yl) methyl] -2- (2,4-dichlorophenyl) -1,3-dioxo-lan-4-yl} methyl) -2H-1,2,4-triazol-3 (4H) -enye.
Isivavanyi-
I-Diluent-Lungisa umxube we-methyl ethyl ketone kunye ne-glacial acetic acid (7: 1).
Inkqubo-Dissolve malunga ne-0.3 g ye-Itraconazole, ilinganiswe ngokuchanekileyo, kwi-70 ml ye-Diluent.I-Titrate kunye ne-0.1 M nge-chloric acid, ukugqiba i-endpoint potentiometrically kwinqanaba lesibini le-inflection.I-mL enye ye-0.1 M nge-chloric acid ilingana ne-35.3 mg ye-C 35H38Cl2N8O4.