I-Itraconazole CAS 84625-61-6 Assay 98.5~101.5%

I-Itraconazole iqukethe amaphesenti angekho ngaphansi kwamaphesenti angu-98.5 futhi angabi ngaphezu kwamaphesenti angu-101.5 we-C35H38Cl2N8O4, abalwe ngesisekelo esomisiwe.
Ukupakisha nokugcina-Londoloza ezitsheni eziqinile, ezimelana nokukhanya, futhi ugcine endaweni yokushisa.
Amazinga ereferensi we-USP <11>-
USP Itraconazole RS
USP Miconazole RS
Ukuhlonza-
A: I-Infrared Absorption <197K>.
Ukuzungezisa i-angular <781A>: phakathi kuka--0.10° no-+0.10°, kukalwa ngo-20°
Isixazululo sokuhlola: 100 mg ngemL ngayinye, ku-methylene chloride
Ibanga lokuncibilika <741>: phakathi kuka-166° no-170°
Ukulahlekelwa ekumisweni <731>-Yomisa cishe i-1 g ku-105 ° amahora angu-4: ilahlekelwa ngaphezu kuka-0.5% wesisindo sayo.
Izinsalela ekushiseni <281>: hhayi ngaphezulu kuka-0.1%, kunqunywa ku-1.0 g.
Izinhlanganisela ezihlobene-
Isixazululo A: 0.08 M tetrabutylammonium hydrogen sulfate.
Isixazululo B: i-acetonitrile
I-Diluent-Lungisa ingxube ye-methanol ne-tetrahydrofuran (1:1).
Isixazululo esijwayelekile-Chaza isamba esikalwe ngokunembile se-USP Itraconazole RS ku-Diluent, ngokwesinyathelo uma kudingeka y, ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-0.05 mg nge-mL ngayinye.
Isixazululo sokuxazulula-Chaza amanani afanelekile e-USP Itraconazole RS kanye ne-USP Miconazole ku-RS ku-Diluent ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-0.05 mg ngayinye nge-mL.
Isixazululo sokuhlola-Chaza inani elinembile lesisindo se-Itraconazole ku-Diluent ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-10 mg nge-mL ngayinye.
Isistimu ye-Chromatographic (bona i-Chromatography <621>)-I-chromatograph ewuketshezi ifakwe umtshina ongu-225-nm kanye nekholomu engu-4.6-mm × 10-cm equkethe 3- μm ukupakisha L1.Izinga lokugeleza licishe libe ngu-1.5 mL ngomzuzu.Ukushisa kwekholomu kugcinwa ku-30 ​​°.Ichromatograph ihlelwe kanje
Isixazululo Sesikhathi Isixazululo B
(amaminithi) (%) (%) I-Elution
0–20 80→50 20→50 igradient yomugqa
20–25 50 50 isokhrasi
25–30 80 20 ukulinganisa
[QAPHELA-Linganisa ikholomu okungenani imizuzu engama-30 nge-acetonitrile ngesilinganiso sokugeleza esingu-1.5 mL ngomzuzu bese ulinganisa ekubunjweni kokuqala okucacile okungenani imizuzu emi-5.]
I-Chromatograph ikhambi Lokuxazululwa, futhi urekhode izimpendulo eziphezulu njengoba kuqondiswe kuNqubo: ukulungiswa, R, phakathi kwe-miconazole ne-itraconazole akukhona ngaphansi kuka-2.0.
Inqubo-Ngokuhlukile jova amavolumu alinganayo (cishe u-10 µL) we-Diluent, isixazululo esijwayelekile kanye nesixazululo sokuhlola ku-chromatograph futhi urekhode ama-chromatogram.Bala iphesenti lokungcola ngakunye engxenyeni ye-Itraconazole ethathwe ifomula:
100(CS / CU)(rU / rS)
lapho i-CS iwukugxila, ngo-mg nge-mL ngayinye, ye-Itraconazole kusixazululo Esijwayelekile;I-CU ukuhlushwa, ngo-mg ngemL ngayinye, ye-Itraconazole kusixazululo sokuhlola;I-rU iyindawo ephakeme kakhulu yokungcola ngakunye kusixazululo sokuhlola;futhi i-rS iyindawo ephakeme kakhulu ye-Itraconazole kusixazululo Esijwayelekile: akutholakali ngaphezu kuka-0.5% wanoma yikuphi ukungcola okucacisiwe, njengoba kuboniswe kuThebula 1, kutholakala;futhi akukho ngaphezu kwe-1.25% yokungcola okuphelele okutholakele.Ziba noma yikuphi ukuphakama okubonwe ku-Diluent nanoma yikuphi ukuphakama okungaphansi kuka-0.05%.
Ithebula 1
Umkhawulo Wegama Elivamile (%)
I-4-Methoxy derivative1 0.5
I-4-Triazolyl isomer2 0.5
I-analog ye-Propyl3 0.5
I-Isopropyl analog4 0.5
I-Epimer5 0.5
n-Butyl isomer6 0.5
I-Didioxolanyl analog7 0.5
1 2-sec-Butyl-4-{4-[4-(4-methoxyphenyl)piperazin-1-yl]phenyl}-2H-1,2,4-triazol-3(4H)-one.
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)-one.
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)-one.
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)-one.
5 4-(4-{4-[4-({(2 ama-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)-one .
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)-one.
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) -one.
Isivivinyo-
I-Diluent-Lungiselela ingxube ye-methyl ethyl ketone ne-glacial acetic acid (7:1).
Inqubo-Chaza cishe u-0.3 g we-Itraconazole, ulinganiswe ngokunembile, ku-70 ml we-Diluent.Titrate ngo-0.1 M nge-chloric acid ngayinye, inquma iphoyinti lokugcina nge-potentiometrically endaweni yesibili yokuguquguquka.I-mL eyodwa ka-0.1 M nge-chloric acid ngayinye ilingana no-35.3 mg we-C 35H38Cl2N8O4.