I-Fosaprepitant dimeglumine / CAS：265121-04-8
Incazelo emfushane:
Igama lomkhiqizo: I-Fosaprepitant dimeglumine
Uhlobo:ZA-N
I-CAS: 265121-04-8
MF:C30H39F7N5O11P
I-MW: 809.63
ISAKHIWO:
incazelo
| Into Yokuhlola | Izindlela Zokwamukela | Umphumela |
| Ukubukeka | Impuphu emhlophe noma engemhlophe | Impuphu emhlophe |
| Ukuncibilika | Lo mkhiqizo uncibilika kalula emanzini kanye ne-methanol, kodwa awuncibiliki ku-ethanol noma i-acetonitrile | Ukuvumelana |
| Ukujikeleza okuqondile | +28.0° kuya ku-＋33.0°
| +31.5°
|
| Ukuhlonza i-UV | Kukhona ukumuncwa okuphezulu kakhulu kuma-wavelength angu-210nm no-263nm | Ukuvumelana
|
| Ukuhlonza kwe-infrared | I-spectrum yokumunca ye-infrared kufanele ihambisane ne-spectrum yento ebhekisele kuyo. | Ukuvumelana
|
| Ukuhlonza i-Chromatographic | Isikhathi sokugcina sencopho eyinhloko yesisombululo sokuhlola kufanele sihambisane nesesixazululo sokubhekisela. | Ukuvumelana
|
| I-Alkalinity | 7.0~9.0 | 7.7 |
| Ukucaca kwesisombululo | Kufanele kucace; Noma yikuphi ukuvuleka okwenziwe akubonakali kakhulu kunokumiswa kwereferensi II | Ukuvumelana
|
| Izinto ezihlobene | Ukungcola A ≤ 0.15% Ukungcola B ≤ 0.1% Ukungcola I3-1 ≤ 0.15% Okunye ukungcola okukodwa ≤ 0.10% Ukungcola okuphelele ≤ 1.0% | 0.08% Akutholakali 0.04% 0.03% 0.15% |
| I-Enantiomer | Akudluli ku-0.15% | Akutholakali |
| Izithasiselo ezisele 1 | I-Methanol ≤3000ppm I-Ethanol ≤5000ppm I-Acetonitrile ≤410ppm I-Ether ≤5000ppm I-Acetone ≤5000ppm I-Methyl tert butyl ether ≤5000ppm I-Toluene ≤890ppm
| 1667ppm 92ppm Akutholakali 54ppm 2636ppm 187ppm Akutholakali
|
| Isinyibilikisi esisele 2 | I-Triethylamine ≤5000ppm
| 58ppm
|
| Okuqukethwe kwamanzi | ≤2.0% | 1.4% |
| Izinsimbi ezisindayo | Akufanele kudlule i-10 ppm | Ukuvumelana |
| I-Palladium | Akudluli ku-5 ppm | Akutholakali |
| I-Chloride | Akufanele kudlule u-0.01% | Ukuvumelana |
| I-Sulfate | Akufanele kudlule u-0.1% | Ukuvumelana |
| I-Meglumine | Ngokwezibalo ezingenamanzi, okuqukethwe yi-C7H17NO5 kufanele kube ngu-37.8% kuya ku-39.8% | 38.5% |
| Ukuhlolwa | Ngokusho kokubala okungenayo i-anhydrous, okuqukethwe yi-C23H22F7N4O6P·2(C7H17NO5) kufanele kube ngu-98.0%~102.0% | 100.4%
|
| I-endotoxin yebhaktheriya | Inani le-endotoxin nge-mg ye-Fosaprepitant Dimeglumine kufanele libe ngaphansi kuka-0.16 EU | Ukuvumelana
|
| Umkhawulo Wezincane | Inani eliphelele lamagciwane asebenza nge-aerobic alidluli ku-100 cfu, inani eliphelele lezikhunta ezihlanganisiwe kanye ne-yeast alidluli ku-50 cfu nge-g ngayinye yesampula yokuhlola kanti i-Escherichia coli ayikho. | Inani eliphelele le-aerobic microbial: 3cfu/g inani eliphelele lezikhunta ezihlanganisiwe kanye nemvubelo:＜10cfu/g I-Escherichia coli: Ayitholakali
|
| Isiphetho | Umkhiqizo uqinisekisa izinga lebhizinisi | |
Ukusetshenziswa
Kunezinhlobo ezintathu zama-neurokinin receptors: i-NK1, i-NK2 kanye ne-NK3. Phakathi kwazo, i-NK1 receptor inekhono eliqine kakhulu lokubopha i-P kanye nokuqukethwe okuphezulu kakhulu esikhungweni sokuhlanza sobuchopho. Ngemva kokuba i-NK1 receptor ibophe i-P ohlelweni lwezinzwa oluphakathi, ibangela uchungechunge lwezinqubo ze-pathophysiological ezifana nokuhlanza, ukukhathazeka kanye ne-migraine. Ama-NK1RA afana ne-apirpitan kanye ne-fosapirpitan avimbela futhi aphathe i-CINV ngempumelelo ngokubopha ngokukhetha i-NK1 receptor. Ngokuvamile, i-CINV ebukhali ihlobene nomsebenzi wendlela yamandla ye-5-HT3 yangaphandle, kuyilapho i-CINV ebambezelekile ihlobene ne-P ephakathi. Ngakho-ke, uma kuqhathaniswa nama-5-HT3RA, i-apirpitan kanye ne-fosapirpitan zibonisa izinzuzo ezisobala zokuhlanza okubambezelekile.
I-Fosapirtan dimethylmeglumine iyi-neurokinin-1receptor antagonist (NK-1RA) eyasungulwa yi-Merck. Yaqala ukwethulwa e-United States ngoJanuwari 2008. I-Fosarpitan dimethylmegalamine iyisidakamizwa esandulela i-aprepitant, umuthi wokuqala we-NK-1RA. Ngemva kokungena emzimbeni, ingaguqulwa ngokushesha ibe yi-aprepitant futhi isetshenziswa ngokwezokwelapha ukuvimbela nokwelapha isicanucanu esibukhali noma esiphuzile kanye nokuhlanza okubangelwa ukusetshenziswa kokuqala nokuphindaphindiwe kwe-chemotherapy ephakathi nendawo kuya ephezulu (kufaka phakathi i-cisplatin enesikali esiphezulu).
Usawoti we-Fosaprepitant dimeglumine (MK-0517) umuthi obangela i-phosphoacyl encibilikayo emanzini we-aprepitant kanye nomphikisi we-NK1.
Ukupakisha Nokuthumela
5kg ，25kg njengezidingo zamakhasimende.
Kungokwempahla evamile futhi kungathunyelwa ngolwandle nangomoya
Gcina futhi ugcine
Isikhathi sokuphila: Izinyanga ezingama-24 kusukela ngosuku lokwenziwa kwento epakishweni lokuqala elingavulwanga, igcinwe endaweni epholile neyomile kude nokukhanya kwelanga okuqondile, amanzi.
Indawo yokugcina izinto enomoya, Ukomisa okuphansi kwezinga lokushisa, Ihlukaniswe nama-oxidants, ama-acid.
