I-Fosaprepitant dimeglumine / CAS：265121-04-8
Inkcazo emfutshane:
Igama lemveliso: iFosaprepitant dimeglumine
Uhlobo:ZA-N
I-CAS: 265121-04-8
MF:C30H39F7N5O11P
I-MW: 809.63
ULWAKHIWO:
iinkcukacha
| Into yoVavanyo | Iikhrayitheriya zoKwamkelwa | Isiphumo |
| Inkangeleko | Umgubo omhlophe okanye omhlophe qhwa | Umgubo omhlophe |
| Ukunyibilika | Le mveliso inyibilika lula emanzini nakwi-methanol, kodwa ayinyibiliki kwi-ethanol okanye kwi-acetonitrile | Ukuvumelana |
| Ujikelezo oluthile | +28.0° ukuya kuthi ga＋33.0°
| +31.5°
|
| Ukuchongwa kwe-UV | Kukho ukufunxwa okuphezulu kwii-wavelengths ze-210nm kunye ne-263nm | Ukuvumelana
|
| Ukuchongwa kwe-infrared | I-spectrum yokufunxa ye-infrared kufuneka ihambelane ne-spectrum yento ebhekisa kuyo | Ukuvumelana
|
| Ukuchongwa kweChromatographic | Ixesha lokugcina incopho ephambili yesisombululo sovavanyo kufuneka lihambelane nelo lesisombululo esibhekisayo | Ukuvumelana
|
| I-Alkalinity | 7.0~9.0 | 7.7 |
| Ukucaca kwesisombululo | Kufuneka kucace; Naluphi na uhlobo lwe-opalescence oluveliswayo alubonakali ngaphezu kolu lwe-reference suspension II | Ukuvumelana
|
| Izinto ezinxulumene noko | Ubumdaka A ≤ 0.15% Ubumdaka B ≤ 0.1% Ubumdaka I3-1 ≤ 0.15% Ezinye izinto ezingcolisayo ezingenanto ≤ 0.10% Ukungcola okupheleleyo ≤ 1.0% | 0.08% Ayibonwanga 0.04% 0.03% 0.15% |
| I-Enantiomer | Akudluli kwi-0.15% | Ayibonwanga |
| Izinyibilikisi eziseleyo 1 | I-Methanol ≤3000ppm I-Ethanol ≤5000ppm I-Acetonitrile ≤410ppm I-Ether ≤5000ppm I-acetone ≤5000ppm I-Methyl tert butyl ether ≤5000ppm IToluene ≤890ppm
| 1667ppm 92ppm Ayibonwanga 54ppm 2636ppm 187ppm Ayibonwanga
|
| Isinyibilikisi esiseleyo 2 | I-Triethylamine ≤5000ppm
| 58ppm
|
| Umthamo wamanzi | ≤2.0% | 1.4% |
| Iintsimbi ezinzima | Akufuneki idlule kwi-10 ppm | Ukuvumelana |
| I-Palladium | Akudluli kwi-5 ppm | Ayibonwanga |
| I-chloride | Akufuneki idlule kwi-0.01% | Ukuvumelana |
| I-Sulfate | Akufuneki idlule kwi-0.1% | Ukuvumelana |
| I-Meglumine | Ngokwendlela yokubala engenamanzi, umxholo we-C7H17NO5 kufuneka ube phakathi kwe-37.8% ukuya kwi-39.8% | 38.5% |
| Uvavanyo | Ngokwendlela yokubala engenamanzi, umxholo we-C23H22F7N4O6P·2(C7H17NO5) kufuneka ibe yi-98.0%~102.0% | 100.4%
|
| I-endotoxin yebhaktheriya | Ubungakanani be-endotoxin kwi-mg nganye yeFosaprepitant Dimeglumine kufuneka bube ngaphantsi kwe-0.16 EU | Ukuvumelana
|
| Umda weeMicrobial | Inani lilonke leentsholongwane ezisebenza nge-aerobic alikho ngaphezulu kwe-100 cfu, inani lilonke lee-molds kunye ne-yeast ezidibeneyo alikho ngaphezulu kwe-50 cfu kwi-g nganye yesampulu yovavanyo kwaye i-Escherichia coli ayikho. | I-aerobic microbial iyonke: 3cfu/g inani lilonke leemibungu kunye negwele ezidityanisiweyo:＜10cfu/g I-Escherichia coli: Ayifumaneki
|
| Isiphelo | Imveliso iqinisekisa umgangatho weshishini | |
Ukusetyenziswa
Kukho iintlobo ezintathu zee-neurokinin receptors: i-NK1, i-NK2 kunye ne-NK3. Phakathi kwazo, i-NK1 receptor inamandla okubopha kakhulu kwi-P kunye nomxholo ophezulu kwiziko lokugabha lobuchopho. Emva kokuba i-NK1 receptor ibophelele kwi-P kwinkqubo ye-nervous ephakathi, ibangela uthotho lweenkqubo ze-pathophysiological ezifana nokuhlanza, ixhala kunye ne-migraine. Ii-NK1RA ezifana ne-apirpitan kunye ne-fosapirpitan zithintela kwaye zinyange i-CINV ngokufanelekileyo ngokubophelela ngokukhetha kwi-NK1 receptor. Ngokwesiqhelo, i-acute CINV inxulumene nomsebenzi wendlela yamandla e-peripheral 5-HT3, ngelixa i-CINV ebambezelekileyo inxulumene ne-P ephakathi. Ke ngoko, xa kuthelekiswa ne-5-HT3RAs, i-apirpitan kunye ne-fosapirpitan zibonisa iingenelo ezicacileyo zokuhlanza okubambezelekileyo.
I-Fosapirtan dimethylmeglumine yi-neurokinin-1receptor antagonist (NK-1RA) eyenziwe yiMerck. Yaqalwa ukuqaliswa eMelika ngoJanuwari 2008. I-Fosarpitan dimethylmegalamine liyeza eliphambili le-aprepitant, iyeza lokuqala le-NK-1RA. Emva kokungena emzimbeni, inokuguqulwa ngokukhawuleza ibe yi-aprepitant kwaye isetyenziselwa ukuthintela nokunyanga isicaphucaphu esibukhali okanye esilibazisekileyo kunye nokuhlanza okubangelwa kukusetyenziswa kokuqala nokuphindaphindiweyo kwe-chemotherapy ephakathi ukuya kwephezulu ye-emetogenic (kubandakanya i-cisplatin enedosi ephezulu).
Ityuwa yeFosaprepitant dimeglumine (MK-0517) sisiyobisi esisandula ukunyibilika emanzini se-aprepitant kunye ne-NK1 antagonist.
Ukupakishwa kunye nokuthunyelwa
5kg ，25kg njengeemfuno zabathengi.
Yeyokwempahla eqhelekileyo kwaye inokuhanjiswa ngolwandle nangomoya
Gcina kwaye ugcine
Ixesha lokuphelelwa: Iinyanga ezingama-24 ukususela kumhla wokwenziwa kwayo kwiphakheji yokuqala engavulwanga igcinwe kwindawo epholileyo neyomileyo kude nelanga elithe ngqo, amanzi.
Indawo yokugcina umoya, Ukomisa kubushushu obuphantsi, Yahlulwe kwii-oxidants, ii-asidi.
