GS-441524 tabyog ib yam tshuaj siv los kho feline infectious peritonitis (FIP). Nws yog cov nquag metabolite ntawm dav -spectrum antiviral tshuaj remdesivir. Remdesivir yog ib qho prodrug, uas yuav hloov mus rau hauv cov khoom xyaw nquag GS-441524 tom qab noj los ntawm cov kab mob. Cov tshuaj no Ameslikas muaj nyob rau hauv hmoov daim ntawv thiab yuav tsum tau diluted ua ntej siv. Nyob rau hauv xyoo tas los no, nrog kev nce qib ntawm cov thev naus laus zis, cov ntsiav tshuaj formulations ntawm GS-441524 kuj tau tshwm sim nyob rau hauv kev ua lag luam, thiab nws qhov ntau npaum li cas tuaj yeem xaiv raws li qhov hnyav ntawm tus miv. Feem ntau hais lus, noj ib nrab ib ntsiav tshuaj ib kilogram ntawm lub cev qhov hnyav (12.5mg / kg) ob zaug ib hnub. Rau cov miv uas muaj qhov muag qhov muag (uveitis) lossis cov tsos mob ntawm lub paj hlwb, cov koob tshuaj yuav tsum tau hloov mus rau 12.5-15mg / kg lossis 15-20mg / kg ob zaug ib hnub.
Cov ntsiav tshuaj tuaj yeem siv ncaj qha rau ntawm qhov ncauj, thiab nws raug nquahu kom coj lawv nrog dej ntawm lub plab khoob (tsawg kawg 1 teev ua ntej lossis 2 teev tom qab noj mov). Thaum siv GS441524, nws raug nquahu kom tsis txhob muaj kev sib xyaw ua ke ntawm cov tshuaj alkaline xws li txhuas sulfate ntsiav tshuaj, aluminium hydroxide ntsiav tshuaj, ntsiav tshuaj soda, ntsiav tshuaj sodium bicarbonate, thiab gastric relaxants. Tsis pub dhau 2 teev tom qab noj cov khoom no, tsis txhob noj cov tshuaj antacids, sucralfate lossis polyphenols / cov tshuaj ntxiv uas muaj hlau, zinc, magnesium lossis txhuas los tiv thaiv kev sib cuam tshuam ntawm cov tshuaj thiab ua mob rau miv.
Nyob rau tib lub sijhawm, peb lub tuam txhab tsis tsuas yog muab GS-441524 ntsiav tshuaj, tab sis kuj muaj kev txhaj tshuaj thiab hmoov. Yog tias xav tau, thov koj xav tiv tauj peb txhua lub sijhawm.
GS-441524, Tus nqi tawm! 50% txo!!!
Tom qab lub Hoobkas thib 3 ua tiav thiab muab tso rau hauv kev siv, qhov muag ntim tau nce 3 zaug ntxiv rau 3 lub hlis dhau los.
Txhawm rau kom loj hlob nrog peb cov neeg siv khoom ruaj khov ua ke, peb rov pib dua tus nqi rau GS-441524 FIP series cov khoom, qee yam khoom poob qis dua 50%!
Xws li API (Pure hmoov), OEM / ODM: Txhaj (20mg, 30mg, 40mg), ntsiav tshuaj (25mg, 45mg, 60mg, 70mg) thiab lwm yam.
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Hais Txog Kev Xa Khoom
Ua tiav kev xa khoom thoob plaws ntiaj teb:
GS-441524 hmoov COA
Cov mis mos molecular ntawm GS-441524 yog C12H13N5O4, nrog rau qhov hnyav molecular ntawm 291.27. Nws cov qauv muaj ntau pawg hydroxyl thiab amino functional pawg, uas ua rau tsis tshua muaj solubility nyob rau hauv aqueous tov (li 0.5 mg / mL) thiab rhiab heev rau pH, ua rau nws yooj yim degrade nyob rau hauv acidic tej yam kev mob. Tsis tas li ntawd, nws cov pab pawg nitrile thiab pyrrolotriazine nplhaib qauv tuaj yeem ua rau lub siab toxicity, thiab cov kev mob tshwm sim yuav tsum raug txo los ntawm cov txheej txheem tsim. Yog li ntawd, kev tsim cov ntsiav tshuaj yuav tsum tau daws cov teeb meem hauv qab no:
Optimization ntawm dissolution tus nqi
Txhim kho qhov tso tawm efficiency ntawm cov tshuaj nyob rau hauv lub gastrointestinal ib ntsuj av
Txhim khu kev ruaj ntseg
Tiv thaiv kom tsis txhob degradation ntawm cov khoom xyaw tshuaj nquag thaum khaws cia thiab ua haujlwm
Kev Txhim Kho Bioaccumulation
Txhim kho kev nqus tshuaj los ntawm kev tsim cov ntawv siv tshuaj.
Kev npaj
Ua ntej kev kho mob ntawm cov tshuaj active tshuaj
Purification thiab ziab
Purification ntawm crude GS-441524 siv recrystallization los yog chromatography los xyuas kom meej purity Ntau tshaj los yog sib npaug rau 98%. Qhov kub kom qhuav yuav tsum tau tswj qis dua 40℃kom tsis txhob hydrolysis ntawm nitrile pawg.
granular tswj
Los ntawm kev siv airflow crushing los yog pob milling cov tswv yim, qhov loj me ntawm cov khoom siv raw yog tswj tsis pub dhau D90 Tsawg dua los yog sib npaug li 20 μ m los txhim kho cov ntsiav tshuaj compression kev ua tau zoo thiab kev sib cais.
Kev xaiv thiab kev faib ua feem ntawm cov khoom pabcuam
| Cov khoom siv pab pawg | Mechanism ntawm Action | Pom zoo npaum li cas (zoo piv) |
| Microcrystalline cellulose | Skeleton kev txhawb nqa thiab kev txhawb nqa kev tawg | 30%-50% |
| Croscarmellose Sodium | Superdisintegrants | 5%-10% |
| Hypromellose | Adhesive thiab qeeb -tso hloov kho | 2%-5% |
| Magnesium stearate | roj nplua nyeem | 0.5%-2% |
| Cov ntaub ntawv txheej | Moisture- pov thawj thiab tswm ciab | 3% -5% |
Cov txheej txheem ntub dej granulation
premix
Muab GS-441524, microcrystalline cellulose, thiab cross-linked carboxymethyl cellulose sodium nyob rau hauv kev faib ua feem rau hauv lub tshuab ntub dej granulation thiab sib tov ntawm qis ceev rau 5 feeb.
Granulation
Nrog hydroxypropyl methylcellulose (5% aqueous tov) raws li cov nplaum, tshuaj tsuag granulation yog nqa tawm los ntawm kev txau sab saum toj lossis tangent spraying, thiab lub atomization siab yog tswj ntawm 0.15-0.3 MPa, thiab lub inlet cua kub yog 45-55 degree.
Qhuav thiab tag nrho granules
Qhuav cov khoom nyob rau hauv ib lub txaj fluidized kom txog thaum cov dej noo tsawg dua los yog sib npaug li 3%, thiab tom qab ntawd lim lawv los ntawm 20 mesh sieve kom lawv tag nrho.
Tablet nias thiab txheej
compression
Siv cov ntsiav tshuaj teb xovxwm, lub ntsiab pressing siab yog tswj ntawm 10-15 kN, thiab pre pressing siab yog 5-8 kN, kom ntseeg tau tias qhov sib txawv ntawm cov ntsiav tshuaj hnyav yog tsawg dua los yog sib npaug rau ± 5% thiab lub brittleness yog tsawg dua los yog sib npaug li 1%.
txheej txheej
Siv lub tshuab ntxhua khaub ncaws fluidized, npaj OBA (lossis zoo sib xws zaj duab xis txheej premix) rau hauv ib qho aqueous dispersion nrog cov ntsiab lus ntawm 10% -15%, ua rau cov txheej hnyav nce ntawm 2% -4%.
Kev nyuaj thiab kev daws teeb meem
Teeb meem kev ruaj ntseg
GS-441524 yog nquag degradation nyob rau hauv kub thiab high humidity tej yam kev mob, tsim hydroxyl oxidation khoom.
- cyclodextrin suav nrog thev naus laus zis tuaj yeem siv los npaj cov khoom sib cais los ntawm kev sib xyaw cov ntaub ntawv raw nrog cyclodextrin hauv 1: 1 molar ratio; Ntxiv 0.1% -0.5% antioxidant (xws li BHT) thaum lub sij hawm granulation theem.
Tablet hardness thiab dissolution tus nqi
Kev nce hardness tuaj yeem ua rau txo qis ntawm kev sib cais.
Cov ntsiav tshuaj nias txheej txheem tsis tuaj yeem ua kom zoo los ntawm kev siv segmented compression txoj kev (preloading 5 kN, lub ntsiab siab 12 kN); Ntxiv qis hloov hydroxypropyl cellulose (L-HPC) ua tus txhawb nqa kev tawg.
Kev ncaj ncees ntawm txheej txheej
Cov txheej txheej yog feem ntau tawg los yog tev.
Cov txheej txheem ua kua dej tuaj yeem tswj tau ntawm 12% thiab 15% kom tsis txhob muaj txheej txheej tsis sib xws los ntawm cov viscosity ntau dhau; Ntxiv 0.5% -1% polyethylene glycol 6000 ua plasticizer rau txheej txheej.
Qhov zoo ntawm feline kis kab mob plab
Txoj kev tswj hwm thiab kev ua raws cai
GS-441524 tabyog muab los ntawm qhov ncauj, txo qhov nyuaj ntawm cov txheej txheem kho mob. Piv nrog rau cov tshuaj txhaj tshuaj uas yuav tsum tau txhaj tshuaj txhua hnub, cov ntsiav tshuaj tuaj yeem ua haujlwm los ntawm cov tswv tsiaj hauv tsev, zam kev ntxhov siab rau miv thiab teeb meem hauv kev ua haujlwm los ntawm kev txhaj tshuaj. Piv txwv li, hauv kev kho mob, qee tus miv yuav hnov ntxhiab tsw, lub cev tawv, thiab txawm tias tawv nqaij ulceration vim kev txhaj tshuaj, tab sis kev siv cov ntsiav tshuaj zoo zam cov teeb meem no. Tsis tas li ntawd, daim ntawv ntsiav tshuaj txo qhov zaus ntawm cov miv nrhiav kev kho mob sab nraud, txo qis kev pheej hmoo ntawm tus kab mob khaub thuas, thiab tshwj xeeb tshaj yog haum rau cov miv tsis muaj zog lossis ntxhov siab.
Kev kho mob zoo thiab cov ntaub ntawv kho mob
Ntau qhov kev tshawb fawb soj ntsuam tau lees paub qhov kev kho mob ntawm GS441524 ntsiav tshuaj. Piv txwv li, hauv Taylor thiab al. txoj kev tshawb fawb, ntau dua 80% ntawm 307 FIP miv kho nrog GS441524 los yog remdesivir tau zoo tag nrho cov tshuaj kho, thiab tsuas yog 9% ntawm cov miv tsis teb. Hauv cov kev tshawb fawb tsom rau neuropathic FIP, cov lus teb ntawm GS441524 yog kwv yees li 75%. Cov ntaub ntawv no qhia tias daim ntawv ntsiav tshuaj tuaj yeem ua tiav cov txiaj ntsig kho mob piv rau kev txhaj tshuaj thaum tswj kev siv tshuaj.
Tus neeg siv kev paub thiab kev noj qab haus huv tsiaj
Kev siv cov ntsiav tshuaj ua rau muaj txiaj ntsig zoo rau tsiaj thaum lub sijhawm kho. Cov txheej txheem txhaj tshuaj feem ntau ua rau cov miv mob hnyav, ua rau muaj kev ntshai thiab tsis kam rau lawv cov tswv, thaum cov ntsiav tshuaj zam qhov teeb meem no thiab pab tswj kev sib raug zoo ntawm tib neeg thiab tsiaj. Piv txwv li, cov tswv tsiaj tau tshaj tawm tias tom qab hloov mus rau kev kho cov ntsiav tshuaj, miv tus cwj pwm ntawm lawv cov tswv tau zoo dua, thiab kev ua raws li kev kho mob tau nce ntxiv. Tsis tas li ntawd, cov ntsiav tshuaj txo cov kev ntxhov siab ntawm cov miv vim kev mus ntsib kws kho mob tsis tu ncua, uas pab kho lawv cov kev noj qab haus huv tag nrho.
Tshuaj stability thiab cia tej yam kev mob
GS441524 ntsiav tshuaj muaj qhov zoo hauv kev khaws cia. Kev txhaj tshuaj yuav tsum tau muab tso rau hauv tub yees thiab muaj kev ruaj ntseg tsis zoo tom qab qhib, thaum cov ntsiav tshuaj tuaj yeem khaws cia hauv chav sov kom yooj yim nqa thiab siv. Qhov no tshwj xeeb tshaj yog haum rau cov miv uas xav tau kev kho mob ntev -, txo qhov kev pheej hmoo ntawm kev txo qis vim kev cia tshuaj tsis raug.
Disadvantages ntawm feline kis kab mob plab
Absorption tus nqi thiab bioavailability
Qhov teeb meem ntawm kev nqus tus nqi hauv cov ntsiav tshuaj daim ntawv tseem yog ib qho kev sib tw loj. Thaum cov miv poob qab los noj mov, plab zom mov, lossis mob raws plab, lawv txoj hnyuv nqus tau txo qis, thiab kev ua tau zoo ntawm cov ntsiav tshuaj yuav txo qis heev. Piv txwv li, hauv kev kho mob, qee cov miv muaj kev ua haujlwm tsis zoo ntawm cov ntsiav tshuaj vim muaj teeb meem digestive, thiab thaum kawg yuav tsum tau hloov mus rau kev txhaj tshuaj. Tsis tas li ntawd, bioavailability ntawm cov ntsiav tshuaj yog qis dua qhov kev txhaj tshuaj, thiab nws yuav tsum tau them nyiaj los ntawm kev siv tshuaj ntau ntxiv lossis kho qhov zaus ntawm kev tswj hwm, uas yuav ua rau cov nqi kho mob thiab kev pheej hmoo ntawm cov tshuaj phiv tshuaj.
Scope ntawm daim ntawv thov thiab kab mob txwv
Cov ntsiav tshuaj tsis haum rau txhua rooj plaub FIP. Rau cov miv uas muaj mob hnyav, ntau lub cev tsis ua haujlwm lossis cov tsos mob ntawm lub paj hlwb, kev nqus thiab cov metabolism hauv cov ntsiav tshuaj yuav tsis ua raws li kev kho mob. Piv txwv li, cov kev tshawb fawb tau pom tias cov miv uas muaj cov tsos mob ntawm lub paj hlwb loj heev muaj cov lus teb qis dua rau GS441524 thiab muaj kev pheej hmoo siab dua. Tsis tas li ntawd, rau cov miv uas tsis tuaj yeem noj ntawm nws tus kheej, kev tswj hwm cov ntsiav tshuaj ua rau muaj kev nyuaj siab thiab yuav tsum muaj kev cuam tshuam xws li cov hlab ntsha nasogastric los pab, uas ua rau muaj kev nyuaj siab thiab kev pheej hmoo ntawm kev kho mob.
Nqe thiab Economic Burden
Txawm hais tias cov nqi ntawm cov ntsiav tshuaj tau txo qis piv rau kev txhaj tshuaj, kev kho mob ntev - tseem ua rau cov nqi lag luam ntau dua. Noj ib lub npe ntawm cov ntsiav tshuaj ua piv txwv, tus nqi ntawm ib lub raj mis yog li 400 yuan. Muab xam raws li kev noj txhua hnub, tag nrho cov nqi kho mob (feem ntau yog 12 lub lis piam) tuaj yeem ncav cuag ntau txhiab yuan. Rau cov tsev neeg uas muaj ntau tus miv lossis cov tswv uas muaj kev lag luam tsawg, cov nuj nqis no yuav ua rau lub nra hnyav. Tsis tas li ntawd, kev lag luam tus nqi ntawm cov ntsiav tshuaj hloov pauv tau zoo heev, nrog rau cov nqi sib txawv ntawm cov khoom sib txawv thiab cov lus qhia tshwj xeeb, uas ua rau kom muaj kev nyuaj ntawm kev xaiv.
Tshuaj zoo thiab qhov txaus ntshai
Kev saib xyuas kev ua lag luam ntawmGS-441524 tabtseem tsis tau zoo tag nrho, thiab muaj kev pheej hmoo ntawm cov khoom cuav thiab cov khoom tsis zoo. Qee lub tuam txhab tshuaj tau txais tus kheej- ua cov ntsiav tshuaj ntawm cov ntaub ntawv raw los ntawm kev txhaum cai, thiab lawv cov purity, ntau npaum li cas, thiab kev ruaj ntseg tsis tuaj yeem lav, uas yuav ua rau muaj kev kho mob tsis zoo lossis muaj kev phiv loj heev.
Kev kis tus miv ib txwm yog ib qho kev sib tw loj rau cov tswv miv thiab kws kho tsiaj, nrog nws cov neeg tuag siab ua rau ntau tus miv lub neej muaj kev phom sij. Txawm li cas los xij, nrog kev tshawb nrhiav kev kho mob txuas ntxiv mus, qhov tshwm sim ntawm GS441524 tau ua rau muaj kev cia siab tshiab rau kev kho mob feline. GS441524, raws li cov nquag metabolite ntawm remdesivir, tau pom tias muaj txiaj ntsig zoo hauv kev kho mob plab hnyuv hauv miv, tab sis kuj tseem muaj qee qhov teeb meem uas xav tau kev saib xyuas. Nkag siab txog cov khoom nta ntawm GS-441524 ntsiav tshuaj thiab lawv qhov zoo thiab qhov tsis zoo hauv kev kho cov kab mob feline kis kab mob hauv plab yog qhov tseem ceeb rau kev siv cov tshuaj no thiab txhim kho kev kho mob ntawm feline kis kab mob hauv plab.
Cov lus nug nquag
GS-441524 siv rau dab tsi?
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Feline infectious peritonitis (FIP) yog ib yam kab mob loj heev uas muaj neeg tuag coob heev. GS-441524 yog adenosine analogue uasua raws li ib tug antiviralthiab tau pom cov lus cog tseg hauv kev kho FIP.
Kuv puas tuaj yeem muab kuv tus miv dewormer yam tsis tau mus rau vet?
Thaum dhau -- cov tshuaj dewormers yuav zoo li yooj yim,nws yog qhov zoo tshaj los sab laj nrog kws kho tsiaj. Lawv tuaj yeem pom zoo kom muaj kev nyab xeeb thiab muaj txiaj ntsig kev kho mob raws li koj tus miv cov kev xav tau tshwj xeeb, ua kom muaj kev noj zaub mov kom raug thiab daws txhua yam teeb meem kev noj qab haus huv.
tapeworms puas tuaj yeem nyob ntawm txaj?
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Tapeworms. Cov kab mob no feem ntau kis tau los ntawm kev noj cov dev mub.Yog tias koj tus miv muaj fleas thiab pw hauv koj lub txaj, nws muaj peev xwm ua rau cov kab mob kab mob, uas zoo li cov nplej me me, tuaj yeem xaus rau ntawm koj lub txaj.. Txawm hais tias kev kis ncaj qha mus rau tib neeg tsis tshua muaj, nws tseem muaj kev txhawj xeeb.
Cim npe nrov: gs-441524 ntsiav tshuaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom