Nerve-Targeting Afoxolaner thiab Milbemycin Oxime Chewable Tablets

Thaum cov kab mob nkag mus rau koj tus dev lub cev, lawv tsim cov kev sib txuas ntawm cov neural uas tso cai rau lawv noj, yug me nyuam, thiab muaj sia nyob. Nkag siab txog li cas cov kws kho tsiaj niaj hnub no cuam tshuam cov tes hauj lwm no qhia txog kev tshawb fawb zoo tom qab tswj cov kab mob parasite zoo. Kab lus no tshawb txog cov txheej txheem neurological meej los ntawm qhov ntawdAfoxolaner thiab Milbemycin Oxime Chewable Tabletstshem tawm cov kab mob sab hauv thiab sab nraud, muab kev tiv thaiv zoo rau cov neeg koom nrog thoob ntiaj teb.

Afoxolaner Thiab Milbemycin Oxime Chewable Tablets

1. General Specification (hauv Tshuag)
(1) API (Ntshiab hmoov)
(2) Tablet
9.375+1.875mg: 2-3.5 kg
18.75+3.75mg: 3.5-7.5kg
37.5+7.5mg:＞7.5-15kg
75+15mg:＞15-30kg
150+30mg: 30-60kg
(3) Ointment
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
PIB: BM-2-117
Lub khw tseem ceeb: Tebchaws Asmeskas, Australia, Brazil, Nyiv, Lub Tebchaws Yelemees, Indonesia, UK, New Zealand, Canada thiab lwm yam.
Chaw tsim tshuaj paus: BLOOM TECH Xi'an Hoobkas

Parasites 'cov paj hlwb txawv ntawm cov tsiaj txhu', uas txhais tau hais tias kev xaiv yuav siv tau rau hauv txoj kev ntse. Afoxolaner thiab Milbemycin Oxime Chewable Tablets coj kom zoo dua ntawm cov kev sib txawv no los ntawm kev ntaus cov hlab ntsha hauv ob txoj hauv kev uas tua kab mob thaum ua kom cov dev muaj kev nyab xeeb.

Selective Neural Intervention hauv Arthropods

Cov kab mob sab nraud xws li dev mub, zuam, thiab mites muaj lub hlwb tshwj xeeb uas nyob ntawm glutamate-gated chloride channels thiab gamma-aminobutyric acid (GABA) receptors. Cov paj hlwb uas tswj kev txav mus los, pub mis, thiab kev yug me nyuam yog tswj los ntawm cov sensors no. Afoxolaner txuas tshwj xeeb heev rau GABA-gated chloride channels thaum nws nkag mus rau hauv lub paj hlwb ntawm ib qho invertebrate. Qhov kev khi no nres cov tshuaj chloride ions los ntawm kev txav ib txwm hla cov paj hlwb ntawm cov hlab ntsha, uas ua rau cov hlab ntsha tawg tsis muaj kev tswj hwm. Cov kab mob cab cov hlab ntsha ua rau tsis muaj peev xwm rov pib dua, uas ua rau nws dhau los ua neeg tuag tes tuag taw, thiab thaum kawg tuag hauv cov xuab moos tom qab raug nthuav tawm.

Neuromuscular Disruption nyob rau hauv Internal Parasites

Cov kab mob plawv thiab lub plab nematodes yog cov piv txwv ntawm cov kab mob sab hauv uas ua haujlwm los ntawm kev sib txawv neural. Milbemycin oxime, uas yog tsim los ntawm ob qho tib si A3 thiab A4 qhov chaw, lub hom phiaj glutamate-gated chloride channels uas tsuas yog pom nyob rau hauv cov hlab ntsha thiab cov leeg hlwb ntawm cov pob txha pob txha. Nws yog thaum milbemycin oxime qhib cov channel uas cov membrane permeability nce los ntawm cov nyiaj loj. Qhov no overpolarization nres cov paj hlwb los ntawm kev mus ncig ib txwm, uas txwv tsis pub cov cab mus. Cov kab mob no raug pov tseg los ntawm cov txheej txheem ntuj tsim vim tias lawv tsis tuaj yeem nyob hauv ib qho chaw hauv tus tswv tsev lossis khaws pub noj.

Mammalian Kev Nyab Xeeb Los Ntawm Kev Tiv Thaiv Kab Mob

Hauv dev, cov ntshav- lub hlwb thaiv yog ib qho tseem ceeb heev tiv thaiv cov tshuaj no.Afoxolaner thiab Milbemycin Oxime Chewable Tablets100 lub sij hawm ntau zog khi rau GABA receptors nyob rau hauv arthropods tshaj rau receptors nyob rau hauv cov tsiaj. Ib yam li ntawd, milbemycin oxime muaj qhov permeability tsawg heev nyob rau hauv cov ntshav - hlwb thaiv hauv dev. Kev tshawb fawb ntawm nws qhov kev sib kis qhia tau hais tias nws tsuas yog ib feem nkag mus rau hauv nruab nrab paj hlwb. Cov tshuaj pharmacokinetic no ua kom paub tseeb tias cov koob tshuaj kho tau tshem tawm cov kab mob kom zoo thaum khaws cov npoo kev nyab xeeb uas ua rau tus tswv tsev tsis tau txais cov kev mob tshwm sim neurological.

 

Kev sib xyaw ua ke muab kev tiv thaiv kev sib koom ua ke los ntawm kev tsom ntau hom kab mob los ntawm cov txheej txheem ua haujlwm ua ke. Txhua yam khoom xyaw ua haujlwm ntawm nws tus kheej, tab sis ua ke lawv pab tshem tawm tag nrho cov kab mob.

Isoxazoline Mechanism ntawm Afoxolaner

Afoxolaner yog ib qho tshuaj tua kab isoxazoline thiab acaricide, uas yog ib qho kev txhim kho tshiab hauv kev kho tsiaj cov kab mob parasitology. Cov tshuaj no ua nws txoj haujlwm los ntawm kev thaiv GABA-gated chloride channels hauv kab. Kev kuaj mob qhia tau tias afoxolaner nce mus txog qib siab tshaj plaws hauv cov ntshav hauv ob mus rau plaub teev tom qab tau txais, thiab tias nws yog bioavailable tag nrho (88% ntawm lub sijhawm). Qhov ntev dua ib nrab-lub neej hauv plasma, uas yog kwv yees li ob lub lis piam, ua kom muaj kev tiv thaiv rau tag nrho lub hlis ntawm koob tshuaj. Cov tshuaj pharmacokinetic profile no ua kom paub tseeb tias cov tshuaj kho tau nyob siab hauv cov hlab ntsha. Qhov no ua rau cov dev kho qhov chaw tuag rau cov kab mob kom sim daws thiab noj.

Kev Ua Haujlwm Macrolide ntawm Milbemycin Oxime

Cov tshuaj no, milbemycin oxime, yog ib tug macrolide anthelmintic. Nws cov qauv zoo ib yam li lwm cov tshuaj avermectin, tab sis nws muaj kev nyab xeeb dua. Nws muaj 80% milbemycin A4 thiab 20% milbemycin A3, uas yog ob qho tib si tshuaj uas ua haujlwm ntawm glutamate-gated chloride channels. Cov kab no feem ntau pom muaj nyob rau hauv lub paj hlwb peripheral ntawm cov leeg tsis muaj zog, tsis nyob hauv lawv lub hauv nruab nrab lub paj hlwb. Milbemycin A4 muaj ib nrab -lub neej ntawm 3.3 hnub, raws li kev tshawb fawb, thaum milbemycin A3 muaj ib nrab - lub neej ntawm 1.6 hnub. Cov qib sib txawv ntawm qhov kev pheej hmoo no ua kom ntseeg tau tias kev tiv thaiv tsis muaj zog ua haujlwm tawm tsam cov kab mob sib txawv ntawm lawv lub neej.

 

Qhov no yog qhov tseem ceeb tshwj xeeb rau kev txwv tsis pub cov kab mob plawv ua ntej lawv tig mus rau cov kab mob laus.

Parasites tau tsim ntau txoj hauv kev kom ciaj sia, yog li yuav tsum muaj kev tiv thaiv tshwj xeeb. Qhov teeb meem no yog daws tau los ntawm dual - nquag muaj pes tsawg leeg, uas ua haujlwm tawm tsam ntau yam kab mob parasite.

Spectrum Kev Pabcuam Thoob Ntiaj Teb Parasite

Tsis pub dhau plaub teev ntawm tus dev noj cov ntsiav tshuaj uas noj tau, fleas pib hnov ​​​​mob rau afoxolaner, thiab lawv tag nrho ploj mus li ntawm yim teev. Ticks uas pub rau cov dev kho mob muaj teeb meem nrog lawv cov hlab ntsha uas txwv tsis pub lawv nyob nrog thiab ua tiav lawv cov ntshav noj. Cov kev tshawb fawb tau ua nyob rau hauv daim teb qhia tias nws yog 100% zoo tiv thaiv kab mob xws li Dermacentor variabilis thiab Rhipicephalus sanguineus rau ib hlis tom qab nws tau thov. Nyob rau tib lub sijhawm, milbemycin oxime nres lub plawv lub qe qe (Dirofilaria immitis) uas kis tau los ntawm yoov tshaj cum los ntawm kev txav mus rau hauv cov hlab ntsha hauv lub ntsws, qhov chaw uas lawv yuav loj hlob mus rau cov neeg laus muaj kab mob txaus ntshai uas tuaj yeem tua tau.

Milbemycin oxime tuaj yeem ua rau tuag tes tuag taw cov leeg ntawm cov kab mob uas nyob hauv cov hnyuv, xws li cov kab mob hookworms, roundworms, thiab whipworms.

Kev Tiv Thaiv Kev Tiv Thaiv Los Ntawm Dual Mechanisms

Thaum ib zaug -hom- ntawm- cov tshuaj ua haujlwm tau siv ntau dua thiab dhau ntawm tib cov kab mob parasite, lawv tuaj yeem tsim kev kam rau siab. Txoj kev sib xyaw ua ke txo qis qhov kev pheej hmoo ntawm kev tawm tsam los ntawm kev ua kom cov kab mob tsim kev tiv thaiv tawm tsam ob lub hom phiaj sib txawv ntawm tib lub sijhawm. Cov kev hloov pauv hauv cov noob uas ua rau koj tiv taus GABA channel inhibitors tsis tiv thaiv koj ntawm glutamate channel activators, thiab lwm yam.

txawm nyob rau hauv qhov chaw uas cov kab mob parasite tau dhau los ua tsis tshua muaj tshuaj lom neeg laus.

Lub neej -Kev Ua Haujlwm Zoo Tshaj Plaws

Thaum lub sij hawm lawv lub neej, cov kab mob sib txawv tawm ntawm cov tswv tsev sib txawv qhib rau kev hem txawv.Afoxolaner thiab Milbemycin Oxime Chewable Tabletscov neeg laus fleas ua ntej lawv nteg qe. Qhov no txwv tsis pub cov dev mub los ntawm kev tsim thiab ua rau ib puag ncig. Nyob rau hauv lub qhov rais tseem ceeb thaum lawv feem ntau yuav cuam tshuam los ntawm macrolides, milbemycin oxime tsom rau cov kab mob plawv tshwj xeeb. Lub neej no- theem tshwj xeeb muaj feem cuam tshuam rau cov kab mob cab thaum xav tau qhov tsawg kawg nkaus ntawm cov koob tshuaj kom zoo.

Kev tshawb fawb ntawm molecular pharmacology qhia tau hais tias cov tshuaj no txuas nrog qee cov qauv protein kom tua kab mob.

Chloride Channel Modulation

Thaum kawg, ob qho khoom xyaw nquag hloov pauv cov chloride ions, tab sis lawv ua li ntawd los ntawm kev sib txawv receptor systems. Afoxolaner blocks GABA receptors yam tsis muaj kev sib tw nrog lawv, noj cov chaw sib txuas uas txwv tsis pub ua haujlwm neurotransmitter. Qhov kev thaiv no tau tshem tawm cov lus uas feem ntau tswj cov neural excitation, uas ua rau cov hlab ntsha tawg tsis muaj kev tswj hwm. Milbemycin oxime ua haujlwm ua tus agonist ntawm glutamate receptors, uas ua rau cov channel qhib dav dua thiab cia cov tshuaj chloride ntau dhau lawm.

Receptor Selectivity thiab Binding Affinity

Cov kev tshawb fawb Crystallography qhia tau hais tias afoxolaner haum rau GABA receptor binding hnab ris ntawm arthropods nrog geometric alignment uas ploj lawm hauv hom tsiaj receptors. Qhov sib txawv ntawm cov amino acid residues nyob rau hauv invertebrate thiab mammalian receptor subtypes ua rau cov tshuaj no muaj peev xwm. Tsis tas li ntawd, glutamate-gated chloride channels yog ib hom receptors uas tsuas pom muaj nyob hauv cov tsiaj txhu thiab tsis nyob hauv cov tsiaj. Cov dev tsis muaj lub hom phiaj receptors, uas piav qhia vim li cas kev kuaj kev nyab xeeb tau pom qhov ntsuas kev kho dav dav.

Pharmacodynamic Profiles

Cov koob tshuaj - teb cov duab rau ob yam tshuaj qhia qhov sib txawv ntawm qhov lawv ua haujlwm zoo li cas.Thaum cov ntshav ntshav siab tshaj 500 ng/mL, afoxolaner tua 95% ntawm fleas, thiab cov qib no nyob twj ywm tib lub sijhawm ntawm kev noj tshuaj txhua hli ntawm cov koob tshuaj pom zoo. Qhov kev txiav txim ntawm milbemycin oxime tawm tsam cov kab mob nematodes uas raug cuam tshuam los kuj tseem yog qhov tseem ceeb- nyob ntawm, thiab cov nqi qis tshaj plaws uas tau txais txiaj ntsig tau khaws cia rau ob peb hnub. Cov tshuaj pharmacodynamic no ua kom paub tseeb tias qhov kev tiv thaiv tsis tu ncua thiab tsis muaj zog ntau dua ua ntej koob tshuaj ntxiv.

Los ntawm kev sib cuam tshuam ntawm molecular mus rau qhov tseeb tshem tawm cov kab mob, muaj ntau yam kev lom neeg uas yuav tsum tau ua. Cov kauj ruam no tig receptor khi rau hauv cov txiaj ntsig kho mob.

Absorption thiab Distribution Dynamics

Thaum noj los ntawm qhov ncauj, Afoxolaner thiab Milbemycin Oxime Chewable Tablets tau nrawm nrawm los ntawm lub cev lub plab zom mov. Daim ntawv chewable pab txhim kho kev nqus los ntawm kev txhawb kev yeem haus dej haus raws li saj thiab los ntawm kev txhim kho txoj kev uas cov tshuaj yaj. Cov afoxolaner nkag mus rau hauv ntau cov ntaub so ntswg (ntau dua 2.6 L / kg), ua kom paub tseeb tias cov qib kho tau mus txog ntawm daim tawv nqaij, qhov twg cov kab mob sab nraud nyob thiab pub. Milbemycin oxime kuj mus rau qhov chaw uas muaj kab mob nyob hauv, xws li lub plab mucosa thiab cov hlab ntsha.

Cov qauv ntawm kev faib tawm no ua rau muaj cov tshuaj nquag hauv kev sib cuag nrog cov kab mob parasites, txawm tias lawv nyob qhov twg ntawm lub cev.

Metabolic Stability thiab tshem tawm

Ob yam tshuaj raug rhuav tshem hauv daim siab los ntawm cytochrome P450 txoj hauv kev, tsim cov khoom lag luam uas tsis muaj zog. Cov tshuaj niam txiv nyob hauv lub cev ntev txaus los tiv thaiv txhua lub hlis, tab sis thaum kawg lawv tawg kom tsis txhob muaj tshuaj lom. Txoj hauv kev tseem ceeb uas cov pov tseg raug tshem tawm yog los ntawm cov quav, tsuas yog ib qho me me nkag mus rau hauv lub raum. Qhov kev tshem tawm no ua rau cov neeg muaj mob raum lossis cov laus tsis tshua txhawj xeeb txog lawv lub raum noj qab haus huv.

Kev kho mob ua tau zoo nyob rau hauv tiag -Cov xwm txheej hauv ntiaj teb

Kev ntsuam xyuas kev cuam tshuam hauv teb chaws tau ua nyob rau hauv ntau qhov chaw hauv thaj chaw rov qab txog yam uas tau pom hauv chav kuaj. Fleas yog 99.9% tsawg dua ntawm cov dev uas tau kho ib hlis ib zaug nrog cov khoom sib tov dua li cov dev uas tsis kho. Kev tiv thaiv kab mob plawv tau ua haujlwm 100% ntawm lub sijhawm nyob rau hauv qhov chaw uas lawv tau tshwm sim thaum kev kho mob pib ua ntej lub caij yoov tshaj cum thiab txuas ntxiv txhua hli thaum lub sijhawm sib kis. Cov txiaj ntsig no los ntawm lub ntiaj teb tiag rov qab los ntawm kev paub txog kev siv tshuab uas tau txais los ntawm kev kawm.

Txoj kev ntawdAfoxolaner thiab Milbemycin Oxime Chewable Tabletsua hauj lwm rau lub hom phiaj ntawm lub paj hlwb yog ib qho piv txwv ntawm yuav ua li cas cov kab mob parasitology siab heev yuav siv tau nyob rau hauv tiag tiag - lub neej veterinary tshuaj. Qhov no ob lub mis- nquag tiv thaiv tawm tsam ob qho tib si sab nraud arthropods thiab sab hauv helminths los ntawm kev ua kom zoo dua ntawm qhov sib txawv ntawm lub paj hlwb ntawm cov kab mob thiab cov tsiaj txhu. Selective receptor binding, zoo pharmacokinetics, thiab complementary mechanisms ntawm kev txiav txim tag nrho ua hauj lwm ua ke los ua kom muaj kev tiv thaiv txhua hli yooj yim rau cov tswv dev kom tso siab rau.

Cov neeg ua haujlwm kho tsiaj thiab cov tswv tsiaj tuaj yeem txiav txim siab zoo dua txog yuav ua li cas tshem cov kab mob thaum lawv nkag siab txog kev tshawb fawb tom qab paj hlwb- tsom rau cov tshuaj tiv thaiv kab mob. Raws li cov kab mob cab txuas ntxiv hloov pauv hauv cov lus teb rau cov kev ntxhov siab sab nraud thiab cov khoom qub qub, cov khoom tshiab zoo li no tseem ua haujlwm los ntawm kev ntaus lawv ntau txoj hauv kev, uas sai dua li lawv tuaj yeem tiv taus.

Bloomtechz yog ib lub tuam txhab tsim nyog uas tsim thiab muag siab -zoo Afoxolaner thiab Milbemycin Oxime Chewable Tablets. Lawv muaj 12 xyoo ntawm kev paub ua tshuaj intermediates thiab kho cov tshuaj synthesis. Peb 100,000-square-meter GMP- cov chaw muaj ntawv pov thawj tau ua tiav ntawm - qhov chaw tshuaj xyuas los ntawm CFDA, US-FDA, PMDA, thiab lwm lub koom haum tswj hwm thoob ntiaj teb. Qhov no ua kom paub tseeb tias txhua batch ua tau raws li cov qauv zoo tshaj plaws. Peb tuaj yeem ua txhua yam ntawm cov ntsiav tshuaj, los ntawm cov hmoov API ntshiab kom tiav cov ntsiav tshuaj chewable, thiab peb tuaj yeem ua rau lawv hauv txhua qhov hnyav. Peb kuj muab kev hloov pauv OEM / ODM kev xaiv kom peb tuaj yeem ua tau raws li koj qhov kev tshawb fawb thiab kev faib khoom xav tau.

24 thoob ntiaj teb cov tuam txhab tshuaj thiab cov chaw tshawb fawb ntseeg peb ua tus khub. Peb muab cov nqi sib tw nrog qhov tseeb ruaj khov - cov qauv paj, cov sij hawm ua cov hmoov txhuas raug taug qab los ntawm peb lub ERP platform, thiab triple - txheej txheej zoo uas lav tag nrho cov nyiaj rov qab rau txhua yam khoom uas tsis ua raws li cov qauv. Peb pawg kws tshaj lij ua kom paub tseeb tias kev sib txuas lus yog qhov tseeb thiab cov saw hlau muab kev tswj hwm zoo, txawm tias koj xav tau ntau npaum li cas rau kev lag luam lossis cov qauv tsim tshwj xeeb rau kev siv tshwj xeeb.

Koj puas tau npaj los nrhiav qhov chaw ntseeg siab rau kojAfoxolaner thiab Milbemycin Oxime Chewable Tabletsxav tau? Email peb pab neeg ntawmSales@bloomtechz.comtam sim no los tham txog koj cov kev xav tau, tau txais cov ntaub ntawv ntxiv, lossis tau txais cov lus sib tw. Bloomtechz muab koj qhov zoo tshaj plaws uas koj xav tau thiab cov kev pabcuam zoo uas koj xav tau kev lag luam.

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2. Prichard R, Ménez C, Lespine A. Moxidectin thiab avermectins: Consanguinity tab sis tsis yog tus kheej. International Journal for Parasitology: Tshuaj thiab Tshuaj Tiv Thaiv . 2012; 2:134-153.

3. Bowman DD, Ohmes CM, Hendershot KL, et al. Kev ua tau zoo ntawm afoxolaner tawm tsam Rhipicephalus sanguineus thiab Dermacentor variabilis ntawm cov dev. Veterinary Parasitology. 2015;213(1-2):37-40.

4. Rufener L, Danelli V, Bertrand D, Sager H. Tus tshiab isoxazoline ectoparasiticide fluralaner: Selective inhibition of arthropod gamma-aminobutyric acid- thiab L-glutamate-gated chloride channels thiab insecticides. Kab Biochemistry thiab Molecular Biology. 2017; 45: 111-124.

5. European Medicines Agency. NexGard Spectra EPAR - Kev Sib Tham Txog Kev Tshawb Fawb. Pawg Neeg Saib Xyuas Kev Noj Qab Haus Huv rau Kev Ntsuas Kev Siv Tshuaj Kho Mob . 2015.

6. Wolstenholme AJ, Rogers AT. Glutamate-gated chloride channels thiab hom kev ua ntawm avermectin/milbemycin anthelmintics. Parasitology . 2005; 131 (Suppl): S85-S95.