Pure Memantine HCl CAS 41100-52-1

Ntshiab memantine HClyog ib qho tshuaj kho dementia tsim los ntawm Merz hauv lub teb chaws Yelemees raws li tshuaj npe 3, 5-Dimethyl-1-aminoadamantane hydrochloride, los yog 3,5-Dimethyltricyclo(3.3.1.1(3.7)) decan -1-amine hydrochloride. Nws muaj cov mis mos molecular C12H21N-HCl thiab molecular hnyav 215.77. Nws yog ib qho tshiab, tsis tshua muaj kev sib raug zoo, voltage-dependent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist uas noncompetitively blocks NMDA receptors thiab txo glutamate induced NMDA receptor hyperexcitability, tiv thaiv apoptosis thiab txhim kho kev nco, nws yog ib qho tshiab. tsim tshuaj los txhim kho kev txawj ntse. Memantine hydrochloride feem ntau yog siv rau kev kho mob me me mus rau qhov hnyav Alzheimer's-hom dementia, uas tuaj yeem txhim kho cov neeg mob hauv kev paub, kev coj cwj pwm, kev kawm, kev nkag siab, thiab kev muaj peev xwm ua txhua hnub, thiab ua rau kev loj hlob ntawm Alzheimer's disease. .

Thaum Lub Ob Hlis 2002, nws tau pom zoo los ntawm European Committee rau Patented Medicinal Products (CPMP) rau kev kho mob ntawm cov neeg mob uas muaj tus kab mob nruab nrab mus rau Alzheimer's mob hnyav, thiab thaum Lub Yim Hli ntawm tib lub xyoo, nws tau tsim tawm hauv Tebchaws Yelemees, thiab thaum Lub Kaum Hli 17, 2003. , nws tau pom zoo los ntawm US Food and Drug Administration (FDA) rau kev kho mob ntawm cov neeg mob uas muaj tus kab mob nruab nrab mus rau mob Alzheimer's. Cov kev tshawb fawb ntxiv tau pom tias Memantine HCl kuj tseem siv tau rau cov neeg mob uas muaj tus kab mob me me mus rau nruab nrab Alzheimer's disease. Alzheimer's disease (AD), tseem hu ua senile dementia, yog ib yam kab mob ntawm cov neeg laus, feem ntau tshwm sim los ntawm kev nco tsis tau thiab kev paub tsis meej, thiab lwm yam. Nws yog ib qho mob neurodegenerative degenerative. Tam sim no, cholinesterase inhibitors (donepezil, carboplatin, galantamine) thiabNtshiab memantine HClraug pom zoo rau kev kho mob Alzheimer's disease.

Ntshiab memantine HClFeem ntau yog siv los kho dementia hauv Alzheimer's disease (AD), tshwj xeeb tshaj yog mob hnyav rau Alzheimer's-type dementia. Nws yog ib qho tshiab, tsis tshua muaj kev sib raug zoo, voltage-dependent, tsis sib tw N-methyl-D-aspartate (NMDA) receptor antagonist, uas muaj peev xwm txo tau glutamate-induced NMDA receptor hyperexcitability thiab tiv thaiv apoptosis los ntawm kev tsis sib tw thaiv ntawm NMDA receptor, yog li txhim kho kev nco.

Tsis tas li ntawd, Memantine HCl kuj tuaj yeem siv rau kev kho mob Parkinson's disease lossis Parkinson's syndrome, thiab lwm yam. Txawm li cas los xij, Memantine HCl tsis haum rau txhua yam mob. Cov neeg uas muaj mob qaug dab peg thiab ua rau muaj mob vwm, cov neeg uas muaj keeb kwm ntawm convulsions, lub raum tsis txaus, me me mus rau nruab nrab hepatic insufficiency, cov neeg mob uas muaj kev puas siab puas ntsws loj, nrog rau cov neeg mob plawv yuav tsum tau ceev faj txog kev siv cov tshuaj no. Nws tseem yog contraindicated nyob rau hauv cov neeg uas muaj kev tsis haum tshuaj rau lub active ingredient ntawm cov khoom los yog nws excipients, raws li zoo raws li nyob rau hauv cov neeg uas muaj mob hepatic insufficiency.

Muaj ob qhov tshwj xeeb siv: Memantine hcl 5 mg thiab memantine hcl 10 mg.

Kev ua tau zoo ntawmMemanine HCl

 

 

Thawj qhov kev ua tau zoo ntawm Memantine HCl yog rau kev kho mob ntawm qhov mob hnyav mus rau Alzheimer's hom dementia. Nws yog ib qho tsis sib tw NMDA receptor antagonist uas tuaj yeem ua los ntawm kev hloov pauv glutamate. Glutamate yog ib qho tseem ceeb neurotransmitter nyob rau hauv lub hlwb uas muaj feem xyuam nrog kev nco, kev kawm thiab kev txawj ntse muaj nuj nqi. Hauv cov neeg mob Alzheimer's disease, glutamate overactivity tuaj yeem ua rau muaj kev puas tsuaj rau neuronal thiab ua haujlwm tsis zoo.

Cov teebmeem tseem ceeb ntawm Memantine hydrochloride tau sau tseg hauv qab no:

1

Tiv thaiv neurons

Los ntawm antagonizing NMDA receptors, Memantine HCl tuaj yeem txo qis glutamate-induced hyperexcitability, yog li tiv thaiv cov neurons los ntawm kev puas tsuaj thiab pab kom qeeb ntawm kev loj hlob ntawm tus kab mob.

2

Txhim kho kev txawj ntse

Memantine HCl txhim kho cov neeg mob kev paub txog kev ua haujlwm, suav nrog kev nco, kev saib xyuas, kev txiav txim siab, thiab kev txawj daws teeb meem. Qhov no pab cov neeg mob ua lub neej txhua hnub thiab kev sib raug zoo.

3

Txo cov tsos mob puas hlwb

Alzheimer's kab mob feem ntau cuam tshuam nrog cov tsos mob ntawm kev puas siab puas ntsws xws li kev ntxhov siab thiab kev nyuaj siab, thiab Memantine HCl txhim kho cov tsos mob thiab lub neej zoo rau cov neeg mob.

4

Kev ncua ntawm kev loj hlob ntawm tus kab mob

Los ntawm kev txhim kho neuronal muaj nuj nqi thiab txo cov tsos mob ntawm kev puas siab puas ntsws, Memantine HCl pab ncua kev loj hlob ntawm Alzheimer's kab mob, yuav cov neeg mob ntau lub sij hawm rau kev kho mob.

Ntshiab memantine HCltau tsim los ntawm xya txoj hauv kev tseem ceeb, thiab cov hauv qab no yog cov lus tseem ceeb ntawm txoj kev hluavtaws los ntawm txoj kev acetonitrile.

(1)1-Bromo-3,5-dimethyladamantane tau los ntawm kev hloov 1,3-dimethyladamantane nrog bromine.

(2) Tom qab ntawd acetamidated kom tau txais 1-acetamido-3, 5-dimethyladamantane.

(3) Hydrolyzed nyob rau hauv alkaline tej yam kev mob.

(4) Acidification rau ntsev, Memantine HCl.

Catalyst thiab kub yog ob yam tseem ceeb hauv kev sib txuas ntawm Memantine HCl los ntawm txoj kev acetonitrile. Catalyst feem ntau yog siv los txhawb cov tshuaj tiv thaiv tus nqi thiab nce cov txiaj ntsig thiab purity ntawm cov khoom. Rau txoj kev acetonitrile, cov concentrated sulfuric acid feem ntau yog siv los ua cov catalyst vim nws tuaj yeem txhawb cov tshuaj tiv thaiv amidation.

Raws li qhov kub thiab txias, nws cuam tshuam rau tus nqi ntawm cov tshuaj tiv thaiv thiab qhov zoo ntawm cov khoom. Nyob rau hauv tus txheej txheem ntawm synthesizing Memantine HCl los ntawm acetonitrile txoj kev, qhov kub ntawm cov tshuaj tiv thaiv yuav tsum tau tswj xyuas kom meej tias cov tshuaj tiv thaiv yuav ua tau smoothly, thiab nyob rau tib lub sij hawm kom tsis txhob kub dhau heev lawm ua rau tshwm sim ntawm sab kev tshwm sim. Qhov tshwj xeeb cov tshuaj tiv thaiv kub yuav txawv raws li cov tshuaj tiv thaiv tshwj xeeb thiab cov khoom siv raw siv, yog li nws yuav tsum tau hloov kho raws li qhov kev sim hauv kev ua haujlwm tiag tiag.

Tsis tas li ntawd, cov ntsiab lus hauv qab no yuav tsum tau muab sau tseg thaum lub sij hawm synthesis:

• Qhov zoo thiab purity ntawm cov ntaub ntawv raw muaj kev cuam tshuam zoo rau qhov zoo thiab cov txiaj ntsig ntawm cov khoom kawg, yog li cov khoom siv raw khoom zoo yuav tsum tau xaiv.
• Thaum lub sij hawm cov txheej txheem tshuaj tiv thaiv, lub sij hawm cov tshuaj tiv thaiv thiab cov tshuaj tiv thaiv tej yam kev mob yuav tsum tau nruj me ntsis tswj xyuas kom meej lub tiav ntawm cov tshuaj tiv thaiv thiab purity ntawm cov khoom.
• Rau cov khoom siv khib nyiab, cov kua khib nyiab thiab cov khoom khib nyiab tsim tawm, kev kho tsim nyog yuav tsum tau ua kom tsis txhob muaj kev puas tsuaj rau ib puag ncig thiab tib neeg lub cev.

Nws yuav tsum raug sau tseg tias txawm hais tias txoj kev acetonitrile yog ib txoj hauv kev zoo rau kev sib txuas ntawmMemantine HCl, tej zaum nws yuav tsum tau hloov kho thiab kho kom zoo raws li qhov xwm txheej tshwj xeeb hauv kev xyaum.

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