Bupropion Hcl nqe Bupropion Hydrochloride Powder
Cov lus piav qhia ntxaws
Bupropion yog hmoov dawb, crystallized los ntawm isopropyl cawv thiab kiag li ethanol, nrog rau ib tug melting point ntawm 233--234 ° C. Solubility (mg/m1): dej 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Yooj yim heev kom nqus dej noo thiab decompose. Soluble nyob rau hauv methanol, ethanol, acetone, ether los yog benzene. Bupropion belongs rau cov chav kawm aminoketone ntawm antidepressants. Nws yog qhov tsim nyog rau cov neeg mob uas muaj kev nyuaj siab rov qab thiab cov uas tsis muaj txiaj ntsig lossis tsis haum rau lwm cov tshuaj tiv thaiv kev ntxhov siab.
Muaj nuj nqi:
1.Bupropion kuj tseem siv tau los ua kev kho mob los tswj kev mob ntshav siab hyperactivity disorder (ADHD).
2. Bupropion kuj tseem yuav raug siv los ua kev kho mob los pab tib neeg txiav luam yeeb los ntawm kev txo qis kev ntshaw thiab kev tshem tawm nicotine.
3. Bupropion tuaj yeem siv los tiv thaiv lub caij nplooj zeeg-lub caij ntuj no kev nyuaj siab (seasonal affective disorder).
4. Bupropion kuj tseem siv tau nrog lwm cov tshuaj los kho cov kab mob bipolar (mob kev nyuaj siab).
5. Bupropion yog siv los ua tshuaj kho mob rau kev nyuaj siab. Nws tuaj yeem txhim kho kev xav thiab kev xav ntawm kev noj qab haus huv. Nws tuaj yeem ua haujlwm los ntawm kev pab kom rov qab qhov sib npaug ntawm qee yam tshuaj ntuj (neurotransmitters) hauv lub hlwb.
Txoj kev tsim khoom
Hauv kev nplawm thiab txias, ntxiv cov tshuaj o-chlorophenylacetonitrile (688g, 5mol) yaj hauv diethyl ether (2.5L) rau cov tshuaj ethylmagnesium bromide (2L, 3mol / L) hauv 40 feeb. Tshav kub hauv qab maj mam reflux rau 5h. Cov tshuaj tiv thaiv yog hydrolyzed nrog txias dilute hydrochloric acid. Tom qab cov ether tau evaporated, cov tshuaj aqueous ntxiv tau muab rhaub ntawm 90 ° C rau 1 teev. Tom qab txias, ntxiv cov noob siv lead ua. Sau cov khoom los ntawm kev pom, ntxuav nrog dej txias, thiab recrystallize nrog methanol kom tau 750g ntawm o-chloropropiophenone, melting point 39-40 ° C.
Dissolve o-chloropropiophenone (698g, 4.15mmol) hauv dichloromethane (3L). Cov tshuaj yog nplawm nrog activated carbon thiab magnesium sulfate rau 2 teev thiab lim. Ib qho kev daws ntawm 662g (4.15mol) bromine yaj hauv dichloromethane (1L) tau ntxiv nrog nplawm. Thaum cov xim bromine ploj tag, mloog zoo rau hauv lub tshuab nqus tsev kom tshem tawm cov kuab tshuaj. Cov roj ntxiv yog o-chloro-α-bromopropiophenone. Nws tuaj yeem siv ncaj qha rau hauv cov tshuaj tiv thaiv tom ntej yam tsis muaj purification.
Cov roj residue tau txais saum toj no tau yaj hauv acetonitrile (1300 ml), thiab cov tshuaj tert-butylamine (733 g) hauv acetonitrile (1300 ml) tau ntxiv hauv qab 32 ° C. Cia nws thaum hmo ntuj, ntxiv 4200ml dej thiab 2700ml ether rau kev faib tawm. Cov txheej txheem dej tau muab rho tawm nrog 1300 ml ntawm diethyl ether. Tom qab cov txheej txheem ether tau ua ke, 4200 ml ntawm dej tau ntxiv, thiab hydrochloric acid tau ntxiv kom txog thaum Ph nqi ntawm cov dej txheej yog 9. Cov txheej txheej aqueous sib cais tau ntxuav nrog 500 ml ntawm diethyl ether. Cov txheej ether tau ua ke, 560g dej khov thiab 324ml ntawm cov concentrated hydrochloric acid tau ntxiv thiab do ua ke. Cais cov ether txheej thiab ntxuav nrog 200ml dej thiab 50ml concentrated hydrochloric acid. Ob txheej txheej kua qaub kawg tau ua ke, muaj zog hauv lub tshuab nqus tsev kom txog thaum crystallization tshwm sim, thiab tom qab ntawd txias rau 5 ° C. Lim, ntxuav nrog acetone, thiab tom qab ntawd recrystallize nrog kev sib xyaw ntawm 3L isopropyl cawv thiab 800ml kiag li ethanol. Analytically ntshiab thiab spectrally ntshiab DL-bupropion hydrochloride tau txais, nrog ib tug melting point ntawm 233 mus rau 234 ° C.
Pharmacological teebmeem: Bupropion muaj qhov cuam tshuam tsis muaj zog ntawm norepinephrine, 5-HT, thiab dopamine reuptake, tab sis tsis muaj qhov cuam tshuam rau monoamine oxidase.
Kev sib cuam tshuam ntawm cov tshuaj:
1. Cov tshuaj metabolized los ntawm cytochrome P450ⅡB6: Kev sim hauv vitro qhia tias bupropion feem ntau metabolized los ntawm cytochrome P450ⅡB6 isoenzyme, yog li muaj peev xwm cuam tshuam nrog lwm cov tshuaj uas cuam tshuam rau cytochrome P450ⅡB6 isoenzyme.
2. MAO inhibitors: Cov kev tshawb fawb tsiaj tau pom tias monoamine oxidase inhibitor (MAOI) phenelzine tuaj yeem ua rau muaj kev mob toxicity ntawm bupropion.
3. Levodopa: Cov ntaub ntawv kho mob qhia tau hais tias qhov tshwm sim ntawm qhov tshwm sim tsis zoo tuaj yeem nce ntxiv tom qab siv tib lub sijhawm ntawm bupropion thiab levodopa. Cov neeg mob noj levodopa yuav tsum ceev faj thaum noj cov khoom no tib lub sijhawm. Pib nrog qhov tsawg kawg nkaus koob tshuaj thiab tom qab ntawd maj mam nce koob.
4. Cov tshuaj uas txo qis qhov qaug dab peg: Cov khoom no yog ua ke nrog cov tshuaj uas txo qis qhov qaug dab peg (xws li tshuaj tiv thaiv kab mob, tshuaj tiv thaiv kev ntxhov siab, theophylline, kab mob steroids, thiab lwm yam) lossis kev kho mob (xws li kev cuam tshuam ntawm benzodiazepines) ) yuav tsum tau siv ua ke. nrog ceev faj heev.
5. Nicotine transdermal thaj: Cov kev tshawb fawb soj ntsuam pom tau tias kev sib xyaw ua ke ntawm bupropion sustained-tso ntsiav tshuaj thiab nicotine transdermal thaj ua rau muaj kev kub ntxhov siab dua. Yog li ntawd, ntshav siab yuav tsum tau saib xyuas kom zoo rau kev siv ob qho tib si.
Specification
