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Bupropion Hcl farashin Bupropion Hydrochloride Foda
Cikakken Bayani
Bupropion wani farin foda ne, crystallized daga isopropyl barasa da cikakken ethanol, tare da ma'anar narkewa na 233--234 ° C. Solubility (mg/m1): ruwa 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Mai sauqi don sha danshi da rugujewa. Mai narkewa a cikin methanol, ethanol, acetone, ether ko benzene. Bupropion na cikin nau'in aminoketone na antidepressants. Ya dace da marasa lafiya da ke fama da rashin ƙarfi da kuma waɗanda ba su da tasiri ko rashin haƙuri ga sauran magungunan antidepressants.
Aiki:
1.Bupropion kuma za a iya amfani da shi azaman magani don sarrafa rashin kulawa da rashin ƙarfi (ADHD).
2. Hakanan za'a iya amfani da Bupropion azaman magani na likitanci don taimakawa mutane su daina shan taba ta hanyar rage sha'awar jima'i da tasirin nicotine.
3. Ana iya amfani da Bupropion don hana damuwa na yanayi na kaka-hunturu (cututtukan yanayi na yanayi).
4. Hakanan za'a iya amfani da Bupropion tare da wasu magunguna a matsayin magani ga cututtukan bipolar (lokacin damuwa).
5. Ana amfani da Bupropion azaman magani na likitanci don damuwa. Zai iya inganta yanayi da jin daɗin rayuwa. Yana iya aiki ta hanyar taimakawa wajen dawo da ma'auni na wasu sinadarai na halitta (neurotransmitters) a cikin kwakwalwa.
Hanyoyin samarwa
A ƙarƙashin motsawa da sanyaya, ƙara maganin o-chlorophenylacetonitrile (688g, 5mol) a cikin diethyl ether (2.5L) zuwa maganin ethylmagnesium bromide (2L, 3mol/L) a cikin minti 40. Yi zafi a ƙarƙashin reflux mai laushi don 5h. Maganin amsawa ya kasance mai ruwa da ruwa tare da ruwan sanyi mai tsarma hydrochloric acid. Bayan da aka fitar da ether, sauran maganin ruwa ya kasance mai zafi a 90 ° C na awa 1. Bayan sanyaya, ƙara iri crystal. Tattara daskararrun ta hanyar tacewa, a wanke da ruwan sanyi, sannan a sake yin recrystallize da methanol don samun 750g na o-chloropropiophenone, wurin narkewa 39-40°C.
Narke o-chloropropiophenone (698g, 4.15mmol) a cikin dichloromethane (3L). An zuga maganin tare da kunna carbon da magnesium sulfate na 2 hours kuma tace. Maganin 662g (4.15mol) bromine da aka narkar da a dichloromethane (1L) an ƙara tare da motsawa. Lokacin da launin bromine ya ɓace gaba ɗaya, mayar da hankali a cikin injin motsa jiki don cire sauran ƙarfi. Sauran man shine o-chloro-a-bromopropiophenone. Ana iya amfani da shi kai tsaye a cikin amsa ta gaba ba tare da tsarkakewa ba.
An narkar da ragowar mai da aka samu a sama a cikin acetonitrile (1300 ml), kuma an ƙara maganin tert-butylamine (733 g) a cikin acetonitrile (1300 ml) a ƙasa da 32 ° C. Bar shi cikin dare, ƙara 4200ml ruwa da 2700ml ether don rarrabawa. An fitar da ruwa mai ruwa tare da 1300 ml na diethyl ether. Bayan da aka haɗa nau'in ether, an ƙara 4200 ml na ruwa, kuma an ƙara hydrochloric acid har sai da darajar Ph na ruwa ya kasance 9. An wanke ruwan da aka raba da ruwa tare da 500 ml na diethyl ether. An haɗu da yadudduka na ether, 560g na kankara da 324ml na maida hankali hydrochloric acid an ƙara kuma an zuga su tare. A raba ether Layer kuma wanke da ruwa 200ml da 50ml maida hankali hydrochloric acid. An haɗu da yadudduka na acid guda biyu na ƙarshe, an tattara su a cikin vacuo har sai crystallization ya bayyana, sa'an nan kuma sanyaya zuwa 5 ° C. Tace, wanke da acetone, sa'an nan kuma recrystallize da cakuda 3L isopropyl barasa da 800ml cikakkar ethanol. An samo DL-bupropion hydrochloride mai tsafta da tsaftataccen tsafta, tare da ma'aunin narkewa na 233 zuwa 234°C.
Magungunan ilimin likitanci: Bupropion yana da tasirin hanawa mai rauni a kan norepinephrine, 5-HT, da dopamine reuptake, amma ba shi da irin wannan tasiri akan monoamine oxidase.
Mu'amalar magunguna:
1. Drugs metabolized by cytochrome P450ⅡB6: In vitro gwaje-gwaje nuna cewa bupropion aka yafi metabolized ta cytochrome P450ⅡB6 isoenzyme, don haka akwai yuwuwar mu'amala da wasu kwayoyi da suka shafi cytochrome P450ⅡB6 isoenzyme.
2. Masu hana MAO: Nazarin dabba sun nuna cewa mai hanawa na monoamine oxidase (MAOI) phenelzine zai iya ƙara yawan guba na bupropion.
3. Levodopa: Bayanan asibiti sun nuna cewa abubuwan da suka faru na mummunan halayen na iya karuwa bayan amfani da bupropion da levodopa lokaci guda. Marasa lafiya masu shan levodopa yakamata suyi taka tsantsan yayin shan wannan samfurin a lokaci guda. Fara tare da mafi ƙarancin kashi sannan a hankali ƙara adadin.
4. Magungunan da ke rage ƙofa na katsewa: An haɗa wannan samfurin tare da magungunan da ke rage ƙofa (kamar antipsychotics, antidepressants, theophylline, steroids na tsarin, da dai sauransu) ko hanyoyin kwantar da hankali (kamar katsewar benzodiazepines kwatsam) )) ya kamata a yi amfani dasu tare tare. tare da taka tsantsan.
5. Nicotine transdermal patch: Nazarin asibiti sun nuna cewa haɗuwa da amfani da bupropion ci gaba da sakewa da allunan da aka yi da nicotine transdermal patch yana da babban abin da ya faru na hawan jini na gaggawa na gaggawa. Saboda haka, ya kamata a kula da hawan jini sosai don haɗuwa da amfani da biyun.
Ƙayyadaddun bayanai
