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Bupropion Hcl qiimaha Bupropion Hydrochloride budada
Sharaxaad faahfaahsan
Bupropion waa budo cad, oo laga soo saaray aalkolada isopropyl iyo ethanol dhammaystiran, oo leh barta dhalaalaysa 233--234 ° C. Solubility (mg/m1): biyaha 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Aad bay u fududahay in la nuugo qoyaanka iyo burburka. Ku milmay methanol, ethanol, acetone, ether ama benzene. Bupropion waxaa iska leh qaybta aminoketone ee daawada niyad-jabka. Waxay ku habboon tahay bukaanada qaba niyad-jabka iyo kuwa aan waxtar lahayn ama u dulqaadan karin daawooyinka kale ee niyadjabka.
Shaqada:
1.Bupropion waxa kale oo loo isticmaali karaa daawaynta si loo maareeyo feejignaanta yaraanta firfircoonida (ADHD).
2. Bupropion waxa kale oo loo isticmaali karaa daawaynta dhakhtar qoray si dadka looga caawiyo joojinta sigaarka iyadoo la dhimayo rabitaanka iyo saamaynta nikotiinta.
3. Bupropion waxaa loo isticmaali karaa si looga hortago niyad-jabka xilliga dayrta-jiilaalka (xilliyeedka xanuunka).
4. Bupropion waxa kale oo loo isticmaali karaa dawooyin kale sida daawaynta xanuunka laba-cirifoodka (wajiga niyad-jabka).
5. Bupropion waxa loo isticmaalaa daawaynta daawaynta ee niyad jabka. Waxay wanaajin kartaa niyadda iyo dareenka fayoobida. Waxaa laga yaabaa inay shaqeyso iyadoo gacan ka geysaneysa soo celinta dheelitirka kiimikooyinka dabiiciga ah qaarkood (neurotransmitters) ee maskaxda.
Hababka wax soo saarka
Marka la walaaqayo iyo qaboojinta, ku dar xal o-chlorophenylacetonitrile (688g, 5mol) oo ku milmay diethyl ether (2.5L) xalka ethylmagnesium bromide (2L, 3mol/L) 40 daqiiqo gudahood. Kuleylka hoostiisa dib-u-kicinta 5 saac. Xalka falcelinta waxaa lagu shubay hydrochloric acid badhax qabow. Ka dib markii ether-ku uumi baxay, xalka aqueous ee soo hadhay ayaa lagu kululeeyay 90 ° C 1 saac. Ka dib qaboojinta, ku dar crystal abuurka. Ku ururi adkaha adigoo sifeynaya, ku maydh biyo qabow, oo ku celi methanol si aad u hesho 750g oo o-chloropropiophenone, barta dhalaalka 39-40°C.
Ku milaan o-chloropropiophenone (698g, 4.15mmol) ee dichloromethane (3L). Xalka waxaa lagu walaaqay kaarboon firfircoon iyo magnesium sulfate 2 saacadood oo la sifeeyay. Xalka 662g (4.15mol) bromine oo lagu milmay dichloromethane (1L) ayaa lagu daray walaaq. Marka midabka bromine uu si buuxda u baaba'o, xooga saar meel faaruq ah si aad uga saarto dareeraha. Saliida soo hadhay waa o-chloro-a-bromopropiophenone. Waxaa si toos ah loo isticmaali karaa falcelinta soo socota iyada oo aan la nadiifin.
Hadhaaga saliidda leh ee kor ku xusan waxaa lagu milmay acetonitrile (1300 ml), iyo xal tert-butylamine (733 g) ee acetonitrile (1300 ml) ayaa lagu daray ka hooseeya 32 ° C. Iska daa habeenkii, ku dar 4200ml oo biyo ah iyo 2700ml ether si loo qaybiyo. Lakabka aqueous waxaa lagu soo saaray 1300 ml oo ah diethyl ether. Ka dib marka la isku daro lakabyada etherka, 4200 ml oo biyo ah ayaa lagu daray, iyo hydrochloric acid ayaa lagu daray ilaa qiimaha Ph ee lakabka biyuhu uu ahaa 9. Lakabka aqueous ee la soocay ayaa lagu dhaqay 500 ml oo ah ether diethyl. Lakabyada ether-ka ayaa la isku daray, 560g oo baraf ah iyo 324ml oo ah hydrochloric acid ayaa lagu daray oo la isku daray. Kala saar lakabka etherka oo ku maydh 200ml oo biyo ah iyo 50ml hydrochloric acid. Labadii lakab ee ugu dambeeyay ayaa la isku daray, waxaa lagu uruuriyay vacuo ilaa ay ka soo baxday crystallization, ka dibna la qaboojiyey ilaa 5°C. Sifee, ku dhaq acetone, ka dibna ku celi isku dar ah 3L isopropyl aalkolo iyo 800ml ethanol buuxda. DL-bupropion hydrochloride lafagur ahaan saafi ah iyo muuqaal saafi ah ayaa la helay, iyada oo barta dhalaalaysa 233 ilaa 234°C.
Saamaynta dawooyinka: Bupropion waxay leedahay saameyn daciif ah oo ka hortag ah oo ku saabsan norepinephrine, 5-HT, iyo dib u soo celinta dopamine, laakiin wax saameyn ah kuma laha monoamine oxidase.
Isdhexgalka daroogada:
1. Daawooyinka ay metabolized by cytochrome P450ⅡB6: In vitro Tijaabooyinku waxay muujinayaan in bupropion ay inta badan metabolized by cytochrome P450ⅡB6 isoenzyme, sidaas darteed waxaa jira isdhexgalka suurtagalka ah ee daawooyinka kale ee saameeya cytochrome P450ⅡB6 isoenzyme.
2. MAO inhibitors: Daraasadaha xayawaanku waxay muujiyeen in monoamine oxidase inhibitor (MAOI) phenelzine ay kordhin karto sunta daran ee bupropion.
3. Levodopa: Xogta caafimaadku waxay muujinaysaa in dhacdooyinka falcelinta xun ay kordhin karaan ka dib isticmaalka isku mar ee bupropion iyo levodopa. Bukaan-socodka qaadanaya levodopa waa in ay taxaddaraan marka ay qaadanayaan alaabtan isku mar. Ka bilow qiyaasta ugu yar ka dibna si tartiib tartiib ah u kordhi qiyaasta.
4. Daawooyinka hoos u dhiga heerka qalalka: Alaabtan waxaa lagu daraa dawooyinka hoos u dhigaya heerka qalalka (sida antipsychotics, antidepressants, theophylline, steroids systemic, iwm) ama daawaynta (sida joojinta degdega ah ee benzodiazepines) ) iyadoo taxadar badan.
5. Nikotiinka transdermal patch: Daraasadaha kiliinikada waxay soo jeedinayaan in isticmaalka wadajirka ah ee kiniiniyada sii-deynta bupropion iyo nicotine transdermal patch ay leedahay dhacdo sare oo ah hypertension daweynta degdega ah. Sidaa darteed, cadaadiska dhiigga waa in si dhow loola socdo isticmaalka wadajirka ah ee labada.
Tilmaamid
