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Bupropion Hcl igiciro Bupropion Hydrochloride Ifu
Ibisobanuro birambuye
Bupropion ni ifu yera, ikozwe muri alcool ya isopropyl na Ethanol yuzuye, hamwe no gushonga ya 233--234 ° C. Gukemura (mg / m1): amazi 312, Ethanol 193, 0.1mol / L hydrochloric aside 333. Biroroshye cyane gukuramo ubuhehere no kubora. Gukemura muri methanol, Ethanol, acetone, ether cyangwa benzene. Bupropion iri mubyiciro bya aminoketone ya antidepressants. Irakwiriye abarwayi bafite ihungabana ridindira hamwe nabadakora neza cyangwa kutihanganira izindi miti igabanya ubukana.
Imikorere ：
1.Bupropion irashobora kandi gukoreshwa nkumuti wo gukemura ikibazo cya hyperactivite defisit (ADHD).
2. Bupropion irashobora kandi gukoreshwa nkumuti wandikirwa kugirango ufashe abantu kureka itabi bagabanya irari ningaruka zo kwikuramo nikotine.
3. Bupropion irashobora gukoreshwa kugirango wirinde kwiheba-igihe cyizuba (ibihe byigihe).
4. Bupropion irashobora kandi gukoreshwa nindi miti nkumuti wa bipolar disorder (icyiciro cya depression).
5. Bupropion imenyerewe nkubuvuzi bwandikiwe kwiheba. Irashobora kunezeza no kwiyumvamo ubuzima bwiza. Irashobora gukora ifasha kugarura uburinganire bwimiti imwe n'imwe (neurotransmitters) mubwonko.
Uburyo bwo gukora
Mugihe cyo gukurura no gukonjesha, ongeramo igisubizo cya o-chlorophenylacetonitrile (688g, 5mol) yashonga muri diethyl ether (2.5L) kugirango gikemurwe na bromide ya Ethylmagnesium (2L, 3mol / L) muminota 40. Shyushya munsi yoroheje ya 5h. Igisubizo cya hydrolyz hamwe na acide hydrochloric ikonje. Ether imaze guhumeka, igisubizo cyamazi gisigaye cyashyutswe kuri 90 ° C kumasaha 1. Nyuma yo gukonjesha, ongeramo imbuto kristu. Kusanya ibikomeye ukoresheje kuyungurura, koza n'amazi akonje, hanyuma usubiremo methanol kugirango ubone 750g ya o-chloropropiophenone, gushonga 39-40 ° C.
Kuramo o-chloropropiophenone (698g, 4.15mmol) muri dichloromethane (3L). Umuti washyizwe hamwe na karubone ikora na magnesium sulfate mumasaha 2 hanyuma uyungurura. Umuti wa 662g (4.15mol) bromine yashonga muri dichloromethane (1L) wongeyeho hamwe no gukurura. Iyo ibara rya bromine ryacitse burundu, shyira mu cyuho kugirango ukureho umusemburo. Amavuta asigaye ni o-chloro-α-bromopropiophenone. Irashobora gukoreshwa muburyo butaziguye reaction itaha.
Ibisigazwa by'amavuta byabonetse haruguru byashongeshejwe muri acetonitrile (1300 ml), hanyuma igisubizo cya tert-butylamine (733 g) muri acetonitrile (1300 ml) kongerwaho munsi ya 32 ° C. Kureka ijoro ryose, ongeramo 4200ml amazi na 2700ml ether kugirango ukwirakwizwe. Igice cyamazi cyakuwe hamwe na ml 1300 ya diethyl ether. Nyuma ya ether imaze guhuzwa, hongewemo ml 4200 yamazi, hanyuma aside hydrochloric yongerwamo kugeza igihe Ph agaciro k’amazi y’amazi kari 9. Igice cy’amazi cyatandukanijwe cyogejwe hamwe na ml 500 ya diethyl ether. Ibice bya ether byahurijwe hamwe, 560g bya barafu na 324ml ya acide hydrochloric yibanze byongewemo hamwe. Tandukanya ether hanyuma ukarabe n'amazi 200ml na acide hydrochloric 50ml yibanze. Ibice bibiri bya nyuma bya acide byahujwe, byibanda muri vacuo kugeza kristalisation igaragara, hanyuma bikonja kugeza kuri 5 ° C. Shungura, oza hamwe na acetone, hanyuma wongere usubiremo uruvange rwa 3L isopropyl alcool na 800ml etanol yuzuye. Isesengura ryera kandi ryera DL-bupropion hydrochloride yabonetse, hamwe no gushonga 233 kugeza 234 ° C.
Ingaruka za farumasi: Bupropion igira intege nke zo kubuza norepinephrine, 5-HT, na dopamine reuptake, ariko nta ngaruka nkizo kuri okiside ya monoamine.
Imikoreshereze yibiyobyabwenge:
1. Ibiyobyabwenge byahinduwe na cytochrome P450ⅡB6: Mu bushakashatsi bwa vitro bwerekana ko bupropion ikoreshwa cyane na cytochrome P450ⅡB6 isoenzyme, bityo hakaba hari imikoranire ishobora kuba hamwe nibindi biyobyabwenge bigira ingaruka kuri cytochrome P450ⅡB6 isoenzyme.
2. Inibitori ya MAO: Ubushakashatsi bw’inyamaswa bwerekanye ko fenelzine ya monoamine oxydease (MAOI) ishobora kongera uburozi bukabije bwa bupropion.
3. Levodopa: Amakuru yubuvuzi yerekana ko ibyago byo kwitwara nabi bishobora kwiyongera nyuma yo gukoresha icyarimwe bupropion na levodopa. Abarwayi bafata levodopa bagomba kwitonda mugihe bafata ibicuruzwa icyarimwe. Tangira numubare muto hanyuma wongere buhoro buhoro.
4. Ibiyobyabwenge bigabanya igipimo cyo gufatwa: Iki gicuruzwa cyahujwe nibiyobyabwenge bigabanya igipimo cyo gufatwa (nka antipsychotics, antidepressants, theophylline, sisitemu steroid, nibindi) cyangwa kuvura (nko guhagarika gutungurana kwa benzodiazepine)) bigomba gukoreshwa hamwe hamwe n'ubwitonzi bukabije.
5. Nicotine transdermal patch: Ubushakashatsi bwubuvuzi bwerekana ko gukoresha hamwe ibinini bya bupropion bikomeza kurekurwa hamwe na nicotine transdermal patch bifite ikibazo kinini cyo kuvura hypertension yihutirwa. Kubwibyo, umuvuduko wamaraso ugomba gukurikiranirwa hafi kugirango ukoreshe byombi.
Ibisobanuro
