0102030405
Bupropion Hcl ọnụahịa Bupropion Hydrochloride ntụ ntụ
Nkọwa zuru ezu
Bupropion bụ ntụ ntụ ọcha, kristal sitere na mmanya isopropyl na ethanol zuru oke, yana ebe agbaze nke 233--234°C. Solubility (mg / m1): mmiri 312, ethanol 193, 0.1mol / L hydrochloric acid 333. Dị mfe ịmịkọrọ mmiri na decompose. Soluble na methanol, ethanol, acetone, ether ma ọ bụ benzene. Bupropion bụ nke klas aminoketone nke antidepressants. Ọ dabara maka ndị ọrịa nwere nkụda mmụọ azụ azụ na ndị na-adịghị arụ ọrụ ma ọ bụ ndị na-anabataghị ọgwụ mgbochi ndị ọzọ.
Ọrụ:
1.Bupropion nwekwara ike iji dị ka ọgwụgwọ jikwaa ntị deficit hyperactivity ọrịa (ADHD).
2. A pụkwara iji Bupropion mee ihe dị ka ọgwụgwọ ndenye ọgwụ iji nyere ndị mmadụ aka ịkwụsị ise siga site n'ibelata agụụ na mwepụ nicotine.
3. Enwere ike iji Bupropion gbochie ịda mba n'oge mgbụsị akwụkwọ-oyi (nsogbu mmetụta oge oge).
4. A pụkwara iji Bupropion na ọgwụ ndị ọzọ dị ka ọgwụgwọ maka ọrịa bipolar (usoro ịda mbà n'obi).
5. A na-eji Bupropion dị ka ọgwụgwọ ọgwụ ndenye maka ịda mbà n'obi. Ọ nwere ike melite ọnọdụ na mmetụta nke ọdịmma. Ọ nwere ike ịrụ ọrụ site n'inyere aka weghachite nguzozi nke ụfọdụ kemịkalụ eke (neurotransmitters) na ụbụrụ.
Ụzọ mmepụta
N'okpuru mkpali na jụrụ oyi, tinye ihe ngwọta nke o-chlorophenylacetonitrile (688g, 5mol) gbazere na diethyl ether (2.5L) na ngwọta nke ethylmagnesium bromide (2L, 3mol/L) n'ime nkeji 40. Kpoo ọkụ n'okpuru reflux dị nro maka awa 5. A na-eji mmiri na-ekpo ọkụ mee ihe ngwọta mmeghachi omume na mmiri oyi na-ekpo ọkụ. Mgbe ether ahụ kpochapụrụ, ihe ngwọta mmiri fọdụrụnụ na-ekpo ọkụ na 90 Celsius maka 1 hour. Mgbe ọ dị jụụ, tinye kristal mkpụrụ. Chịkọta ihe siri ike site na nzacha, sachaa na mmiri oyi, were methanol recrystalize wee nweta 750g nke o-chloropropiophenone, ebe mgbaze 39-40°C.
Gbarie o-chloropropiophenone (698g, 4.15mmol) na dichloromethane (3L). A kpalitere ngwọta ya na carbon na magnesium sulfate na-arụ ọrụ maka awa 2 wee kpochaa ya. Ihe ngwọta nke 662g (4.15mol) bromine gbazere na dichloromethane (1L) na-akpali akpali. Mgbe agba bromine na-apụ n'anya kpamkpam, tinye uche na oghere iji wepụ ihe mgbaze. Mmanụ fọdụrụnụ bụ o-chloro-a-bromopropiophenone. Enwere ike iji ya ozugbo na mmeghachi omume na-esote na-enweghị ọcha.
A na-agbaze ihe fọdụrụ mmanụ a na-enweta n'elu na acetonitrile (1300 ml), na ngwọta nke tert-butylamine (733 g) na acetonitrile (1300 ml) ka agbakwunyere n'okpuru 32 ° C. Hapụ ya n'abali, tinye 4200ml mmiri na 2700ml ether maka nkesa. Ejiri 1300 ml nke diethyl ether wepụta oyi akwa ahụ. Mgbe e jikọtara akwa ether, a na-agbakwunye 4200 ml mmiri, na hydrochloric acid na-agbakwunye ruo mgbe Ph uru nke mmiri oyi akwa bụ 9. A na-asacha akwa mmiri mmiri dị iche iche na 500 ml nke diethyl ether. A na-ejikọta akwa ether ahụ, 560g nke ice na 324ml nke hydrochloric acid gbanyere mkpọrọgwụ ka agbakwunyere ma kpalie ọnụ. Kewaa akwa ether ma were mmiri 200ml na 50ml concentrated hydrochloric acid saa. A na-ejikọta akwa acid abụọ ikpeazụ, tinye ya na vacuo ruo mgbe kristal pụtara, wee mee ka ọ dị jụụ ruo 5 Celsius. Nzacha, saa na acetone, wee recrystallize na ngwakọta nke 3L isopropyl mmanya na 800ml zuru oke ethanol. E nwetara DL-bupropion hydrochloride n'ụzọ dị ọcha na nke pụrụ iche, yana ebe mgbaze nke 233 ruo 234°C.
Mmetụta ọgwụ ọgwụ: Bupropion nwere mmetụta mgbochi na-adịghị ike na norepinephrine, 5-HT, na dopamine reuptake, ma ọ nweghị mmetụta dị otú ahụ na monoamine oxidase.
Mmekọrịta ọgwụ:
1. Ọgwụ metabolized site cytochrome P450ⅡB6: In vitro nnwale na-egosi na bupropion bụ tumadi metabolized site cytochrome P450ⅡB6 isoenzyme, otú e nwere ike mmekọrịta na ọgwụ ndị ọzọ na-emetụta cytochrome P450ⅡB6 isoenzyme.
2. MAO inhibitors: Ọmụmụ anụmanụ egosila na monoamine oxidase inhibitor (MAOI) phenelzine nwere ike ime ka oke nsi nke bupropion dịkwuo elu.
3. Levodopa: Data ụlọ ọgwụ na-egosi na mmetụta nke mmeghachi omume ọjọọ nwere ike ịbawanye mgbe ejiri bupropion na levodopa mee ihe n'otu oge. Ndị ọrịa na-ewere levodopa kwesịrị ịkpachara anya mgbe ha na-ewere ngwaahịa a n'otu oge. Malite na opekempe dose wee jiri nwayọọ nwayọọ mụbaa dose ahụ.
4. Ọgwụ ndị na-ebelata ọnụ ụzọ ọdịdọ: A na-ejikọta ngwaahịa a na ọgwụ ndị na-ebelata ọnụ ụzọ ọdịdọ (dị ka antipsychotics, antidepressants, theophylline, systemic steroids, wdg) ma ọ bụ ọgwụgwọ (dị ka nkwụsị mberede nke benzodiazepines) ) kwesịrị ijikọ ọnụ. jiri oke ịkpachara anya.
5. Nicotine transdermal patch: Nnyocha ụlọ ọgwụ na-atụ aro na ijikọta bupropion na-ahapụ mbadamba nkume na nicotine transdermal patch nwere nnukwu ọnọdụ nke ọbara mgbali elu ọgwụgwọ mberede. Ya mere, a ga-enyocha ọbara mgbali elu maka ijikọta ọnụ nke abụọ ahụ.
Nkọwapụta
