Bupropion Hcl ixabiso Bupropion Hydrochloride Powder
Inkcazo eneenkcukacha
I-Bupropion i-powder emhlophe, i-crystallized kwi-isopropyl alcohol kunye ne-ethanol epheleleyo, ene-melting point ye-233--234 ° C. Ukunyibilika (mg/m1): amanzi 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Kulula kakhulu ukufunxa umswakama kunye nokubola. Inyibilika kwi-methanol, i-ethanol, i-acetone, i-ether okanye ibenzene. I-Bupropion yeyodidi lwe-aminoketone lwe-antidepressants. Ilungele izigulane ezinoxinzelelo olude kunye nezo zingasebenziyo okanye ezinganyamezeliyo kwezinye ii-antidepressants.
Umsebenzi:
I-1.I-Bupropion ingasetyenziselwa njengonyango lokulawula ukusilela kwe-hyperactivity disorder (ADHD).
2. I-Bupropion ingasetyenziselwa njengonyango lonyango lokunceda abantu bayeke ukutshaya ngokunciphisa iminqweno kunye nemiphumo yokuhoxiswa kwe-nicotine.
3. I-Bupropion ingasetyenziselwa ukukhusela ukudakumba kwexesha lekwindla-ebusika (i-seasonal affective disorder).
4. I-Bupropion ingasetyenziselwa kunye namanye amayeza njengonyango lwe-bipolar disorder (isigaba sokudakumba).
5. I-Bupropion isetyenziselwa njengonyango lonyango lokudakumba. Inokuphucula isimo sengqondo kunye neemvakalelo zokuphila kakuhle. Inokusebenza ngokunceda ukubuyisela ulungelelwaniso lweekhemikhali ezithile zendalo (neurotransmitters) engqondweni.
Iindlela zokuvelisa
Ngaphantsi kokuvuselela kunye nokupholisa, yongeza isisombululo se-o-chlorophenylacetonitrile (688g, 5mol) echithwe kwi-diethyl ether (2.5L) kwisisombululo se-ethylmagnesium bromide (2L, 3mol / L) kwimizuzu engama-40. Ukufudumala phantsi kwe-reflux ethambileyo ye-5h. Isisombululo sokusabela sifakwe nge-hydrolyzed nge-dilute ebandayo ye-hydrochloric acid. Emva kokuba i-ether ikhutshwe, isisombululo esisele samanzi satshiswa kwi-90 ° C ngeyure eli-1. Emva kokupholisa, yongeza ikristale yembewu. Qokelela okuqinileyo ngokuhluza, hlamba ngamanzi abandayo, kwaye uphinde udibanise ngemethanol ukuze ufumane i-750g ye-o-chloropropiophenone, indawo yokunyibilika 39-40 °C.
Dissolve o-chloropropiophenone (698g, 4.15mmol) kwi-dichloromethane (3L). Isisombululo saxutywa ngekhabhoni esebenzayo kunye ne-magnesium sulfate kwiiyure ze-2 kwaye yahluzwa. Isisombululo se-662g (4.15mol) i-bromine echithwe kwi-dichloromethane (1L) yongezwa ngokuvuselela. Xa umbala we-bromine uphela ngokupheleleyo, gxininisa kwi-vacuum ukususa i-solvent. Ioli eseleyo yi-o-chloro-α-bromopropiophenone. Ingasetyenziswa ngokuthe ngqo kwimpendulo elandelayo ngaphandle kokuhlanjululwa.
Intsalela yeoli efunyenwe ngasentla yachithwa kwi-acetonitrile (1300 ml), kunye nesisombululo se-tert-butylamine (733 g) kwi-acetonitrile (1300 ml) yongezwa ngaphantsi kwe-32 ° C. Yiyeke ngobusuku, yongeza amanzi angama-4200ml kunye ne-2700ml ether ukuze usasazeke. Uluhlu olunamanzi lukhutshwe nge-1300 ml ye-diethyl ether. Emva kokuba i-ether layers idibaniswe, i-4200 ml yamanzi yongezwa, kwaye i-hydrochloric acid yongezwa kwaze kwaba yilapho ixabiso le-Ph lomgangatho wamanzi liyi-9. Uluhlu oluhlukeneyo lwamanzi luhlanjwe nge-500 ml ye-diethyl ether. Iingqimba ze-ether zidibene, i-560g yeqhwa kunye ne-324ml ye-hydrochloric acid edibeneyo yongezwa kwaye ixutywe kunye. Ukwahlula i-ether layer kwaye uhlambe ngamanzi angama-200ml kunye ne-50ml egxininisiweyo ye-hydrochloric acid. Iileya ezimbini zokugqibela ze-asidi zidityanisiwe, zigxininiswe kwi-vacuo de kuvele icrystallization, emva koko ipholiswe kwi-5°C. Hlunga, hlamba nge-acetone, uze uphinde udibanise ngomxube we-3L isopropyl alcohol kunye ne-800ml absolute ethanol. Uhlalutyo olusulungekileyo kunye ne-spectrally pure DL-bupropion hydrochloride yafunyanwa, kunye nendawo yokunyibilika ye-233 ukuya kwi-234 ° C.
Iziphumo ze-Pharmacological: I-Bupropion ine-inhibitory effect ebuthathaka kwi-norepinephrine, i-5-HT, kunye ne-dopamine reuptake, kodwa ayinayo impembelelo enjalo kwi-monoamine oxidase.
Ukudibana kweziyobisi:
1. Iziyobisi ezixutywe nge-cytochrome P450ⅡB6: Uvavanyo lwe-in vitro lubonisa ukuba i-bupropion i-metabolized ikakhulu yi-cytochrome P450ⅡB6 isoenzyme, ngoko ke kukho ukusebenzisana okunokwenzeka kunye nezinye iziyobisi ezichaphazela i-cytochrome P450ⅡB6 isoenzyme.
2. I-MAO inhibitors: Izifundo zezilwanyana zibonise ukuba i-monoamine oxidase inhibitor (MAOI) phenelzine inokunyusa i-toxicity enzima ye-bupropion.
3. I-Levodopa: Idatha yeklinikhi ibonisa ukuba iziganeko zokusabela okubi zingakhula emva kokusetyenziswa ngaxeshanye kwe-bupropion kunye ne-levodopa. Izigulane ezithatha i-levodopa kufuneka zilumke xa zithatha le mveliso ngexesha elifanayo. Qala ngedosi encinci kwaye unyuse ngokuthe ngcembe umthamo.
4. Iziyobisi ezinciphisa umda wokubamba: Le mveliso idityaniswe kunye neziyobisi ezinciphisa umda wokuhlutha (ezifana ne-antipsychotics, i-antidepressants, i-theophylline, i-systemic steroids, njl.) okanye unyango (njengokuphazamiseka ngokukhawuleza kwe-benzodiazepines) kufuneka zisetyenziswe kunye. ngononophelo olukhulu.
5. I-Nicotine transdermal patch: Izifundo zeklinikhi zibonisa ukuba ukusetyenziswa okudibeneyo kwe-bupropion i-tablet yokukhululwa okuqhubekayo kunye ne-nicotine i-transdermal patch ineziganeko eziphezulu ze-hypertension yonyango oluphuthumayo. Ngoko ke, uxinzelelo lwegazi kufuneka lubekwe esweni ngokusondeleyo kusetyenziso oludibeneyo lwezi zibini.
Inkcazo
