0102030405
I-Bupropion Hcl intengo I-Bupropion Hydrochloride Powder
Incazelo Eningiliziwe
I-Bupropion iyimpushana emhlophe, eyenziwe ngekristalu kusuka ku-isopropyl alcohol kanye ne-ethanol ephelele, enephuzu lokuncibilika lika-233--234 ° C. Ukunyibilika (mg/m1): amanzi 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Kulula kakhulu ukumunca umswakama nokubola. Incibilika ku-methanol, i-ethanol, i-acetone, i-ether noma i-benzene. I-Bupropion ingeyesigaba se-aminoketone sama-antidepressants. Ilungele iziguli ezinokucindezeleka okunesikhathi eside kanye nalezo ezingasebenzi noma ezingabekezeleli amanye ama-antidepressants.
Umsebenzi:
I-1.I-Bupropion ingase isetshenziswe njengendlela yokwelapha ukuphatha ukunakwa kwe-attention deficit hyperactivity disorder (ADHD).
2. I-Bupropion ingase isetshenziswe njengomuthi wokwelapha ukuze usize abantu bayeke ukubhema ngokunciphisa izifiso kanye nemiphumela yokuhoxiswa kwe-nicotine.
3. I-Bupropion ingase isetshenziselwe ukuvimbela ukucindezeleka kwenkathi yekwindla-ebusika (i-seasonal affective disorder).
4. I-Bupropion ingase isetshenziswe neminye imithi njengokwelashwa kwe-bipolar disorder (isigaba sokucindezeleka).
5. I-Bupropion isetshenziselwa njengendlela yokwelashwa yokwelashwa yokucindezeleka. Kungathuthukisa imizwa nemizwa yenhlalakahle. Ingase isebenze ngokusiza ukubuyisela ibhalansi yamakhemikhali athile emvelo (ama-neurotransmitters) ebuchosheni.
Izindlela zokukhiqiza
Ngaphansi kokunyakazisa nokupholisa, engeza isixazululo se-o-chlorophenylacetonitrile (688g, 5mol) encibilikiswe ku-diethyl ether (2.5L) kusixazululo se-ethylmagnesium bromide (2L, 3mol/L) phakathi nemizuzu engu-40. Shisisa ngaphansi kwe-reflux emnene amahora angu-5. Isixazululo sokusabela sasi-hydrolyzed nge-dilute hydrochloric acid ebandayo. Ngemva kokuba i-ether ihwamukile, isixazululo samanzi esisele sashiswa ku-90 ° C ihora elingu-1. Ngemuva kokupholisa, engeza i-crystal imbewu. Qoqa okuqinile ngokuhlunga, geza ngamanzi abandayo, bese uphinda ukristale nge-methanol ukuze uthole u-750g we-o-chloropropiophenone, indawo encibilikayo engu-39-40°C.
Chaza i-o-chloropropiophenone (698g, 4.15mmol) ku-dichloromethane (3L). Isixazululo sixutshwe nge-activated carbon ne-magnesium sulfate amahora angu-2 futhi sihlungiwe. Isixazululo se-662g (4.15mol) bromine encibilikiswe ku-dichloromethane (1L) sengezwe ngokushukumisa. Lapho umbala we-bromine uphela ngokuphelele, gxila ku-vacuum ukuze ususe i-solvent. Amafutha asele i-o-chloro-α-bromopropiophenone. Ingasetshenziswa ngokuqondile ekuphenduleni okulandelayo ngaphandle kokuhlanzwa.
Izinsalela ezinamafutha ezitholwe ngenhla zancibilika ku-acetonitrile (1300 ml), futhi isixazululo se-tert-butylamine (733 g) ku-acetonitrile (1300 ml) yengezwe ngaphansi kuka-32°C. Yishiye ubusuku bonke, engeza amanzi angu-4200ml kanye ne-ether engu-2700ml ukuze usatshalaliswe. Ungqimba olunamanzi lukhishwe ngo-1300 ml we-diethyl ether. Ngemva kokuhlanganiswa kwezingqimba ze-ether, i-4200 ml yamanzi yanezelwa, futhi i-hydrochloric acid yanezelwa kuze kube yilapho inani le-Ph lengqimba lamanzi liyi-9. Isendlalelo samanzi esihlukanisiwe sagezwa nge-500 ml ye-diethyl ether. Izingqimba ze-ether zahlanganiswa, i-560g yeqhwa kanye ne-324ml ye-concentrated hydrochloric acid yafakwa futhi yahlanganiswa ndawonye. Hlukanisa isendlalelo se-ether bese ugeza ngamanzi angu-200ml kanye ne-50ml egxilile ye-hydrochloric acid. Izendlalelo ezimbili zokugcina ze-asidi zahlanganiswa, zagxilwa ku-vacuo kuze kuvele ikristalu, bese zipholiswa zibe ngu-5°C. Hlunga, geza nge-acetone, bese uphinda ukristale ngengxube ye-3L isopropyl alcohol kanye ne-800ml absolute ethanol. Kutholwe i-DL-bupropion hydrochloride ehlanzekile ngokohlaziyo, enephuzu lokuncibilika elingu-233 kuya ku-234°C.
Imiphumela ye-Pharmacological: I-Bupropion inomphumela obuthakathaka wokuvimbela i-norepinephrine, i-5-HT, ne-dopamine reuptake, kodwa ayinawo umphumela onjalo ku-monoamine oxidase.
Ukusebenzisana kwezidakamizwa:
1. Izidakamizwa ezigaywe nge-cytochrome P450ⅡB6: Ukuhlolwa kwe-in vitro kubonisa ukuthi i-bupropion igaywe ngokuyinhloko yi-cytochrome P450ⅡB6 isoenzyme, ngakho-ke kukhona ukuxhumana okungase kube khona nezinye izidakamizwa ezithinta i-cytochrome P450ⅡB6 isoenzyme.
2. I-MAO inhibitors: Ucwaningo lwezilwane luye lwabonisa ukuthi i-monoamine oxidase inhibitor (MAOI) phenelzine ingandisa ubuthi obukhulu be-bupropion.
3. I-Levodopa: Idatha yomtholampilo ibonisa ukuthi ukusabela okubi kungase kwande ngemva kokusetshenziswa kanyekanye kwe-bupropion ne-levodopa. Iziguli ezithatha i-levodopa kufanele ziqaphele lapho zithatha lo mkhiqizo ngesikhathi esifanayo. Qala ngomthamo omncane bese ukhulisa kancane kancane umthamo.
4. Izidakamizwa ezehlisa umkhawulo wokubanjwa: Lo mkhiqizo uhlanganiswa nezidakamizwa ezehlisa umkhawulo wokubanjwa (njengama-antipsychotic, ama-antidepressants, i-theophylline, i-systemic steroids, njll.) noma izindlela zokwelapha (njengokuphazamiseka okungazelelwe kwe-benzodiazepines) ) kufanele zisetshenziswe ndawonye. ngokuqapha okukhulu.
5. I-Nicotine transdermal patch: Ucwaningo lwezokwelapha lubonisa ukuthi ukusetshenziswa okuhlangene kwamaphilisi e-bupropion-release-release kanye ne-nicotine transdermal patch kunesigameko esiphezulu se-hypertension yokwelapha ephuthumayo. Ngakho-ke, umfutho wegazi kufanele uqashwe ngokucophelela ukuze kusetshenziswe kokubili okuhlangene.
Ukucaciswa
