0102030405
Bupropion Hcl kumu kūʻai ʻo Bupropion Hydrochloride Powder
Ka wehewehe kikoʻī
He pauka keʻokeʻo ʻo Bupropion, i hoʻoheheʻe ʻia mai ka isopropyl alcohol a me ka ethanol piha, me kahi helu heheʻe o 233--234°C. Solubility (mg/m1): wai 312, ethanol 193, 0.1mol/L hydrochloric acid 333. Maʻalahi loa e komo i ka makū a me ka decompose. Hiki ke hoʻoheheʻe ʻia i ka methanol, ethanol, acetone, ether a i ʻole benzene. Aia ka Bupropion i ka papa aminoketone o nā antidepressants. He kūpono ia no nā poʻe maʻi me ka puʻuwai haʻahaʻa a me ka poʻe i kūpono ʻole a ʻae ʻole i nā antidepressants ʻē aʻe.
Hana:
1. Hiki ke hoʻohana ʻia ʻo Bupropion ma ke ʻano he lāʻau lapaʻau no ka mālama ʻana i ka maʻi maʻi hoʻohaʻahaʻa deficit hyperactivity (ADHD).
2. Hiki ke hoʻohana ʻia ka bupropion ma ke ʻano he lāʻau lapaʻau e kōkua ai i ka poʻe e haʻalele i ka puhi paka ma ka hoʻemi ʻana i ka makemake a me nā hopena hoʻihoʻi nicotine.
3. Hiki ke ho'ohana 'ia ka bupropion no ka pale 'ana i ke kaumaha o ke kau o ke kau-ho'oilo.
4. Hiki ke hoʻohana pū ʻia ka bupropion me nā lāʻau lapaʻau ʻē aʻe ma ke ʻano he lapaʻau no ka maʻi maʻi maʻi maʻi (kahi o ke kaumaha).
5. Hoʻohana ʻia ʻo Bupropion ma ke ʻano he lāʻau lapaʻau lāʻau no ke kaumaha. Hiki iā ia ke hoʻomaikaʻi i ke ʻano a me nā manaʻo o ka maikaʻi. Hiki ke hana ma ke kōkua ʻana i ka hoʻihoʻi ʻana i ke koena o kekahi mau kemika kūlohelohe (neurotransmitters) i loko o ka lolo.
Hana hana
Ma lalo o ka hoʻoulu ʻana a me ka hoʻoluʻu ʻana, hoʻohui i kahi hopena o ka o-chlorophenylacetonitrile (688g, 5mol) i hoʻoheheʻe ʻia i ka diethyl ether (2.5L) i ka hopena o ka ethylmagnesium bromide (2L, 3mol/L) i loko o 40 mau minuke. E wela ma lalo o ka reflux mālie no 5h. Ua hydrolyzed ka hopena hopena me ka waika hydrochloric dilute anuanu. Ma hope o ka hoʻoheheʻe ʻia ʻana o ka etera, ua hoʻomehana ʻia ke koena wai wai i 90 ° C no 1 hola. Ma hope o ka hoʻoluʻu ʻana, hoʻohui i ke aniani hua. E hōʻiliʻili i ka paʻa ma ka kānana ʻana, holoi me ka wai anuanu, a hana hou me ka methanol no ka loaʻa ʻana o 750g o ka o-chloropropiophenone, wahi hoʻoheheʻe 39-40°C.
Hoʻopau i ka o-chloropropiophenone (698g, 4.15mmol) i loko o ka dichloromethane (3L). Hoʻoulu ʻia ka hopena me ka carbon activated a me ka magnesium sulfate no 2 mau hola a kānana. Ua hoʻohui ʻia kahi hopena o 662g (4.15mol) bromine i hoʻoheheʻe ʻia i loko o ka dichloromethane (1L) me ka hoʻoulu ʻana. Ke nalo loa ka waihoʻoluʻu bromine, e noʻonoʻo i loko o kahi ʻūhā e wehe i ka mea hoʻoheheʻe. ʻO ke koena aila he o-chloro-α-bromopropiophenone. Hiki ke hoʻohana pololei i ka hopena aʻe me ka hoʻomaʻemaʻe ʻole.
ʻO ke koena aila i loaʻa ma luna nei ua hoʻoheheʻe ʻia i loko o ka acetonitrile (1300 ml), a ua hoʻohui ʻia kahi hopena o tert-butylamine (733 g) i ka acetonitrile (1300 ml) ma lalo o 32°C. E waiho i ka pō, e hoʻohui i 4200ml wai a me 2700ml ether no ka hāʻawi ʻana. Ua unuhi ʻia ka papa wai me 1300 ml o diethyl ether. Ma hope o ka huiʻana o nā papa etera, ua hoʻohuiʻia ka 4200 ml o ka wai, a ua hoʻohuiʻia ka waiuma hydrochloric a hiki i ka helu Ph o ka papa wai he 9. Ua holoiʻia ka papa wai i hoʻokaʻawaleʻia me ka 500 ml o diethyl ether. Hoʻohui ʻia nā papa ether, 560g o ka hau a me 324ml o ka waika hydrochloric concentrated i hoʻohui ʻia a hoʻoulu ʻia. E hoʻokaʻawale i ka papa ether a holoi me ka wai 200ml a me ka waika hydrochloric concentrated 50ml. Hoʻohui ʻia nā papa ʻakika hope ʻelua, hoʻopaʻa ʻia i loko o ka vacuo a hiki i ka ʻike ʻia ʻana o ka crystallization, a laila hoʻomaha ʻia i 5°C. E kānana, holoi me ka acetone, a laila hana hou me ka hui ʻana o 3L isopropyl alcohol a me 800ml ethanol piha. Ua loaʻa mai ka DL-bupropion hydrochloride maʻemaʻe a me ka maʻemaʻe, me kahi helu heheʻe o 233 a 234 ° C.
Nā hopena lāʻau lapaʻau: Loaʻa i ka Bupropion kahi hopena paʻakikī i ka norepinephrine, 5-HT, a me ka dopamine reuptake, akā ʻaʻohe hopena like i ka monoamine oxidase.
Nā pilina lāʻau:
1. ʻO nā lāʻau lapaʻau i hoʻololi ʻia e ka cytochrome P450ⅡB6: Hōʻike nā hoʻokolohua in vitro i ka nui o ka bupropion i hoʻoheheʻe ʻia e ka cytochrome P450ⅡB6 isoenzyme, no laila aia nā pilina me nā lāʻau ʻē aʻe e pili ana i ka isoenzyme cytochrome P450ⅡB6.
2. MAO inhibitors: Ua hōʻike nā haʻawina holoholona e hiki i ka monoamine oxidase inhibitor (MAOI) phenelzine ke hoʻonui i ka meaʻawaʻawa o ka bupropion.
3. Levodopa: Hōʻike ka ʻikepili maʻi i ka piʻi ʻana o nā hopena ʻino ma hope o ka hoʻohana like ʻana o ka bupropion a me ka levodopa. Pono nā poʻe maʻi e lawe ana i ka levodopa e makaʻala i ka lawe ʻana i kēia huahana i ka manawa like. E hoʻomaka me ka liʻiliʻi liʻiliʻi a laila e hoʻonui mālie i ka nui.
4. ʻO nā lāʻau lapaʻau e hoʻohaʻahaʻa i ka paepae hopu: Ua hui pū ʻia kēia huahana me nā lāʻau e hoʻohaʻahaʻa i ka paepae hopu (e like me nā antipsychotics, antidepressants, theophylline, systemic steroids, etc.) a i ʻole nā mea lapaʻau (e like me ka hoʻopau koke ʻana o benzodiazepines) ) pono e hoʻohana pū ʻia. me ka akahele loa.
5. Nicotine transdermal patch: Hōʻike nā noiʻi maʻi i ka hoʻohana pū ʻia ʻana o nā papa hoʻokuʻu i hoʻokuʻu ʻia i ka bupropion a me ka patch transdermal nicotine i ʻoi aku ka nui o ka maʻi hypertension therapeutic. No laila, pono ke nānā pono ʻia ke koko no ka hoʻohana ʻana i nā mea ʻelua.
Hōʻike
