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Bupropion Hcl mtengo Bupropion Hydrochloride Powder
Kufotokozera Mwatsatanetsatane
Bupropion ndi ufa woyera, wonyezimira kuchokera ku isopropyl mowa ndi ethanol mtheradi, ndi malo osungunuka a 233--234 ° C. Kusungunuka (mg / m1): madzi 312, ethanol 193, 0.1mol / L hydrochloric acid 333. Zosavuta kwambiri kuyamwa chinyezi ndikuwola. Amasungunuka mu methanol, ethanol, acetone, ether kapena benzene. Bupropion ndi m'gulu la aminoketone la antidepressants. Ndioyenera kwa odwala omwe ali ndi vuto lochedwa kuvutika maganizo komanso omwe sagwira ntchito kapena salolera mankhwala ena ochepetsa nkhawa.
Ntchito:
1.Bupropion ingagwiritsidwenso ntchito ngati chithandizo chothandizira kuchepetsa chidwi cha matenda osokoneza bongo (ADHD).
2. Bupropion ingagwiritsidwenso ntchito ngati chithandizo chamankhwala chothandizira anthu kusiya kusuta mwa kuchepetsa zilakolako ndi zotsatira zochotsa chikonga.
3. Bupropion angagwiritsidwe ntchito kuteteza kuvutika maganizo kwa nyengo ya autumn-yozizira (nyengo yachisokonezo).
4. Bupropion ingagwiritsidwenso ntchito ndi mankhwala ena monga chithandizo cha matenda a bipolar (depression phase).
5. Bupropion amagwiritsidwa ntchito ngati mankhwala ochizira matenda ovutika maganizo. Ikhoza kusintha maganizo ndi malingaliro a moyo wabwino. Zitha kugwira ntchito pothandizira kubwezeretsa kukhazikika kwamankhwala ena achilengedwe (ma neurotransmitters) muubongo.
Njira zopangira
Poyambitsa ndi kuziziritsa, onjezerani njira ya o-chlorophenylacetonitrile (688g, 5mol) yosungunuka mu diethyl ether (2.5L) ku yankho la ethylmagnesium bromide (2L, 3mol / L) mkati mwa mphindi 40. Kutenthetsa pansi pa reflux wofatsa kwa 5h. The njira yothetsera anali hydrolyzed ndi ozizira kuchepetsa hydrochloric acid. Etha itasungunuka, njira yotsala yamadzimadzi idatenthedwa pa 90 ° C kwa ola limodzi. Pambuyo kuzirala, onjezerani kristalo wa mbewu. Sonkhanitsani zolimba posefera, sambani ndi madzi ozizira, ndi kukonzanso ndi methanol kuti mupeze 750g ya o-chloropropiophenone, malo osungunuka 39-40 ° C.
Sungunulani o-chloropropiophenone (698g, 4.15mmol) mu dichloromethane (3L). The yankho anasonkhezeredwa ndi adamulowetsa mpweya ndi magnesium sulphate kwa 2 hours ndi osasankhidwa. Njira yothetsera 662g (4.15mol) bromine yosungunuka mu dichloromethane (1L) inawonjezeredwa ndi kusonkhezera. Pamene mtundu wa bromine utatha, ganizirani mu vacuum kuchotsa zosungunulira. Mafuta otsalawo ndi o-chloro-α-bromopropiophenone. Ikhoza kugwiritsidwa ntchito mwachindunji muzotsatira zotsatila popanda kuyeretsedwa.
Zotsalira zamafuta zomwe zapezedwa pamwambapa zidasungunuka mu acetonitrile (1300 ml), ndipo yankho la tert-butylamine (733 g) mu acetonitrile (1300 ml) linawonjezedwa pansi pa 32 ° C. Siyani usiku wonse, onjezerani madzi 4200ml ndi 2700ml ether kuti mugawidwe. Wosanjikiza wamadzimadzi adatengedwa ndi 1300 ml ya diethyl ether. Pambuyo pophatikiza zigawo za ether, 4200 ml ya madzi anawonjezeredwa, ndipo hydrochloric acid anawonjezeredwa mpaka Ph mtengo wa madzi wosanjikiza anali 9. Kupatukana kwamadzimadzi kunatsukidwa ndi 500 ml ya diethyl ether. Zigawo za ether zinaphatikizidwa, 560g ya ayezi ndi 324ml ya concentrated hydrochloric acid anawonjezeredwa ndi kusonkhezera pamodzi. Alekanitse wosanjikiza etha ndi kusamba ndi 200ml madzi ndi 50ml anaikira hydrochloric acid. Zigawo ziwiri zomaliza za asidi zidaphatikizidwa, zokhazikika mu vacuo mpaka crystallization itawonekera, kenako itakhazikika mpaka 5 ° C. Sefa, sambani ndi acetone, ndiyeno muwonjezerenso ndi kusakaniza kwa 3L isopropyl mowa ndi 800ml mtheradi wa ethanol. DL-bupropion hydrochloride yoyera komanso yowoneka bwino idapezedwa, yokhala ndi malo osungunuka a 233 mpaka 234 ° C.
Zotsatira za mankhwala: Bupropion ili ndi mphamvu yofooka yolepheretsa norepinephrine, 5-HT, ndi dopamine reuptake, koma ilibe mphamvu yotereyi pa monoamine oxidase.
Kuyanjana ndi mankhwala:
1. Mankhwala opangidwa ndi cytochrome P450ⅡB6: Kuyesera kwa in vitro kumasonyeza kuti bupropion makamaka imapangidwa ndi cytochrome P450ⅡB6 isoenzyme, kotero pali zotheka kuyanjana ndi mankhwala ena omwe amakhudza cytochrome P450ⅡB6 isoenzyme.
2. MAO inhibitors: Maphunziro a zinyama asonyeza kuti monoamine oxidase inhibitor (MAOI) phenelzine ikhoza kuonjezera poizoni woopsa wa bupropion.
3. Levodopa: Deta yachipatala imasonyeza kuti zochitika zowonongeka zimatha kuwonjezeka pambuyo pa kugwiritsa ntchito bupropion ndi levodopa panthawi imodzi. Odwala omwe amatenga levodopa ayenera kusamala akamamwa mankhwalawa nthawi imodzi. Yambani ndi mlingo wocheperako ndipo pang'onopang'ono muwonjezere mlingo.
4. Mankhwala omwe amachepetsa kulanda: Mankhwalawa amaphatikizidwa ndi mankhwala omwe amachepetsa kugwidwa (monga antipsychotics, antidepressants, theophylline, systemic steroids, etc.) kapena mankhwala (monga kusokonezeka mwadzidzidzi kwa benzodiazepines) ayenera kugwiritsidwa ntchito pamodzi. ndi kusamala kwambiri.
5. Chikoka cha Nicotine transdermal patch: Maphunziro a zachipatala amasonyeza kuti kugwiritsa ntchito mapiritsi osakanikirana a bupropion ndi nicotine transdermal patch ali ndi chiwerengero chapamwamba cha kuthamanga kwa magazi kwadzidzidzi. Choncho, kuthamanga kwa magazi kuyenera kuyang'aniridwa mosamala kuti agwiritse ntchito pamodzi awiriwa.
Kufotokozera
