Kaha mochine o motenya o fokotseha butle butle ka nako ea ho kenella ka vitro, e tlase ea li-metabolis tse tlase, tse ka tlase li sebelisa lithethefatsi tse ngata tsa metabobole butle haholo[1]. Khabareng,hepatocyteS e na le li-enzyme tse ngata tse hlokahalang bakeng sa oxidation, phokotso, hydrolysis le karabelo e makatsang ha li bapisoa leLi-Microsomes, le maemong a vitro, mefuta e mengata ea mehala e tloahelehileng e thehiloe hohepatocyte Sistimi le ho etsisa ho hongata tikolohong ea vivo ho etsa hore nako ea ho ts'oaroa ha ts'ebetso ea enzyme hohepatocyteS, 'me ho nka nako ea nako ea ho kenella ho fana ka monyetla oa ho beha leihlo phetoho e lekaneng ea metaboliction ea metaboli e liehang haholo[1,2].
Ka lebaka lena, Iphase e ne e le moetapele oa bulsosa a VIDR, ho kenyeletsoa semeloang sa meralo ea Hepatomar le Hepatocon ™ le Hepatocon ™ le Hepatocon ™hepatocyteS Ka mohlala, 'me bobeli li ile tsa qala ho ikemisetsa ha ketsahalo le metabola ea metabolite ea mefuta ea enzyme ea metaboolide ka matsatsi a 10 le matsatsi a 7 ho netefatsa litsamaiso. Metabolite e eketsa boleng ba karabelo ka matsatsi le tšebetsong ea 10 le tšebetso le botsitso ba metaboli ka matsatsi a 7 ka matsatsi a 7 ba ne ba ikemiselitse ho tiisa lits'ebetso.
- (1) Mekhoa e meraro ea kalafo ea kalafo ea lithethefatsi e tjena:
Iphase - Hepatomax ™Ke lengolo la CO - Tsamaiso ea Litloaelo tsa Frozen e nang le li-hipacytes tsa mantlha tsa batho le lisele tse shoelang. Li-prepatocyte tsa mantlha tsa batho li ile tsa qaloa ebile li kenella ka lisele tse chesang tsa aqosi e spileng, 'me metabolium ea lithibela-holo ea hepatodo ™ e ne e le sethethefatsi feela ntle le ho fetola se mahareng. Kakaretso ea 4, 72, 168 le 240 ka mor'a tsamaiso ea lithethefatsi, boleng bo kenyellelitsoeng ka lithethefatsi ba ne ba ikemiselitse ho hlahlojoa.
Iphase - Hepatoon ™, ka lehlakoreng le leng, ke sistimi ea ho hlaolela li-fupacente tsa mathomo tsa batho ba Mathomo tsa Mathomo tsa Hepatoon ™. Kamora ho hlakola motho oa mantlhahepatocyteS, polelo ea lithethefatsi Tsamaiso e entsoeng ka mor'a matsatsi a 3 a bosupa a Hepatoon ™ le nako e latelang ea tsamaiso, mokhoa oa setso o ne o tšoana le oa sistimi ea hepatomax.
Ho sa le joalo, ho netefatsa ho nepahala le liphetho tsa Iphase, Iphase e ile ea etsa taolo ea mekhahlelo (sele - Liphetho tse tharo, 'me litholoana li bontšitse horeIphase - Hepatomax ™ mmeIphase - Hepatoon ™ Litsamaiso li hlahisitse karabelo e matla ea metabolite ho tloha ka letsatsi ho tloha ka letsatsi, le hore bobeli ba bona ba bonts'a sekhahla se matla sa metabolic.
- (2) Metabolism ea lithethefatsi e itšetlehile haholo ka hepatocyteCyp450Stimmy, 'me ts'ebetso ea eona e ka lekanngoa ho hlahlojoa hantle.
TheIphase - Hepatomax ™ mmeIphase - Hepatoon ™ Litsamaiso li na le ts'ebeliso e ntle.
Iphase e behile mekhahlelo e mene ea taolo ea mahareng (ha ho lisele), hepatomax ™ le lisele tse monko. U sebelisa lerako - motho ea amanang le 'onahepatocyteS Ka mohlala, litekanyetso tsa metabolite tsaCyp1a2, Cyp2b6mmeCyp3a4li netefalitsoe ka letsatsi 0, 3 le 7 kamorahepatocytePheta ka matsatsi a 3 a sebelisa Provesertide, Bupropion le Midazlam e le likarolo, ka ho latellana. Metabolite keketseho ea boleng bo bonts'ang seo ka bobeliIphase - Hepatomax ™ mmeIphase - Hepatoon ™ Litsamaiso li bontšitse tšebetso ea enzyme ka letsatsi la 7, e khothaletsa metabolism e tloaelehileng ea lithethefatsi.
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Iphase a behile mekhahlelo e meraro ea hepatomax ™ le lisele tse chesang ho tseba hore na litsietsi tse 80 li sebelisa matsatsi a 3 a mathomohepatocyteS, 'me liphetho li bontšitse hore bobeli baIphase - Hepatomax ™ mmeIphase - Hepatoon ™ Litsamaiso ka bobeli li bontšitse ts'ebetso ea ho ts'oaroa metabolic ka nako e telele ka ho fetisisa ea nako.
Ka kakaretso, Iphase, e ne e le moetapele naheng ea VID, Bio - Reagens, e se e thehiloeIphase hepatomax ™ mmeIphase hepatocon ™ Meetso ea vitro e thehiloeng leboteng - E sebelisitse motho oa mantlha, Monkey, Canine, Rat le mousehepatocyteS le lisele tse nang le lisele tse fapaneng tsa mofuta o fapaneng, tse nang le mesebetsi e mecha ea metabolic le ho ba le molekane ea bohlokoa oa metabolians ho lemoha ho senyeha ha lithethefatsi! TheIphase hepatomax ™ mmeIphase hepatocon ™ Lits'ebetso tsa vitro li fana ka litefiso tse ngata tsa metaboliver, mesebetsi e sebetsang ea enzelic le metabolic e sebetsang, 'me ke molekane ea bohlokoa oa ho fumana bala.
Resort:
[1] 阮婷婷, 鞠武建 的 的 低清除率药物. 低清除率药物 的 代谢稳定性预测模型研究进展. 中国药科大学学报, 2019 (2): 152 - 160.
[2] di l, trapa p, ebsach r s, et al. Mokhoa o ratoang o phetoang bakeng sa ho khetholla Low - j]. Ho sebetsana le Metabolism le Tefello, 402, 40 (9): 1860 - 1865.
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