1. Kuyambitsa: Kumvetsetsa microsomes yamunthu
Pogwiritsa ntchito mankhwala amakono, kulosera momwe mankhwala amathandizo amathandizira thupi la munthu ndikofunikira pakuwonetsetsa kuti paliponse komanso chitetezo.Microomes yamunthu. Izi zimathandiza ofufuza pambiri akumvetsetsa momwe mankhwalawa amathandizira asanalowe m'mayesero azachipatala, ndikuchepetsa nthawi yachitukuko komanso mtengo.Nkhaniyi ikuwunika gawo la ma microsomes a anthu pagayidwecabolism, momwe amapangidwira phangacokinetics, ndi tanthauzo lawo pakukonzanso mankhwala osokoneza bongo ndi chitetezo.
2. Kodi microosomes ya anthu ndi iti?
Ma microomes a chiwindi ndi gawo lazigawo lochokera ku chiwindi cha anthu. Amakhala ndi ma enzy ofunikira pakupanga mankhwala osokoneza bongo, makamaka:Cytochrome p450 michere (cyp4500s)- Udindo wa gawo ndi kagayidwe, kuphatikizapo makutidwenation, hydroxty, ndi nkhawa.
UDP - GlucuronosyltransTases (UGTS)- Kutengera gawo la gawo la Gawoli ku II, monga gluculanida, kuwonjezera mankhwala osokoneza bongo chifukwa cha kuchuluka.
Ma HLM amakhala ngati mu vitro system ya chiwindi kagayidwe, ndikuwapangitsa kukhala kofunikira kuti apeze mankhwala ndi chitukuko. Ma microsomes awa amalola ofufuza kuti aphunzire njira za metabolic, kudziwa kuchuluka kwa mankhwala osokoneza bongo, ndikuneneratu zomwe zingayambitse zoopsa zomwe zingachitike ziyeso zisanachitike.
3. Momwe Ma microomies a chiwindi amakhudzira pharmacokinetics
Pharmacokinetics (PK) amatanthauza kusuntha kwa mankhwala kudzera mu thupi, kuphatikizapo kuyamwa kwake, kugawa, kagayidwe, ndi mawu (adme). Mwa awa, kagayidwe kake ndi chinthu chofunikira kwambiri chikukhudza kugwiritsa ntchito mankhwala osokoneza bongo komanso chitetezo, ndipo ma Holms amatenga mbali yofunika kwambiri yomvetsetsa izi.Kukhazikika kwa metabolic- Imasankha theka - moyo ndi chilolezo cha mankhwala, kukhumudwitsidwa ndi malamulo.
Mapangidwe a metabolites- Amazindikiritsa metabolites kapena zoopsa zomwe zingakhudze mankhwala pogwiritsa ntchito mankhwala kapena chitetezo.
Mankhwala - Zosintha Mankhwala (DDI) - Ayeseni ngati mankhwala osokoneza bongo amaletsa kapena kuwononga michere ya metabolic, yomwe ingasinthe mphamvu kapena poizoni kutumikiridwa.
Mwa kusanthula zinthuzi, ofufuza amatha kuneneratu ngati mankhwala azikhala achangu mokwanira kuti akhale ogwira mtima kapena kuti aphatikizidwe mwachangu ndipo amafunikiranso dosing.
4. Mapulogalamu a ma microsomes aumunthu pakukula kwa mankhwala
4.1 Kulosera za mankhwala osokoneza bongo ndi chilolezo
HLMS imathandizira kudziwa kuti mankhwalawa amapangidwa mwachangu bwanji mu chiwindi, omwe amakhudza mwachindunji Mlingo wake ndi makonzedwe ake. Mankhwala osokoneza bongo okhala ndi mitengo yayikulu amatha kufuna mtengo wokwera kapena pafupipafupi, pomwe omwe ali ndi pang'onopang'ono metabolism amatha kudziunjikira, omwe angayambitse kuopsa.4.2 Kuzindikira VOTOVATE - Zogwirizana ndi Mankhwala (DDIS)
Mankhwala ena amatha kuyika kapena kuyambitsa michere ya cyp450, kumapangitsa kuti zisakhale zovuta mosayembekezereka akaphatikizidwa ndi mankhwala ena. HLM - Kafukufuku Wochokera ku mankhwala opangira mankhwala amapeza ngoziyi isanachitike mayesero azachipatala.4.3 Kuzindikira Poizoni Metabolites
Mankhwala ena amatulutsa metabolites yomwe imatha kuyambitsa chiwopsezo cha chiwindi kapena zovuta zina. Kuyang'ana ndi ma HLM kumathandizira kuzindikira ma metabolites awa kumayambiriro kwa ma metaboli oyambilira, kuchepetsa zoopsa zomwe zimakhudzana ndi kuvulala kwa chiwindi (kuwonongeka).5. Ubwino ndi zofooka zogwiritsa ntchito ma microsies a chiwindi
5.1 zabwino
Mtengo - ogwira ntchito - chuma chochulukirapo kuposa kuthamanga - Mayesero Olimbitsa.Zotsatira zoberekera - zimapereka zotsatira zosasinthika motsogozedwa ndi labu.
Righ - Kuyipitsa - kumathandizira kusanthula mwachangu kwa ogwiritsa ntchito mankhwala ambiri.
5.2 Zopanda malire
Zosavuta ndi chiwindi - si akaunti yonyamula zonyamula zomwe zimakhudzidwa ndi gawo iii metabolism.Sangayerekeze ndi chiwindi chiwindi zotsatira - siyikanikanso zenizeni - Mphamvu Yoyenda Mwamagazi.
Kusiyana kwa mitundu - deta kuchokera ku microsis ya nyama singaneneretu za mankhwala osokoneza bongo.
6.
Kumpoto kwa North Wales, Pennsylvania,Ifase biosciesNdiwopatsa chidwi komanso zatsopano - Mbiri Yogwiritsa Ntchito Yoperekedwa Kufufuza, Kukula, ndi kupanga kwachilengedwe - Microsomes ya anthu. Ndi kudzipereka kwamphamvu ku kupambana kwa sayansi, gulu lathu limapereka zida zothandizira padziko lonse lapansi, zomwe zimapangitsa kuti nthaka ikhale yolimbana ndi ma metabolism mu mankhwala ndi pharmacokinetics (DMP).7. PANGANO: gawo la Microsie Misroomes Popanga Mankhwala Kukula
Ma HLMS amatenga mbali yovuta kwambiri pomvetsetsa mankhwala opatsira mankhwala, ndikuonetsetsa kuti chitetezo, ndikutha kukonza mankhwala osokoneza bongo. Pophatikizira hlm - Makampani ophatikizika amathandizira kukonzekera mankhwala, kukonza bwino mankhwala osokoneza bongo, komanso chitetezo chodwala.Pa ufa wa ufa, ndife odzipereka kuthandizira ofufuzawo ndi opanga zinthu zapamwamba kwambiri, kuthandiza kuyendetsa zinthu zasayansi zomwe zimayambitsa tsogolo la zamankhwala.
Post Nthawi: 2025 - 02 - 17 16:22:44