Yintoni Ukuhlaziywa?

Funda ngokungafihli, okanye izinga apho isilwanyana sithatha khona

I-Bioavailability (BA) ligama elisetyenziswe kwi-pharmacology kunye nesayensi yesondlo kunye nezendalo. Kwi-pharmacology, ibhekisela kwisilinganiso kunye nesantya apho isicatshulwa esilawulwayo sithatyathwa yinkqubo yomzimba, ukujikelezwa kweenkqubo.

Ukufumaneka kwezinto kuyisisombululo sokubaluleka esibalulekileyo kuba ibeka umlinganiselo ochanekileyo wokulawulwa okungenakunyango kweziyobisi. Kwizilingo zophando lweekliniki , ukufumaneka kwezilwanyana kubaluleke kakhulu ukuba kulandwe kwiSigaba se-1 kunye neSigaba sesi-2.

Ukuqulunqa ukuhlaziywa ngokuthe ngqo kweziyobisi kwenziwa ngophando lwe- pharmacokinetic . Ukuxilongwa kwezilwanyana zeplasma zicwangciswe malunga nexesha kunye nemilinganiselo yokuxininisa vs ixesha emva kokulawulwa kwe-intravenous non-intravenous. Izicelo ezingenayo i-intraveous zibandakanya ngomlomo, emacaleni, ezitshintshiweyo, ezicatshulwa kunye nezicatshulwa.

Ukulinganiselwa kokungabi naso kubonakaliswe yileta f okanye iF xa iboniswe ngepesenti. Ukuxhaswa kwe-bioavailability yindlela esetyenziselwa ukuhlola i-bioequivalence (BE) phakathi kwemveliso yeziyobisi.

Ukuze ufumane i-FDA imvume yokusetyenziswa kweziyobisi eziqhelekileyo, umxhasi wezidakamizwa kufuneka abonise i-90 yepesenti yokwethenjwa kwemveliso kweso sonyango esibalulekileyo.

Ukufumaneka kwezinto ezikhoyo kubaluleke kakhulu kwizixhobo ezibalulekileyo ekuphuculweni kweziyobisi ngokuxhomekeka kobungozi kufuneka kuthathelwe ingqalelo xa kubalwa ama-dosages kwiindlela ezingenayo i-intravenous zokulawulwa ngokubhekiselele ekutheni ukutyunjwa.

Ipesenteji yeziyobisi ezithathwayo yindlela yokuqulunqa iziyobisi ukuhambisa isiza kwisiza ekujoliswe kuso.

"Inani elithathwayo" lilinganiselwe ngokukodwa kwimiqathango emibini, nokuba yindawo engaphantsi kwexesha le-curve (i-AUC) okanye isixa-mali esipheleleyo (isibalo) sesilwanyana esikhankanywe kwi-urine emva kokulawulwa kweziyobisi, "ngokutsho kweBoston University School lwezeMpilo. Ulwalamano olunxulumene lukhona phakathi "kwendawo phantsi kwekhalo" kunye ne dose xa iqhekeza lesichengisiso lixhomekeke lizimeleyo kwesazi, kwaye izinga lokuphelisa (isigxina-nobomi) kunye nokukhutshwa komthamo zimeleyo kwifom kunye nefayili yefayili.

Ukulungelelana kobudlelwane phakathi kwendawo engaphantsi kwekhava kunye ne dose kwenzeka ukuba, umzekelo, inkqubo yokumunca iyinto enokutsha, okanye ukuba isicatshulwa siphumelele ukufikelela kwindlela yokuhambisa umbane ngenxa, umzekelo, ukubopha kwezilwanyana kumathumbu okanye kwi-biotransformation isibindi ngexesha lokuqala kwezidakamizwa kwi-portal system. "

Izinto ezichaphazela ukufumaneka

Xa ilawulwa yindlela engeyiyo yendlela, ukufumaneka kwezidakamizwa kuyahlukahluka kumntu kumntu. Ingathatyathwa yimizimba kunye nezinye izinto ezibandakanya ukuba isicatshulwa sithathwa kunye nezinye iziyobisi okanye ngaphandle kokutya, nokuba kukho isifo esichaphazela isistim somzimba okanye umsebenzi wesibindi.

Ezinye izinto ezichaphazela ukukhubazeka kwezidakamizwa zizinto eziphathekayo, ukuveliswa kweziyobisi, ezifana nokukhululwa ngokukhawuleza okanye ukukhululwa ngokukhawuleza, isingqimba somntu we-circadian, ukusebenzisana kwezidakamizwa, ukusebenzisana kokutya, izinga lokusetyenziswa kwe-metabolism (umphumo we-enzyme induction or inhibition nezinye iziyobisi kunye nokutya ), impilo yegciwane lesisu, iminyaka yesigulane, nesigaba sesifo.

Xa isilwanyana silawulwa nge-intravenously, sinokufumaneka kwe-100 ekhulwini (F

Ukuba isicatshulwa sithathwa ngomlomo, sifikela ngokukhawuleza esiswini, sitshabalalisa kwaye enye yaso ibanjwe ngumathumbu omncinci.

Ukususela emathunjini amancinci, uhambela kwi-hepatic portal vein phambi kokuba ufikelele kwi-systemic circulation. Ezinye zezinto ezinokuthintela izidakamizwa ukuba zifikelele kwi-systemic circulation zeziphathamandla zezilwanyana kunye nesimo somzimba wesigulane.

Isilwanyana ezifana ne-benzyl penicillin asikwazi ukujamelana nesimo esiphantsi se-pH esiyichithayo. Ii-enzyme ze-digestive zingonakalisa i-insulin kunye ne-heparin.

Izidakamizwa eziphezulu kakhulu ezingenakucholwa ngokukhawuleza ngenxa yokuba zingenayo i-body fluids, ngelixa izidakamizwa ezinamandla kakhulu-ezikhangela izikhuhlane-ayikwazi ukuwela i-lipid-rich cells membranes.