Ukutholakala kwe-bioavailability kanye ne-bioquivalence kokubili amagama asetshenziselwa ukwelashwa ukuchaza izenzo nezakhiwo ezithile zomkhiqizo wezidakamizwa.
I-bioavailability ichaza umuntu we-dose ephathekayo yalokho esetshenziselwa ukujikeleza esegazini lapho umuthi uhanjiswa ngomlomo, nge-intravenously noma nganoma iyiphi enye indlela (isb., Ama-rectal, izinhlamvu ezingezansi, ama-nasal, transdermal, njll)
Ngencazelo, izidakamizwa ezihanjiswe ngaphakathi zikhona ukutholakala kwe-100% ngoba ihanjiswa ngqo egazini.
Kunezici eziningi ezingathinta ukutholakala kwezidakamizwa. Zihlanganisa phakathi kwezinye izinto:
- Izakhiwo zomzimba zalesi sidakamizwa, kuhlanganise nezidakamizwa zempilo
- Ukwakhiwa kwezidakamizwa (isib. Ukukhululwa ngokushesha, ukukhululwa kwesikhathi)
- Impilo yomzimba yesiguli
- Ubudala besiguli, okungasithinta ijubane lokudakwa kwezidakamizwa
- Kungakhathaliseki ukuthi isidakamizwa sithathwe noma ngaphandle kokudla
- I-Renal (izinso) nomsebenzi we-hepatic (isibindi), othembisa ukunikezwa kwezidakamizwa
Ukusebenzisana nezinye izidakamizwa noma ukudla kungaphazamisa ngokuqondile ukutholakala kwemvelo. Ngokwelashwa kwegciwane lesandulela ngculaza nengculaza , isibonelo, imithi ye - antiretroviral Norvir (ritonavir) -yasetshenziselwa "ukukhulisa" ukuxilongwa kwezidakamizwa ze-serum yezinye izidakamizwa ze-HIV- kungabuye kwandise ukutholakala kwemithi efana ne- Viagra (sildenafil citrate) . Ngokwenza kanjalo, kungakwazi kakhulu ukunweba ingxenye yokuphila kweViagra ngenkathi kukhuliswa imiphumela emibi.
Ngakolunye uhlangothi, i-anti-magnesium- ne-aluminium-based antacids (njenge-Tums noma iMilk Magnesia) inganciphisa kakhulu ukutholakala kwezidakamizwa eziningi ze-HIV lapho kuthathwa ngesikhathi esisodwa - kuze kube ngu-74% ngezidakamizwa ezifana ne- Tivicay (dolutegravir) - futhi, ngokwenza kanjalo, kungase kube yilapho kunciphise imigomo yokwelapha.
I-bioequivalence yigama elisetshenziselwa imithi yezokwelapha ukuchaza imikhiqizo emibili yezidakamizwa ezihlukene, ezisekelwe ekusebenzeni kwazo kanye nokuphepha, zifana ngokufanayo.
I-US Food and Drug Administration (i-FDA) ichaza i-bioquivalence ngokuthi "ukungabi khona kwemehluko ephawulekayo ngesilinganiso nokulinganisa ukuthi isithako esisebenzayo noma ingxenye esebenzayo emithini yokulinganisa imithi noma ezinye izindlela zokwelapha zizotholakala esiteshini sesenzo sezidakamizwa uma kulawulwa umthamo olinganayo wezimiso ngaphansi kwezimo ezifanayo esifundweni esenziwe ngokufanele. "
Ukutholakala kwe-biovailability kanye ne-bioquivalence kuhlobene ngokuqondile ngokuhambisana nokuhlaziywa kwezihlobo (okusho ukuthi ukuhlaziywa komuthi owodwa kufana nokunye) kungenye yezinyathelo ezisetshenziselwa ukuhlola i-bioquivalency yezidakamizwa.
Ukuze kuvunyelwe i-FDA, imithi ejwayelekile kufanele ikhombise isikhala sokuzithemba se-90% (CI) kokubili kanye nesilinganiso sokutholakala kwezinto eziphilayo uma kuqhathaniswa neyomuthi ovela kuwo, isibheke.
> Imithombo:
> Muirhead, G .; UWuff, M .; Fielding, A .; et al. "Ukusebenzisana kwama-pharmacokinetic phakathi kwe-sildenafil ne-saquinavir / ritonavir." I-British Journal ye-Clinical Pharmacology. Agasti 2000; 50 (2): 99-107.
> Ingoma, I .; Borland, J .; I-Arya, N .; et al. "Umphumela we-calcium nezinsiza ze-iron kwi-pharmacokinetics ye- dolutegravir > ezifundweni ezinempilo." I-15th International Workshop e-Clinical Pharmacology ye-HIV ne-Hepatitis Therapy; Washington, DC; May 19-21, 2014; abstract P_13.
> Ukuphathwa Kwezokudla Nezidakamizwa zase-US (FDA). "Isiqondiso Sezezimboni: Ukutholakala Kwezinto Eziphilayo kanye Neziqu ze-Bioequivalence zeMikhiqizo Yezokwelapha Ezilawulwa Ngokwemvelo - Ukucatshangelwa Okuvamile." I-Silver Springs, e-Maryland.