Luav coccidiosis yog kab mob ubiquitous tshwm sim los ntawm ib los yog ntau tshaj ntawm 16 hom ntawm apicomplexan genusEimeria stiedae.^1-4Cov tsos mob ntawm tus kab mob no tshwm sim los ntawm dullness, txo cov zaub mov noj, raws plab los yog cem quav, daim siab o, ascites, icterus, mob plab, thiab tuag.³Coccidiosis hauv luav tuaj yeem tiv thaiv thiab kho siv tshuaj.^1,3,5,6Toltrazuril (Tol), 1-[3-methyl-4-(4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Daim duab 1), yog ib qho symmetrical triazinetrione compound uas yog dav siv los tiv thaiv thiab tiv thaiv coccidiosis.^7-10Txawm li cas los xij, vim tsis muaj dej tsis zoo, Tol yog qhov nyuaj rau kev nqus los ntawm txoj hnyuv (GI). Cov teebmeem kev kho mob ntawm Tol tau raug txo qis vim nws cov solubility hauv GI ib puag ncig.

Daim duab 1 Cov qauv tshuaj ntawm toltrazuril.

Qhov tsis zoo aqueous solubility ntawm Tol tau kov yeej los ntawm qee cov tswv yim, xws li cov khoom tawg, lub zog ultrafine, thiab nanoemulsion.^11-13Raws li tam sim no cov txheej txheem ua tau zoo tshaj plaws rau kev nce solubility, Tol khoom dispersion tsuas yog nce lub solubility ntawm Tol mus rau 2,000 zaug,¹¹uas qhia tau hais tias nws cov solubility tseem yuav tsum tau kho kom zoo dua los ntawm lwm cov txheej txheem. Tsis tas li ntawd, cov khoom dispersion thiab nanoemulsion tsis ruaj khov thiab tsis yooj yim rau khaws cia, thaum lub zog ultrafine xav tau cov cuab yeej ntse los tsim.

β-cyclodextrin (β-CD) yog nyob rau hauv kev siv dav vim nws cov kab noj hniav tshwj xeeb, kev ua haujlwm ntawm cov tshuaj complexation, thiab txhim kho cov tshuaj stability, solubility, thiab bioavailability.^14,15Rau nws txoj cai tswjfwm, β-CD tau teev nyob rau hauv ntau qhov chaw muag tshuaj, suav nrog US Pharmacopoeia / National Formulary, European Pharmacopoeia, thiab Japanese Pharmaceutical Codex.^16,17Hydroxypropyl-β-CD (HP-β-CD) yog hydroxyalkyl β-CD derivative uas tau kawm ntau hauv cov tshuaj suav nrog vim nws muaj peev xwm suav nrog thiab dej solubility siab.^18-21Cov kev tshawb fawb Toxicology tau tshaj tawm txog kev nyab xeeb ntawm HP-β-CD hauv kev tswj hwm qhov ncauj thiab qhov ncauj rau tib neeg lub cev,²²thiab HP-β-CD tau siv rau hauv kev kho mob formulations kom kov yeej cov teeb meem solubility tsis zoo thiab txhim kho bioavailability.²³

Tsis yog txhua yam tshuaj muaj peev xwm ua rau muaj kev sib txuam nrog HP-β-CD. Tol tau pom tias muaj cov khoom siv raws li ntau ntawm kev tshuaj ntsuam xyuas ua haujlwm. Txhawm rau ua kom cov solubility thiab bioavailability ntawm Tol los ntawm kev sib xyaw ua ke nrog HP-β-CD, toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (Tol-HP-β-CD) tau npaj los ntawm txoj kev daws teeb meem hauv txoj kev tshawb no, thiab nyias. -layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy, thiab nuclear magnetic resonance (NMR) spectroscopy tau ua hauj lwm los qhia qhov tau txais Tol-HP-β-CD. Cov tshuaj pharmacokinetic profiles ntawm Tol thiab Tol-HP-β-CD hauv luav tom qab kev tswj hwm qhov ncauj tau muab piv rau hauv vivo.