I-Rabbit coccidiosis sisifo esixhaphakileyo esibangelwa yintlobo enye okanye ngaphezulu kwezili-16 ze-apicomplexan genus.Eimeria stiedae.^1-4Iimpawu zeklinikhi eziqhelekileyo zesi sifo zibonakaliswa bubuthuntu, ukunciphisa ukusetyenziswa kokutya, isifo sohudo okanye ukuqunjelwa, ukwanda kwesibindi, i-ascites, i-icterus, i-distention yesisu kunye nokufa.³I-Coccidiosis kwimivundla inokuthintelwa kwaye inyangwe ngokusebenzisa amayeza.^1,3,5,6I-Toltrazuril (iTol), 1-[3-methyl-4- (4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Umfanekiso woku-1), i-symmetrical triazinetrione compound esetyenziswa ngokubanzi ukukhusela kunye nokulwa ne-coccidiosis.^7-10Nangona kunjalo, ngenxa yokunganyibiliki kakuhle kwamanzi, iTol kunzima ukufunxwa yiphecana lesisu (GI). Iziphumo zeklinikhi zeTol ziye zathotywa ngenxa yokunyibilika kwayo kwiphecana le-GI.

Umzobo 1 Isakhiwo seKhemikhali se-toltrazuril.

Ukunyibilika okulambathayo kwe-aqueous kwe-Tol kuye koyiswa zezinye iindlela, ezinje ngokusasazwa okuqinileyo, amandla e-ultrafine, kunye ne-nanoemulsion.^11-13Njengezona ndlela zisebenzayo ngoku zokwandisa ukunyibilika, ukusasazwa okuqinileyo kweTol kwandisa kuphela ukunyibilika kweTol ukuya kumaxesha angama-2,000,¹¹ebonisa ukuba ukunyibilika kwayo kusafuna ukuphuculwa kakhulu ngezinye iindlela. Ukongezelela, i-dispersion eqinile kunye ne-nanoemulsion ayizinzile kwaye ayinzima ukuyigcina, ngelixa amandla e-ultrafine adinga izixhobo eziyinkimbinkimbi ukuvelisa.

I-β-cyclodextrin (β-CD) isetyenziswa ngokubanzi ngenxa yobukhulu bayo obukhethekileyo bomgodi, ukusebenza kakuhle kobunzima beziyobisi, kunye nokuphucula ukuzinza kweziyobisi, ukunyibilika, kunye ne-bioavailability.^14,15Kwimeko yayo yokulawula, i-β-CD idweliswe kwimithombo emininzi ye-pharmacopoeia, kubandakanywa ne-US Pharmacopoeia / i-National Formulary, i-European Pharmacopoeia, kunye ne-Japan Pharmaceutical Codex.^16,17I-Hydroxypropyl–β-CD (HP-β-CD) yi-hydroxyalkyl β-CD derivative ephononongwa ngokubanzi kwi-complex yokufakwa kweziyobisi ngenxa yokukwazi ukubandakanywa kunye nokunyibilika kwamanzi okuphezulu.^18-21Izifundo ze-Toxicologic ziye zabika malunga nokhuseleko lwe-HP-β-CD kwi-intravenous kunye nokulawulwa ngomlomo kumzimba womntu,²²kunye ne-HP-β-CD isetyenziswe kwimixube yekliniki ukoyisa imiba yokunyibilika okulambathayo kunye nokuphucula ukufumaneka kwezinto eziphilayo.²³

Ayingawo onke amachiza aneempawu ekumele enziwe abe nzima nge-HP-β-CD. I-Tol yafunyanwa ineepropati ezisekelwe kwinani elikhulu lomsebenzi wokuhlola uphando. Ukwandisa i-solubility kunye ne-bioavailability ye-Tol ngokubandakanya ukubunjwa kwe-complex kunye ne-HP-β-CD, i-toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (i-Tol-HP-β-CD) yalungiswa ngendlela yokuvuselela isisombululo kule sifundo, kwaye incinci. -Layer chromatography (TLC), iFourier transform infrared (FTIR) spectroscopy, kunye nenuclear magnetic resonance (NMR) I-spectroscopy yasetyenziselwa ukubonakalisa i-Tol-HP-β-CD efunyenweyo. Iiprofayili ze-pharmacokinetic ze-Tol kunye ne-Tol-HP-β-CD kwimivundla emva kokulawulwa komlomo zifaniswa ngakumbi kwi-vivo.