Motsoako oa hydroxypropyl-β-cyclodextrin oa toltrazuril bakeng sa ho ntlafatsa bioavailability

Rabbit coccidiosis ke lefu le atileng hohle le bakoang ke mofuta o le mong kapa ho feta ho tse 16 tsa mofuta oa apicomplexan.Eimeria stiedae.1-4Matšoao a tloaelehileng a kliniki ea lefu lena a khetholloa ke ho ba lerootho, ho fokotsa tšebeliso ea lijo, letšollo kapa ho patoa, ho atolosoa ha sebete, ascites, icterus, ho senya mpa le lefu.3Coccidiosis ho meutlanyana e ka thibeloa le ho phekoloa ka ho sebelisa lithethefatsi.1,3,5,6Toltrazuril (Tol), 1-[3-methyl-4-(4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Setšoantšo sa 1), ke motsoako oa symmetrical triazinetrione o sebelisoang haholo ho thibela le ho loantša coccidiosis.7-10Leha ho le joalo, ka lebaka la ho fokola ha metsi a qhibilihang, Tol e thata ho monngoa ke pampitšana ea gastrointestinal (GI). Litlamorao tsa bongaka tsa Tol li theotsoe ka lebaka la ho qhibiliha ha eona pampitšaneng ea GI.

Setšoantšo sa 1 Sebopeho sa lik'hemik'hale sa toltrazuril.

Ho qhibiliha ho fokolang ha metsi ha Tol ho hlōtsoe ke mekhoa e meng, e kang ho hasana ho tiileng, matla a ultrafine, le nanoemulsion.11-13Joalo ka mekhoa e sebetsang ka ho fetesisa ea ho eketsa solubility, Tol solid dispersion e ekelitse feela ho qhibiliha ha Tol ho makhetlo a 2,000,11e bontšang hore ho qhibiliha ha eona ho ntse ho hloka ho ntlafatsoa haholo ka mekhoa e meng. Ho phaella moo, ho qhalakanngoa ho tiileng le nanoemulsion ha ho tsitsa ebile ha ho bonolo ho boloka, ha matla a ultrafine a hloka lisebelisoa tse rarahaneng ho hlahisa.

β-cyclodextrin (β-CD) e sebelisoa haholo ka lebaka la boholo ba eona bo ikhethang ba sekoti, katleho ea ho rarahana ha lithethefatsi, le ho ntlafatsa botsitso ba lithethefatsi, ho qhibiliha, le bioavailability.14,15Bakeng sa boemo ba eona ba taolo, β-CD e thathamisitsoe mehloling e mengata ea pharmacopoeia, ho kenyelletsa le US Pharmacopoeia/National Formulary, European Pharmacopoeia, le Japanese Pharmaceutical Codex.16,17Hydroxypropyl–β-CD (HP-β-CD) ke motsoako oa hydroxyalkyl β-CD o ithutoang haholo ka ho kenyelletsa lithethefatsi ka lebaka la bokhoni ba eona ba ho kenyelletsa le ho qhibiliha ha metsi ho phahameng.18-21Lithuto tsa Toxicologic li tlalehile ka polokeho ea HP-β-CD tsamaisong ea methapo le ea molomo ho 'mele oa motho,22le HP-β-CD e 'nile ea sebelisoa mefuteng ea meriana ho hlōla mathata a fokolang a ho qhibiliha le ho matlafatsa bioavailability.23

Ha se litlhare tsohle tse nang le thepa e lokelang ho etsoa e rarahaneng ka HP-β-CD. Tol o ile a fumanoa a e-na le thepa e ipapisitseng le palo e kholo ea mosebetsi oa ho etsa lipatlisiso. Ho eketsa solubility le bioavailability ea Tol ka ho kenyelletsa sebopeho se rarahaneng le HP-β-CD, toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (Tol-HP-β-CD) e ile ea lokisetsoa ka mokhoa oa ho hlohlelletsa tharollo thutong ena, 'me e tšesaane. -layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy, le nuclear magnetic resonance (NMR) spectroscopy e ile ea sebelisoa ho khetholla Tol-HP-β-CD e fumanoeng. Lintlha tsa pharmacokinetic tsa Tol le Tol-HP-β-CD ka mebutlanyana ka mor'a tsamaiso ea molomo li ile tsa bapisoa le ho feta ka vivo.


Nako ea poso: Nov-11-2021