Ole hydroxypropyl-β-cyclodextrin lavelave ole toltrazuril mo le faʻaleleia o le bioavailability

Lapiti coccidiosis o se fa'ama'i so'o se mea e mafua mai i le tasi pe sili atu fo'i o ituaiga e 16 o le apicomplexan genus.Eimeria stiedae.14O faʻamaoniga lautele o le faʻamaʻi o le faʻamaʻi o loʻo faʻaalia i le faʻamaʻi, faʻaitiitia le taumafaina o meaʻai, manava manava poʻo le maʻi, faʻateleina o le ate, ascites, icterus, faʻamaʻi manava, ma le oti.3Coccidiosis i lapiti e mafai ona puipuia ma togafitia i le faʻaaogaina o vailaʻau.1,3,5,6Toltrazuril (Tol), 1-[3-methyl-4-(4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Ata 1), o se fa'aupuga triazinetrione tutusa e fa'aaogaina lautele e puipuia ma fa'afefe ai le coccidiosis.710Ae peitai, ona o le le lelei o le solubility i le vai, e faigata ona mitiia Tol e le gastrointestinal (GI) tract. O a'afiaga fa'afoma'i a Tol ua fa'aitiitia ona o lona solu i totonu ole GI tract.

Ata 1 Fa'asologa o vaila'au o le toltrazuril.

O le leaga o le solubility aqueous o Tol ua faatoilaloina e nisi o metotia, e pei o le solo solo, malosi ultrafine, ma nanoemulsion.1113I le avea ai ma auala sili ona aoga mo le faʻateleina o le solubility, o le faʻasalalau malosi o Tol naʻo le faʻateleina o le solubility o Tol i le 2,000 taimi,11lea e fa'ailoa mai ai o lona solubility e mana'omia pea ona fa'aleleia atili e ala i isi metotia. E le gata i lea, o le dispersion malosi ma le nanoemulsion e le mautu ma e le faigofie ona teuina, ae o le mana ultrafine e manaʻomia meafaigaluega faʻapitoa e gaosia.

β-cyclodextrin (β-CD) o loʻo faʻaaogaina lautele ona o lona tulaga faʻapitoa o le lua, lelei o le faʻalavelave faʻasaina, ma le faʻaleleia atili o le mautu o vailaʻau, solubility, ma le bioavailability.14,15Mo lona tulaga fa'atulafonoina, β-CD o lo'o lisiina i le tele o puna'oa mo vaila'au, e aofia ai le US Pharmacopoeia/National Formulary, European Pharmacopoeia, ma le Japanese Pharmaceutical Codex.16,17O le Hydroxypropyl-β-CD (HP-β-CD) o le hydroxyalkyl β-CD o loʻo suʻesuʻeina tele i totonu o vailaʻau faʻalavelave faʻalavelave ona o lona gafatia faʻapipiʻi ma le maualuga o le vai.1821O suʻesuʻega toxicologic ua lipotia mai i luga o le saogalemu o le HP-β-CD i totonu o le toto ma le tautala i le tino o le tagata,22ma le HP-β-CD ua faʻaaogaina i faʻataʻitaʻiga falemaʻi e foia ai faʻafitauli le lelei o le solubility ma faʻaleleia ai le bioavailability.23

E le o vaila'au uma e iai ni meatotino e fa'apipi'i fa'atasi ma le HP-β-CD. Na maua e Tol ia meatotino e fa'atatau i le tele o galuega su'esu'e. Ina ia faʻateleina le solubility ma le bioavailability o Tol e ala i le faʻapipiʻiina o faʻalavelave faʻalavelave faʻatasi ma le HP-β-CD, toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (Tol-HP-β-CD) na saunia e ala i fofo-faʻaosoina metotia i lenei suʻesuʻega, ma manifinifi. -Layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy, ma le nuclear magnetic resonance (NMR) spectroscopy na faʻaaogaina e faʻamaonia ai. le Tol-HP-β-CD na maua. O faʻamatalaga pharmacokinetic o Tol ma Tol-HP-β-CD i lapiti pe a maeʻa le tuʻu gutu na faʻatusatusa atili i vivo.


Taimi meli: Nov-11-2021