Haɗaɗɗen hydroxypropyl-β-cyclodextrin na toltrazuril don haɓaka bioavailability

Rabbit coccidiosis cuta ce ta ko'ina ta haifar da ɗayan ko fiye na nau'ikan 16 na apicomplexan.Eimeria stiedae.1-4Gabaɗaya alamomin cutar na cutar suna nuna rashin ƙarfi, rage cin abinci, zawo ko maƙarƙashiya, haɓakar hanta, ascites, icterus, ɓacin ciki, da mutuwa.3Coccidiosis a cikin zomaye za a iya hanawa da kuma bi da su ta amfani da kwayoyi.1,3,5,6Toltrazuril (Tol), 1-[3-methyl-4- (4-trifluoromethylsulfanyl-phenoxy) -phenyl] -3-methyl-1,3,5-triazin-2,4,6-trioneHoto 1), wani fili ne na triazinetrione mai ma'ana wanda aka yi amfani da shi sosai don rigakafi da magance coccidiosis.7-10Duk da haka, saboda rashin ƙarfi na ruwa, Tol yana da wuya a sha shi ta hanyar gastrointestinal (GI). Sakamakon asibiti na Tol an rage shi saboda rashin narkewa a cikin sashin GI.

Hoto 1 Tsarin sinadarai na toltrazuril.

Wasu fasahohi sun shawo kan ƙarancin ruwa mai ƙarfi na Tol, kamar tarwatsewa mai ƙarfi, ƙarfin ultrafine, da nanoemulsion.11-13Kamar yadda a halin yanzu mafi inganci dabaru don ƙara solubility, Tol m watsawa kawai ƙara solubility na Tol zuwa 2,000 sau.11wanda ke nuni da cewa har yanzu ana bukatar a inganta karfinta ta hanyar wasu dabaru. Bugu da kari, m watsawa da nanoemulsion ne m kuma m don adana, yayin da ultrafine ikon bukatar sophisticated kayan aiki don samar.

β-cyclodextrin (β-CD) yana cikin amfani da yawa saboda girmansa na musamman, ingantaccen hadadden magani, da haɓaka kwanciyar hankali na miyagun ƙwayoyi, solubility, da bioavailability.14,15Don matsayin tsarin sa, an jera β-CD a cikin maɓuɓɓugan magunguna masu yawa, gami da US Pharmacopoeia/National Formulary, European Pharmacopoeia, da Jafananci Pharmaceutical Codex.16,17Hydroxypropyl-β-CD (HP-β-CD) wani nau'in hydroxyalkyl β-CD ne wanda aka yi nazari sosai a cikin hadaddun hada magunguna saboda iyawar sa da kuma babban narkewar ruwa.18-21Nazarin toxicologic sun ba da rahoto game da amincin HP-β-CD a cikin intravenous da gudanarwa na baka ga jikin mutum,22kuma an yi amfani da HP-β-CD a cikin ƙirar asibiti don shawo kan matsalolin rashin ƙarfi mara kyau da haɓaka bioavailability.23

Ba duk magunguna ba ne ke da kaddarorin da za a yi su zama hadaddun tare da HP-β-CD. An gano Tol ya mallaki kaddarorin bisa babban adadin aikin bincike na nunawa. Don ƙara solubility da bioavailability na Tol ta hada hadaddun samuwar tare da HP-β-CD, toltrazuril-hydroxypropyl-β-cyclodextrin hada hadaddun hadaddun (Tol-HP-β-CD) da aka shirya ta hanyar warware-tafiya hanya a cikin wannan binciken, kuma bakin ciki. -Layer chromatography (TLC), Fourier canza infrared (FTIR) spectroscopy, da makaman nukiliya maganadisu (NMR) spectroscopy sun kasance. aiki don siffata samu Tol-HP-β-CD. Bayanan pharmacokinetic na Tol da Tol-HP-β-CD a cikin zomaye bayan gudanar da baki an kara kwatanta su a cikin vivo.


Lokacin aikawa: Nuwamba 11-2021