Iyo hydroxypropyl-β-cyclodextrin yakaoma ye toltrazuril yekusimudzira bioavailability.

Rabbit coccidiosis chirwere chinowanikwa kwose kwose chinokonzerwa nemhando imwe kana kupfuura gumi nenhanhatu dze apicomplexan genus.Eimeria stiedae.1-4General kliniki zviratidzo zvechirwere zvinoratidzirwa nekusagadzikana, kuderedzwa kwekudya kwekudya, manyoka kana kuvhara, kuwedzera kwechiropa, ascites, icterus, dumbu redumbu, uye rufu.3Coccidiosis mutsuro inogona kudzivirirwa uye kurapwa nemishonga.1,3,5,6Toltrazuril (Tol), 1- [3-methyl-4- (4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Mufananidzo 1), iri symmetrical triazinetrione compound iyo inoshandiswa zvakanyanya kudzivirira nekurwisa coccidiosis.7-10Nekudaro, nekuda kwekusagadzikana kweaqueous solubility, Tol inonetsa kubatwa nemudumbu (GI) turakiti. Makiriniki emhedzisiro yeTol yakaderedzwa nekuda kwekunyungudika kwayo muGI turakiti.

Mufananidzo 1 Kemikari chimiro che toltrazuril.

Kunyungudika kwemvura kwakashata kweTol kwakakundwa nedzimwe nzira, dzakaita sekupararira kwakasimba, simba rekupedzisira, uye nanoemulsion.11-13Semaitiro anonyanya kushanda ekuwedzera solubility, Tol solid dispersion yakangowedzera kunyungudika kweTol kusvika ku2,000 nguva,11izvo zvinoratidza kuti kunyungudika kwayo kuchiri kuda kuvandudzwa zvakanyanya kuburikidza nehumwe hunyanzvi. Pamusoro pezvo, kupararira kwakasimba uye nanoemulsion haina kugadzikana uye haina kunetsa kuchengeta, nepo ultrafine simba rinoda hunyanzvi hwekugadzira.

β-cyclodextrin (β-CD) iri kushandiswa kwakapararira nekuda kwehukuru hwayo hwakasiyana-siyana, kushanda kwemishonga yakaoma, uye kuwedzera kwekugadzikana kwezvinodhaka, kunyunguduka, uye bioavailability.14,15Nezvemamiriro ayo ekutonga, β-CD yakanyorwa mune akawanda pharmacopoeia masosi, kusanganisira iyo US Pharmacopoeia/National Formulary, European Pharmacopoeia, uye Japanese Pharmaceutical Codex.16,17Hydroxypropyl–β-CD (HP-β-CD) inotorwa nehydroxyalkyl β-CD inodzidzwa zvakanyanya mumishonga inosanganisirwa yakaoma nekuda kwekugona kwayo kusanganisa uye kunyungudika kwemvura.18-21Toxicologic zvidzidzo zvakashuma nezvekuchengetedzwa kweHP-β-CD mune intravenous uye nemuromo manejimendi kumuviri wemunhu,22uye HP-β-CD yakashandiswa mukuumbwa kwekiriniki kukunda nyaya dzisina kugadzikana uye kuwedzera bioavailability.23

Haisi mishonga yese ine zvivakwa zvekuitwa zvakaomarara neHP-β-CD. Tol akawanikwa aine zvivakwa zvakavakirwa pahuwandu hukuru hwekuongorora basa rekutsvagisa. Kuwedzera kunyungudika uye bioavailability yeTol nekubatanidza kuumbwa kwakaoma neHP-β-CD, toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (Tol-HP-β-CD) yakagadzirirwa nekugadzirisa-kukurudzira nzira muchidzidzo ichi, uye yakaonda. -layer chromatography (TLC), Fourier inoshandura infrared (FTIR) spectroscopy, uye nyukireya magnetic resonance (NMR) spectroscopy yakashandiswa kuratidza yakawanikwa Tol-HP-β-CD. Iyo pharmacokinetic profiles yeTol uye Tol-HP-β-CD mutsuro mushure mekutonga nemuromo yakawedzera kuenzaniswa mu vivo.


Nguva yekutumira: Nov-11-2021