ʻO ka coccidiosis rabbit kahi maʻi maʻamau i hoʻokumu ʻia e hoʻokahi a ʻoi aku paha o 16 mau ʻano o ka genus apicomplexan.Eimeria stiedae.^1–4Hōʻike ʻia nā hōʻailona lapaʻau maʻamau o ka maʻi e ka ʻūlū, hoʻemi ʻia ka ʻai ʻana i ka meaʻai, ka maʻi maʻi a i ʻole ka constipation, ka hoʻonui ʻana o ke akepaʻa, ascites, icterus, distention abdominal, a me ka make.³Hiki ke pale a mālama ʻia ka coccidiosis me ka lāʻau lapaʻau.^1,3,5,6Toltrazuril (Tol), 1-[3-methyl-4-(4-trifluoromethylsulfanyl-phenoxy)-phenyl]-3-methyl-1,3,5-triazin-2,4,6-trione (Helu 1), he pūhui triazinetrione symmetrical i hoʻohana nui ʻia e pale a hakakā i ka coccidiosis.^7–10Eia nō naʻe, ma muli o ka hoʻoheheʻe ʻana i ka wai, paʻakikī ke komo ʻana o Tol e ka ʻāpana ʻōpū (GI). Ua hōʻemi ʻia nā hopena lapaʻau o Tol ma muli o kona solubility i ka ʻāpana GI.

Kiʻi 1 ʻO ke kinona o ka toltrazuril.

Ua lanakila ʻo Tol e kekahi mau ʻenehana, e like me ka dispersion paʻa, ka mana ultrafine, a me ka nanoemulsion.^11–13ʻOiai ʻo nā ʻenehana maikaʻi loa i kēia manawa no ka hoʻonui ʻana i ka solubility, ʻo Tol solid dispersion i hoʻonui i ka solubility o Tol i 2,000 mau manawa,¹¹e hōʻike ana he pono e hoʻonui nui ʻia kona solubility ma o nā ʻenehana ʻē aʻe. Eia kekahi, ʻo ka dispersion paʻa a me ka nanoemulsion ʻaʻole paʻa a paʻakikī hoʻi e mālama, ʻoiai ʻo ka mana ultrafine e pono ai nā mea hana maʻalahi e hana ai.

Hoʻohana nui ʻia ka β-cyclodextrin (β-CD) ma muli o ka nui o ka lua kū hoʻokahi, ka pono o ka paʻakikī o ka lāʻau, a me ka hoʻonui ʻana i ka paʻa o ka lāʻau, solubility, a me ka bioavailability.^14,15No kona kūlana hoʻoponopono, helu ʻia ka β-CD ma nā kumu lāʻau lapaʻau he nui, me ka US Pharmacopoeia/National Formulary, European Pharmacopoeia, a me Japanese Pharmaceutical Codex.^16,17ʻO ka Hydroxypropyl-β-CD (HP-β-CD) he hydroxyalkyl β-CD derivative i aʻo nui ʻia i loko o ka paʻakikī hoʻohui lāʻau ma muli o kona hiki ke hoʻokomo a me ka wai kiʻekiʻe.^18–21Ua hōʻike ʻia nā haʻawina Toxicologic e pili ana i ka palekana o ka HP-β-CD i loko o nā lawelawe intravenous a me ka waha i ke kino kanaka,²²a ua hoʻohana ʻia ʻo HP-β-CD i loko o nā hoʻolālā lapaʻau e lanakila ai i nā pilikia solubility maikaʻi ʻole a hoʻonui i ka bioavailability.²³

ʻAʻole loaʻa nā waiwai i nā lāʻau a pau e hana paʻakikī me HP-β-CD. Ua ʻike ʻia ʻo Tol i nā waiwai e pili ana i ka nui o ka hana noiʻi screening. No ka hoʻonui ʻana i ka solubility a me ka bioavailability o Tol ma o ka hoʻokumu ʻana i ka paʻakikī me HP-β-CD, ua hoʻomākaukau ʻia ka toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex (Tol-HP-β-CD) ma ke ʻano hoʻonā hoʻonā i kēia haʻawina, a lahilahi. -layer chromatography (TLC), Fourier transform infrared (FTIR) spectroscopy, a me ka nuclear magnetic resonance (NMR) spectroscopy i hoʻohana ʻia e hōʻike. ka Tol-HP-β-CD i loaʻa. Ua hoʻohālikelike hou ʻia nā ʻōlelo pharmacokinetic o Tol a me Tol-HP-β-CD i nā rabbit ma hope o ka lawelawe waha i loko o vivo.