Ehoro coccidiosis jẹ arun ti gbogbo ibi ti o ṣẹlẹ nipasẹ ọkan tabi diẹ ẹ sii ti awọn eya 16 ti iwin apicomplexan.Eimeria stiedae.^1–4Awọn aami aisan gbogbogbo ti arun na jẹ ijuwe nipasẹ ṣigọgọ, idinku lilo ounjẹ, gbuuru tabi àìrígbẹyà, gbooro ẹdọ, ascites, icterus, distention inu, ati iku.³Coccidiosis ninu awọn ehoro le ṣe idiwọ ati tọju pẹlu lilo awọn oogun.^1,3,5,6Toltrazuril (Tol), 1- [3-methyl-4- (4-trifluoromethylsulfanyl-phenoxy) -phenyl] -3-methyl-1,3,5-triazin-2,4,6-trioneOlusin 1), jẹ iṣiro triazinetrione asymmetrical ti o jẹ lilo pupọ lati ṣe idiwọ ati koju coccidiosis.^7–10Bibẹẹkọ, nitori solubility olomi ti ko dara, Tol nira lati gba nipasẹ ọna ikun ati inu (GI). Awọn ipa ile-iwosan ti Tol ti jẹ ẹdinwo nitori iyọkuro rẹ ninu aaye GI.

Aworan 1 Kemikali be ti toltrazuril.

Solubility olomi ti ko dara ti Tol ti bori nipasẹ diẹ ninu awọn ilana, gẹgẹbi pipinka ti o lagbara, agbara ultrafine, ati nanoemulsion.^11–13Gẹgẹbi awọn imọ-ẹrọ ti o munadoko julọ lọwọlọwọ fun jijẹ solubility, pipinka to lagbara Tol nikan pọ si solubility ti Tol si awọn akoko 2,000,¹¹eyi ti o tọkasi wipe awọn oniwe-solubility si tun nilo lati wa ni imudara significantly nipasẹ miiran imuposi. Ni afikun, pipinka to lagbara ati nanoemulsion jẹ riru ati korọrun lati fipamọ, lakoko ti agbara ultrafine nilo ohun elo fafa lati gbejade.

β-cyclodextrin (β-CD) wa ni lilo ni ibigbogbo nitori iwọn iho alailẹgbẹ rẹ, ṣiṣe ti idiju oogun, ati awọn imudara ti iduroṣinṣin oogun, solubility, ati bioavailability.^14,15Fun ipo ilana rẹ, β-CD jẹ atokọ ni ọpọlọpọ awọn orisun pharmacopoeia, pẹlu US Pharmacopoeia/Formulary National, European Pharmacopoeia, ati Codex Pharmaceutical Japanese.^16,17Hydroxypropyl-β-CD (HP-β-CD) jẹ itọsẹ hydroxyalkyl β-CD ti a ṣe iwadi ni pipọ ni eka ifisi oogun nitori agbara ifisi ati omi solubility giga.^18–21Awọn ijinlẹ Toxicologic ti royin lori aabo ti HP-β-CD ninu iṣọn-ẹjẹ ati awọn iṣakoso ẹnu si ara eniyan,²²ati HP-β-CD ti lo ni awọn agbekalẹ ile-iwosan lati bori awọn ọran solubility ti ko dara ati imudara bioavailability.²³

Kii ṣe gbogbo awọn oogun ni awọn ohun-ini lati ṣe si eka pẹlu HP-β-CD. A rii Tol lati ni awọn ohun-ini ti o da lori nọmba nla ti iṣẹ iwadii iboju. Lati mu solubility ati bioavailability ti Tol pọ si nipa ifisi idasile eka pẹlu HP-β-CD, toltrazuril – hydroxypropyl – β-cyclodextrin inclusion complex (Tol-HP-β-CD) ni a pese sile nipasẹ ọna idarudapọ ojutu ninu iwadi yii, ati tinrin. -Layer chromatography (TLC), Fourier transform infurarẹẹdi (FTIR) spectroscopy, ati iparun se resonance (NMR) spectroscopy wà ṣiṣẹ lati ṣe apejuwe Tol-HP-β-CD ti o gba. Awọn profaili pharmacokinetic ti Tol ati Tol-HP-β-CD ninu awọn ehoro lẹhin iṣakoso ẹnu ni a ṣe afiwe siwaju ni vivo.