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已发表论文
妥曲珠利的羟丙基-β-环糊精复合物可用于提高生物利用度
Authors Zhang L, Liu MX, Lu CC, Ren DD, Fan GQ, Liu C, Liu MJ, Shu G, Peng GN, Yuan ZX, Zhong ZJ, Zhang W, Fu HL
Received 20 November 2017
Accepted for publication 14 December 2017
Published 19 March 2018 Volume 2018:12 Pages 583—589
DOI https://doi.org/10.2147/DDDT.S157611
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Palas Chanda
Peer reviewer comments 2
Editor who approved publication: Dr Qiongyu Guo
Introduction: Toltrazuril (Tol) is
used to prevent and combat coccidiosis. However, its low aqueous solubility and
poor oral bioavailability limit clinical application.
Methods: To overcome the shortcomings, toltrazuril–hydroxypropyl–β-cyclodextrin inclusion complex (Tol-HP-β-CD) was prepared and characterized. The comparative plasma disposition kinetics of Tol was analyzed after a single orally administered dose of 10 mg/kg Tol or Tol-HP-β-CD in rabbits. Solution-stirring method was selected to prepare the inclusion complex. Complex formation was characterized by thin-layer chromatography, Fourier transform infrared spectrophotometry, and 1H nuclear magnetic resonance spectroscopy. In plasma profile, plasma samples were collected between 1 and 10 days following administration. Plasma Tol concentrations were determined by high-performance liquid chromatography.
Results: In rabbit plasma, the time to peak concentration (T max) of Tol-HP-β-CD was shorter than that of Tol (12 h vs 24 h). C max (19.92±1.02 µg/mL) and area under the concentration–time curve (AUC0-∞, 1,176.86±70.26 mg/L h) of the Tol-HP-β-CD group significantly increased (p <0.01) than those of the Tol group (C max, 8.02±1.04 µg/mL; AUC0-∞, 514.03±66.65 mg/L h).
Conclusion: It can be concluded that the Tol-HP-β-CD increased the aqueous solubility and enhanced the oral bioavailability in rabbits. Complexation with HP-β-CD is a feasible way to prepare a rapidly absorbed and more bioavailable Tol oral product.
Keywords: toltrazuril, coccidian, hydroxypropyl–β-cyclodextrin, inclusion complex, pharmacokinetics
Methods: To overcome the shortcomings, toltrazuril–hydroxypropyl–β-cyclodextrin inclusion complex (Tol-HP-β-CD) was prepared and characterized. The comparative plasma disposition kinetics of Tol was analyzed after a single orally administered dose of 10 mg/kg Tol or Tol-HP-β-CD in rabbits. Solution-stirring method was selected to prepare the inclusion complex. Complex formation was characterized by thin-layer chromatography, Fourier transform infrared spectrophotometry, and 1H nuclear magnetic resonance spectroscopy. In plasma profile, plasma samples were collected between 1 and 10 days following administration. Plasma Tol concentrations were determined by high-performance liquid chromatography.
Results: In rabbit plasma, the time to peak concentration (T max) of Tol-HP-β-CD was shorter than that of Tol (12 h vs 24 h). C max (19.92±1.02 µg/mL) and area under the concentration–time curve (AUC0-∞, 1,176.86±70.26 mg/L h) of the Tol-HP-β-CD group significantly increased (p <0.01) than those of the Tol group (C max, 8.02±1.04 µg/mL; AUC0-∞, 514.03±66.65 mg/L h).
Conclusion: It can be concluded that the Tol-HP-β-CD increased the aqueous solubility and enhanced the oral bioavailability in rabbits. Complexation with HP-β-CD is a feasible way to prepare a rapidly absorbed and more bioavailable Tol oral product.
Keywords: toltrazuril, coccidian, hydroxypropyl–β-cyclodextrin, inclusion complex, pharmacokinetics
