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地克珠利口服制剂在家兔体内的药动学研究

胡连栋1*, 刘慈1, 徐文2   

  1. 1. 河北大学药学院, 河北 保定 071002
    2. 第二军医大学长征医院 药学部, 上海 200003
  • 收稿日期:2009-06-07 修回日期:2009-08-10 出版日期:2009-09-15 发布日期:2009-09-15
  • 通讯作者: 胡连栋*

Pharmacokinetics of diclazuril after oral administration of clinical doses to rabbits

Lian-Dong Hu1*, Ci Liu1, Wen Xu2   

  1. 1. College of Pharmacy, Hebei University, Baoding 071002, China
    2. Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China
  • Received:2009-06-07 Revised:2009-08-10 Online:2009-09-15 Published:2009-09-15
  • Contact: Lian-Dong Hu*

摘要: 本实验中采用高效液相色谱法 (HPLC) 测定血浆浓度评价地克珠利固体分散体及地克珠利物理混合物在家兔体内的药动学参数及生物利用度。地克珠利固体分散体和物理混合物的药时曲线下面积 (AUC0–∞) 分别为 247.8±18.1 μg/h/mL 和145.4±12.6 μg/h/mL; Cmax分别为33.72±4.75 μg/mL 和 16.42±3.48 μg/mL; t1/2分别为9.53±1.37 h 和 9.23±1.20 h。地克珠利固体分散体的口服生物利用度是物理混合物的1.7倍。表明地克珠利固体分散体可应用于制备地克珠利抗球虫制剂。

关键词: 地克珠利, 家兔, 药物动力学, 口服制剂, 高效液相色谱法 HPLC

Abstract: The purpose of this study was to evaluate the pharmacokinetic parameters and bioavailability of the solid dispersion formulation of diclazuril after oral administration in rabbits in comparison with its known premix form with feed additive. Plasma concentrations were determined by high-performance liquid chromatography (HPLC). The areas under the plasma concentration curves (AUC0–∞) of diclazuril in solid dispersion and premix were 247.8±18.1 μg/h/mL and 145.4±12.6 μg/h/mL, respectively. The Cmax of diclazuril in solid dispersion and premix were 33.72±4.75 μg/mL and 16.42±3.48 μg/mL, respectively. The t1/2 were 9.53±1.37 and 9.23±1.20 min, respectively. The oral bioavailability of drug solid dispersion was 1.7-fold higher than that of premix. From these data we concluded that diclazuril solid dispersion may be used as a potential anticoccidial preparation.

Key words: Diclazuril, Diclazuril, Rabbits, Rabbits, Pharmacokinetics, Pharmacokinetics, Oral administration, Oral administration, High-performance liquid chromatography, High-performance liquid chromatography

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*Corresponding author. Tel: 86-0312-5971107; e-mail: pharm126@126.com