China Animal Husbandry and Veterinary Medicine ›› 2022, Vol. 49 ›› Issue (1): 386-394.doi: 10.16431/j.cnki.1671-7236.2022.01.041

• Basic Veterinary Medicine • Previous Articles     Next Articles

Pharmacokinetics and Bioequivalence of Two Cephalexin Formulations in Beagle Dogs

YANG Yuxin1,2, ZHAO Fuhua3, LIU Yu1,2, QIU Jicheng1,2, CAO Yuying1,2, ZHANG Lu1,2, BAI Runian4, WANG Jianzhong5, CAO Xingyuan1,2   

  1. 1. College of Veterinary Medicine, China Agricultural University, Beijing 100193, China;
    2. Reference Laboratory for the Test of Veterinary Drug Residues, Beijing 100193, China;
    3. China Institute of Veterinary Drug Control, Beijing 100081, China;
    4. Beijing Center for Animal Diseases Prevention and Control, Beijing 100013, China;
    5. College of Veterinary Medicine, Shanxi Agricultural University, Taigu 030801, China
  • Received:2021-07-06 Online:2022-01-05 Published:2021-12-29

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Abstract: [Objective] The purpose of the experiment was to study the bioequivalence of cephalexin test and reference formulations in Beagle dogs. [Method] Twenty-two Beagle dogs were randomly allocated to two equal-sized treatment groups in a randomized dual-cycle and dual-sequence cross-over design. The test (Trolevis®300) and the reference (Rilexine®300) formulations were orally administered in a single dose of 30 mg/kg BW. Blood samples were collected from brachiocephalic vein at 0, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 17 and 24 h after administration. The specificity, linearity, detection limit, accuracy, precision, and stability of UPLC-MS/MS method were investigated. The concentration of cephalexin in plasma was determined by UPLC-MS/MS. The pharmacokinetic parameters were analyzed and calculated with WinNonlinTM 8.1. [Result] The methodological results showed good correlation over the concentration range of 100-5 000 ng/mL with a correlation coefficient (R2) ≥ 0.99 and a standard curve equation of y=10.6828x-176.481. Relative recoveries were 105.63%, 104.35% and 102.40% for high, medium and low concentrations. Coefficient variations of intra-day and inter-day were all less than 15%, and the limit of detection and the limit of quantification were 50 and 100 ng/mL, respectively. The pharmacokinetic parameters of the two groups were as follows:Tmax were (1.77±0.55) and (2.70+4.68) h, Cmax were (28.09±5.09) and (26.82±7.94) μg/mL;T1/2 were (3.39±1.43) and (3.12±1.05) h;AUC0-t were (121.81±25.80) and (116.34±36.30) μg·h/mL. The plasma profiles of cephalexin following the administration of both formulations were similar. And the ratio of the average Cmax, AUC0-t and AUC0-∞ of the test/reference preparation were 99.51%, 99.27% and 99.30% respectively, the 90% CI all fell between 80.00%-125.00%. [Conclusion] The UPLC-MS/MS method established in this experiment was accurate and reliable, and could be used to determine the concentration of cephalexin. The two formulations were bioequivalent for cephalexin, and could be used clinically for the treatment of related diseases.

Key words: pharmacokinetics; bioequivalence; Beagle dog; cephalexin tablets; UPLC-MS/MS

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