ACTA VETERINARIA ET ZOOTECHNICA SINICA ›› 2014, Vol. 45 ›› Issue (12): 2050-2056.doi: 10.11843/j.issn.0366-6964.2014.12.020

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Pharmacokinetics and Bioavailability of Benazepril and Its Metabolite Benazeprilat in Cats

ZHENG Jing-cheng，ZHOU Lian-gen，QU Ying，QIU Zhen-zhen，CAO Chang-fu，ZHAO Hui-min，ZENG Zhen-ling *   

  1. (National Reference Laboratory of Veterinary Drug Residues，College of Veterinary Medicine，South China Agricultural University，Guangzhou 510642，China)
  • Received:2014-04-08 Online:2014-12-23 Published:2014-12-23

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Abstract:

The pharmacokinetics and bioavailability of the benazepril and its metabolite benazeprilat，were investigated in cats.A single intravenous (i.v.) or oral (p.o.) administration of benazepril hydrochloride tablets at a dosage of 5 mg was performed in six healthy cats according to a two-period crossover design.The concentration of benazepril and benazeprilat was analysed by high-performance liquid chromatography with tandem mass spectrometry detection (LC-MS/MS) using ESI.The pharmacokinetic parameters were calculated by non-compartmental analysis with WinNonlin 5.2.1 software.The main pharmacokinetic parameters of benazepril in cats were as follows：(1) after a single intravenous administration，the elimination half time (t1/2) was 1.91±0.37 h，area under the curve AUC0-∞ was 1 177.19±227.28 h•ng•mL-1，apparent volume of distribution ±Vd) was 3.32±0.74 L•kg-1，body clearance ±CLB) was 2.38±0.92 L•h-1•kg-1，mean residence time ±MRT) was 1.91±0.37 h；(2) after a single oral administration，t1/2 was 1.92±0.31 h，AUC0-∞ was 624.36±93.15 h•ng•mL-1，peak time (Tmax) was 0.54±0.10 h，peak concentration (Cmax) was 565.32±148.33 ng•mL-1，MRT was 2.43±0.54 h，mean absorb time (MAT) was 0.90(0.64 h，bioavailability (F) was 57.38±18.83 %.The main pharmacokinetic parameters of benazeprilat in cats were as follows：(1) after a single intravenous administration，t1/2 was 2.89±0.66 h, AUC0-∞ was 1 595.37±540.37 h•ng•mL-1，Tmax was 0.46±0.10 h，Cmax was 687.11±68.74 ng•mL-1，MRT was 4.17±0.61 h；(2) after a single oral administration，t1/2 was 2.63±0.19 h，AUC0-∞ was 594.61±90.75 h•ng•mL-1，Tmax was 1.17±0.41 h, Cmax was 124.86±25.67 ng•mL-1，MRT was 4.99±0.40 h.The results of present studies showed that benazepril hydrochloride tablets have characteristics of rapid absorption，extensive distribution and medium bioavailability in cats，and the recommended clinical regimen of benazepril hydrochloride tablets is 5 mg per day.

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