以0.1 mg/kg体重的剂量研究美洛昔康片在比格犬中的药代动力学和生物利用度。采用HPLC分析血浆中的药物浓度,Win Nonlin 6.4非房室模型计算药动学参数。比格犬内服美洛昔康片后测得0~48 h美洛昔康的T_(1/2)、C_(max)、T_(max)和AUC_(0-t)分别为14.55±2.18 h、296.16±74.15 ng·m L~(-1)、6.0±0.00 h和6356.79±1089.78 ng·h·m L~(-1);比格犬静脉注射美洛昔康溶液后,测得0~48 h美洛昔康的T_(1/2)和AUC_(0-t)分别为11.54±4.18 h和5510.68±1075.29 ng·h·m L~(-1)。内服美洛昔康片剂的绝对生物利用度为115.35%。美洛昔康片在比格犬体内消除速率较慢,消除半衰期较长,在体内滞留时间较长,具有绝对生物利用度高,药物在体内作用时间较长的药动学特征。
This study was designed to investigate the pharmacokinetic and bioavailability of meloxicam (MLX) tablet in beagle dogs at a dose of 0.1 mg/kg bodyweight. The drug concentrations were analyzed using high performance liquid chromatography. The main PK parameters for p.o. and i.v, groups with WinNonlin 6.4 software, respectively, were as followings: T1/2 , Cmax, Tmax and AUC0-48, 14.55 ± 2.18 h,296.16 ± 74.15 ng·mL-1, 6.0 ± 0.00 h and 6356.79 ± 1089.78 ng·h·mL-1; T1/2 and AUC0-48, 11.54 ± 4.18 h and 5510.68 ± 1075.29 ng·h·mL-1. The absolute bioavailability of MLX via p.o. was 115.35%. The results demonstrated that MLX tablet was rapid absorption, slow elimination and high bioavailability.