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美洛昔康片剂在比格犬内的药代动力学及生物利用度研究
郝俊玺,叶妮,王建中,王海挺,曹兴元
0
(内蒙古农业大学科技园区管理办公室;中国农业大学动物医学院)
摘要:
本研究以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。HPLC分析血浆中的药物浓度,WinNonlin 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T1/2、Cmax、Tmax和AUC0-t分别为14.55 ± 2.18 h、296.16 ± 74.15 ng·mL-1、6.0 ± 0.00 h和6356.79 ± 1089.78 ng·h·mL-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T1/2和AUC0-t分别为11.54 ± 4.18 h和5510.68 ± 1075.29 ng·h·mL-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,绝对生物利用度高,药物在体内作用时间较长等药动学特征。
关键词:  美洛昔康    药代动力学  生物利用度
DOI:
投稿时间:2017-05-25修订日期:2017-06-30
基金项目:国家自然科学基金(31672599);2017年国家农产品质量安全风险评估项目(GJFP201700701);科技部“十三五”重大专项子项目(2016YFD0501309-1)
Pharmacokinetics and Bioavailability of Meloxicam Tablet in beagle dogs
(1 Inner Mongolia Agricultural University Science and Technology Park Management Office)
Abstract:
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.
Key words:  meloxicam  dog  pharmacokinetic  bioavailability

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