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纸质出版:2012
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张建明,吴江,方晓玲.吡罗昔康环糊精包合物在Beagle犬体内的药物动力学研究[J].陆军军医大学学报(原第三军医大学学报),2012,34(12):1240-1243.
Zhang Jianming,Wu Jiang,Fang Xiaoling.Pharmacokinetics of piroxicam-β-cyclodextrin inclusion complexes in Beagle dogs[J].J Amry Med Univ (J Third Mil Med Univ),2012,34(12):1240-1243.
目的 研究吡罗昔康环糊精包合物Beagle犬体内药物动力学。 方法 6只Beagle犬采用随机、双周期交叉给药,单剂量灌胃给予吡罗昔康受试制剂或参比制剂,用HPLC法测定吡罗昔康血浆浓度,用统计矩原理进行血药浓度-时间数据分析。 结果 吡罗昔康包合物的达峰时间t
max
快于普通片剂,分别为(0.89±0.09)、(3.92±0.49)h,两者有显著差异(P0.01),两者的半衰期t
1/2
分别为(31.30±4.38)、(29.38±1.83)h,曲线下面积(AUC
0~t
)分别为(242.92±30.04)、(230.55±8.06)μg/(h·ml),最高血药浓度(C
max
)分别为(7.82±0.44)、(7.49±0.36)μg/ml,清除率(Cl)分别为(80.92±10.65)、(85.27±2.95)ml/h,表观分部容积(V
d
)分别为(3.36±0.51)、(3.22±0.19)L,均无明显差异(P0.05),吡罗昔康包合物相对于市售片剂的相对生物利用度为106.74%。 结论 建立的HPLC分析方法准确可靠。两种剂型的生物利用度相似,将吡罗昔康制成包合物后能大大加快药物在体内的吸收速度,使其更快发挥药效。
Objective To study the pharmacokinetics of piroxicam-β-cyclodextrin inclusion complexes in Beagle dogs. Methods An open randomized two-period crossover self-control trial was conducted in 6 Beagle dogs. Piroxicam in the plasma was assayed by HPLC after a single oral dose of 20 mg piroxicam in test complexes (capsules) and reference tablets. The serum concentration-time data were analyzed by non-compartmental model. Results The t
max
of the capsules and the tablets wer
e 0.89±0.09 and 3.92±0.49 h
respectively
with the former significantly shorter than the latter. The t
1/2
were 31.30±4.38 and 29.38±1.83 h
respectively. The AUC were 242.92±30.04 and 230.55±8.06 g/(h·ml). The C
max
were 7.82±0.44 and 7.49±0.36 g/ml. The Cl were 80.92±10.65 and 85.27±2.95 ml/h. The V
d
were 3.36±0.51 and 3.22±0.19 L
respectively. These above indexes had no significant difference between 2 groups. The relative bioavailability of capsules was 106.74% compared to that of tablets. Conclusion The established HPLC method is accurate and reliable. Though the 2 two piroxicam agent are bioequivalent
the capsules of inclusion complexes significantly accelerate the dissolution and absorption rate.
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