摘要
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tmax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(P<0.01),两者的半衰期t1/2分别为(31.30±4.38)、(29.38±1.83)h,曲线下面积(AUC0~t)分别为(242.92±30.04)、(230.55±8.06)μg/(h.ml),最高血药浓度(Cmax)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(Vd)分别为(3.36±0.51)、(3.22±0.19)L,均无明显差异(P>0.05),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 tmax of the capsules and the tablets were 0.89±0.09 and 3.92±0.49 h,respectively,with the former significantly shorter than the latter.The t1/2 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 Cmax 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 Vd 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.
出处
《第三军医大学学报》
CAS
CSCD
北大核心
2012年第12期1240-1243,共4页
Journal of Third Military Medical University
关键词
吡罗昔康
β-环糊精
包合物
药动学
生物等效性
piroxicam
β-cyclodextrin
inclusion complex
pharmacokinetics
bioavailability