骨正胶囊中双氯芬酸钠的药代动力学研究

Pharmacokinetic Study of Diclofenic in the Gu Zheng Capsule

目的 研究骨正胶囊中主药双氯芬酸钠的药代动力学 ,为临床应用提供依据。方法 照中国药典释放度测定法 ,用紫外分光光度法在λ =2 73.4nm测定骨正胶囊中双氯芬酸钠的体外溶出度和家兔体内血药浓度 ,用药代动力学计算程序 3P87软件包计算药代动力学参数。结果 骨正胶囊有良好的释药性能 ,其 T1/ 2 (Ke) =1.980± 0 .0 2 2 9h与药粉胶囊 T1/ 2 (Ke) =0 .5 0 4 2± 0 .0 14 2 7h相比有显著性差异 (P <0 .0 1) ,其主要药动学参数Cmax =3.0 0 16± 0 .10 5 7μg·ml-1,Tpeak =2 .0 2 6 4± 0 .0 3h ,V/F(c) =6 .32 99± 0 .2 190mg/ (μg·ml-1) ,Cl/F(s) =3.6 6 2 0± 0 .0 96 0lmg/h/ (μg·ml-1)。结论 口服双氯芬酸钠兔体内代谢符合一室模型规律 ,表明骨正胶囊的研制为非甾体抗炎药的剂型改造提供了另外一条新途径。

Aim To investigate the pharmacokinetic parameters of Gu Zheng capsule’s main drug,diclofenac,in order to provide evidences for clinical practical.Method We determined the dissolubility according to the Chinese Pharmacopoeia of the diclofenac in Gu Zheng capsule with UV at λ=273.4nm,in vitro,and the dissolubility and blood concentration of drug in vivo of rabbit.We calculated the pharmacokinetic parameters of diclofenic with 3P87 procedure bag.Result The preparation of Gu Zheng capsule has a good property of release,its T 1/2 (ke)=1.908±0.022 9h vs diclofenac capsule T 1/2 (Ke)=0.504 2±0.014 27h and both of them have statistical difference(P<0.01).The main pharmacokinetic parameters:C max =3.001 6±0.105 7μg·ml -1 ,T peak =2.026 4±0.03h,V/F(c)=6.329 9±0.219 0mg/(μg·ml -1 ),Cl/F(s)=3.662 0±0.096 01mg/h/(μg·ml -1 ).Conclusion The metabolism of taking diclofenac by oral in rabbit fits the rule of one room model.Our results demonstrate that Gu Zheng capsule preparation provide another a new path for transforming the forms of NSAID.