健康志愿者中两种国产双氯芬酸钠缓释剂的相对生物利用度

Relative bioavailability and pharmacokinetics of diclofenac sodium sustained-release tablets in Chinese volunteers

目的 :研究两种国产双氯芬酸钠缓释剂在 12名男性健康志愿者中的药物动力学和相对生物利用度。方法 :根据交叉试验方案po单剂量 10 0 m g及多剂量两种双氯芬酸钠缓释制剂 ,采用反相高效液相色谱法测定血清中双氯芬酸钠的浓度。结果 :po单剂量10 0 mg研制片 AUC、cmax、tmax、T1 /2α、T1 /2β分别为 (5 75 3± 2 16 1) (h· ng) /m l、(6 75 .4± 141.6 ) ng/ml、(2 .2 84± 0 .5 42 ) h、(0 .9430± 0 .5 82 4) h、(6 .713± 2 .2 0 8) h;对照片为 (5 15 0± 2 16 7) (h· ng) /ml、(6 2 0 .1± 187.1) ng/ml、(2 .491± 0 .6 45 ) h、(1.0 6 0 0± 0 .6 82 9) h、(6 .15 9± 2 .372 ) h,研制片的相对生物利用度为 10 7.9%。po多剂量研制片 AUC、cmax、tmax、T1 /2α和 T1 /2β分别为 (5 915± 1112 ) (h· ng) /m l、(76 6 .5± 173.0 ) ng/ml、(2 .6 70± 0 .770 ) h、(1.6 90± 1.0 6 0 ) h、(5 .46 0± 2 .0 70 ) h;对照片为(5 781± 1849) (h· ng) /m l、(75 9.2± 2 16 .3) ng/ml、(2 .310± 0 .5 2 0 ) h、(1.2 0 0± 0 .830 ) h、(6 .16 0± 2 .2 10 ) h,研制片的相对生物利用度为 10 2 .3%。两种国产缓释制剂的所有药物动力学参数经统计学 (SPSS软件 )处理均无显著性差异 (P>0 .0 5 ) ,用双?

AIM:To study the pharmacokinetics and relative bioavailability of 2 domestic diclofenac sodium sustained release tablets in 12 normal male volunteers. METHODS: A single oral dose of 100 mg and a multi oral dose were given according to a crossover design. The diclofenac sodium concentrations in plasma were determined by reversed phase high performance liquid chromatography. RESULTS: The concentration time curves of 2 products fitted to two compartment open model. In the single dose experiment tablets (A) the AUC , c max , t max , T 1/2α and T 1/2β of the subject were ( 5 753 ±216) (h·ng)/ml, (675 4±141 6) ng/ml, (2 284±0 542) h, ( 0 943 0 ± 0 582 4 ) h, (6 713±2 208) h; the standard tablets (B) were ( 5 150 ± 2 167 ) (h·ng)/ml,( 620 1±187 1) ng/ml, (2 491±0 645) h, ( 1 060 0 ± 0 682 9 ) h, (6 159±2 372) h, respectively. In the multi oral dose experiment the AUC, c max , t max , T 1/2α and T 1/2β were ( 5 915 ± 1 112 ) (h·ng)/ml, (766 5±173 0) ng/ml, (2 670±0 770) h, (1 690±1 060) h, (5 460± 2 070) h; the standard tablets were ( 5 781 ± 1 849 ) (h·ng)/ml, (759 2±216 3) ng/ml, (2 310±0 520) h,(1 200±0 830) h, (6 160±2 210) h, respectively. The relative bioavailability of the subject tablets were 107 9% in the single dose experiment and 102 3% in the multi oral dose experiment. The results obtained from our studies showed no significant difference between 2 products ( P >0 05). CONCLUSION: The 2 preparations are bioequivalent.