磺胺间甲氧嘧啶钠注射液A、B在猪体内的药代动力学比较试验

Comparison Study on Pharmacokinetics of Sulfamonomethoxine Sodium A and B in Pigs

为了能更好地了解新研制处方磺胺间甲氧嘧啶钠注射液A、B的临床应用,对这2种处方注射液在猪体内的药代动力学进行了对比试验。将荣昌区杂交健康猪10头分成2组,每组5头,按50 mg/kg·bw剂量在耳后方颈部肌肉分别注射磺胺间甲氧嘧啶钠注射液A、B,并于给药后0.25、0.5、1、2、3、5、7、9、12、24、36、48、72 h,自前腔静脉采集血样2~3 mL分别置于含肝素钠的离心管中,采用高效液相色谱法测定血样中的药物浓度,用3P97药代动力学程序软件计算药代动力学参数。结果显示,磺胺间甲氧嘧啶钠注射液A、B的半衰期t1/2α分别为(1.63±0.11)h和(1.76±3.18)h,t1/2β分别为(20.75±1.29)h和(6.73±1)h,AUC分别为(1968.72±75.71)(μg/mL)×h和(2484.74±209.89)(μg/mL)×h,T(peak)分别为(2.15±0.12)h和(0.42±0.05)h,C(max)分别为(146.98±7.61)μg/mL和(270.83±16.71)μg/mL。表明A制剂具有较长的半衰期,有效血液浓度持续时间较长,能够起到较好的治疗效果,且肌肉注射给药具有延缓吸收的作用,可达到缓释的效果;而B制剂作用效果快,但有效血液浓度维持短,在临床治疗上需多次注射才能达到治疗要求,增加了复杂性。

In order to better understand the clinical application of the newly developed sulfamonomethoxine sodium injections A and B,we compared the pharmacokinetics of the two prescription injections in pigs.10 pairs of Rongchang cross-breeding pigs were divided into two groups with 5 in each group,and were then injection with Sulfamonomethoxine sodium injection A and B at 50 mg/kg·bw dose in the neck muscles behind the ear,respectively.At 0.25,0.5,1,2,3,5,7,9,12,24,36,48,72 h after injection,blood samples were collected and placed in centrifuge tubes containing heparin sodium,and then the drug concentration in blood samples was determined by using high performance liquid chromatography.Pharmacokinetic parameters were calculated using 3 P97 pharmacokinetics program software.Results showed that the half-life t1/2α α of sulfamonomethoxine sodium injections A and B were(1.63±0.11)h,(1.76±3.18)h,t1/2β were(20.75±1.29)h,(6.73±1)h,AUC were(1968.72±75.71)(μg/mL)×h,(2484.74±209.89)(μg/mL)×h,T(peak)was(2.15±0.12)h,(0.42±0.05)h,C(max)were(146.98±7.61)μg/mL,(270.83±16.71)μg/mL,respectively.The results indicated that a injection had a long half-life,and effective blood concentration for a long time,suggesting a good therapeutic effect.Intramuscular administration delayed absorption and slowed down the absorption.Injection B had a long half-life and the effect was rapid,but the effective blood concentration is maintained short,implying that the clinical treatment requires multiple injections to meet the treatment requirements.