家兔卡络磺钠无针注射的药动学研究  

Pharmacokinetics of Carbazochrome Sodium Sulfonate in Rabbits Given by Needle-Free Injection

作　　者：罗远菊[1,2] 刘宏[1] 吕玲[1] 喻晶[1] 陈丹[1] 宋梦姣[1] 

机构地区：[1]广州军区武汉总医院药剂科,武汉430070 [2]湖北中医药大学,武汉430065

出　　处：《中国药学杂志》2012年第20期1648-1652,共5页Chinese Pharmaceutical Journal

基　　金：国家科技重大专项资助项目(No.2008ZXJ09014-004)

摘　　要：目的研究卡络磺钠无针注射在家兔体内的药动学规律,比较无针注射器与传统有针注射器肌内注射的注射效果。方法以日本大耳兔为研究对象,分别通过无针注射及有针肌内注射给药,提取血清,采用高效液相色谱法进行检测,以0.12%磷酸二氢铵溶液-乙腈(91∶9)为流动相,检测波长363 nm。结果所测得血药浓度及取血时间数据经DAS2.1.1药动学软件拟合,卡络磺钠无针注射和有针肌内注射药动学过程均符合单室模型,主要药动学参数AUC0-t、tmax、ρmax及t1/2分别为:(162.43±17.09)μg·min·mL-1、(5.00±1.41)min、(5.93±0.02)μg·mL-1、(23.54±3.89)min及(180.82±15.29)μg·min·mL-1、(23.00±2.01)min、(5.09±0.29)μg·mL-1、(18.28±2.47)min。结论与传统有针注射相比,无针注射可使达峰时间显著提前、达峰浓度增加,其他药动学参数经统计学处理无显著差异,表明无针注射卡络磺钠可达到与有针注射相似的注射效果。OBJECTIVE To research the pharmacokinetic characteristics of carbazochrome sodium sulfonate given by needle-free injection in rabbits, to compare it with that of carbazochrome sodium sulfonate given by traditional syringe injection . METHODS Japanese big ear white rabbits were administered carbazochrome sodium sulfonate solution by needle-free injection and intramuscular in- jection with needle syringe. Plasma samples were extracted and assayed by high performance liquid chromatography technology. The mobile phase was composed of 0. 12% NH4H2PO4and acetonitrile（91： 9） , and the detection wave length was 363 nm. RESULTS The measured blood drug concentration-time data was fitted by DAS 2. 1.1 pharmacokinetic software. The pharmacokinetic processes of carbazochrome sodium sulfonate given by both needle-free injection and intramuscular injection were in line with one-compartment model, and the major pharmacokinetic parameters AUC0.,, t Pmax and tl/2 were （ 162.43 ± 17.09 ） μg · min ~ mL- 1 , （5. 00 ± 1. 41 ） min, （5. 93 ±0. 02） μg · mL^-1 , （23.54 ±3.89） min and（ 180. 82 ± 15.29） μg ＂ min · mL^-1, （23.00 ±2. 01 ） min, （5.09 ±0. 29） μg · mL^-1and （18.28 ± 2.47 ）rain, respectively. CONCLUSION Compared with the traditional needle syringe injeetion, the peak time was significantly shortened and the peak concentration was increased with needle-free injection, while the other pharmacokinetic parameters showed no statistically significant difference, which indicated that carbazochrome sodium sulfonate given by needle-free injection may have similar effect with that of traditional injection.

关 键 词：卡络磺钠 无针注射 有针注射 高效液相色谱法 药动学 

分 类 号：R969.1[医药卫生—药理学]