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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 study the pharmacokinetics of carbachol sodium needle-less injection in rabbits and compare the injection effect of needleless syringe and traditional needle-injected intramuscular injection. Methods Japanese rabbits were used as experimental subjects. Serum was extracted by needle-free injection and intramuscular injection respectively, and detected by high performance liquid chromatography with 0.12% ammonium dihydrogen phosphate solution - acetonitrile (91: 9 ) As the mobile phase, detection wavelength 363 nm. Results The measured plasma concentration and blood sampling time were fitted by DAS 2.1.1 pharmacokinetic software, and the kinetics of injecting carbachol sodium and intramuscular injection of aconitine were in accordance with single-compartment model. The main pharmacokinetics The parameters AUC0-t, tmax, ρmax and t1 / 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 ) and (180.82 ± 15.29) μg · min · mL-1, (23.00 ± 2.01) min and (5.09 ± 0.29) μg · mL-1 and (18.28 ± 2.47) min respectively. Conclusion Compared with the traditional acupuncture injection, the needle injection can significantly advance the peak time, the peak concentration increased, the other pharmacokinetic parameters were no significant difference by statistical analysis, indicating that needle-free injection of sodium sulfonate card can reach with A similar injection of injection needle effect.