温控型胰岛素液体肛门栓在糖尿病模型兔体内的药动学研究

Pharmacokinetic Study of Thermosensitive Insulin anal Liquid Suppository

目的考察温控型胰岛素液体肛门栓在四氧嘧啶致糖尿病兔体内的药动学。方法 36只糖尿病兔随机分成6组,对照组分别给生理氯化钠溶液和空白栓剂,实验组分别进行单剂量低、中、高剂量和肌注给药,用增强化学发光免疫法测定糖尿病兔体内的血清胰岛素浓度;并与皮下给药、空白对照、辅料对照组进行比较,计算主要药动学参数。结果 Cmax低、中、高剂量组和皮下注射组分别为:(109.7±36.6)、(115.2±28.1)、(151.3±40.3)、(151.8±27.4)μIU·ml-1;Tmax低、中、高剂量组和皮下注射组分别为:(90.0±21.2)、(90.0±18.9)、(78.0±24.0)、(108.0±18.5)min;AUC0-t低、中、高剂量组和皮下注射组分别为:(19 406.9±3751.7)、(23 863.7±1203.8)、(27 128.2±9200.2)、(29 624.5±3640.4)μIU·min·ml-1;相对生物利用度低、中、高剂量组分别为32.86%、20.20%、15.31%。结论温控型胰岛素液体肛门栓在糖尿病兔体内吸收良好。

Objective To investigate the pharmacokinetics of thermosensitive insulin anal liquid suppository in alloxan diabetic rabbits. Methods 36 diabetic rabbits were randomly divided into 6 groups. The control group was given respectively NS and blank suppositories,while the experimental group was given respectively a single low,medium and high dose and intramuscular injection. Using enhanced chemiluminescence immunoassay,the serum insulin concentration in the body of these diabetic rabbits was determined. The main pharmacokinetic parameters. Results In the low-dose,middle-dose high-dose and intramuscular injection groups,Cmaxwas（ 109. 7 ± 36. 6）,（ 115. 2 ± 28. 1）,（ 151. 3 ± 40. 3）,（151.8 ±27.4） μIU·min- 1respectively,Tmaxwas（ 90. 0 ± 21. 2）,（ 90. 0 ± 18. 9）,（ 78. 0 ± 24. 0）,（ 108. 0 ± 18. 5） min respectively,AUC0- twas（ 19 406. 9 ±3751. 7）,（ 23 863. 7 ±1203. 8）,（ 27 128. 2 ±9200. 2）,（ 29 624. 5 ± 3640. 4） μIU·min·ml- 1respectively,The relative bioavailability was 32. 86%,20. 20%,15. 31% respectively. Conclusion The in vivo absorption of thermosensitive insulin anal liquid suppository in diabetic rabbits is good.