Pharmacokinetics of cyclosporine in type 1 diabetic rat model
10.13699/j.cnki.1001-6821.2017.17.016
- VernacularTitle:环孢素在1型糖尿病大鼠体内的药代动力学
- Author:
Yan JIANG
1
;
Rong CHEN
;
Li LIU
;
Yi CHU
;
Ying-Juan TANG
;
Su-Lan ZOU
;
Nan HU
Author Information
1. 常州市第一人民医院药剂科
- Keywords:
type 1 diabetes;
cyclosporine;
pharmacokinetics;
enzyme-multiplied immunoassay technique
- From:
The Chinese Journal of Clinical Pharmacology
2017;33(17):1665-1667
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the pharmacokinetics of cyclosporine(CsA) in type 1 diabetes of rats.Methods Rats with type 1 diabetes were induced by intraperitoneal administration of 65 mg· kg-1 streptozotocin (STZ).Pharmacokinetics of CsA (10 mg· kg-1) was compared between diabetic and normal rats on the 5 weeks after STZ injection.Concentration of CsA in whole blood was measured by enzyme multiplied immunoassay technique.Results Type 1 diabetes rats were successfully induced as the fasting blood glucose levels exceeded 11.1 mmol · L-1 after STZ injection for 1 week.Beside glucose,total cholesterol (TC) and triacylglycerol (TG) in serum of diabetic rats were significantly higher than those in normal rats after STZ injection for 5 weeks.Unlike normal rats,the pharmacokinetics of CsA in diabetic rats exhibited a double peak after oral administration.The Tmax and Cmax were lower in diabetic rats than normal rats,although without statistical differences as follows:Tmaxwas (3.3±1.6),(3.2 ±2.5) h,Cmax was (579.0±208.5),(453.0 ± 104.8) ng· mL-1 in normal and diabetic rats.Compared with normal rats,AUC and t1/2 of CsA in diabetic rats decreased significantly,which were 0.51 and 0.70 times those of normal rats,respectively;AUC was (7343.2 ± 2333.7),(3729.7 ± 1106.6) h ·ng · mL-1,t1/2 was (8.5 ± 1.5),(6.0 ± 0.9) h in normal and diabetic rats.Conclusion The oral pharmacokinetics of CsA was significantly different in type 1 diabetic rat model compared to normal controls,which should be taken into consideration in clinical medication.
