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Pharmacokinetic difference between S-(+)- and R-(-)-etodolac in rats

  
@article{APS8326,
	author = {Jing-min SHI and Shun-guo LAI and Chang-jiang XU and Geng-li DUAN and Guan LI},
	title = {Pharmacokinetic difference between S-(+)- and R-(-)-etodolac in rats},
	journal = {Acta Pharmacologica Sinica},
	volume = {25},
	number = {8},
	year = {2016},
	keywords = {},
	abstract = {AIM:
To study whether etodolac enantiomers have pharmacokinetic difference after oral administration.
METHODS:
Fourteen rats, divided into two groups randomly, were orally given S-(+)- or R-(-)-etodolac at a single dose of 20 mg/kg, respectively. Blood samples were collected before and at 5, 10, 20, 30 min and 1, 3, 6, 12, 24, 48, 72 h after treatment. The plasma samples were analyzed with a high-performance liquid chromatographic method.
RESULTS:
The calibration curves were linear in the range of 0.5-50.0 mg/L (r=0.9999) to S-(+)-etodolac and 2.0-200.0 mg/L (r=0.9999) to R-(-)-etodolac, respectively. The main pharmacokinetic parameters of S-(+)- and R-(-)-etodolac were as follows: t1/2(lambdaz) 18+/-4 h vs 19.4+/-2.2 h, tmax 3.3+/-2.6 h vs 4+/-4 h; Cmax 29+/-6 mg/L vs 97+/-14 mg/L, AUC0-t 706+/-100 h.mg.L(-1) vs 2940+/-400 h mg.L(-1), CL(s) 0.030+/-0.006 L.kg(-1).h(-1) vs 0.0065+/-0.0010 L.kg(-1).h(-1) and V/F 0.25+/-0.22 L.kg(-1) vs 0.03+/-0.05 L.kg(-1). There was no significant difference in t1/2(lambdaz), and tmax between S-(+)- and R-(-)-etodolac (P>>0.05). The Cmax, and AUC0-t of R-(-)-etodolac were markedly higher (P},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/8326}
}