大鼠服用丹酚酸B合用匹伐他汀后药动学和肝细胞摄取能力的改变

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Abstract Objective To study the pharmacokinetics of salvianolic acid B combined with pitavastatin and the uptaking of salvianolic acid B in rat hepatocytes. Methods SD male rats were randomly divided into two groups (n=6).One group was given salvianolic acid B 2.5 g/kg and another group was given salvianolic acid B combined with pitavastatin 0.5 mg/kg. For combined administration, the salvianolic acid B was first gavaged and then pitavastatin. Interval time lasted about 15 min. Blood samples were collected from the orbital vein. The effect of OATP1B1 substrate of pitavastatin on the pharmacokinetics of salvianolic acid B in rats was examined. Then the primary rat hepatocytes were separated, the effect of pitavastatin on the hepatocytes uptaking of salvianolic acid B was studied. Results The pharmacokinetic characteristics of salvianolic acid B significantly changed when salvianolic acid B was combined with pitavastatin, the parameters of AUC (0-t), AUC (0- ∞) and Cmax were significantly increased by 54.63%, 69.72%, and 50.56%. Simulatneously, the inhibitory action for uptaking of salvianolic acid B in rat hepatocytes increased gradually with increasing pitavastatin concentration. The IC₅₀ was (5.21±1.68) μmol. Conclusions The uptaking of salvianolic acid B in hepatocytes may be closely related to OATP.

Key words： salvianolic acid B hepatocytes transport pitavastatin

Received: 12 April 2014

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	Articles by authors
	XIAO Pin
	WEI Xiao-Hua
	SHENG Xiang-Yuan
	ZHONG Hai-Li
	ZOU De-Qin
	ZHENG Xue-Lian
	PENG Hong-Wei
	CAI Jun
	WEN Jin-Hua

Cite this article:

XIAO Pin,WEI Xiao-Hua,SHENG Xiang-Yuan等. In vivo Pharmacokinetics of salvianolic acid B combined with pitavastatin and uptaking of salvianolic acid B in hepatocytes of rats[J]. , 2014, 25(8): 816-819.

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http://journal08.magtechjournal.com/Jwk_wjyx/EN/ OR http://journal08.magtechjournal.com/Jwk_wjyx/EN/Y2014/V25/I8/816

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