CYP3A4、PXR和IL-10基因多态性对43名中国健康受试者空腹及餐后口服氨氯地平药代动力学特征的影响

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Abstract Objective To investigate the effect of gene polymorphisms of cytochrome P450 3A4 (CYP3A4), pregnane X receptor (PXR) and interleukin-10 (IL-10) on the pharmacokinetics of amlodipine in 43 healthy Chinese subjects.Methods Genetic polymorphisms of CYP3A4, PXR, and IL-10 were evaluated for 43 healthy Chinese male subjects from a study permitted by ethical committee of the hospital and finalized in 2015. CYP3A4 genotype in 17776 A insertion, 15820C>G, 13989A>G, and PXR genotype in 24381A>C, 3'UTR11193T>C, 3'UTR10719G>A, and IL-10 genotype in 1082G>A, 819C>T and 592C>A were assessed by PCR–RFLP assays. The plasma concentrations of amlodipine in subjects after being orally administrated 10 mg Amlodipine were measured by liquid chromatography tandem mass spectrometry (LC-MS/MS) method. Results Three CYP3A4 genotypes, three PXR genotypes and three IL-10 genotypes had no significant effect on the pharmacokinetic parameters of amlodipine in vivo (P＞0.05). The peak concentration (cmax), area under the curve (AUC0-t) and AUC0-∞of amlodipine in postprandial group were higher than those in fasting group, and the differences were statistically significant (P＜0.05). Conclusion There are no influences of the genetic polymorphisms of CYP3A4, PXR, IL-10 on the pharmacokinetics of Amlodipine in Chinese healthy subjects.And the high-fat and high-calorie diet could significantly promote the absorption of Amlodipine in human.

Key words： Cytochrome P450 3A4 Interleukin -10;Pregnane X receptor Gene polymorphism Amlodipine;Pharmacokinetics

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	Articles by authors
	LIU Lin-lin
	IsaiahTakau
	LIU Jian-fang
	CHEN Lin
	LIU Dan
	XIE Hong-bo
	LIU Ming-yi
	XIA Chun-hua

Cite this article:

LIU Lin-lin,IsaiahTakau,LIU Jian-fang, et al. Effect of CYP3A4, PXR and IL-10 polymorphisms on the pharmacokinetics of Amlodipine in 43 healthy Chinese subjects before and after meal[J]. 中国当代医药, 2021, 28(30): 4-7转12.

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http://dangdaiyiyao.com/EN/ OR http://dangdaiyiyao.com/EN/Y2021/V28/I30/4

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