胡椒碱对那格列奈抗高血糖活性及药代动力学的影响。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-08-01 Epub Date: 2012-06-29 DOI:10.1055/s-0032-1314849
V Sama, M Nadipelli, P Yenumula, M R Bommineni, R Mullangi
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引用次数: 21

摘要

胡椒碱(CAS no: 94-62-2)是一种从胡椒和长叶胡椒中提取的生物碱,是一种已知的多种酶(CYP同工酶)的抑制剂,负责药物的生物转化。胡椒碱通过抑制药物的代谢,提高药物的生物利用度。在本研究中,当胡椒碱(10 mg/kg)与那格列奈一起使用时,通过葡萄糖激发和四氧嘧啶诱导的糖尿病模型评估,胡椒碱(105816-04-4)显著增加那格列奈(CAS no: 105816-04-4)的剂量依赖性降糖活性。当与胡椒碱一起使用时,那格列奈的血浆浓度也增加。当与胡椒碱一起给药时,那格列奈的协同抗高血糖活性可归因于那格列奈血浆浓度的增加。本研究结果表明,胡椒碱可与那格列奈一起作为潜在的生物增强剂使用。
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Effect of piperine on antihyperglycemic activity and pharmacokinetic profile of nateglinide.

Piperine (CAS no: 94-62-2), an alkaloid obtained from Piper nigrum and P. longum is a known inhibitor of various enzymes (CYP isozymes) responsible for biotransformation of drugs. By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs. In the present study piperine (10 mg/kg) significantly increased the dose-dependent anti-hyperglycemic activity of nateglinide (CAS no: 105816-04-4) as evaluated by glucose challenged and alloxan-induced diabetic models, when it was administered with nateglinide. Nateglinide plasma concentrations were also increased, when administered with piperine. The synergistic anti-hyperglycemic activity of nateglinide when administered with piperine can be attributed to increased plasma concentration of nateglinide. The results of this study demonstrate that piperine could be used as a potential bioenhancer along with nateglinide.

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