Sama V, Nadipelli M, Yenumula P, Bommineni M R, Mullangi R
G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad, India.
Arzneimittelforschung. 2012 Aug;62(8):384-8. doi: 10.1055/s-0032-1314849. Epub 2012 Jun 29.
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.
胡椒碱（CAS编号：94 - 62 - 2）是一种从黑胡椒和长胡椒中提取的生物碱，是已知的负责药物生物转化的各种酶（细胞色素P450同工酶）的抑制剂。通过抑制药物代谢，胡椒碱可提高药物的生物利用度。在本研究中，当与那格列奈（CAS编号：105816 - 04 - 4）联合给药时，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（10毫克/千克）显著增强了那格列奈剂量依赖性的降血糖活性。当与胡椒碱联合给药时，那格列奈的血浆浓度也有所增加。那格列奈与胡椒碱联合给药时的协同降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用作潜在的生物增强剂。
