a Department of Pharmaceutical Chemistry , Bharati Vidyapeeth (Deemed to be) University, Poona College of Pharmacy Erandwane , Pune , Maharashtra , India.
Drug Dev Ind Pharm. 2019 Apr;45(4):664-668. doi: 10.1080/03639045.2019.1569034. Epub 2019 Feb 11.
Piperine has been widely used as a bioenhancer. Simvastatin belongs to a group of medicines known as statins. It acts by inhibiting HMG CoA reductase and acts primarily as a hypolipidemic agent. In this study some derivatives of Piperine were synthesized. They were studied for their bioenhencing effect (10 mg kg) and this effect was compared with that of Piperine. The pharmacokinectic profile of Simvastatin alone and in combination with Piperine and Piperine derivatives were investigated by validated HPLC method as per USFDA guidelines. It was seen that the two synthesized derivatives of Piperine significantly improved the bioavailability of Simvastatin in Wistar rats. The 5-(benzo) [1,3]dioxol-5-yl)-N-(pyridin-4-yl)penta-2,4-dienamide was better amongst the synthesized in increasing the bioavailability of Simvastatin in Wistar rat.
胡椒碱被广泛用作生物增强剂。辛伐他汀属于他汀类药物的一种。它通过抑制 HMG CoA 还原酶起作用，主要作为一种降脂药。在这项研究中，合成了一些胡椒碱的衍生物。它们被研究了其生物增强效果（10mg/kg），并将其效果与胡椒碱进行了比较。根据美国 FDA 的指导原则，使用经过验证的 HPLC 方法研究了辛伐他汀单独以及与胡椒碱和胡椒碱衍生物联合使用的药代动力学特征。结果表明，这两种合成的胡椒碱衍生物显著提高了辛伐他汀在 Wistar 大鼠中的生物利用度。在所合成的化合物中，5-（苯并）[1,3]二氧戊环-5-基）-N-（吡啶-4-基）戊-2,4-二烯酰胺可更好地提高 Wistar 大鼠中辛伐他汀的生物利用度。
