Piperine is an alkaloid isolated from Piper nigrum Linn., (family-Piperaceae) a natural bioenhancer and is known to enhance the bioavailability of the drugs by inhibiting cytochrome P450. In the present study, the effect of piperine was investigated on antihyperlipidemic properties of simvastatin (SV) and the effects were supported with measurement of plasma concentrations. The results confirm that piperine enhanced the antihyperlipidemic activity of simvastatin in tyloxypol induced hyperlipidemic rats. The co-administration of SV along with piperine showed a greater percent protection when compared to animals receiving SV alone at dose levels of 50, 75, 100 mg/kg. Test animals receiving 100 mg/kg of SV along with piperine at dose of 10 mg/kg showed a maximum reduction in cholesterol and triglycerides. From the study it was observed that the plasma concentration of SV was high during the 2nd h of the study, but maximum % protection was observed during the 4th h, this might be due to the conversion of SV to simvastatin hydroxyl acid an active metabolite in high concentration. The finding of present study confirmed that piperine could be used as bioenhancer when co-administered with simvastatin.
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