Bioenhancers are the agents capable of enhancing bioavailability of certain drugs with which it is co-administered. Piperine (CAS no:94-62-2), an alkaloid obtained from Piper nigrum and P. longum has been shown to possess diverse biochemical and pharmacological activities and known inhibitor of various enzymes like CYP (Cytochrome P450) 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 dose-dependent antihyperglycemic activity of metformin (CAS no: 1115-70-4) which was correlated with increased plasma concentration of metformin as evaluated by glucose challenged and alloxan-induced diabetic models, when it was administered with metformin. The increased plasma concentration of metformin when co-administered with piperine may be due to modification in gastrointestinal epithelial cell membrane permeability or inhibition of gastrointestinal transit or gastric emptying time or modifications in intestinal motility or increase in gastrointestinal blood supply, which results in increasing the bioavailability of metformin. The results of this study demonstrate that piperine could be used as a potential bioenhancer along with metformin.
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