The effect of piperine on the bioavailability and pharmacokinetics of propranolol and theophylline has been examined in a crossover study. Six subjects in each group received a single oral dose of propranolol 40 mg or theophylline (150 mg) alone or in combination with piperine 20 mg daily for 7 days. An earlier tmax and a higher Cmax and AUC were observed in the subjects who received piperine and propranolol. It produced a higher Cmax, longer elimination half-life and a higher AUC with theophylline. In clinical practice, the enhanced systemic availability of oral propranolol and theophylline could be exploited to achieve better therapeutic control and improved patient compliance.
Pharmacokinetics of phenytoin were studied in healthy subjects. In a crossover study five volunteers received either a single oral dose (300 mg) of phenytoin alone or in combination with multiple doses of piperine (20mg x 7 days) followed by an oral dose of phenytoin. Blood samples were col-lectedat0.5, 1,2,3,4,8, 12,24,and48hafter drug administration and analysed for phenytom by the enzyme multiplied immunoassay technique (EMIT). The results obtained revealed that a single daily dose of piperine for 7 days decreased the absorption haiflife (P < 0.05), prolonged the elimination halflife (P < 0.01), and produced a higher area under the drug concentration curve (P < 0.05) in comparison to phenytoin alone. It is therefore concluded that piperine on multiple dose administration alters the pharmacokinetic parameters of the antiepileptic.
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