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Effect of Piperine on Caffeine Salivary Concentration in Healthy Volunteers
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A Gholampour *   , M Hashemi , MM Rezaee , MR Shiran , AA Moghadamnia |
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Abstract: (8810 Views) |
BACKGROUND AND OBJECTIVE: Piperine (the alkaloid of piper nigrum) can change the activities of microsomal enzymes. Caffeine probe were applied to determination of CYP1A2 enzyme activity. CYP1A2 enzyme is important enzymes in drugs metabolism that induces over 13% of liver cytochromes. This study was done to determine of piperine pretreatment role on caffeine concentration.
METHODS: This cross over study was performed on 20 healthy volunteers (10 men and 10 women) in two groups of placebo and piperine before using caffeine. After recording personal data including age, gender, height and weight piperine (15mg) was orally administered during consecutive 3 days and at the 4th day after taking saliva sample, 50mg caffeine given to individuals and saliva samples were taken at 0.5, 2.5 and 5h after using caffeine. The caffeine saliva levels were assayed using HPLC method (C8 analytical column, 40: 60 methanol: water as mobile phase, UV detector at 210nm wave length and 0.8ml/min rate of fluid flow). Data were fitted in a “double-compartment PK model” using P-Pharm 1.5 software and analyzed under statistical tests. Pharmacokinetics parameters including clearance, volume of distribution and half-life were compared in two groups.
FINDINGS: The mean ± SD of the age and body mass index were 21.1±1.37 years (range: 19-23 years) and 24.71±4.69, respectively and the body weight range was 45-120 kg. The half-life and clearance of caffeine were respectively lower and higher than in piperine pretreatment group compared to the placebo, (3.59±1.42 vs 4.39±0.74h, p=0.01 and 20.17±8.76 vs 14.94±1.86ml/min, p<0.01) respectively. The elimination ratio constants in piperine group was greater than placebo (0.22±0.09 vs 0.16±0.02, p=0.008). The difference between all PK parameters except volume of distribution was significant.
CONCLUSION: According to the results, it is suggested that piperine may induce CYP1A2 enzyme activity in hepatic microsomal system.
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| Keywords: Piperine, CYP1A2, Caffeine, Clearance, HPLC, Hepatic metabolism. |
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Full-Text [PDF 709 kb]
(2434 Downloads)
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Type of Study: Research |
Subject:
Biochemical
Accepted: 2014/06/11 | Published: 2014/06/11
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