PLASMA CONCENTRATION-TIME PROFILE OF A SINGLE DOSE OF ENTERIC-COATED OMEPRAZOLE IN MALE AND FEMALE HEALTHY VOLUNTEERS

Yıl 2000, Cilt: 13 Sayı: 3, 127 - 130, 03.12.2016

Ece İskender Neslihan Aslan Zafer Gören Tahir Tellioğlu Serap Akın Nuray Erin Rezzan Aker Filiz Onat Kemal Berkman Şule Oktay

Öz

Objective: The bioavailability of a single dose (20 mg) of two enteric-coated omeprazole formulations, marketed in Turkey, given 10-15 min before breakfast, was studied in 12 healthy volunteers (6 males and 6 females) in a doubleblind, crossover design.
Methods: Blood samples were collected prior to and at 10 time points within 12 hrs. after dosing. Plasma omeprazole concentrations were measured by HPLC technique in our laboratory.
Results and Conclusions: The two products were found to be bioequivalent in terms of extent of absorption (the area under the plasma concentration-time curves). Multipeak plasma concentration profiles were seen in most of the subjects with both products. Time to the earlier peaks was 1-2 hrs. and those peaks were lower in amplitude than the peaks reached approximately 4.5 hrs. after the application. Interestingly, the multipeak profile was more frequent and the earlier peaks were significantly higher in female subjects than in males. The reason for this gender difference in multipeak plasma concentration - time profile of oral omeprazole needs further investigation.
Key Words: Omeprazole - Bioavailability - Enteric - coated capsules - Gender difference

Kaynakça

• /. Eellenius E, Berglindh T, Sachs G. Substituted benzimidazoles inhibit gastric acid secretion by blocking (flb)-ATPase. nature 1981;290:159-161.
• Wallmark B, Lorentzon P, Larsson II. The mechanism of action of omeprazole: a survey of its inhibitory actions in vitro. Scand J Gastroenterol I985;20 (Supply 108):37-51.
• Clissold SP, Campoli-Richards DPI. Omeprazole: a preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic in peptic ulcer disease and Zollinger-Ellison syndrome. Drugs 1986;32:15-4 7.
• Lind T, Cederberg C. Ekenved G, flaglund U, Olbe L. Effect of omeprazole - a gastric proton pump inhibitor - on pentagastrin stimulated acid secretion in man. Gut 1983:24:270-276.
• bob ay as hi b, Chiba b, Sohn DR, Rato Y, Ishizaki T. Simultaneously determination of omeprazole and its metabolites in plasma and urine by reverse-phase high-performance liquid chromatography with an alkaline- resistant polymer-coated C ¡g column. J Chromatography 1992;5 79:299-305.
• Andersson T, Andren b, Cederberg C,
• fleggelund A, Lundborg P, Rohss b. Bioavailability of omeprazole as enteric coated (EC) granules in conjunction with food on the first and seventh days of treatment. Drug In vest 1990;2:184-188.
• Andersson T, Andren b, Cederberg C,
• fleggelund A, Lundborg P. The pharmacokinetics of single and repeated once-daily doses of 10,20 and 40 mg omeprazole as enteric coated granules. Drug Invest 1991;3:45-52.
• Garg Sb, Chugh Y, Tripathi Sb, bumar N, Sharma PL. Comparative bioavailability of two enteric-coated capsules of omeprazole in healthy volunteers. Int J Clin Pharmacol Ther Toxicol 1993;31:96-99.
• Prichard PJ, Yeomans HD, Mihaly GW, et at. Omeprazole: A study of its inhibition of gastric pfl and oral pharmacokinetics after morning or evening dosage. Gastroenterology 1985;88:64-69.