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Information Journal Paper

Title

PHARMACOKINETIC STUDY OF TRAMADOL AND ITS THREE METABOLITES IN PLASMA, SALIVA AND URINE

Pages

  245-255

Abstract

 Background and the purpose of the study: PHARMACOKINETIC parameters of TRAMADOL and its three METABOLITEs in plasma, SALIVA and URINE following administration of 100 mg single oral dose were investigated in 24 healthy volunteers.Materials and Methods: 12 male and 12 female healthy volunteers received a single oral dose of TRAMADOL and Plasma, mixed SALIVA -secreted samples without any stimulation and URINE were analyzed for TRAMADOL and its main METABOLITEs by HPLC method.Results and Disscusion: Almost 16.2% of TRAMADOL and 11.2, 1.1 and 5.0% of O-desmethylTRAMADOL (M1), N-desmethylTRAMADOL (M2) and N,O-didesmethylTRAMADOL (M5) respectively were recovered in 30 hrs collected URINE. Renal clearance of TRAMADOL, M1, M2 and M5 were 114.7 ± 44.5, 193.9 ± 67.6, 116.1 ± 61.8 and 252.0±91.5 (mL/min) respectively. The maximum plasma concentration of TRAMADOL, M1, M2 and M5 were 349.3 ± 76.7, 88.7±30.3, 23.1 ±11.4 and 30.0 ± 11.7 (ng/mL) at 1.6 ± 0.4, 2.4 ± 0.7, 2.8 ± 1.0 and 2.7 ± 1.4 hrs after drug administration respectively. TRAMADOL and its METABOLITEs appeared in a significant amount in SALIVA with the SALIVA/plasma ratios of 9.0, 1.6, 12.3 and 2.8 for TRAMADOL, M1, M2 and M5 according to AUC(0-24) respectively. Conclusion: Conclusion Strong correlations were found between plasma and SALIVA concentrations for all studied compounds and a dissection to pre and post absorption components improved these correlations. Results o f this study suggests that SALIVA is a suitable alternative to plasma for clinical and toxicological studies of TRAMADOL and in addition to passive diffusion, a possible active transport is also suggested to describe the elevated SALIVA/plasma ratios for these compounds.

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    APA: Copy

    HOSSEINZADEH ARDAKANI, Y., & ROUINI, M.R.. (2009). PHARMACOKINETIC STUDY OF TRAMADOL AND ITS THREE METABOLITES IN PLASMA, SALIVA AND URINE. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 17(4), 245-255. SID. https://sid.ir/paper/275520/en

    Vancouver: Copy

    HOSSEINZADEH ARDAKANI Y., ROUINI M.R.. PHARMACOKINETIC STUDY OF TRAMADOL AND ITS THREE METABOLITES IN PLASMA, SALIVA AND URINE. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2009;17(4):245-255. Available from: https://sid.ir/paper/275520/en

    IEEE: Copy

    Y. HOSSEINZADEH ARDAKANI, and M.R. ROUINI, “PHARMACOKINETIC STUDY OF TRAMADOL AND ITS THREE METABOLITES IN PLASMA, SALIVA AND URINE,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 17, no. 4, pp. 245–255, 2009, [Online]. Available: https://sid.ir/paper/275520/en

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