Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects
Two randomized, single dose, 2-period, 2-sequence crossover studies were conducted to evaluate the comparative bioavailability of two clopidogrel formulations under fasting and fed conditions. Assessment of bioequivalence was based upon measurement of plasma concentrations of the parent drug, clopid...
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2014-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | http://www.degruyter.com/view/j/acph.2014.64.issue-1/acph-2014-0001/acph-2014-0001.xml?format=INT |
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| author | Brvar Nina Lachance Sylvain Lévesque Ann Breznik Marjanca Cvitkovič Marčič Lea Merslavič Mateja Grabnar Iztok Mateovič-Rojnik Tatjana |
| author_facet | Brvar Nina Lachance Sylvain Lévesque Ann Breznik Marjanca Cvitkovič Marčič Lea Merslavič Mateja Grabnar Iztok Mateovič-Rojnik Tatjana |
| author_sort | Brvar Nina |
| collection | DOAJ |
| description | Two randomized, single dose, 2-period, 2-sequence crossover studies were conducted to evaluate the comparative bioavailability of two clopidogrel formulations under fasting and fed conditions. Assessment of bioequivalence was based upon measurement of plasma concentrations of the parent drug, clopidogrel, and its major (inactive) metabolite, clopidogrel carboxylic acid, using improved methanol-free extraction. Bioequivalence of Krka’s formulation to the innovator’s formulation was demonstrated under both fasting and fed conditions on 205 volunteers. Confidence intervals for AUC0-t, AUC0-inf and Cmax of clopidogrel and its main metabolite were well within the acceptance range of 80.00 to 125.00 %. Food substantially increased the bioavailability of clopidogrel from both formulations, while no effect of food on the extent and rate of exposure to the metabolite was observed. The effect of food was comparable between the two formulations, as indicated by the same direction and rank of food impact on the bioavailability of both formulations. |
| format | Article |
| id | doaj-art-1b962bf7cf92448783d1cce8b934c83d |
| institution | Kabale University |
| issn | 1330-0075 1846-9558 |
| language | English |
| publishDate | 2014-03-01 |
| publisher | Sciendo |
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| series | Acta Pharmaceutica |
| spelling | doaj-art-1b962bf7cf92448783d1cce8b934c83d2025-02-02T04:52:47ZengSciendoActa Pharmaceutica1330-00751846-95582014-03-01641456210.2478/acph-2014-0001acph-2014-0001Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjectsBrvar Nina0Lachance Sylvain1Lévesque Ann2Breznik Marjanca3Cvitkovič Marčič Lea4Merslavič Mateja5Grabnar Iztok6Mateovič-Rojnik Tatjana7Krka, d.d., Novo mesto 8501 Novo mesto, SloveniainVentiv Health Clinical Québec, CanadainVentiv Health Clinical Québec, CanadaKrka, d.d., Novo mesto 8501 Novo mesto, SloveniaKrka, d.d., Novo mesto 8501 Novo mesto, SloveniaKrka, d.d., Novo mesto 8501 Novo mesto, SloveniaUniversity of Ljubljana, Faculty of Pharmacy, 1000 Ljubljana SloveniaKrka, d.d., Novo mesto 8501 Novo mesto, SloveniaTwo randomized, single dose, 2-period, 2-sequence crossover studies were conducted to evaluate the comparative bioavailability of two clopidogrel formulations under fasting and fed conditions. Assessment of bioequivalence was based upon measurement of plasma concentrations of the parent drug, clopidogrel, and its major (inactive) metabolite, clopidogrel carboxylic acid, using improved methanol-free extraction. Bioequivalence of Krka’s formulation to the innovator’s formulation was demonstrated under both fasting and fed conditions on 205 volunteers. Confidence intervals for AUC0-t, AUC0-inf and Cmax of clopidogrel and its main metabolite were well within the acceptance range of 80.00 to 125.00 %. Food substantially increased the bioavailability of clopidogrel from both formulations, while no effect of food on the extent and rate of exposure to the metabolite was observed. The effect of food was comparable between the two formulations, as indicated by the same direction and rank of food impact on the bioavailability of both formulations.http://www.degruyter.com/view/j/acph.2014.64.issue-1/acph-2014-0001/acph-2014-0001.xml?format=INTbioavailabilityfood effectclopidogrelclopidogrel carboxylic acid |
| spellingShingle | Brvar Nina Lachance Sylvain Lévesque Ann Breznik Marjanca Cvitkovič Marčič Lea Merslavič Mateja Grabnar Iztok Mateovič-Rojnik Tatjana Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects Acta Pharmaceutica bioavailability food effect clopidogrel clopidogrel carboxylic acid |
| title | Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects |
| title_full | Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects |
| title_fullStr | Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects |
| title_full_unstemmed | Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects |
| title_short | Comparative bioavailability of two oral formulations of clopidogrel: Determination of clopidogrel and its carboxylic acid metabolite (SR26334) under fasting and fed conditions in healthy subjects |
| title_sort | comparative bioavailability of two oral formulations of clopidogrel determination of clopidogrel and its carboxylic acid metabolite sr26334 under fasting and fed conditions in healthy subjects |
| topic | bioavailability food effect clopidogrel clopidogrel carboxylic acid |
| url | http://www.degruyter.com/view/j/acph.2014.64.issue-1/acph-2014-0001/acph-2014-0001.xml?format=INT |
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