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Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers

Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic f...

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Autores principales: Pawar, Yogesh B., Munjal, Bhushan, Arora, Saurabh, Karwa, Manoj, Kohli, Gunjan, Paliwal, Jyoti K., Bansal, Arvind K.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834932/
https://www.ncbi.nlm.nih.gov/pubmed/24300368
http://dx.doi.org/10.3390/pharmaceutics4040517
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author Pawar, Yogesh B.
Munjal, Bhushan
Arora, Saurabh
Karwa, Manoj
Kohli, Gunjan
Paliwal, Jyoti K.
Bansal, Arvind K.
author_facet Pawar, Yogesh B.
Munjal, Bhushan
Arora, Saurabh
Karwa, Manoj
Kohli, Gunjan
Paliwal, Jyoti K.
Bansal, Arvind K.
author_sort Pawar, Yogesh B.
collection PubMed
description Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic formulation of CRM (CRM-LF) in human subjects. C(max), T(max) and AUC(0–∞) were found to be 183.35 ± 37.54 ng/mL, 0.60 ± 0.05 h and 321.12 ± 25.55 ng/mL respectively, at a dose of 750 mg. The plasma profile clearly showed three distinct phases, viz., absorption, distribution and elimination. A close evaluation of the primary pharmacokinetic parameters provided valuable insight into the behavior of the CRM after absorption by CRM-LF. CRM-LF showed a lag time (T(lag)) of 0.18 h (around 12 min). Pharmacokinetic modeling revealed that CRM-LF followed a two-compartment model with first order absorption, lag time and first order elimination. A high absorption rate constant (K(01), 4.51/h) signifies that CRM-LF ensured rapid absorption of the CRM into the central compartment. This was followed by the distribution of CRM from the central to peripheral compartment (K(12), 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K(21), 0.15/h) was slow. This encourages higher tissue levels of CRM as compared with plasma levels. The study provides an explanation of the therapeutic efficacy of CRM, despite very low/undetectable levels in the plasma.
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spelling pubmed-38349322013-11-21 Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers Pawar, Yogesh B. Munjal, Bhushan Arora, Saurabh Karwa, Manoj Kohli, Gunjan Paliwal, Jyoti K. Bansal, Arvind K. Pharmaceutics Article Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic formulation of CRM (CRM-LF) in human subjects. C(max), T(max) and AUC(0–∞) were found to be 183.35 ± 37.54 ng/mL, 0.60 ± 0.05 h and 321.12 ± 25.55 ng/mL respectively, at a dose of 750 mg. The plasma profile clearly showed three distinct phases, viz., absorption, distribution and elimination. A close evaluation of the primary pharmacokinetic parameters provided valuable insight into the behavior of the CRM after absorption by CRM-LF. CRM-LF showed a lag time (T(lag)) of 0.18 h (around 12 min). Pharmacokinetic modeling revealed that CRM-LF followed a two-compartment model with first order absorption, lag time and first order elimination. A high absorption rate constant (K(01), 4.51/h) signifies that CRM-LF ensured rapid absorption of the CRM into the central compartment. This was followed by the distribution of CRM from the central to peripheral compartment (K(12), 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K(21), 0.15/h) was slow. This encourages higher tissue levels of CRM as compared with plasma levels. The study provides an explanation of the therapeutic efficacy of CRM, despite very low/undetectable levels in the plasma. MDPI 2012-10-09 /pmc/articles/PMC3834932/ /pubmed/24300368 http://dx.doi.org/10.3390/pharmaceutics4040517 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Pawar, Yogesh B.
Munjal, Bhushan
Arora, Saurabh
Karwa, Manoj
Kohli, Gunjan
Paliwal, Jyoti K.
Bansal, Arvind K.
Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_full Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_fullStr Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_full_unstemmed Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_short Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_sort bioavailability of a lipidic formulation of curcumin in healthy human volunteers
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834932/
https://www.ncbi.nlm.nih.gov/pubmed/24300368
http://dx.doi.org/10.3390/pharmaceutics4040517
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