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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2012-10-01
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author | Arvind K. Bansal Gunjan Kohli Jyoti K. Paliwal Manoj Karwa Bhushan Munjal Saurabh Arora Yogesh B. Pawar |
author_facet | Arvind K. Bansal Gunjan Kohli Jyoti K. Paliwal Manoj Karwa Bhushan Munjal Saurabh Arora Yogesh B. Pawar |
author_sort | Arvind K. Bansal |
collection | DOAJ |
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. Cmax, Tmax and AUC0–¥ 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 (Tlag) 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 (K01, 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 (K12, 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K21, 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 | doaj.art-b8d1a91b544f4389904a73b190e928ff2022-12-22T04:01:28ZengMDPI AGPharmaceutics1999-49232012-10-014451753010.3390/pharmaceutics4040517Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human VolunteersArvind K. BansalGunjan KohliJyoti K. PaliwalManoj KarwaBhushan MunjalSaurabh AroraYogesh B. PawarNumerous 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. Cmax, Tmax and AUC0–¥ 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 (Tlag) 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 (K01, 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 (K12, 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K21, 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.http://www.mdpi.com/1999-4923/4/4/517curcuminbioavailabilityabsorptionpharmacokinetic modeling |
spellingShingle | Arvind K. Bansal Gunjan Kohli Jyoti K. Paliwal Manoj Karwa Bhushan Munjal Saurabh Arora Yogesh B. Pawar Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers Pharmaceutics curcumin bioavailability absorption pharmacokinetic modeling |
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 | curcumin bioavailability absorption pharmacokinetic modeling |
url | http://www.mdpi.com/1999-4923/4/4/517 |
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