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Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab-160062, India
Auriga Research Limited, Kirti Nagar Industrial Area, New Delhi-110015, India
* Author to whom correspondence should be addressed.
Received: 15 June 2012; in revised form: 21 August 2012 / Accepted: 27 September 2012 / Published: 9 October 2012
Abstract: 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.
Keywords: curcumin; bioavailability; absorption; pharmacokinetic modeling
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Pawar, Y.B.; Munjal, B.; Arora, S.; Karwa, M.; Kohli, G.; Paliwal, J.K.; Bansal, A.K. Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers. Pharmaceutics 2012, 4, 517-530.
Pawar YB, Munjal B, Arora S, Karwa M, Kohli G, Paliwal JK, Bansal AK. Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers. Pharmaceutics. 2012; 4(4):517-530.
Pawar, Yogesh B.; Munjal, Bhushan; Arora, Saurabh; Karwa, Manoj; Kohli, Gunjan; Paliwal, Jyoti K.; Bansal, Arvind K. 2012. "Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers." Pharmaceutics 4, no. 4: 517-530.