Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers

Pharmaceutics

Yogesh B. Pawar²  Bhushan Munjal²  Saurabh Arora¹  Manoj Karwa¹  Gunjan Kohli²  Jyoti K. Paliwal² 

[1] Auriga Research Limited, Kirti Nagar Industrial Area, New Delhi-110015, India;Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab-160062, India;

关键词: curcumin;    bioavailability;    absorption;    pharmacokinetic modeling;   

DOI  :  10.3390/pharmaceutics4040517

来源: mdpi

【 摘 要 】

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 (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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.