Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar, Punjab, 160062, India.
Drug Deliv Transl Res. 2011 Aug;1(4):322-31. doi: 10.1007/s13346-011-0033-3.
The aim of the present study was to study the oral bioavailability of seven different formulations of curcumin (CRM). CRM formulations viz. aqueous suspension, micronized suspension, nanosuspension, amorphous solid dispersion, hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex, combination with piperine, and spray-dried CRM-milk composite were compared for oral bioavailability in male Sprague-Dawley rats at a CRM dose of 250 mg/kg body weight using a validated high-performance liquid chromatography method. Aqueous suspension provided a C max and AUC(0 - t) of 28.9 ng/ml and 26.9 ng h/ml, respectively. In comparison, statistically significant increase in the oral bioavailability was obtained with the nanosuspension, HP-β-CD inclusion complex, and amorphous solid dispersion with 251%, 567%, and 446% increase in terms of AUC(0 - t) and 405%, 415%, and 270% in terms of C max. However, no significant increase in AUC(0 - t) and C max was observed with piperine and micronized suspension. The milk composite reduced the oral bioavailability of CRM (10% and 37% in terms of AUC(0 - t) and C max). A statistically significant increase in the T max was observed with piperine and in HP-β-CD complex, while the T max was reduced for nanosuspension. The results provide interesting insights into the role of solubility enhancement and metabolism inhibition, for improving the oral bioavailability of CRM.
本研究旨在研究七种不同姜黄素（CRM）制剂的口服生物利用度。在雄性 Sprague-Dawley 大鼠中，以 250mg/kg 体重的 CRM 剂量，用经验证的高效液相色谱法比较了 CRM 制剂，即水性混悬液、微米化混悬液、纳米混悬液、无定形固体分散体、羟丙基-β-环糊精（HP-β-CD）包合物、与胡椒碱联合使用以及喷雾干燥的 CRM-牛奶复合物的口服生物利用度。水性混悬液提供了 28.9ng/ml 的 C max 和 26.9ng·h/ml 的 AUC(0-t)。相比之下，纳米混悬液、HP-β-CD 包合物和无定形固体分散体的口服生物利用度显著增加，AUC(0-t)分别增加了 251%、567%和 446%，C max 分别增加了 405%、415%和 270%。然而，胡椒碱和微米化混悬液并没有显著增加 AUC(0-t)和 C max。牛奶复合物降低了 CRM 的口服生物利用度（AUC(0-t)和 C max 分别降低了 10%和 37%）。胡椒碱和 HP-β-CD 复合物使 T max 统计学上显著增加，而纳米混悬液使 T max 降低。结果为提高 CRM 的口服生物利用度提供了关于溶解度增强和代谢抑制作用的有趣见解。
