新型基于脂质的姜黄素口服制剂：通过实验设计方法的开发和优化。
Novel lipid based oral formulation of curcumin: development and optimization by design of experiments approach.
机构信息
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab 160062, India.
出版信息
Int J Pharm. 2012 Oct 15;436(1-2):617-23. doi: 10.1016/j.ijpharm.2012.07.031. Epub 2012 Jul 27.
The clinical utility of curcumin (CRM) is limited due to its poor oral bioavailability. Lipid based oral formulations (LBOFs) are emerging as useful oral drug delivery systems for 'difficult to deliver' molecules like CRM. In present study, we report novel Type IV LBOF for CRM using Gelucire 44/14, Labrasol, Vit. E TPGS and PEG 400 with superior CRM loading and enhanced oral bioavailability. The optimization of LBOF for CRM loading and post dilution droplet size was carried out by design of experiments (DoE) approach with Box-Behnken design. Oral bioavailability of optimized LBOF (O-LBOF) was evaluated in male Sprague-Dawley (SD) rats at a dose of 250 mg/kg. Raw CRM (control) showed C(max) and AUC(0-∞) of 32.29 ng/ml and 38.07 ng h/ml, respectively. O-LBOF improved C(max) and AUC(0-∞) by 11.6 and 35.8 folds respectively over control.
姜黄素（CRM）的临床实用性受到其口服生物利用度差的限制。基于脂质的口服制剂（LBOF）作为一种有前途的口服药物递送系统，正在为 CRM 等“难输送”分子的应用提供新的途径。在本研究中，我们报道了一种新型的 IV 型 LBOF，用于 CRM，使用 Gelucire 44/14、Labrasol、Vit. E TPGS 和 PEG 400，具有优异的 CRM 载药量和增强的口服生物利用度。通过 Box-Behnken 设计的实验设计（DoE）方法，对 LBOF 用于 CRM 载药量和稀释后液滴尺寸的优化进行了研究。在 250mg/kg 的剂量下，在雄性 Sprague-Dawley（SD）大鼠中评估了优化 LBOF（O-LBOF）的口服生物利用度。原始 CRM（对照）的 C(max)和 AUC(0-∞)分别为 32.29ng/ml 和 38.07ng h/ml。O-LBOF 使 C(max)和 AUC(0-∞)分别提高了 11.6 倍和 35.8 倍。
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