Hadi Mohd Abdul, Raghavendra Rao Nidagurthi Guggilla, Srinivasa Rao Avanapu
Department of Pharmaceutics, Bhaskar Pharmacy College, Yenkapally (V), Moinabad (M), R. R. District, Hyderabad-500075, Telangana, India.
Department of Pharmaceutics, Sree Chaitanya Institute of Pharmaceutical Sciences, LMD Colony, Thimmapur, Karimnagar-505001, Telangana, India.
Sci Pharm. 2015 Jun 2;83(4):645-58. doi: 10.3797/scipharm.1503-16. Print 2015 Oct-Dec.
This research work aims to determine the pharmacokinetic parameters and in vitro-in vivo correlation of the selected ileocolonic-targeted coated mini-tablet filled capsule formulation of naproxen. The pure suspension and coated mini-tablet filled capsule formulation of naproxen were administered to adult albino rabbits through the oral route. The samples were analyzed for naproxen by an HPLC method. For the pure drug suspension, the peak plasma concentration was found as 8.499±0.029 μg/ml at 1.139±0.010 hours and the half-life was found to be 9.459±0.387 hours, whereas for the formulation the peak plasma concentration was found as 6.814±0.037 μg/ml at 8.042±0.069 hours and the half-life was found to be 19.657±0.359 hours. This decreased the peak plasma concentration at a delayed time and increased the half-life of the capsule formulation in comparison with the pure drug suspension which showed that naproxen was only targeted to the ileocolonic region. A significant in vitro-in vivo correlation (i.e. R(2)=0.9901) was also obtained. Thus, the results of these findings suggest that naproxen formulated as coated mini-tablets can be suitable for targeted ileocolonic drug delivery.
本研究旨在确定所选用的萘普生结肠靶向包衣迷你片填充胶囊制剂的药代动力学参数及体内外相关性。将萘普生的纯混悬液和包衣迷你片填充胶囊制剂经口服途径给予成年白化兔。采用高效液相色谱法分析样品中的萘普生。对于纯药物混悬液，在1.139±0.010小时时测得的血浆峰浓度为8.499±0.029μg/ml，半衰期为9.459±0.387小时；而对于该制剂，在8.042±0.069小时时测得的血浆峰浓度为6.814±0.037μg/ml，半衰期为19.657±0.359小时。与纯药物混悬液相比，该胶囊制剂延迟了血浆峰浓度出现的时间并延长了半衰期，这表明萘普生仅靶向于结肠区域。同时还获得了显著的体内外相关性（即R(2)=0.9901）。因此，这些研究结果表明，制成包衣迷你片的萘普生适合于结肠靶向给药。
