复方布洛芬缓释片研究

Development of the Compound Sustained-release Tablets of Ibuprofen with Pseudoephedrine Hydrochloride

研究了由布洛芬和盐酸伪麻黄碱组成的复方骨架型级释片。根据两药溶解度的不同设计了处方，并探讨了药物从缓释系统中的释放机理，同时选用12名受试者采用2×2交叉设计，比较了缓释片与进口普通片的生物利用度和体内药动学特征。结果表明，缓释片体外释药可用Korsmeyer／Pappas方程描述，药物均显示出良好的缓释行为。体内结果显示，缓释片与普通片相比生物利用度相等，而药物吸收速度较慢，血药浓度较为平缓、持久。

Development of the novel sustained- release matrix tablet of ibuprofen (IB ) combined with pseu doephedrine hydrochloride (PE-HCl) was described. The formulation of the sustained-release system was designed tentatively based on the different solubilities of two drugs, and was optimized according to the mechanism of drugs releasing from the matrix. The bioavailability and pharmacokinetics of IB and PE-HCl from the final sustained-release tablet were compared with a conventional reference standard tablet in 12 normal subjects under a two-way crossover design. Results showed that, the sustained-release tablet exhibited excellent sustained release profile in vitro, which cou1d be well described by korsmeyer/Pappas equation. In vivo studies showed that, the final sustainedrelease tablet had the same bioavailability as the reference tablet and could produce more stable and durable plasma drug levels than those of the reference tablet. Moreover, the fraction absorbed in vivo and the fraction released in vitro of IB or PE-HCl from sustained-release tablets were well correlated, and these correlations can be used to propose manufacturing specifications.