Majid Khan G, Zhu J B
Zhong Kun Pharmaceutical Research Institute, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, P.R. China.
J Control Release. 1998 Dec 4;56(1-3):127-34. doi: 10.1016/s0168-3659(98)00080-7.
The objective of this study was to investigate the mechanism of ibuprofen (IBF) release from tablets prepared by wet granulation method, using Surelease as a granulating agent. The influence of certain parameters such as the levels of Surelease solids content (SSC), pH of dissolution media, selected dissolution method, and agitation speed on the release profiles of IBF was investigated. The effect of partial replacement of lactose (primary excipient) by various coexcipients such as microcrystalline cellulose, starch, polyvinylpyrrolidone (PVP), sodium alginate, hydroxypropylmethylcellulose (HPMC), and sodium carboxymethyl cellulose (CMC-Na) was also studied. Tablets prepared with surelease as a granulating agent were non-disintegrating and exhibited prolonged release rates as compared to control tablets. The release of IBF from the tablets appears to occur either via water-filled pores or by diffusion through membrane, depending on the levels of SSC. At higher SSC levels pH independent release profiles for IBF were achieved. Dissolution method and agitation speed exhibited no significant effect on the release profiles. All the coexcipients studied enhanced the release rates, irrespective of whether the coexcipients were water-soluble or water-insoluble.
本研究的目的是研究以Surelease作为制粒剂，通过湿法制粒制备的片剂中布洛芬（IBF）的释放机制。研究了某些参数，如Surelease固含量（SSC）水平、溶出介质的pH值、选定的溶出方法和搅拌速度对IBF释放曲线的影响。还研究了用微晶纤维素、淀粉、聚乙烯吡咯烷酮（PVP）、海藻酸钠、羟丙基甲基纤维素（HPMC）和羧甲基纤维素钠（CMC-Na）等各种辅料部分替代乳糖（主要辅料）的效果。与对照片剂相比，用Surelease作为制粒剂制备的片剂不崩解，且释放速率延长。片剂中IBF的释放似乎通过充满水的孔隙或通过膜扩散发生，这取决于SSC的水平。在较高的SSC水平下，实现了IBF的pH无关释放曲线。溶出方法和搅拌速度对释放曲线没有显著影响。所有研究的辅料都提高了释放速率，无论辅料是水溶性的还是水不溶性的。
