Immediate release of ibuprofen from Fujicalin®-based fast-dissolving self-emulsifying tablets
Immediate release of ibuprofen from Fujicalin®-based fast-dissolving self-emulsifying tablets
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DOI：
10.3109/03639045.2011.571695
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发表时间：
2011-11-01
影响因子：
3.4
通讯作者：
Chi, Sang-Cheol
中科院分区：
文献类型：
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作者：
Kang, Myung Joo;Jung, Soo Young;Chi, Sang-Cheol
背景：固体形式的自乳化给药系统（SEDDS）由于其强吸附和与载体的物理相互作用，极大地限制了药物的释放。为了促进药物在胃中的释放，研究了酸溶性粉状载体Fujicalin (R)与不同崩解剂和亲水性润滑剂的作用。方法：以布洛芬（ibuprofen， IBU）的固态自乳化剂（SEDDS）、各种崩解剂和润滑剂为原料，制备布洛芬（IBU）速释自乳化片（IR-SETs），并对其进行药物释放评价，制备出与液体SEDDS的IBU释放率相近的IR-SET。结果：液体SEDDS由Capryol 90、cremoophor EL、Labrasol和IBU组成，比例为3:4:3:3，并采用各种吸附剂固化。采用直接压片法将其制成粉末状。以Fujicalin (R)为基础的SEDDS片与Neusilin (R)和Neosyl (R)为基础的SEDDS片相比，IBU的溶出率显著提高。以Fujicalin (R)为吸附剂，Polyplasdone (R)为崩解剂，碳酸氢钠为助崩解剂制备的IBU IR-SET配方显示，在pH为1.2的刺激胃液中，5min内IBU的初始负荷释放量超过90%，与液体SEDDS的IBU释放率几乎相当。粒径分析显示，液体（116 nm）和IR-SET （110 nm）形成的微乳液滴大小无显著差异。结论：新型IR-SET具有快速起效的特点，有望作为IBU的速释SEDDS片。
Background: Drug release from a solid form of self-emulsifying drug delivery system (SEDDS) has greatly been limited due to strong adsorption and physical interaction with carriers. To facilitate drug release process in the stomach, an acid-soluble powderizing carrier, Fujicalin (R) was evaluated together with different disintegrants and hydrophilic lubricants.Method: Immediate-release self-emulsifying tablets (IR-SETs) of ibuprofen (IBU) was prepared with solidified SEDDS of IBU, various disintegrants, and lubricants, and drug release was evaluated to develop IR-SET that can release IBU with a similar IBU release rate to that obtained with liquid SEDDS.Results: The liquid SEDDS consisted of Capryol 90, Cremophor EL, Labrasol, and IBU at a ratio of 3: 4: 3: 3, and was solidified with various adsorbents. The powderized SEDDS was tabletted by a direct compression. Fujicalin (R)-based SEDDS tablets demonstrated remarkably higher dissolution rate of IBU compared with Neusilin (R) and Neosyl (R)-based SEDDS tablets. The IR-SET formula of IBU prepared with Fujicalin (R) as an adsorbent, Polyplasdone (R) as a disintegrant, and sodium bicarbonate as a co-disintegrant showed over 90% of initially loaded dose of IBU released within 5 min in a stimulated gastric juice (pH 1.2), exhibiting almost equivalent rate of IBU release to that shown by liquid SEDDS. The particle size analysis revealed no significant differences in droplet sizes of the microemulsions formed from liquid (116 nm) and IR-SET (110 nm).Conclusion: The novel IR-SET can be promising as a fast-releasing SEDDS tablet of IBU for fast onset of action.