碱性调节剂对布洛芬固体分散体体外溶出度的影响

Effect on the dissolution rate of the solid dispersion of Ibuprofen by the alkalizer

目的:采用溶剂-冷冻干燥法制备布洛芬(ibuprofen,IBU)固体分散体,通过添加碱性调节剂进一步来提高其溶出速率。方法:将药物分别与不同载体及碱性调节剂制备成SD,通过测定其体外溶出度,来选择最优辅料及比例,结果:当以聚乙烯吡咯烷酮K30(PVPk30)为载体,Na2CO3为碱性调节剂,且IBU:PVPk30:Na2CO3=1:5:5%时,药物的溶出速率显著提高,2h内累积溶出度达到了98%,明显高于IBU及未加碱性调节剂的SD。

OBJECTIVE: Prepare the solid dispersions of ibuprofen with alkalizer by the solvent-freeze drying method to enhance the dissolution rate of the drug. METHODS: The solid dispersions of ibuprofen have been prepared with different carriers and alkalizers, respectively. Then chose the optimal materials and the ratio by the dissolution rate data. CONCLUSION: The dissolution rate improved to the 98% during 2h, when used PVPk30 as the carriers, Na2CO3 as the alkalizer and the ratio of IBU: PVPk30:Na2CO3was 1:5:5% in this solid dispersion system. The dissolution rate of the drug in this SD system higher than others.