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目的 选择不同亲水性及空间构型的添加剂,研究其对聚乳酸聚乙烯醇酸共聚物(polylactic co glycolicacid, PLGA)药物释放动力学的影响,为心血管药物局部用药控释制剂的研究提供理论依据。方法 用抗细胞增生药物2 氨基色酮(U 86)作为代表性药物,用溶剂浇铸和压膜结合的方法制备药物/PLGA/添加剂双层膜,在37℃磷酸缓冲液中测定体外药物释放并用扫描电镜观察表面形态。结果 水溶性添加剂明显地提高了U- 86的释放率,并转变为近似的单阶段模式。药物释放速率与基质的失重速率非常吻合。水溶性添加剂的基质在水中形成高度多孔的结构。结论 添加剂的水溶性、分子量大小及空间构型等对于聚合物基质的孔隙结构具有决定性作用,而这些孔隙结构的特征又影响着药物释放机制以及释放动力学模式。
OBJECTIVE To study the effects of different hydrophilic and steric additives on the drug release kinetics of polylactic co-glycolic acid (PLGA), and to provide a theoretical basis for the study of controlled release formulations of topical cardiovascular drugs Theoretical basis. Methods The drug / PLGA / bilayer was prepared by antimicrobial drug 2 aminocrotonic acid (U 86) as a representative drug. The drug / PLGA / additive bilayer membrane was prepared by solvent casting and press bonding. The in vitro drug release was measured in phosphate buffered solution at 37 ℃. Scanning electron microscope to observe the surface morphology. Results Water-soluble additives significantly increased the release rate of U-86 and shifted to an approximately single-stage model. Drug release rate and matrix weight loss rate is very consistent. The matrix of water-soluble additives forms a highly porous structure in water. Conclusion The water solubility, molecular weight and spatial configuration of the additives play a decisive role in the pore structure of polymer matrix. The characteristics of these pore structures also affect the drug release mechanism and the release kinetic model.