海藻酸微球及骨架片中苯基偶氮苯的释放特性

目的：研究海藻酸微球及由海藻酸微球、果胶、HPMC组成的骨架片中苯基偶氮苯的释放特性。方法：海藻酸微球通过喷雾-凝聚法制得，苯基偶氮苯(PAA)作为疏水性模型药物通过吸附法被微球载运。制备了由海藻酸微球、果胶、HPMC组成的骨架片。测定了海藻酸微球及骨架片中苯基偶氮苯的释放。为进一步探讨药物释放机制，进行了骨架片的溶胀实验。结果：微球中PAA的释放依赖于释放介质，其中在水中释放不完全，在人工胃肠液中呈延缓到肠内释放的特性。在骨架片中也观察在人工胃肠液中的延缓释放行为。果胶酶有一定的加速骨架片释放的的作用。释放度和溶胀实验数据均证明骨架片为溶胀控制。结论：海藻酸微球可以作为一种疏水性药物的延缓释放载药系统。

Release Characteristics of 4-Phenylazoaniline From Alginate Microparticles and Matrix Tablets

AIM:To investigate the release cha racteristics of insoluble drug from algi nate macroparticles and matrix tablets METHOD:Alginate micropar ti cles were manufactured by spray-coagulation method 4-phenylazoaniline (PAA) wa s selected as a insoluble model drug PAA was loaded into alginate microparticl e s by adsorption method Matrix tablets composed of PAA loaded alginate micropar t icles, HPMC (K4M), pectin were directly compressed The release experiments of P AA from alginate microparticles and matrix tablets were conducted in different m edium To elucidate the release mechanism, swelling experiments were conducted, the erosion front, diffusion front and swelling front of tablets were measured RESULT:The release of PAA from the microparticles was found to de pend upon the release medium and incomplete %in vitro% release in deionized wa ter was observed Delayed release of PAA from both microparticles and matrix ta b lets in simulated gastrointestinal (GI) fluid were observed Pectinase could in c rease the release rate of PAA from the matrix tablets Both release data and sw e lling data indicated that the release of PAA from matrix tablets was controlled by swelling process CONCLUSION: Alginate microparticles could b e useful in delayed release of insoluble drugs