PREPARATION AND CHARACTERIZATION OF MICROOSPHERES CONTAINING THE ANTI-INFLAMMATORY AGENTS, INDOMETHACIN, IBUPROFEN, AND KETOPROFEN
PREPARATION AND CHARACTERIZATION OF MICROOSPHERES CONTAINING THE ANTI-INFLAMMATORY AGENTS, INDOMETHACIN, IBUPROFEN, AND KETOPROFEN
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DOI：
10.1016/0168-3659(89)90059-x
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发表时间：
1989-11-01
影响因子：
10.8
通讯作者：
CHEN, H
中科院分区：
文献类型：
--
作者：
BODMEIER, R;CHEN, H
抗炎剂吲哚美辛、布洛芬和酮洛芬通过溶剂蒸发法使用聚合物如乙基纤维素、聚（ε-聚氧乙烯）、聚氧乙烯醚和聚氧乙烯醚包封。己内酯）、聚（甲基丙烯酸甲酯）、聚苯乙烯和Eudragit RS和RL。体外溶出度研究，扫描电子显微镜，差示扫描量热法被用来表征微球。与布洛芬和酮洛芬的释放相反，吲哚美辛从乙基纤维素微球中的释放对于口服使用来说太慢，即使在高载药量下。吲哚美辛的释放可以通过使用更渗透的聚合物或聚合物共混物来增加。在微球形成过程中聚合物和药物沉淀的速率取决于所选择的有机溶剂。当选择氯仿作为有机溶剂时，药物在聚合物和吲哚美辛晶体在微球表面上可见之前沉淀。使用二氯甲烷，聚合物在药物之前沉淀，并且没有观察到药物晶体。通过差示扫描量热法对微球的分析是不确定的，因为药物在加热步骤期间溶解在熔融聚合物中。吲哚美辛-聚（ε-己内酯）微球通过熔融分散技术而不使用有机溶剂来制备。
The anti-inflammatory agents, indomethacin, ibuprofen, and ketoprofen, were encapsulated by the solvent evaporation method using polymers such as ethylcellulose, poly(.epsilon.-caprolactone), poly(methyl methacrylate), polystyrene, and Eudragit RS and RL. In vitro dissolution studies, scanning electron microscopy, and differential scanning calorimetry were used to characterized the microspheres. In contrast to the release of ibuprofen and ketoprofen, the release of indomethacin from ethylcellulose microspheres was too slow for oral use even at high drug loadings. The indomethacin release could be increased by using more permeable polymers or polymer blends. The rates of polymer and drug precipitation during microsphere formation were dependent upon the organic solvent selected. When chloroform was selected as the organic solvent, the drug precipitated before the polymer and indomethacin crystals were visible on the microsphere surface. With methylene chloride, the polymer precipitated before the drug, and drug crystals were not observed. The analysis of the microspheres by differential scanning calorimetry was inconclusive since the drugs dissolved in the molten polymer during the heating step. Indomethacin-poly(.epsilon.-caprolactone) microspheres were prepared by a melt-dispersion technique without the use of organic solvents.