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关节腔注射用双醋瑞因聚乳酸-羟基乙酸共聚物微球的制备及相关性质研究
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| 篇名： | 关节腔注射用双醋瑞因聚乳酸-羟基乙酸共聚物微球的制备及相关性质研究 |
| TITLE： | |
| 摘要： | 目的：制备关节腔注射用双醋瑞因（DCR）聚乳酸-羟基乙酸共聚物（PLGA）微球，并考察其相关性质。方法：以PLGA为微球材料，采用乳化-溶剂挥发法制备DCR-PLGA微球；以高效液相色谱法测定DCR-PLGA微球的含量并计算载药量及包封率；以包封率为评价指标，采用正交试验设计优化制备工艺；通过光学显微镜、扫描电镜观察微球的形态及粒径；以体外释放试验考察其累积释放度。结果：DCR的检测质量浓度线性范围为2.1～105.0 μg/mL（r＝0.999 9）；精密度、稳定性、重复性、回收率试验的RSD均小于2.0％；最优工艺条件为PLGA的质量浓度为200 mg/mL，油水两相的体积比为1 ∶ 50，聚乙烯醇体积分数为1％。所得DCR-PLGA微球形态圆整，平均粒径为（11.2±4.7）μm，载药量为（4.25±0.26）％，包封率为（92.30±1.93）％，360 h内累积释放度为（73.08±5.33）％。结论：成功制得DCR-PLGA微球，其形态良好，粒径适宜，具有较好的缓释作用，适合关节腔注射给药。 |
| ABSTRACT： | OBJECTIVE： To prepare Diacerein （DCR）-loaded （poly lactic-co-glycolic acid） PLGA microspheres for intra-articular injection and investigate its related properties. METHODS： PLGA was used as microspheres material， and the microsphere was prepared by emulsification solvent evaporation method. The contents of DCR-PLGA microspheres were determined by HPLC， and drug-loading amount and entrapment efficiency were also calculated. Using entrapment efficiency as evaluation index， the preparation technology was optimized by orthogonal test. The morphology and particle size of microspheres were observed by optical microscope and SEM. Accumulative release rate was investigated by using in vitro release test. RESULTS： The linear range of DCR was 2.1-105.0 μg/mL （r＝0.999 9）. RSDs of precision， stability， reproducibility and recovery tests were all lower than 2.0％. The optimal technology was PLGA concentration of 200 mg/mL， volume ratio of oil-water 1 ∶ 50， polyvinyl alcohol concentration of 1％. The prepared DCR-PLGA microspheres were spherical， average particle size was （11.2±4.7）μm， drug-loading amount was（4.25±0.26）％ and encapsulation rate was（92.30±1.93）％， respectively. The drug release rate of DCR-PLGA microspheres within 360 h was about（73.08±5.33）％. CONCLUSIONS： DCR-PLGA microspheres are prepared successfully with good morphology， suitable particle size and obvious sustained release effect， which are suitable for intra-articular injection. |
| 期刊： | 2018年第29卷第12期 |
| 作者： | 蔡雁，钦富华，胡英，魏瑞龙 |
| AUTHORS： | CAI Yan，QIN Fuhua，HU Ying，WEI Ruilong |
| 关键字： | 双醋瑞因；关节腔注射；聚乳酸-羟基乙酸共聚物；微球；体外释放；性质 |
| KEYWORDS： | Diacerein； Intra-articular injection； PLGA； Microspheres； in vitro drug release； Property |
| 阅读数： | 431 次 |
| 本月下载数： | 7 次 |
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