利培酮PLGA长效注射微球的稳定性考察

Investigation on Stability of Long-acting Risperidone-containing PLGA Microspheres for Injection

本课题组前期研究中利用自主研发的超细微粒制备系统构建了利培酮聚乳酸-羟基乙酸共聚物(PLGA)长效注射微球,本课题进一步探究其稳定性,为工业化生产、包装、贮存及运输条件提供理论依据。通过影响因素、加速及长期稳定性试验,考察利培酮PLGA长效注射微球的外观性状、分散性、主药含量、有关物质及释放行为。温度、湿度和光照对注射微球的稳定性均有影响,导致其释药速率显著加快,建议密封于棕色西林瓶中低温贮存,在此包装条件下,注射微球的加速和长期稳定性在3个月内均合格。本研究结果提示,利培酮PLGA长效注射微球应置于棕色西林瓶中封装,并在低温、干燥的环境中贮存。

In our previous study,risperidone-containing PLGA microspheres(RIS-PLGA MS)for injection were fabricated by ultra-fine particles processing system,which were developed previously by our group.However,the stability of RIS?PLGA MS was still unknown.The objective of this study was to perform the stability investigation to provide a theory basis for the industrialized production,packaging,storage and transportation.Stress stability,accelerate stability and long-term stability of RIS?PLGA MS were conducted.The appearance,dispersibility,drug content,related substances and release behavior of RIS-PLGA MS were detected.The stability of RIS-PLGA MS was affected by temperature,humidity and illumination,which leading to a higher release rate.It was recommended to keep RIS?PLGA MS at sealed brown vials in the low temperature,where could render a desirable quality within three months in accelerate and long-term stability tests.In conclusion,RIS-PLGA MS should be stored at sealed brown vials in the dry and low temperature condition.