a School of Pharmacy , University of Connecticut , Storrs , CT , USA.
Expert Opin Drug Deliv. 2016;13(4):593-608. doi: 10.1517/17425247.2016.1134484. Epub 2016 Feb 1.
This review discusses advances in the field of microsphere testing.
In vitro release-testing methods such as sample and separate, dialysis membrane sacs and USP apparatus IV have been used for microspheres. Based on comparisons of these methods, USP apparatus IV is currently the method of choice. Accelerated in vitro release tests have been developed to shorten the testing time for quality control purposes. In vitro-in vivo correlations using real-time and accelerated release data have been developed, to minimize the need to conduct in vivo performance evaluation. Storage stability studies have been conducted to investigate the influence of various environmental factors on microsphere quality throughout the product shelf life. New tests such as the floating test and the in vitro wash-off test have been developed along with advancement in characterization techniques for other physico-chemical parameters such as particle size, drug content, and thermal properties.
Although significant developments have been made in microsphere release testing, there is still a lack of guidance in this area. Microsphere storage stability studies should be extended to include microspheres containing large molecules. An agreement needs to be reached on the use of particle sizing techniques to avoid inconsistent data. An approach needs to be developed to determine total moisture content of microspheres.
本综述讨论了微球测试领域的进展。
体外释放测试方法，如样品分离法、透析膜囊法和 USP 仪器 IV 法，已被用于微球的测试。基于这些方法的比较，USP 仪器 IV 法目前是首选方法。为了缩短质量控制测试时间，已经开发了加速体外释放测试方法。已经开发了实时和加速释放数据的体外-体内相关性，以尽量减少进行体内性能评估的需要。进行了储存稳定性研究，以研究各种环境因素对整个产品货架期内微球质量的影响。随着对粒径、药物含量和热性能等其他物理化学参数的表征技术的进步，已经开发了新的测试方法，如漂浮测试和体外冲洗测试。
尽管在微球释放测试方面已经取得了重大进展，但该领域仍缺乏指导。微球储存稳定性研究应扩展到包含大分子的微球。需要就粒径技术的使用达成一致，以避免数据不一致。需要开发一种方法来确定微球的总水分含量。
