Research Center Pharmaceutical Engineering (RCPE) GmbH, Inffeldgasse 13, 8010 Graz, Austria.
Worldwide Research and Development, Pfizer Inc., Sandwich, UK.
J Pharm Biomed Anal. 2022 Aug 5;217:114791. doi: 10.1016/j.jpba.2022.114791. Epub 2022 Apr 26.
Cellulose acetate (CA) is the main component of controlled-release (CR) coating of formulations such as osmotic-controlled release oral delivery system (OROS) and CR microspheres. Despite multiple applications, there are limited or no reports dealing with the characterization and quantification of CA in the formulated systems. Thus, the present investigation deals with the development of the Quantitative Carbon-13 Nuclear Magnetic Resonance (qCNMR) spectroscopy method for the determination of CA amount in the CR microsphere formulations. The developed qCNMR method was also verified using control CA samples from marketed OROS formulation. Thereafter, the concentration of CA in the microspheres was calculated. Furthermore, the impact of different concentrations of CA on the critical quality attributes such as the drug release profile from the formulation was investigated. The study demonstrated the CA coating levels to be inversely proportional to the extent and rate of release of API. The developed qCNMR method was found to be accurate and precise and can be explored further to investigate the effect of different stability conditions on the degree of polymerization and degradation of CA resulting in altered quality of pharmaceutical products.
醋酸纤维素（CA）是控释（CR）制剂的主要成分，如渗透控释口服给药系统（OROS）和 CR 微球。尽管有多种应用，但对配方系统中 CA 的特性和定量研究有限或没有报道。因此，本研究旨在开发用于定量测定 CR 微球制剂中 CA 含量的定量 13C 核磁共振（qCNMR）光谱法。所开发的 qCNMR 方法还使用市售 OROS 制剂中的对照 CA 样品进行了验证。然后，计算了微球中 CA 的浓度。此外，还研究了 CA 浓度对制剂中药物释放特性等关键质量属性的影响。研究表明，CA 涂层水平与 API 的释放程度和速率成反比。所开发的 qCNMR 方法被发现是准确和精密的，可以进一步探索不同稳定性条件对 CA 的聚合度和降解的影响，从而改变药物产品的质量。
