Analytical Development, Bayer Schering Pharma AG, Berlin, Germany.
J Pharm Sci. 2011 May;100(5):1773-82. doi: 10.1002/jps.22408. Epub 2011 Jan 6.
High-performance liquid chromatography (HPLC) methods using a charged aerosol detector (CAD), a mass selective detector (MSD), and a diode array detector (DAD) were developed to characterize the nonionic surfactants d-α-tocopheryl polyethylene glycol (1000) succinate (TPGS) and Surfhope sugar ester D-1216 (sucrose laurate). The molecular structure and the heterogeneous composition resulting from different isomers and various lengths of polyethylene glycol (PEG) chains make it difficult to develop sensitive and specific analytical methods for both surfactants. Hence, there is lack of knowledge about the stability and grade of impurity of these compounds. Sucrose laurate does not possess any chromophore, thus UV detection is not applicable. Therefore, CAD and MSD have been used for determination. The aim of the study was to characterize these nonionic surfactants and to examine chemical stability at pH 1.0 and 37 °C, simulating harsh gastric conditions. It was shown that both compounds are liable to degradation under these conditions. Sucrose monolaurate exhibited a massive degradation within 8 h incubation due to cleavage of the glycosidic bondage. About 50% of sucrose monolaurate broke down, whereas a marginal amount of 3.4% (± 0.4%) of TPGS degraded into d-α-tocopheryl succinate and the associated PEG chain.
建立了采用电喷雾检测器(CAD)、质量选择检测器(MSD)和二极管阵列检测器(DAD)的高效液相色谱法,用于对非离子表面活性剂 d-α-生育酚聚乙二醇(1000)琥珀酸酯(TPGS)和 Surfhope 糖酯 D-1216(月桂酸蔗糖酯)进行特征分析。由于不同异构体和不同长度的聚乙二醇(PEG)链的异构组成,使得这两种表面活性剂的分析方法既敏感又具有特异性变得非常困难。因此,人们对这些化合物的稳定性和杂质等级知之甚少。月桂酸蔗糖酯不含任何生色团,因此不适用紫外检测。因此,采用 CAD 和 MSD 进行了测定。本研究的目的是对这些非离子表面活性剂进行特征分析,并在 pH 值 1.0 和 37°C 下考察其化学稳定性,模拟苛刻的胃环境。结果表明,这两种化合物在这些条件下都容易降解。蔗糖月桂酸酯在孵育 8 小时内由于糖苷键的断裂而大量降解。约 50%的蔗糖月桂酸酯分解,而 TPGS 则有少量(3.4%±0.4%)降解为生育酚琥珀酸酯和相关的 PEG 链。