乙酰半胱氨酸与一些常用片剂辅料的相容性研究

Compatibility study between acetylcysteine and some commonly used tablet excipients.

作者信息

Kerc J, Srcic S, Urleb U, Kanalec A, Kofler B, Smid-Korbar J

机构信息

Department of Research and Development, Lek Pharmaceutical and Chemical Works, Ljubljana, Slovenia, Yugoslavia.

出版信息

J Pharm Pharmacol. 1992 Jun;44(6):515-8. doi: 10.1111/j.2042-7158.1992.tb03657.x.

DOI:10.1111/j.2042-7158.1992.tb03657.x

PMID:1359077

Abstract

Differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FT-IR), HPLC and TLC were used to investigate the interactions between the mucolytic drug acetylcysteine and a number of commonly used tablet and capsule excipients. Acetylcysteine was found to be compatible with microcrystalline cellulose (Avicel PH 101), sodium carboxymethylcellulose, amorphous silicon dioxide (Aerosil), PVP, cross-linked PVP (Polyplasdone XL), corn starch, saccharose and magnesium stearate. Acetylcysteine thermal stability (onset degradation temperature) was decreased in mixtures with corn starch, magnesium stearate, saccharose and lactose. Interactions of acetylcysteine with lactose, PEG 4000 and 6000, glycine, adipic acid and saccharin sodium were found using DSC and studied in detail with FT-IR, HPLC and TLC. The results suggest that acetylcysteine in mixtures with PEG 4000, glycine or saccharin sodium is degraded during storage at conditions of high temperature and humidity.

摘要

采用差示扫描量热法（DSC）、傅里叶变换红外光谱法（FT-IR）、高效液相色谱法（HPLC）和薄层色谱法（TLC）研究了黏液溶解药物乙酰半胱氨酸与多种常用片剂和胶囊辅料之间的相互作用。结果发现，乙酰半胱氨酸与微晶纤维素（微晶纤维素PH 101）、羧甲基纤维素钠、无定形二氧化硅（气相二氧化硅）、聚乙烯吡咯烷酮（PVP）、交联聚乙烯吡咯烷酮（交联聚维酮）、玉米淀粉、蔗糖和硬脂酸镁具有相容性。在与玉米淀粉、硬脂酸镁、蔗糖和乳糖的混合物中，乙酰半胱氨酸的热稳定性（起始降解温度）降低。利用DSC发现了乙酰半胱氨酸与乳糖、聚乙二醇4000和6000、甘氨酸、己二酸和糖精钠之间的相互作用，并通过FT-IR、HPLC和TLC进行了详细研究。结果表明，乙酰半胱氨酸与聚乙二醇4000、甘氨酸或糖精钠的混合物在高温高湿条件下储存时会发生降解。