Deákné R E, Guti Z, Rádi E
Richter Gedeon Vegyészeti Gyár Rt., Budapest.
Acta Pharm Hung. 1992 May;62(3):115-20.
As a consequence of the presence of two ester groups in its molecule the main decomposition route of pipecuronium bromide (active ingredient of Arduan injection) is hydrolysis. In addition to this, autoxidation can also take place. In order to obtain a stable dosage form liophylized ampoules containing mannitol were prepared. Mannitol is not only a filling material but its role is also to decrease the dielectric constant of the solvent water thus increasing the stability of the drug substance before and during the liophylization procedure and after the dissolution of the content of the ampoules for administration. In order to protect the drug molecule against oxidation inert gas atmosphere was used during the production of the ampoules. The preparation is compatible with basic infusion solutions.
由于其分子中存在两个酯基,哌库溴铵(阿端注射液的活性成分)的主要分解途径是水解。除此之外,自动氧化也可能发生。为了获得稳定的剂型,制备了含有甘露醇的冻干安瓿。甘露醇不仅是一种填充材料,其作用还在于降低溶剂水的介电常数,从而在冻干过程之前、期间以及安瓿内容物溶解以供给药后提高药物物质的稳定性。为了保护药物分子免受氧化,在安瓿生产过程中使用了惰性气体气氛。该制剂与碱性输液溶液相容。