Department of Pharmacy, Health & Nutritional Sciences, Rende (CS), Italy.
Future Med Chem. 2014 Jan;6(1):35-43. doi: 10.4155/fmc.13.187.
The improvement of barnidipine photostability was investigated in cyclodextrin or liposome matrices and in appropriate combinations of these matrices. These supramolecular systems allowed the preparation of liquid formulations, as an alternative to the current solid commercial specialties.
MATERIALS & METHODS: Photodegradation stressing tests were performed according to the ICH rules and monitored by derivative spectrophotometry. Optimization was evaluated in terms of drug-inclusion efficiency.
The photodegradation rate of barnidipine in ethanol proved rapid (residual percentage of 29.81%) after a radiation exposure of 225 kJ/m(2). The residual concentrations detected for liposome and cyclodextrin complexes were 42.90 and 72.03%, respectively. The best results were obtained when the drug-cyclodextrin complex was in turn entrapped in liposomes (residual percentage of 90.78%).
The stability of the drug-in-cyclodextrin-in-liposome system increased significantly with a value close to that of solid formulations whose residual percentage was 96.03%.
本研究旨在环糊精或脂质体基质及其组合中改善巴尼地平的光稳定性。这些超分子体系允许制备液体制剂，作为目前固体商业制剂的替代。
按照 ICH 规则进行光降解强化试验，并通过导数分光光度法进行监测。以药物包封效率为指标进行优化评价。
在 225kJ/m(2)辐射暴露下，巴尼地平在乙醇中的光降解速度很快（残留率为 29.81%）。脂质体和环糊精复合物的残留浓度分别为 42.90%和 72.03%。当药物-环糊精复合物依次包封在脂质体中时，获得了最佳效果（残留率为 90.78%）。
药物-环糊精-脂质体系统的稳定性显著提高，接近于残留率为 96.03%的固体制剂。
