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含超氧化物歧化酶的局部用制剂:制剂组成对物理稳定性和酶活性的影响。

Topical formulations with superoxide dismutase: influence of formulation composition on physical stability and enzymatic activity.

作者信息

Di Mambro Valéria M, Borin Maria F, Fonseca Maria J V

机构信息

Faculdade de Ciências Farmacêuticas de Ribeirão Preto-USP, Departamento de Ciências Farmacêuticas, av. do Café s/n, Ribeirao Preto 14049-903, São Paulo, Brazil.

出版信息

J Pharm Biomed Anal. 2003 Apr 24;32(1):97-105. doi: 10.1016/s0731-7085(03)00055-4.

Abstract

Three different topical formulations were supplemented with superoxide dismutase (SOD) and evaluated concerning physical and chemical stabilities in order to determine the most stable formulation that would maintain SOD activity. Physical stability was evaluated by storing the formulation at room temperature, and at 37 and 45 degrees C for 28 days. Samples were collected at 7-day intervals for assessment of rheological behavior. Chemical stability was evaluated by the measurement of enzymatic activity in formulations stored at room temperature and at 45 degrees C for 75 days. The formulations showed a pseudoplastic behavior, with a flow index of less than 1. There was no significant difference in the initial values of flow index, hysteresis loop or minimum apparent viscosity. The simple emulsion and the one stabilized with hydroxyethylcellulose showed decreased viscosity by the 21st day and with higher temperature, but no significant changes concerning the presence of SOD. Although there were no significant changes concerning storage time or temperature, the formulation stabilized with hydroxyethylcellulose showed a marked loss of SOD activity. The addition of SOD to the formulations studied did not affect their physical stability. Simple emulsions or emulsions stabilized with carboxypolymethylene seem to be better bases for enzyme addition than emulsion stabilized with hydroxyethylcellulose.

摘要

三种不同的局部用制剂添加了超氧化物歧化酶(SOD),并对其物理和化学稳定性进行了评估,以确定能保持SOD活性的最稳定制剂。通过将制剂分别在室温、37℃和45℃下储存28天来评估物理稳定性。每隔7天收集样品以评估流变行为。通过测量在室温及45℃下储存75天的制剂中的酶活性来评估化学稳定性。这些制剂表现出假塑性行为,流动指数小于1。流动指数、滞后环或最小表观粘度的初始值没有显著差异。简单乳液和用羟乙基纤维素稳定的乳液在第21天时粘度降低,且温度越高粘度越低,但SOD的存在没有显著变化。尽管储存时间或温度没有显著变化,但用羟乙基纤维素稳定的制剂显示出SOD活性明显丧失。在所研究的制剂中添加SOD并不影响其物理稳定性。与用羟乙基纤维素稳定的乳液相比,简单乳液或用羧基聚亚甲基稳定的乳液似乎是添加酶的更好基质。

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