Honorato Sara B, da Silva Cecília C P, de Oliveira Yara S, Mendonça Jorge S, Boechat Nubia, Ellena Javier, Ayala Alejandro P
Departamento de Física, Universidade Federal do Ceará, C. P. 6030, Fortaleza, Ceará 60455-970, Brazil.
Instituto de Física de São Carlos, Universidade de São Paulo, C.P. 369, São Carlos, São Paulo 13560-970, Brazil.
J Pharm Sci. 2016 Aug;105(8):2437-43. doi: 10.1016/j.xphs.2016.06.003. Epub 2016 Jul 7.
Diethylcarbamazine, administered as a water-soluble citrate salt, has been used for more than 50 years as the first-line drug in the treatment of lymphatic filariasis. Mass drug administration programs have been successful in reducing microfilaremia and providing important collateral deworming benefits. One of these initiatives is based on the addition of diethylcarbamazine citrate to table salt. The fortified salt retaining the efficacy of the drug in reducing microfilaremia, but there is little information about its behavior above room temperature. In this study, the thermal stability of diethylcarbamazine, as a free base and a citrate salt, was investigated by differential scanning calorimetry and thermogravimetry under different conditions. Diethylcarbamazine does not release hazardous degradation substances above its melting point. It was also confirmed that this drug is stable at normal cooking temperatures, even when dry heat cooking methods, such as baking or grilling, are considered. However, if the drug is formulated as a salt, as in the case of the citrate, special attention needs to be given to the degradation substances of the counter ion.
作为水溶性柠檬酸盐给药的乙胺嗪，已作为治疗淋巴丝虫病的一线药物使用了50多年。大规模药物给药计划已成功降低了微丝蚴血症，并带来了重要的辅助驱虫益处。其中一项举措是在食盐中添加枸橼酸乙胺嗪。强化盐在降低微丝蚴血症方面保持了药物的疗效，但关于其在室温以上的行为的信息很少。在本研究中，通过差示扫描量热法和热重分析法在不同条件下研究了作为游离碱和柠檬酸盐的乙胺嗪的热稳定性。乙胺嗪在其熔点以上不会释放有害降解物质。还证实，即使考虑干热烹饪方法（如烘焙或烧烤），该药物在正常烹饪温度下也是稳定的。然而，如果药物被制成盐，如柠檬酸盐的情况，需要特别关注抗衡离子的降解物质。
