Mack Ines, Sharland Mike, Brussee Janneke M, Rehm Sophia, Rentsch Katharina, Bielicki Julia
Paediatric Infectious Diseases, University Children's Hospital Basel, 4056 Basel, Switzerland.
Paediatric Infectious Diseases Research Group, Institute for Infection and Immunity, St George's University of London, London SW17 0QT, UK.
Antibiotics (Basel). 2021 Feb 23;10(2):225. doi: 10.3390/antibiotics10020225.
Amoxicillin-clavulanic acid (AMC) belongs to the WHO Essential Medicines List for children, but for optimal antimicrobial effectiveness, reconstituted dry powder suspensions need to be stored in a refrigerated environment. Many patients in low- and middle-income countries who are sold AMC suspensions would be expected not to keep to the specified storage conditions. We aimed to assess the stability of both ingredients in liquid formulations and dispersible tablets, combined with nationally representative data on access to appropriate storage. Degradation of amoxicillin (AMX) and clavulanic-acid (CLA) was measured in suspensions and dispersible tablets commercially available in Switzerland at different ambient temperatures (8 °C vs. 28 °C over 7 days, and 23 °C vs. 28 °C over 24 h, respectively). Data on access to refrigeration and electricity were assessed from the USAID-funded Demographic and Health Survey program. In suspensions, CLA degraded to a maximum of 12.9% (95% CI -55.7%, +29.9%) at 8°C and 72.3% (95% CI -82.8%, -61.8%) at a 28 °C ambient temperature during an observation period of 7 days. Dispersible tablets were observed during 24 h and CLA degraded to 15.4% (95% CI -51.9%, +21.2%) at 23 °C and 21.7% (-28.2%, -15.1%) at a 28 °C ambient temperature. There is relevant degradation of CLA in suspensions during a 7-day course. To overcome the stability challenges for all active components, durable child-appropriate formulations are needed. Until then, prescribers of AMC suspensions or pharmacists who sell the drug need to create awareness for the importance of proper storage conditions regarding effectiveness of both antibiotics and this recommendation should be reflected in the WHO Essential Medicines List for children.
阿莫西林-克拉维酸(AMC)属于世界卫生组织儿童基本药物清单,但为达到最佳抗菌效果,重新配制的干粉混悬液需储存在冷藏环境中。预计在低收入和中等收入国家购买AMC混悬液的许多患者不会遵守规定的储存条件。我们旨在评估液体制剂和分散片两种成分的稳定性,并结合全国代表性的适当储存条件获取数据。在瑞士市售的混悬液和分散片中,分别在不同环境温度下(7天内8℃与28℃,以及24小时内23℃与28℃)测量阿莫西林(AMX)和克拉维酸(CLA)的降解情况。从美国国际开发署资助的人口与健康调查项目中评估制冷和电力获取数据。在混悬液中,在7天的观察期内,CLA在8℃时降解最多达12.9%(95%置信区间-55.7%,+29.9%),在28℃环境温度下为72.3%(95%置信区间-82.8%,-61.8%)。分散片在24小时内观察,CLA在23℃时降解至15.4%(95%置信区间-51.9%,+21.2%),在28℃环境温度下为21.7%(-28.2%,-15.1%)。在7天疗程中,混悬液中的CLA存在显著降解。为克服所有活性成分的稳定性挑战,需要耐用的适合儿童的制剂。在此之前,AMC混悬液的开处方者或销售该药物的药剂师需要让人们认识到正确储存条件对两种抗生素有效性的重要性,并且这一建议应反映在世界卫生组织儿童基本药物清单中。