Faculty of Arts and Sciences, Holy Spirit University of Kaslik (USEK), Jounieh, Lebanon.
School of Engineering, Holy Spirit University of Kaslik (USEK), Jounieh, Lebanon.
BMC Pharmacol Toxicol. 2020 Feb 22;21(1):15. doi: 10.1186/s40360-020-0390-y.
In developing countries, brand-generic substitution is not based on validated scientific evidence that confirm the therapeutic equivalence of the generic to the originator. Rather, decisions are made based on the availability of generic medications. Substitution by inappropriate preparations applies to antibiotics, which may increase the risk of resistance in case of underdosing. This analytical study aims to dose and assess for the accuracy of labeling three oral antibiotic preparations, namely ciprofloxacin hydrochloride, amoxicillin trihydrate and amoxicillin trihydrate-clavulanate potassium, the active pharmaceutical ingredients (APIs) found in brand and generic tablets available on the Lebanese market.
One brand and 4 generics of ciprofloxacin tablets, 3 generic amoxicillin tablets, and 1 brand and 4 generics of amoxicillin-clavulanic acid medications, were quantified, taking 2 batches of each. According to the United States Pharmacopeia (USP) guidelines, ultra-high pressure liquid chromatography was used to measure the APIs content within tablets. The USP required assay limit of the API was taken as the main comparison criteria.
Out of the 5 ciprofloxacin medications tested, all 5 were out of the 2% required range, thus being substandard. For amoxicillin, all 3 medications were within the 20% range. As for amoxicillin-clavulanic acid medications, 4 out of 5 medications met the 30% required range of clavulanic acid and one exceeded the claimed amount of clavulanic acid, while all 5 met the assay limit for amoxicillin.
These findings raise safety and efficacy concerns, providing solid grounds for potential correlations of antibiotic resistance/substandard antibiotics.
在发展中国家，品牌仿制药的替代并非基于经过验证的科学证据，以确认仿制药与原研药的治疗等效性。相反，决策是基于仿制药的供应情况做出的。不适当的制剂替代适用于抗生素，这可能会增加剂量不足导致耐药性的风险。本分析性研究旨在对在黎巴嫩市场上可获得的品牌和仿制药片剂中含有的三种口服抗生素制剂（盐酸环丙沙星、三水合阿莫西林和三水合阿莫西林-克拉维酸钾）进行剂量测定和标签准确性评估。
对 1 个品牌和 4 个仿制药的环丙沙星片剂、3 个普通阿莫西林片剂以及 1 个品牌和 4 个仿制药的阿莫西林-克拉维酸药物进行了定量分析，每种药物均采集了 2 批。根据美国药典（USP）指南，使用超高效液相色谱法测定片剂中的 API 含量。USP 规定的 API 测定限被视为主要比较标准。
在所测试的 5 种环丙沙星药物中，有 5 种药物的含量均不在 2%的要求范围内，因此属于不合格产品。对于阿莫西林，所有 3 种药物均在 20%的范围内。至于阿莫西林-克拉维酸药物，有 4 种药物的克拉维酸含量符合 30%的要求范围，1 种药物的克拉维酸含量超过了声称的含量，而所有 5 种药物的阿莫西林含量均符合测定限。
这些发现引起了对安全性和疗效的关注，为抗生素耐药性/不合格抗生素的潜在相关性提供了确凿的依据。
