Al Sabbagh Chantal, Agapova Elena, Boudy Vincent, Mignet Nathalie
Faculté de Pharmacie, Université de Paris, UTCBS (Unité de Technologies Chimiques et Biologiques pour la Santé), Paris, France.
Pharmaceutical R&D Department, Agence Générale des Equipements et Produits de Santé (AGEPS), Paris, France.
J Oncol Pharm Pract. 2022 Sep;28(6):1303-1314. doi: 10.1177/10781552211020808. Epub 2021 May 30.
FOLFOX is the most common chemotherapy combination prescribed in colorectal cancer. It is composed of calcium levofolinate, 5-fluorouracil and oxaliplatin which demonstrated synergistic outcome. Nowadays, the lack of all-in-one formulation is due to the chemical composition of the pharmaceutical products and the highly pH-dependent stability of each drug. Herein, we aimed to investigate the stability of a ternary mixture of 5-fluorouracil, oxaliplatin and calcium levofolinate, knowing that coadministering these drugs would improve their efficacy. The effect of three pHs (5.0, 6.0 and 7.5) and two drug concentrations (8/3/6 and 1/1/1 mg/ml for 5-fluorouracil, oxaliplatin and calcium levofolinate, respectively) were examined. A high-performance liquid chromatography method was developed to separate and quantify the three drugs in one run. At higher concentrations, the ternary mixture was unstable regardless of pH. By reducing concentration, drug stability and compatibility in the mixture was improved at pH 5.0 for up to 3 days at +5°C ± 3 °C. In addition, binary mixtures provided stable properties at defined pHs. 5-fluorouracil/oxaliplatin mixture was stable at pH 5.0 over 48 hours while 5-fluorouracil/calcium levofolinate mixture was stable at pHs 6.0 and 7.5 up to 7 days.
FOLFOX是结直肠癌中最常用的化疗组合。它由亚叶酸钙、5-氟尿嘧啶和奥沙利铂组成,已证明具有协同效果。目前,缺乏三合一制剂是由于药品的化学成分以及每种药物对pH高度依赖的稳定性。在此,我们旨在研究5-氟尿嘧啶、奥沙利铂和亚叶酸钙三元混合物的稳定性,因为我们知道联合使用这些药物会提高它们的疗效。研究了三种pH值(5.0、6.0和7.5)以及两种药物浓度(5-氟尿嘧啶、奥沙利铂和亚叶酸钙分别为8/3/6和1/1/1毫克/毫升)的影响。开发了一种高效液相色谱方法,可在一次运行中分离和定量这三种药物。在较高浓度下,无论pH值如何,三元混合物都不稳定。通过降低浓度,在5.0的pH值下,混合物在+5°C±3°C时的药物稳定性和相容性可提高至3天。此外,二元混合物在特定pH值下具有稳定的性质。5-氟尿嘧啶/奥沙利铂混合物在pH 5.0下48小时内稳定,而5-氟尿嘧啶/亚叶酸钙混合物在pH 6.0和7.5下长达7天稳定。