Acebedo-Martínez Francisco Javier, Domínguez-Martín Alicia, Alarcón-Payer Carolina, Garcés-Bastida Carolina, Verdugo-Escamilla Cristóbal, Gómez-Morales Jaime, Choquesillo-Lazarte Duane
Laboratorio de Estudios Cristalográficos, IACT, CSIC-Universidad de Granada, Avda. de las Palmeras 4, 18100 Armilla, Spain.
Department of Inorganic Chemistry, Faculty of Pharmacy, University of Granada, 18071 Granada, Spain.
Pharmaceutics. 2023 Jan 29;15(2):449. doi: 10.3390/pharmaceutics15020449.
According to the World Health Organization, more than 422 million people worldwide have diabetes. The most common oral treatment for type 2 diabetes is the drug metformin (MTF), which is usually formulated as a hydrochloride to achieve higher water solubility. However, this drug is also highly hygroscopic, thus showing stability problems. Another kind of worldwide prescribed drug is the non-steroidal anti-inflammatory drug (NSAID). These latter, on the contrary, show a low solubility profile; therefore, they must be administered at high doses, which increases the probability of secondary effects. In this work, novel drug-drug pharmaceutical solids combining MTF-NSAIDs have been synthesized in solution or by mechanochemical methods. The aim of this concomitant treatment is to improve the physicochemical properties of the parent active pharmaceutical ingredients. After a careful solid-state characterization along with solubility and stability studies, it can be concluded that the new molecular salt formulations enhance not only the stability of MTF but also the solubility of NSAIDs, thus giving promising results regarding the development of these novel pharmaceutical multicomponent solids.
根据世界卫生组织的数据,全球有超过4.22亿人患有糖尿病。2型糖尿病最常见的口服治疗药物是二甲双胍(MTF),它通常被制成盐酸盐以获得更高的水溶性。然而,这种药物也具有很强的吸湿性,因此存在稳定性问题。另一种全球范围内开具的药物是非甾体抗炎药(NSAID)。相反,这些药物的溶解度较低;因此,必须高剂量给药,这增加了产生副作用的可能性。在这项工作中,通过溶液法或机械化学方法合成了新型的MTF-NSAIDs药物组合固体。这种联合治疗的目的是改善母体活性药物成分的物理化学性质。经过仔细的固态表征以及溶解度和稳定性研究,可以得出结论,新的分子盐制剂不仅提高了MTF的稳定性,还提高了NSAIDs的溶解度,因此在这些新型药物多组分固体的开发方面给出了有前景的结果。