Preparation of diclofenac epolamine on a 100 g batch scale

Tóm tắt

Diclofenac epolamine offers distinct advantages in solubility and permeability over other diclofenac salts, making it an excellent candidate for formulating transdermal patches or gels. Despite these benefits, existing published methods for preparing this ingredient remain hindered by several limitations. This article introduces a method for preparing diclofenac epolamine, achieving exceptional yield and purity, and utilizing commercially available, cost-effective diclofenac sodium as the starting material. The procedure employs three straightforward stages: acidification, salt formation, and purification, delivering an overall yield of 79.7% on a 100 g batch scale. The content of the resulting product ranges from 99.9% to 100.3%, as verified by high-performance liquid chromatography (HPLC). Structural confirmation of the synthesized compounds was established through a suite of spectroscopic techniques, including ¹H-NMR, ¹³C-NMR, mass spectrometry (MS), Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). This route demonstrates significant potential for industrial-scale production of diclofenac epolamine, providing a reliable source of raw material for topical formulations.