Stability, characterization, and manufacturing optimization of ferrous Ascorbate

Ferrous ascorbate, an essential pharmaceutical compound used in the treatment of iron deficiency anemia, exhibits unique physicochemical and solid-state properties that influence its manufacturability and clinical efficacy. This study investigates the stability and characterization of ferrous ascorbate produced by West Bengal Chemical Industries Ltd. Kolkata, India (WBCIL), focusing on preformulation studies, force degradation assessments, and analytical techniques including UV, IR spectroscopy, and HPLC. Key challenges such as hygroscopicity, flow properties, and tablet integrity were addressed through rigorous testing protocols, including flow parameter studies and swelling index evaluations. Comprehensive force degradation studies under various conditions revealed the compound's susceptibility to thermolysis and photolysis while highlighting its stability in acidic, basic, and oxidative environments. Flow properties, UV, and IR characterization studies confirmed alignment ...

Drugs are typically not administered as pure chemical entities; rather, they are formulated into various pharmaceutical dosage forms such as compressed tablets, sustained-release products, solutions, and injections [1]. The physicochemical properties of a drug play a crucial role in determining its bioavailability and final dosage form. The solid-state form of a compound impacts several solid-state properties including particle size, density, flowability, wettability, surface area, solubility, and hygroscopicity [1]. These properties significantly influence the manufacturability of the drug product and its clinical performance. Key parameters such as wettability, surface area, and solubility can affect the dissolution rate of the drug product without altering its equilibrium solubility. Consequently, preformulation studies are essential to develop a stable and efficacious pharmaceutical product [1, 2]. Ferrous ascorbate, chemically designated as L-(+)-Ascorbic acid iron (II) salt, is synthesized using ferrous sulphate as the precursor. It is prescribed for the treatment of iron deficiency anemia. Ferrous ascorbate is a hygroscopic, fine dark violet powder that is odorless and tasteless [3]. Iron is optimally absorbed in its ferrous state, although most dietary iron exists in the ferric form. Absorption of iron in the stomach is minimal; however, gastric secretions (HCl) facilitate the dissolution of iron, enabling it to form soluble complexes with ascorbic acid. Vitamin C and other substances aid in reducing iron to its ferrous form, which is essential for patients with partial gastrectomy, who often experience iron deficiency anemia [4]. Iron absorption predominantly occurs in the upper part of the small intestine, specifically the duodenum and upper jejunum