Apo-Gefitinib Description

Each tablet contains 250 mg gefitinib.
Chemical Name: N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine.
Molecular Formula and Molecular Mass: C₂₂H₂₄ClFN₄O₃; 446.91 g/mol.
Physicochemical Properties: Gefitinib is a white to off-white powder. Gefitinib is a free base. The molecule has pKa's of 5.4 and 7.2 and therefore ionizes progressively in solution as the pH falls. Gefitinib can be defined as sparingly soluble at pH 1, but is practically insoluble above pH 7, with the solubility dropping sharply between pH 4 and pH 6. In non-aqueous solvents, gefitinib is freely soluble in glacial acetic acid and dimethylsulphoxide, soluble in pyridine, sparingly soluble in tetrahydrofuran, and slightly soluble in methanol, ethanol (99.5%), ethyl acetate, propan-2-ol and acetonitrile.
Excipients/Inactive Ingredients: In addition to the active ingredient gefitinib 250 mg, each tablet contains the following non-medicinal ingredients: amino methacrylate copolymer, colloidal silicon dioxide, crospovidone, ferric oxide red, magnesium stearate, polyethylene glycol, polyvinyl alcohol, talc and titanium dioxide.