Xipamide is a sulfonamide diuretic drug marketed by Eli Lilly under the trade names Aquaphor and Aquaphoril. It is used for the treatment of oedema and hypertension. Xipamide acts primarily at the distal convoluted tubule of the nephron to inhibit sodium chloride reabsorption, producing increased urinary excretion of sodium and water with a moderate kaliuretic effect. The active pharmaceutical ingredient is well absorbed after oral administration with peak plasma concentrations typically reached within 1 to 2 hours and an elimination half life in the range of about 5 to 8 hours. It is substantially bound to plasma proteins and is cleared mainly by renal excretion of unchanged drug together with minor metabolic pathways. For pharmaceutical development and quality control, xipamide is characterized by chromatographic and spectrometric techniques including HPLC, LC-MS and NMR, and formulated as oral tablets with excipients selected to ensure stability, acceptable dissolution and bioavailability.
Parent: Xipamide
Parent: Xipamide
Related substances observed in xipamide batches are typically monitored by validated HPLC methods and characterized by LC-MS when required. Typical specification limits applied in quality control are: each specified related substance not more than 0.20 percent w/w, each unspecified impurity not more than 0.05 percent w/w, and total impurities not more than 0.50 percent w/w. Common related compound classes include dehalogenated derivatives, N-dealkylation products, sulfonamide cleavage products and minor oxidative or hydrolytic products. Residual solvents are controlled in accordance with ICH Q3C limits, heavy metals are limited to not more than 20 parts per million, and water content by Karl Fischer is typically controlled to not more than 1.5 percent.
Xipamide is used to treat oedema associated with cardiac, hepatic or renal disease and to manage hypertension when a thiazide-like diuretic is indicated.
Xipamide is classified as a sulfonamide-derived, thiazide-like diuretic that acts on the distal convoluted tubule to inhibit sodium chloride reabsorption.
