XIGDUO XR (dapagliflozin propanediol monohydrate/metformin hydrochloride) modified release tablets contain two oral antihyperglycaemic drugs used in the management of type 2 diabetes: dapagliflozin propanediol monohydrate and metformin hydrochloride.
XIGDUO XR is available for oral administration as tablets containing the following active ingredients: XIGDUO XR 10/500: 10 mg dapagliflozin (as dapagliflozin propanediol monohydrate) and 500 mg metformin hydrochloride.
XIGDUO XR 10/1000: 10 mg dapagliflozin (as dapagliflozin propanediol monohydrate) and 1000 mg metformin hydrochloride.
XIGDUO XR 5/1000: 5 mg dapagliflozin (as dapagliflozin propanediol monohydrate) and 1000 mg metformin hydrochloride.
Dapagliflozin: Dapagliflozin drug substance is a white to off-white powder, is non-hygroscopic, crystalline. Dapagliflozin is non-ionisable; thus, its aqueous solubility and partition coefficient are not affected by changes in pH. Dapagliflozin is a Biopharmaceutical Classification System (BCS) Class III drug.
Dapagliflozin propanediol monohydrate is an orally-active inhibitor of the human renal sodium-glucose co-transporter 2 (SGLT2), the major transporter responsible for renal glucose reabsorption. Dapagliflozin is described chemically as (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol, (S)-propylene glycol, monohydrate.
Molecular formula: C21H25ClO6·C3H8O2·H2O.
Molecular weight: 502.98.
Metformin hydrochloride: Metformin hydrochloride is a white to off-white crystalline compound. Metformin hydrochloride is freely soluble in water, slightly soluble in alcohol, and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68.
Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a biguanide with antihyperglycaemic effects.
Molecular formula: C4H11N5·HCl.
Molecular weight: 165.63.
Excipients/Inactive Ingredients: Each film-coated tablet of XIGDUO XR contains the following inactive ingredients: carmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, lactose, crospovidone, silicon dioxide, polyvinyl alcohol, macrogol 3350, titanium dioxide, purified talc, iron oxide red CI77491 (XIGDUO XR 10/500 and XIGDUO XR 5/1000 tablets), iron oxide yellow CI77492 (XIGDUO XR 10/1000 tablets).