QTERN 5/10 is available as a film-coated tablet containing 5 mg saxagliptin as saxagliptin hydrochloride and dapagliflozin propanediol monohydrate equivalent to 10 mg dapagliflozin.
QTERN (saxagliptin/dapagliflozin) fixed dose combination tablets contain two oral antihyperglycaemic drugs used in the management of type 2 diabetes: saxagliptin and dapagliflozin.
Saxagliptin: Saxagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.
Saxagliptin is described chemically as (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo [22.214.171.124,7] dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, monohydrate.
Molecular formula: C18H25N3O2·H2O.
Molecular weight: 333.43 (monohydrate).
Saxagliptin is a white to light yellow or light brown powder, non-hygroscopic, crystalline. It is soluble in polyethylene glycol 400, acetone, acetonitrile, ethanol, isopropyl alcohol, methanol; sparingly soluble in water and slightly soluble in ethyl acetate.
Dapagliflozin: 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.
Dapagliflozin drug substance is a white to off-white powder, is non-hygroscopic, crystalline. Dapagliflozin is 4.5 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.
Excipients/Inactive Ingredients: Each tablet contains the following inactive ingredients: microcrystalline cellulose, croscarmellose sodium, lactose, magnesium stearate, silicon dioxide, polyvinyl alcohol, macrogol 3350, titanium dioxide, purified talc, red iron oxide (CI77491), yellow iron oxide (CI77492) and OPACODE monogramming ink S-1-10619 Blue.