Xigduo XR Description

XIGDUO XR 5 mg/1000 mg: Each film-coated tablet contains 5 mg dapagliflozin as dapagliflozin propanediol and 1000 mg metformin hydrochloride extended-release.
XIGDUO XR 10 mg/1000 mg: Each film-coated tablet contains 10 mg dapagliflozin as dapagliflozin propanediol and 1000 mg metformin hydrochloride extended-release.
Dapagliflozin: Dapagliflozin propanediol is described chemically as D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl) methyl]phenyl]-,(1S)-, compounded with (2S)-1,2-propanediol, hydrate (1:1:1). The empirical formula is C₂₁H₂₅ClO₆•C₃H₈O₂•H₂O and the formula weight is 502.98.
Metformin hydochloride: Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a white to off-white crystalline compound with a molecular formula of C₄H₁₁N₅•HCl and a molecular weight of 165.63. 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.
System components and performance: XIGDUO XR fixed dose combinations (FDCs) are bi-layer tablets compressed with extended-release metformin as the first layer and immediate-release dapagliflozin as the second layer. The extended-release metformin layer comprises a dual hydrophilic polymer matrix system. Metformin hydrochloride is combined with a drug release controlling polymer to form an "inner" phase, which is then incorporated as discrete particles into an "external" phase of a second polymer. After oral administration, the dapagliflozin layer dissolves immediately. The metformin layer absorbs the fluid from the gastrointestinal (GI) tract, causing the polymers to hydrate and swell. Drug is released slowly from the metformin layer by a process of diffusion through the gel matrix that is essentially independent of pH. The hydrated polymer system is not rigid and is expected to be broken up by normal peristalsis in the GI tract. The biologically inert components of the tablet may occasionally remain intact during GI transit and will be eliminated in the feces as a soft, hydrated mass.
Excipients/Inactive Ingredients: Each film-coated tablet of XIGDUO XR contains 5 mg or 10 mg of dapagliflozin and 1000 mg of metformin and the following inactive ingredients: Dapagliflozin layer for 5 mg and 10 mg FDCs: microcrystalline cellulose, anhydrous lactose, crospovidone, silicon dioxide, and magnesium stearate.
Metformin Layer for 1000 mg FDCs: carboxymethylcellulose sodium, Hypromellose 2208, silicon dioxide, and magnesium stearate.
Coating: polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and iron oxides (5/1000 and 10/1000).