TRIJARDY XR Extended-release tablet Ref.[50504] Active ingredients: Empagliflozin Linagliptin Metformin

TRIJARDY XR tablets for oral use contain: empagliflozin, linagliptin, and metformin hydrochloride.

Empagliflozin

Empagliflozin is an inhibitor of the sodium-glucose co-transporter 2 (SGLT2).

The chemical name of empagliflozin is D-Glucitol,1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S).

The molecular formula is C₂₃H₂₇ClO₇ and the molecular weight is 450.91.

The structural formula is:

Empagliflozin is a white to yellowish, non-hygroscopic powder. It is very slightly soluble in water, sparingly soluble in methanol, slightly soluble in ethanol and acetonitrile, soluble in 50% acetonitrile/water, and practically insoluble in toluene.

Linagliptin

Linagliptin is an inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.

The chemical name of linagliptin is 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]7(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-

The molecular formula is C₂₅H₂₈N₈O₂ and the molecular weight is 472.54.

The structural formula is:

Linagliptin is a white to yellowish, not or only slightly hygroscopic solid substance. It is very slightly soluble in water. Linagliptin is soluble in methanol, sparingly soluble in ethanol, very slightly soluble in isopropanol, and very slightly soluble in acetone.

Metformin hydrochloride

Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a biguanide. Metformin 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 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.

The structural formula is:

TRIJARDY XR

Each film coated tablet of TRIJARDY XR consists of an extended-release metformin hydrochloride core tablet that is coated with the immediate-release drug substances: empagliflozin and linagliptin.

TRIJARDY XR tablets for oral administration are available in four strengths containing:

• 5 mg empagliflozin/2.5 mg linagliptin/1000 mg metformin hydrochloride extended-release
• 10 mg empagliflozin/5 mg linagliptin/1000 mg metformin hydrochloride extended-release
• 12.5 mg empagliflozin/2.5 mg linagliptin/1000 mg metformin hydrochloride extended-release
• 25 mg empagliflozin/5 mg linagliptin/1000 mg metformin hydrochloride extended-release

Each film-coated tablet of TRIJARDY XR contains the following inactive ingredients: Tablet Core: polyethylene oxide, hypromellose, and magnesium stearate. Film Coatings and Printing Ink: hydroxypropyl cellulose, hypromellose, talc, titanium dioxide, arginine, polyethylene glycol, carnauba wax, purified water, shellac glaze, n-butyl alcohol, propylene glycol, ammonium hydroxide, isopropyl alcohol, ferrosoferric oxide and ferric oxide yellow (5 mg/2.5 mg/1000 mg and 25 mg/5 mg/1000 mg), ferric oxide yellow and ferric oxide red (10 mg/5 mg/1000 mg), and ferrosoferric oxide and ferric oxide red (12.5 mg/2.5 mg/1000 mg).