Claims for Patent: 11,944,621

Summary for Patent: 11,944,621

Title:	Oral gliptin compositions and method for preparation thereof
Abstract:	Described is an aqueous liquid oral gliptin composition comprising a gliptin or a pharmaceutically acceptable salt or ester thereof, and an artificial non-sugar alcohol sweetening agent, the solution having a sugar alcohol content of less than 25 w/v %. The composition has an improved taste and stability as compared to known compositions. Also described is a method comprising the steps of heating 80-95 v/v % of the water to 40-65° C., admixing the antioxidant, and, if present, the chelating agent and buffering agent, optionally, cooling down to 25-35° C., admixing sweetener, and, if present, preservative agent, and optionally pH adjusting agent or a portion of the pH adjusting agent, admixing the gliptin, if necessary, adjust the pH to the envisaged value by addition of a pH adjusting agent, admix the thickening agent, optionally in the form of a solution of the thickening agent in a co-solvent, homogenising the obtained mixture, admixing, if present, the wetting agent, if necessary, adjust the final volume by adding from the rest of the water, optionally filter through a 10 μm sieve, and filling in an appropriate container.
Inventor(s):	Ioannis Psarrakis, Konstantinos Lioumis
Assignee:	Pharma Data Research And Development Single Member SA
Application Number:	US17/771,387
Patent Claims:	1. An aqueous liquid oral gliptin composition comprising: 2-4 w/v % of sitagliptin or a pharmaceutically acceptable salt thereof; a thickening agent, wherein the thickening agent is selected from the group consisting of hydroxyethylcellulose, hydroxypropylcellulose, sodium alginate, sodium carboxymethylcellulose, gellan gum, polyethylene oxide polymer, and any combination thereof; wherein the thickening agent is present in the aqueous liquid oral gliptin composition at 0.1-2.0 w/v %; 0.8-2.0 w/v % of sucralose; 0.2-1.0 w/v % of acesulfame-K, 0.01-0.10 w/v % of butylated hydroxyanisole; 0.1-1.0 w/v % of trisodium citrate dihydrate; 0.1-0.5 w/v % of methyl paraben or a salt thereof; 0.01-0.1 w/v % of disodium edentate; 0.05-0.25 w/v % of polysorbate 80; 0.02-0.15 w/v % of citric acid; optionally a flavouring agent, a colouring agent, or a combination thereof; wherein the aqueous liquid oral gliptin composition has a sugar alcohol content of less than 10 w/v %, and wherein the pH of the aqueous liquid oral gliptin composition is from 4 to 7. 2. The aqueous liquid oral gliptin composition of claim 1, wherein the sitagliptin is in the form of a chloride or a phosphate salt. 3. The aqueous liquid oral gliptin composition of claim 1, wherein the pH of the aqueous liquid oral gliptin composition is from 4.5 to 6.5. 4. The aqueous liquid oral gliptin composition of claim 1, wherein the aqueous liquid oral gliptin composition comprises at less than 0.2% total impurities after storage of 2 months at 25° C. and 60% humidity. 5. The aqueous liquid oral gliptin composition of claim 1, wherein the aqueous liquid oral gliptin composition comprises at less than 1% total impurities after storage of 9 months at 25° C. and 60% humidity. 6. The aqueous liquid oral gliptin composition of claim 1, wherein the aqueous liquid oral gliptin composition comprises at least 95% of the gliptin or a pharmaceutically acceptable salt or ester thereof after storage of 18 months at 25° C. and 60% humidity. 7. The aqueous liquid oral gliptin composition of claim 1, wherein the aqueous liquid oral gliptin composition comprises at less than 1.5% total impurities after storage of 24 months at 25° C. and 60% humidity. 8. The aqueous liquid oral gliptin composition of claim 1, wherein the composition has a sugar alcohol content of less than 5 w/v %. 9. The aqueous liquid oral gliptin composition of claim 1, wherein the thickening agent is selected from the group consisting of hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, and any combination thereof. 10. The aqueous liquid oral gliptin composition of claim 1, wherein the thickening agent is present in the aqueous liquid oral gliptin composition at 0.1-0.8 w/v %. 11. The aqueous liquid oral gliptin composition of claim 1, wherein the thickening agent is present in the aqueous liquid oral gliptin composition at 0.4-0.6 w/v %. 12. The aqueous liquid oral gliptin composition of claim 1, wherein the flavouring agent is present in the aqueous liquid oral gliptin composition. 13. The aqueous liquid oral gliptin composition of claim 12, wherein the flavouring agent is forest fruits flavour, strawberry, raspberry, cherry, cranberry, blueberry, black currant, red currant, gooseberry, or lingonberries. 14. The aqueous liquid oral gliptin composition of claim 1, wherein the aqueous liquid oral gliptin composition comprises: 2.5-3.5 w/v % of sitagliptin or a pharmaceutically acceptable salt thereof; 0.1-2.0 w/v % of hydroxyethylcellulose; 0.8-2.0 w/v % of sucralose; 0.2-1.0 w/v % of acesulfame-K; 0.01-0.10 w/v % of butylated hydroxyanisole; 0.1-1.0 w/v % of trisodium citrate dihydrate; 0.1-0.5 w/v % of methyl paraben or a salt thereof; 0.01-0.1 w/v % of disodium edentate; 0.05-0.25 w/v % of polysorbate 80; 0.02-0.15 w/v % of citric acid; optionally a flavouring agent, a colouring agent, or a combination thereof; and wherein the pH of the aqueous liquid oral gliptin composition is from 4 to 7. 15. The aqueous liquid oral gliptin composition of claim 14, wherein the sitagliptin is in the form of a chloride salt. 16. The aqueous liquid oral gliptin composition of claim 14, wherein the pH of the aqueous liquid oral gliptin composition is from 4.5 to 6.5. 17. The aqueous liquid oral gliptin composition of claim 14, wherein the flavouring agent is present in the aqueous liquid oral gliptin composition. 18. The aqueous liquid oral gliptin composition of claim 17, wherein the flavouring agent is selected from the group consisting of forest fruits flavour, strawberry, raspberry, cherry, cranberry, blueberry, black currant, red currant, gooseberry, lingonberries, and any combination thereof.