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Last Updated: December 16, 2025

Claims for Patent: 12,403,095

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Summary for Patent: 12,403,095

Title:	Stabilized tacrolimus composition
Abstract:	The invention relates to a stable pharmaceutical composition comprising comprising a solid dispersion of tacrolimus in a vehicle further comprising e stabilizing agent capable of providing a pH below 7 in the composition, as measured after re-dispersion in water, and preventing or reducing the formation upon storage of major degradation products of tacrolimus, in particular the 8-epitacrolimus.
Inventor(s):	Nikolaj Skak, Per Holm
Assignee:	Veloxis Pharmaceuticals Inc
Application Number:	US17/857,442
Patent Claims:	1. A pharmaceutical composition comprising a solid dispersion of tacrolimus in a mixture of a vehicle and a stabilizing agent that is a metal chelating agent and provides a pH below 7 in the composition, wherein (i) the composition comprises from about 0.5 to about 5% of tacrolimus, based upon 100% total weight of composition, (ii) the composition contains no more than 0.5% more 8-epitacrolimus after storage at 40° C. at 75% relative humidity for 5 weeks compared to the pharmaceutical composition prior to storage, based upon 100% total weight of tacrolimus, and (iii) the tacrolimus is the sole active ingredient in the composition, and (iv) the vehicle does not include a cyclo-dextrin. 2. The composition of claim 1, wherein the pH in the composition is in the range of 2.5 to 4.0. 3. The composition of claim 1, wherein the pH in the composition is in the range of 3.0 to 3.6. 4. The composition of claim 1, wherein the metal chelating agent is an organic acid selected from mono-, di-, oligo- or polycarboxylic acids. 5. The composition of claim 4, wherein the organic acid is selected from the group consisting of succinic acid, citric acid, tartaric acid, acrylic acid, benzoic acid, malic acid, maleic acid, and sorbic acid. 6. The composition of claim 1, wherein the stabilizing agent comprises citric acid. 7. The composition of claim 1, wherein the stabilizing agent comprises tartaric acid. 8. The composition of claim 1, wherein the vehicle is a mixture of polyethylene glycol and poloxamer. 9. The composition of claim 1, wherein the composition comprises about 1% tacrolimus, based upon 100% total weight of composition. 10. The composition of claim 1, wherein a sufficient amount of the stabilizing agent is present in the composition such that the composition comprises less than 0.5% by weight of 8-epitacrolimus after 12 weeks of storage at 25° C. and 60% relative humidity, based upon 100% total weight of tacrolimus. 11. A pharmaceutical composition comprising a solid dispersion of tacrolimus in a mixture of a vehicle and a stabilizing agent that is a metal chelating agent and provides a pH below 7 in the composition, wherein (i) the composition comprises from about 0.5 to about 5% of tacrolimus, based upon 100% total weight of composition, (ii) the composition contains no more than 0.2% more 8-epitacrolimus after storage at 25° C. at 60% relative humidity for 5 weeks compared to the pharmaceutical composition prior to storage, based upon 100% total weight of tacrolimus, (iii) the tacrolimus is the sole active ingredient in the composition, and (iv) the vehicle does not include a cyclo-dextrin. 12. The composition of claim 11, wherein the pH in the composition is in the range of 2.5 to 4.0. 13. The composition of claim 11, wherein the pH in the composition is in the range of 3.0 to 3.6. 14. The composition of claim 11, wherein the metal chelating agent is an organic acid selected from mono-, di-, oligo- or polycarboxylic acids. 15. The composition of claim 14, wherein the organic acid is selected from the group consisting of succinic acid, citric acid, tartaric acid, acrylic acid, benzoic acid, malic acid, maleic acid, and sorbic acid. 16. The composition of claim 11, wherein the stabilizing agent comprises citric acid. 17. The composition of claim 11, wherein the stabilizing agent comprises tartaric acid. 18. The composition of claim 11, wherein the vehicle is a mixture of polyethylene glycol and poloxamer. 19. The composition of claim 11, wherein the composition comprises about 1% tacrolimus, based upon 100% total weight of composition. 20. The composition of claim 11, wherein a sufficient amount of the stabilizing agent is present in the composition such that the composition comprises less than 0.5% by weight of 8-epitacrolimus after 12 weeks of storage at 25° C. and 60% relative humidity, based upon 100% total weight of tacrolimus. 21. The composition of claim 1, wherein the composition is in the form of a tablet.

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