➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

Express Scripts
AstraZeneca
McKinsey
Dow
Boehringer Ingelheim
McKesson

Last Updated: September 20, 2021

DrugPatentWatch Database Preview

Claims for Patent: 9,549,918


Email this page to a colleague

« Back to Dashboard

Summary for Patent: 9,549,918
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 a 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): Skak; Nikolaj (Virum, DK), Holm; Per (Vanlose, DK)
Assignee: VELOXIS PHARMACEUTICALS A/S (Horsholm, DK)
Application Number:13/029,304
Patent Claims: 1. A solid sustained release oral dosage form comprising a solid dispersion of tacrolimus in a mixture of a vehicle and tartaric acid, wherein the vehicle comprises polyethylene glycol and poloxamer.

2. The dosage form according to claim 1, wherein the pH in the dosage form is in the range of 3.0-3.6.

3. The dosage form according to claim 1, wherein the pH in the dosage form is in the range of 2.5-4.0.

4. The dosage form according to claim 1, wherein the tartaric acid is present in a concentration of less than 5% w/w, based on the total amount of tacrolimus, vehicle and tartaric acid.

5. The dosage form according to claim 1, which comprises 8 -epitacrolimus in an amount of less than 5% w/w, based upon the total weight of tacrolimus. vehicle and tartaric acid.

6. The dosage form of claim 1, wherein the dosage form comprises from about 0.5 to about 5% of tacrolimus, based upon 100% total weight of the dosage form.

7. The dosage form of claim 1, wherein the dosage form comprises from about 1 to about 4% tacrolimus, based upon 100% total weight of the dosage form.

8. A tablet comprising a solid dispersion of tacrolimus in a mixture of a vehicle and tartaric acid, wherein (a) the tablet contains 8-epitacrolimus, and the 8epitacrolimus is present at a concentration below 0.2% by weight, based upon the total weight of the tablet, and (b) the vehicle comprises polyethylene glycol and poloxamer.

9. The tablet of claim 8, wherein the solid dispersion is substantially free of organic solvent.

10. A tablet comprising (i) a dispersion of tacrolimus in a mixture of a vehicle and tartaric acid, and (ii) 8-epitacrolimus, wherein (a) the tablet comprises less than 0.5% by weight of the 8-epitacrolimus after 12 weeks of storage at 25.degree. C. and 60% relative humidity, based upon 100% total weight of tacrolimus, and (b) the vehicle comprises polyethylene glycol and poloxamer.

11. A tablet comprising (i) a dispersion of tacrolimus in a mixture of a vehicle and tartaric acid, and (ii) 8-epitacrolimus, wherein (a) the tablet comprises less than 0.5% by weight of the 8-epitacrolimus after 10 months of storage at 25.degree. C. and 60% relative humidity, based upon 100% total weight of tacrolimus, and (b) the vehicle comprises polyethylene glycol and poloxamer.

12. A tablet comprising a solid dispersion of tacrolimus in a mixture of a vehicle and tartaric acid, wherein (i) the tablet contains (a) no more than 0.5% by weight more 8-epitacrolimus after storage at 40.degree. C. at 75% relative humidity for 5 weeks compared to the tablet prior to storage, or (b) no more than 0.2% by weight more 8-epitacrolimus after storage at 25.degree. C. at 60% relative humidity for 5 weeks compared to the dosage form prior to storage, based upon 100% total weight of tacrolimus, (ii) the vehicle comprises polyethylene glycol and poloxamer.

13. A stabilized tablet comprising (a) a solid dispersion of tacrolimus in a mixture of a vehicle and tartaric acid and (b) 8-epitacrolimus, wherein (i) the tablet contains (a) no more than 0.5% by weight of the 8-epitacrolimus, (b) no more than 0.5% by weight of the Diene of tacrolimus, (c) no more than 0.5% by weight of the C4-epimer diene of tacrolimus, and/or (d) no more than 0.5% by weight of Regioisomer A of tacrolimus, after storage at 25.degree. C. at 60% relative humidity for 5 weeks, based upon 100% total weight of tacrolimus, and (ii) the vehicle comprises polyethylene glycol and poloxamer.

14. A tablet comprising tacrolimus in a mixture of vehicle and tartaric acid, wherein (i) the tablet comprises from about 0.05 to about 0.6% by weight of tartaric acid, based on the total amount of tacrolimus, vehicle and tartaric acid, and (ii) the vehicle comprises polyethylene glycol and poloxamer.

15. A tablet comprising tacrolimus in a mixture of a vehicle and tartaric acid, wherein the weight ratio of tacrolimus to tartaric acid is about 19:0.5 to about 20:6 and (ii) the vehicle comprises polyethylene glycol and poloxamer.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

Merck
Medtronic
Moodys
McKinsey
Colorcon
Dow

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.