You're using a free limited version of DrugPatentWatch: Upgrade for Complete Access

Last Updated: December 22, 2024

Claims for Patent: 6,525,057


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 6,525,057
Title: Sustained release ranolazine formulations
Abstract:A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 550 and 7500 ng base/mL.
Inventor(s): Wolff; Andrew A. (San Francisco, CA), Baker; Fiona (Dunfermline, GB), Langridge; John (Wrexham, GB)
Assignee: CV Therapeutics, Inc. (Palo Alto, CA)
Application Number:09/925,871
Patent Claims: 1. A method for treating variant or exercise-induced angina in a human, comprising administering to said human a sustained release ranolazine formulation that includes at least 50% by weight ranolazine, and an admixture of at least one pH-dependent binder and at least one pH-independent binder.

2. The method of claim 1, wherein the sustained release ranolazine formulation is administered in no more than two tablets per dose.

3. The method of claim 2, wherein the sustained release ranolazine formulation is administered once, twice or three times over 24 hours.

4. The method of claim 1 wherein the sustained release ranolazine formulation is administered at a frequency such that the peak to trough plasma ranolazine level does not exceed 4:1 over a 24 hour period.

5. The method of claim 1 wherein the sustained release ranolazine formulation is administered at a frequency such that the peak to trough plasma ranolazine level does not exceed 3:1 over a 24 hour period.

6. The method of claim 1 wherein the sustained release ranolazine formulation includes an amount of ranolazine sufficient to maintain ranolazine plasma levels in the human patient of about 550 to about 7500 ng base/mL for at least 24 hours.

7. The method of claim 1 wherein the sustained release ranolazine formulation includes from about 70 to about 80 wt % ranolazine.

8. The method of claim 7 wherein the sustained release ranolazine formulation includes from about 5 to about 12.5 wt % pH-dependent binders.

9. The method of claim 8 wherein the pH-dependent binder is at least one methacrylic acid copolymer.

10. The method of claim 9 wherein the sustained release ranolazine formulation includes from about 1 to about 3 wt % of pH-independent binders.

11. The method of claim 10 wherein the pH-independent binder is hydroxypropylmethyl cellulose.

12. The method of claim 11 wherein each tablet includes from about 350 to about 800 mg ranolazine.

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

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.