.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 4,963,551

« Back to Dashboard

Claims for Patent: 4,963,551

Title: Stable lyophilized form of (S)-(+)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione and solutions thereof
Abstract:The present invention is directed to a stable, rapidly soluble lyophilized injectable composition containing up to about 6% moisture and capable of being stored at room temperature comprising the hydrochloric or sulfate salt of a compound selected from the group consisting of (S)-(+)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione and (R)-(-)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione; wherein said lyophilized composition is prepared from a bulk solution comprising from about 25 mg/mL to about 40 mg/mL of said compound dissolved in a hydrochloric acid or sulfuric acid; wherein the pH of said bulk solution is from about 1.0 to about 2.0. The invention is further directed to an isotonic solution which is formed upon reconstitution of the lyophilizate of the invention with a pharmaceutically acceptable diluent.
Inventor(s): Palepu; Nagesh R. (Franklin County, OH), Martin; Joyce W. (Franklin County, OH)
Assignee: Erbamont Inc. (Dublin, OH)
Application Number:07/463,844
Patent Claims: 1. A stable, rapidly soluble, lyophilized injectable composition containing up to about 6% moisture and capable of being stored at room temperature comprising the hydrochloric acid or sulfuric acid salt of (S)-(+ )-bis-4,4'-(1-methyl-1,2- ethanediyl)2,6-piperazinedione or (R)-(-)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione; wherein said lyophilized composition is prepared from a bulk solution comprising from about 25 mg/mL to about 40 mg/mL of said compound dissolved in hydrochloric or sulfuric acid; and wherein the pH of said bulk solution is from about 1.0 to about 2.0.

2. A composition according to claim 1 wherein said acid is hydrochloric acid.

3. A composition according to claim 2 wherein said bulk solution contains 30 mg/mL of said compound.

4. A composition according to claim 3 wherein said compound is (S)-(+)-bis-4,4'-(1-methyl-1,2ethanediyI)2,6-piperazinedione.

5. A composition according to claim 3 wherein said compound is (R)-(-)-bis-(1-methyl-1,2-ethanediy-)2,6piperazinedione.

6. A composition according to claim 1 which dissolves in about 5 sec. upon reconstitution with a pharmaceutically acceptable diluent.

7. A composition according to claim 1 which is stable at room temperature for up to about 11/2 years.

8. A composition according to claim 1 wherein said acid is sulfuric acid.

9. A sterile, intravenously injectable aqueous solution obtained, upon reconstitution of the lyophilized bulk solution is from about 1.0 to about 2.0.

10. An isotonic solution which is suitable for intravenous administration to a patient in need of treatment which has a pH of from about 3.0 to about 6.0, wherein said isotonic solution is prepared by reconstituting a lyophilizate with a pharmaceutically acceptable diluent; wherein said lyophilizate is a stable, rapidly soluble lyophilized injectable composition containing up to about 6% moisture and capable of being stored at room temperature comprising the hydrochloride or sulfate salt of (S)-(+)-bis-4,4'-(a-methyl-1,2-ethanediyl)2,6-piperazinedione or (R)-(-)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-pierazinedione; wherein said lyophilized composition is prepared from a bulk solution comprising from about 25 mg/mL to about 40 mg/mL of said compound dissolved in hydrochloric or sulfuric acid; wherein the pH of said bulk solution is from about 1.0 to about 2.0.

11. An isotonic solution according to claim 10 wherein said acid is hydrochloric acid.

12. An isotonic solution according to claim 11 having a pH of from about 4.0 to about 5.0.

13. An isotonic solution according to claim 12 having a pH of about 5.0.

14. An isotonic solution according to claim 12 containing about 10 mg/mL of the HCl salt of (S)-(+)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione.

15. An iosotonic solution according to claim 12 containing about 10 mg/mL of the HCl salt of (R)-(-)-bis-4,4'-(1-methyl-1,2-ethanediyl)2,6-piperazinedione.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

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 verifification 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.

`abc