Stable lyophilized form of (S)-(+)-bis-4,4'-(1-methyl-1,2-ethane

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514970, 544357, A61K 31495

Patent

active

049635514

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.

REFERENCES:
patent: 3196153 (1965-07-01), Dazzi
patent: 4275063 (1981-06-01), Creighton
patent: 4764614 (1988-08-01), Miller
Repta et al., J. Pharm. Sci., 1976, 65(2), 238-42.

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