Title:  Non-aqueous polar aprotic peptide formulations

United States Patent:  6,124,261

Inventors:  Stevenson; Cynthia L. (Mountain View, CA); Prestrelski; Steven J. (Mountain View, CA)

Appl. No.:  293839

This invention relates to stable non-aqueous polar aprotic formulations of peptide compounds. These stable formulations comprise peptide in non-aqueous polar aprotic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.

SUMMARY OF THE INVENTION

The present invention provides stable non-aqueous formulations which are solutions of peptide compounds in polar aprotic solvents. In particular, the peptide compounds are formulated at concentrations of at least about 10%. These stable formulations may be stored at elevated temperatures (e.g., 37^oC.) for long periods of time and are especially useful in implantable delivery devices for long term delivery (e.g., 1-12 months or longer) of drug.

In one aspect, the invention provides stable non-aqueous formulations of peptide compounds, said formulations comprising at least one peptide compound in at least one polar aprotic solvent. In a preferred embodiment, the formulation comprises at least about 10% (w/w) peptide compound.

In another aspect, the invention provides methods for preparing a stable non-aqueous formulation of a peptide compound, said methods comprising dissolving at least one peptide compound in at least one polar aprotic solvent. Preferred formulations comprise at least about 10% (w/w) peptide compound.

In yet a further aspect, the invention provides methods for treating a subject suffering from a condition which may be alleviated by administration of a peptide compound, said methods comprising administering to said subject an effective amount of a stable non-aqueous formulation comprising at least one peptide compound in at least one polar aprotic solvent.

Claim 1 of 41 Claims

What is claimed is:

1. A stable non-aqueous formulation of a peptide compound comprising:

a) at least one peptide compound; and

b) at least one polar aprotic solvent, wherein said polar aprotic solvent is selected from the group consisting of DMSO and DMF.

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