Solubilization of proteins for pharmaceutical compositions using polymer conjugation
First Claim
1. A pharmaceutical preparation comprising a non-toxic, inert, pharmaceutically acceptable aqueous carrier medium in which is dissolved an immunotherapeutic effective amount of biologically active, selectively conjugated, recombinant interleukin-2 protein, wherein the protein is covalently conjugated via up to ten amino acid residues on the protein to a water-soluble polymer selected from the group consisting of polyethylene glycol homopolymers and polyoxyethylated polyols, wherein said homopolymer is unsubstituted or substituted at one end with an alkyl group and said polyol is unsubstituted and wherein said protein in its unconjugated form is normally hydrophobic.
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Abstract
A pharmaceutical composition is prepared wherein a biologically active conjugated protein which is β-interferon, interleukin-2, or an immunotoxin is dissolved in an aqueous carrier medium without the presence of a solubilizing agent. The unconjugated protein, which is not water-soluble or not readily soluble in water at pH 6-8 without such solubilizing agent, is selectively conjugated to a water-soluble polymer selected from polyethylene glycol homopolymers or polyoxyethylated polyols.
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15 Claims
- 1. A pharmaceutical preparation comprising a non-toxic, inert, pharmaceutically acceptable aqueous carrier medium in which is dissolved an immunotherapeutic effective amount of biologically active, selectively conjugated, recombinant interleukin-2 protein, wherein the protein is covalently conjugated via up to ten amino acid residues on the protein to a water-soluble polymer selected from the group consisting of polyethylene glycol homopolymers and polyoxyethylated polyols, wherein said homopolymer is unsubstituted or substituted at one end with an alkyl group and said polyol is unsubstituted and wherein said protein in its unconjugated form is normally hydrophobic.
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15. A composition comprising biologically active, normally hydrophobic recombinant interleukin-2 protein that is covalently conjugated via up to ten amino acid residues on the protein to a water-soluble polymer selected from the group consisting of polyethylene glycol homopolymers and polyoxyethylated polyols, wherein said homopolymer is unsubstituted or substituted at one end with an alkyl group and said polyol is unsubstituted.
Specification