# US 5,344,644 A · Water-soluble composition for sustained-release

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- Number: US 5,344,644 A
- Document ID: US5344644A
- Status: Granted
- Kind: A
- Application number: 07/919,401
- Filed: 1992-07-23
- Granted: 1994-09-06
- Earliest claimed: 1991-08-01
- Assignees: Takeda Chemical Industries, Ltd.
- Inventors: Yasutaka Igari; Minoru Yamada; Seiko Ishiguro
- Web page: https://patentgrep.com/patent/US5344644A

## CPC

- A61K 38/09: Luteinising hormone-releasing hormone [LHRH] {, i.e. Gonadotropin-releasing hormone [GnRH]}; Related peptides
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 38/066: {TRH, thyroliberin, thyrotropin releasing hormone}
- A61K 38/1816: {Erythropoietin [EPO]}
- A61K 38/193: {Colony stimulating factors [CSF]}
- A61K 38/2013: {IL-2}
- A61K 38/212: {IFN-alpha}
- A61K 38/28: Insulins
- A61K 38/29: Parathyroid hormone, i.e. parathormone; Parathyroid hormone-related peptides
- A61K 38/446: {Superoxide dismutase (1.15)}
- A61K 38/58: from leeches, e.g. hirudin, eglin
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A water soluble composition is described which comprises (a) a water soluble pharmacologically active peptide selected from the group consisting of cytokines or haematopoietic factors and (b) a sulfate group-containing acidic mucopolysaccharide and/or a desulfated modification of a naturally occurring sulfate group containing acidic mucopolysaccharide, and which brings about prolonged action of pharmacologically active peptides in a living body.

## Claims

### Claim 1

A water-soluble parenteral composition for injection which comprises (a) a water soluble pharmacologically active peptide selected from the group consisting of cytokines or hematopoietic factors, and (b) an alkali metal salt of a sulfate group-containing acidic mucopolysaccharide and/or a desulfated modification of a naturally occurring sulfate group-containing acidic mucopolysaccharide, wherein the weight ratio between (a) and (b) is about 0.001 to about 1:1, and wherein prior to injection, the tonicity and viscosity of the composition are adjusted by the addition of sterile water or sterile saline, to obtain a solution such that the viscosity of the solution is lower than 500 cP and the tonicity of the solution is from one-half to twice as high as that of physiological saline.

### Claim 2 (depends on 1)

A water-soluble composition as claimed in claim 1, wherein the water-soluble pharmacologically active peptide is erythropoietin, granulocyte colony stimulating factor (G-CSF), macrophage colony stimulating factor (M-CSF), granulocyte-macrophage colony stimulating factor (GM-CSF), interferons or interleukins.

### Claim 3 (depends on 1)

A water-soluble composition as claimed in claim 1, wherein the sulfate group containing acidic mucopolysaccharide and/or the desulfated modification of a naturally occurring sulfate group-containing acidic mucopolysaccharide is chondroitin sulfate, heparan sulfate, keratan sulfate, chondroitin or heparan.

### Claim 4 (depends on 1)

A water soluble composition as claimed in claim 1, further comprising a water-soluble protein selected from the group consisting of serum albumin, globulin, collagen and gelatin, wherein the weight ratio between the water-soluble protein and the mucopolysaccharide is from about 0.0001:1 to 100:1.

### Claim 5 (depends on 1)

A water soluble composition as claimed in claim 1, wherein the viscosity of said solution of the water soluble composition is lower than 400 cP.