# US 8,771,734 B2 · Sustained-release hydrogel preparation

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- Number: US 8,771,734 B2
- Document ID: US8771734B2
- Status: Granted
- Kind: B2
- Application number: 10/549,695
- Filed: 2004-03-15
- Published: 2006-11-09
- Granted: 2014-07-08
- Earliest claimed: 2003-03-17
- Assignees: Medgel Corporation
- Applicants: Yasuhiko Tabata
- Inventors: Yasuhiko Tabata
- Web page: https://patentgrep.com/patent/US8771734B2

## CPC

- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- 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 sustained-release preparation is provided which comprises a drug and a bioabsorbable polymer hydrogel, wherein a concentration gradient of the drug is formed in the hydrogel. Also disclosed is a method of sustained release of a drug in vivo using the sustained-release preparation of the invention. The directionality of the drug release may be controlled by employing the sustained-release preparation of the invention. The sustained-release preparation of the invention is particularly useful as an anti-cancer agent.

## Claims

### Claim 1

A sustained-release preparation which comprises:
a drug having a molecular weight of about 10,000 or less; and
a gelatin hydrogel,
wherein the drug is impregnated into said gelatin hydrogel through a surface thereof and is immobilized in said hydrogel by physiochemical interaction, and
said hydrogel having a concentration gradient of the drug such that said concentration gradient being higher at said surface than in other parts of said hydrogel in said sustained-release preparation, and the drug is immobilized within said hydrogel by said physiochemical interaction, thereby controlling the directionality of the sustained release of the drug upon administration of the sustained-release preparation, and
said sustained-release preparation is sterile.

### Claim 2

A method of sustained release of a drug in vivo comprising:
administering a sustained-release preparation to a patient in need thereof, said preparation comprising a drug having a molecular weight of about 10,000 or less and a gelatin hydrogel, wherein said hydrogel has a concentration gradient of the drug in said sustained-release preparation, wherein degradation of the gelatin hydrogel in vivo causes more drug to be released from a region with higher drug concentration, thereby giving said sustained release of the drug, wherein the drug is impregnated into said gelatin hydrogel through a surface thereof and is immobilized in said hydrogel by physiochemical interaction, said concentration gradient being higher at said surface than in other parts of said hydrogel, and said sustained-release preparation is sterile.

### Claim 3 (depends on 2)

The method of claim 2, where said administration is topical.

### Claim 4 (depends on 1)

The sustained-release preparation of claim 1, wherein the drug is impregnated into said gelatin hydrogel by ionic bonding.

### Claim 5 (depends on 1)

The sustained-release preparation of claim 1, wherein the preparation is in solid or semi-solid form.

### Claim 6

A sustained-release preparation which comprises:
a drug having a molecular weight of about 10,000 or less; and
a crosslinked gelatin hydrogel,
said sustained-release preparation being made by adding an aqueous solution of said drug dropwise to said crosslinked gelatin hydrogel, thereby impregnating said drug into said crosslinked gelatin hydrogel through a surface thereof, immobilizing said drug in said crosslinked gelatin hydrogel by physiochemical interaction between said drug and crosslinked gelatin hydrogel, and forming a concentration gradient of the drug in the crosslinked gelatin hydrogel such that said concentration gradient is higher at said surface than in other parts of said hydrogel in said sustained-release preparation, wherein the amount of aqueous solution being added dropwise causes swelling of the crosslinked gelatin hydrogel and wherein said sustained-release preparation is sterile.

### Claim 7 (depends on 1)

The sustained-release preparation of claim 1, in a form suitable for topical application.

### Claim 8 (depends on 6)

The sustained-release preparation of claim 6, in a form suitable for topical application.

### Claim 9 (depends on 1)

The sustained-release preparation of claim 1, which is in a solid or semisolid single dose form containing 0.01 to 10,000 μg of said drug.

### Claim 10 (depends on 2)

The method of claim 2, wherein said sustained release preparation is in a solid or semisolid single dose form containing 0.01 to 10,000 μg of said drug.

### Claim 11 (depends on 6)

The sustained-release preparation of claim 6, in a solid or semisolid single dose form containing 0.01 to 10,000 μg of said drug.

### Claim 12 (depends on 1)

The sustained-release preparation of claim 1, which is in a solid single dose form containing 0.1 to 1,000 μg of said drug.

### Claim 13 (depends on 2)

The method of claim 2, wherein said sustained release preparation is in a solid single dose form containing 0.1 to 1,000 μg of said drug.

### Claim 14 (depends on 6)

The sustained-release preparation of claim 6, in a solid single dose form containing 0.1 to 1,000 μs of said drug.
