Pharmaceutical preparations comprised of salts of hyaluronic acid with local anaesthetics

• US 6,224,857 B1
• Filed: 07/19/1999
• Issued: 05/01/2001
• Est. Priority Date: 10/17/1996
• Status: Expired due to Term

• Current Assignee: Fidia S.P.A.
• Original Assignee: Fidia S.P.A.
• Inventors: Silvestrini, Bruno, Kirschner, Gunter, Romeo, Aurelio
• Primary Examiner(s): Azpuru, Carlos A.
• Application Number:
  US09/284,668
• Time in Patent Office: 652 Days
• Field of Search: 424/443, 424/78.04
• US Class Current: 424/78.04
• CPC Class Codes: A61K 31/416 condensed with carbocyclic ring systems, e.g. indazole
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/728 Hyaluronic acid
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system

Abstract

Pharmaceutical preparations are described, comprised of salts of hyaluronic acid with a basic anesthetic containing aliphatics and/or amino groups, particularly salts with benzydamine or bupivacaine.

Claims

1. A medicament for topical administration comprising a stoichiometrically neutral salt of hyaluronic acid with benzydamine or bupivacaine, in which at least 50% of the carboxy groups of the hyaluronic acid are salified with the benzydamine or bupivacaine and the remaining carboxy groups are salified with an alkaline or alkaline earth metal, wherein the hyaluronic acid has a molecular weight in the range of 50-350 kDa or 500-730 kDa or 750-1,200 kDa.

2. A medicament for topical administration according to claim 1, wherein the alkaline metal is sodium.

3. A medicament for topical administration according to claim 1, wherein the alkaline earth metal is calcium.

4. A medicament for topical administration according to any one of claims 1-3, wherein the carboxy groups of hyaluronic acid are salified with benzydamine or bupivacaine in the range between 70 and 100%.

5. A medicament for topical administration according to claim 4, wherein the carboxy groups of hyaluronic acid are salified with benzydamine in a percentage of about 75%.

6. A medicament for topical administration according to claim 4, wherein the carboxy groups of hyaluronic acid are salified with bupivacaine in a percentage of about 100%.

7. A medicament for topical administration according to claim 5, wherein the hyaluronic acid has a molecular weight in the range of 50-350 kDa.

8. A medicament for topical administration according to claim 6, wherein the hyaluronic acid has a molecular weight in the range of 500-730 kDa.

9. A medicament as defined in claim 1 for use in ophthalmology.

10. A method for the treatment of inflammatory processes in the mouth or primary airways, including rhinitis, mucositis caused by radiotherapy or chemotherapy, by intubation during surgery or for diagnostic purposes, in periodontal or gingival conditions, in inflammatory processes in the auditory canal, in conjunctivitis of various origin, in vulvovaginitis, urethritis, or for proctological applications which comprises administering an effective amount of a medicament according to claim 1.

11. A medicament as defined in claim 1, for use as an anesthetic.

12. A medicament according, claim 1 which is in the form of collirium, mouth wash, spray, cream or vaginal solution.