Method and preparation for administration to the mucosa of the oral or nasal cavity

• US 4,250,163 A
• Filed: 12/13/1979
• Issued: 02/10/1981
• Est. Priority Date: 03/05/1979
• Status: Expired due to Term

• Current Assignee: Teijin Limited
• Original Assignee: Teijin Limited
• Inventors: Suzuki, Yoshiki, Ikura, Hiroshi, Machida, Yoshiharu, Nagai, Tsuneji
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/103,558
• Time in Patent Office: 425 Days
• Field of Search: 424/14, 424/16, 424/19, 424/22, 424/28, 424/78, 424/81, 106/35, 128/260
• US Class Current: 514/772.1
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays

Abstract

A method for administering a medicament which comprises adhering to the mucosa of the oral or nasal cavity a pharmaceutical preparation comprising

(a) a water-swellable and mucosa-adhesive polymeric matrix comprising about 50 to about 95% by weight of a cellulose ether and about 50 to about 5% by weight of a homo- or copolymer of acrylic acid or a pharmaceutically acceptable salt thereof, and

(b) dispersed therein, a pharmaceutically effective amount of the medicament,

said preparation releasing continuously the medicament at a controlled rate; and causing the released medicament to be absorbed through the mucosa or enterally; said mucosa-adhesive preparation; and process for said preparation.

Claims

1. In a method for administering a medicament which comprises adhering with a polyacrylate to the mucosa of the oral cavity a pharmaceutical preparation, the improvement comprising adhering said medicament with

(a) a water-swellable and mucosa-adhesive polymeric matrix comprising about 50 to about 95% by weight of a cellulose ether and about 50 to about 5% by weight of a homo- or copolymer of acrylic acid or pharmaceutically acceptable salt thereof, and

(b) dispersed therein, a pharmaceutically effective amount of the medicament to be adhered to the oral mucosa,

said preparation releasing continuously the medicament at a controlled rate;

and causing the released medicament to be absorbed through the mucosa or enterally.

2. The method of claim 1 wherein said polymeric matrix comprises about 65 to about 90% by weight of the cellulose ether and about 35 to about 10% by weight of the homo- or copolymer of acrylic acid or its pharmaceutically acceptable salt.

3. The method of claim 1 wherein the cellulose ether is a lower alkyl or hydroxy lower alkyl ether of cellulose.

4. The method of claim 1 wherein the cellulose ether is selected from the group consisting of methyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose and hydroxypropyl cellulose.

5. The method of claim 1 wherein the cellulose ether is hydroxypropyl cellulose having a viscosity, determined at 20°

C. for a 2% by weight aqueous solution thereof, of 3 to 10,000 centipoises.

6. The method of claim 1 wherein the polymer of acrylic acid has a viscosity of 360 to 165,000 centipoises when it is measured at 25.0±

5°

C. for an aqueous solution of the sodium salt of the polymer having a pH of 7 to 7.5 and a concentration of 0.2% by weight as free polymer.

7. The method of claim 1 wherein the pharmaceutical preparation further comprises an excipient dispersed in the matrix.

8. The method of claim 1 wherein the medicament is selected from the group consisting of analgesic and anti-inflammatory agents, anti-inflammatory enzyme preparations, anti-inflammatory steroids, antihistamines, antibiotics, antibacterial agents, chemotherapeutic agents, local anaesthesias, cardiac tonics, vasodilators, antitussive and expectorants, oral antiseptics, enzyme proteins, hypoglycemic agents, hemostats, hormones, hypotensive agents, sedatives or tranquilizers, anti-tumor agents, gastro intestinal drugs and antacids.

9. The method of claim 1 wherein the pharmaceutical preparation is in the form of tablets, granules, fine granules, powders and dental cone.