Soft buccal

• US 4,572,832 A
• Filed: 10/07/1983
• Issued: 02/25/1986
• Est. Priority Date: 10/07/1982
• Status: Expired due to Fees

• Current Assignee: Takeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
• Original Assignee: Grelan Pharmaceutical Co., Ltd. (ASKA Pharmaceutical Company Limited)
• Inventors: Shimizu, Hiroaki, Watabe, Kazuo, Ogawa, Yasuaki, Koyama, Osamu, Kigasawa, Kazuo, Hayashi, Toshihiro, Tanizaki, Akira, Wakisaka, Kikuo
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/540,161
• Time in Patent Office: 872 Days
• Field of Search: 424/19-22, 424/DIG. 15, 424/81, 514/773, 514/774, 514/775
• US Class Current: 514/772.1
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2004 Excipients; Inactive ingredients

Abstract

A soft buccal containing (1) a medicament to be absorbed through the oral mucosa, (2) a water-soluble protein, (3) a polyhydric alcohol, and (4) a fatty acid ester or/and a carboxyvinyl polymer, has various advantages such as good feeling in use, good retainability within the mouth, slow release, improved absorbability of drug through the mucosa, improved bioavailability, etc., and therefore can be used an excellent pharmaceutical preparation for administration to the mucous membrane of the mouth.

Claims

1. A soft buccal suitable for retention in the cavity of the mouth particularly suitable for prolonged residence in said cavity due to the softness thereof, said soft buccal containing

(1) a pharmaceutically effective amount of a medicament to be absorbed through the oral mucosa and to be delivered over the desired residence period of said soft buccal in said cavity;

(2) a water-soluble protein in an amount of from 0.5 to 150 parts by weight per part of drug (1);

(3) 0.01 to 3 parts by weight of a polyhydric alcohol per part of protein (2); and

(4) 0.01 to 10 parts by weight of fatty acid ester or a carboxyvinyl polymer, per part of protein (2).

2. A soft buccal of claim 1 wherein the component (4) comprises a mixture of said fatty acid ester and said carboxyvinyl polymer.

5. A method of providing a sustained release of a medicament to a subject which comprises placing a soft buccal of claim 1 in the mouth cavity of said subject, whereby a sustained release of said medicament is delivered to said subject.

6. A soft buccal as claimed in claim 1, wherein the water-soluble protein is at least one selected from gelatin;

solubilized collagen;

casein;

glue;

hydrolysates from gelatin, solubilized collagen, casein or glue;

polyalanine;

polylysine and polyglutamine.

7. A soft buccal as claimed in claim 1, wherein the water-soluble protein is gelatin.

8. A soft buccal as claimed in claim 1, wherein the polyhydric alcohol is at least one selected from glycol, triol and polyol.

9. A soft buccal as claimed in claim 1, wherein the polyhydric alcohol is at least one selected from ethylene glycol;

propylene glycol;

butylene glycol;

polyethylene glycol;

glycerin;

trimethylolpropane;

polyvinyl alcohol;

methylcellulose;

ethylcellulose;

propylcellulose;

hydroxymethylcellulose;

hydroxyethylcellulose;

carboxymethylcellulose or an alkali metal salt thereof;

glucose;

galactose;

fructose;

mannose;

mannitol;

sorbitol;

maltose;

lactose;

sucrose;

carboxymethyl-starch;

hydroxypropyl-starch;

dextrin;

dextran;

chitin;

alginic acid;

glycogen;

Purlan®

;

mannan;

pectin; and

gum arabic.

10. A soft buccal as claimed in claim 1, wherein the polyhydric alcohol is glycerin or propylene glycol.

11. A soft buccal as claimed in claim 1, wherein the fatty acid ester is a monoalcohol or polyalcohol ester of a saturated or unsaturated fatty acid.

12. A soft buccal as claimed in claim 1, wherein the fatty acid ester is a sucrose fatty acid ester.

13. A soft buccal as claimed in claim 1, wherein the carboxyvinyl polymer is polyacrylic acid, polymethacrylic acid or a salt thereof.

3. A soft buccal base material suitable for accepting a drug, whereby upon incorporation of said drug to form a soft buccal which is capable of retention in the cavity of the mouth, particularly suitable for prolonged residence in said cavity due to the softness thereof, said soft buccal base material comprising

(a) a water-soluble protein;

(b) 0.01 to 3 parts by weight of a polyhydric alcohol per part of protein (a); and

(c) 0.01 to 10 parts by weight of fatty acid ester or a carboxyvinyl polymer, per part of protein (a).

4. A base material of claim 3 wherein the component (c) comprises a mixture of said fatty acid ester and said carboxyvinyl polymer.