Water soluble film for oral administration with instant wettability

• US 5,948,430 A
• Filed: 08/01/1997
• Issued: 09/07/1999
• Est. Priority Date: 11/11/1996
• Status: Expired due to Term

• Current Assignee: LTS Lohmann Therapie-Systeme GmbH
• Original Assignee: LTS Lohmann Therapie-Systeme GmbH
• Inventors: Serino, Anthony, Guo, Jian-Hwa, Zerbe, Horst Georg
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US08/904,607
• Time in Patent Office: 767 Days
• Field of Search: 424/435
• US Class Current: 424/435
• CPC Class Codes: A61K 8/0208 Tissues; Wipes; Patches
• CPC Class Codes: A61K 8/39 Derivatives containing from 2 to 10 oxyalkylene groups
• CPC Class Codes: A61K 8/4926 having six membered rings
• CPC Class Codes: A61K 8/731 Cellulose; Quaternized cellulose derivatives
• CPC Class Codes: A61K 8/8176 Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
• CPC Class Codes: A61K 8/90 Block copolymers A61K8/89 takes precedence
• CPC Class Codes: A61K 8/922 of vegetable origin
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61P 1/02 Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 25/26 Psychostimulants, e.g. nicotine, cocaine
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61Q 11/00 Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

A composition containing therapeutic agents and/or breath freshening agents for use in the oral cavity is disclosed. The carrier comprises water-soluble polymers in combination with certain ingredients and provides a therapeutic and/or cosmetic effect. The film is coated and dried utilizing existing coating technology and exhibits instant wettability followed by rapid dissolution/disintegration upon administration in the oral cavity.

Claims

1. A monolayer film formed from a mucoadhesive composition which comprises

at least one water-soluble polymer;

at least one member selected from the group consisting of a polyalcohol, a surfactant and a plasticizer;

at least one cosmetic or pharmaceutically ingredient; and

a flavoring agent

said film being one which rapidly softens and completely disintegrates in the oral environment and having a dry film thickness which is suitable for application into the month without causing adverse feeling the mouth.

2. A monolayer film according to claim 1 wherein the dry film thickness is about 70 μ

m.

3. A monolayer film according to claim 1 wherein the concentration of water-soluble polymer is between 20 and 75% (w/w), the concentration of surfactant is between 0.1 and 5% (w/w), the concentration of polyalcohol is between 0.1 and 5% (w/w) and the amount of pharmaceutically active ingredient is between 0.01 and 20% (w/w).

4. A monolayer film according to claim 1, wherein the water-soluble polymer is selected from the group consisting of hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidone, carboxymethyl cellulose polyvinyl alcohol sodium alginate, polyethylene glycol, xanthane gum, tragacantha guar gum, acacia gym, arabic gum, polyacrylic acid, methylmethacrylate copolymer carboxyvinyl polymer and copolymers and mixtures thereof.

5. A monolayer film according to claim 1, wherein the concentration of the water-soluble polymer in the dry film lies between 20 and 75% (w/w).

6. A composition according to claim 1, wherein the polyalcohol is selected from the group consisting of glycerol, polyethylene glycol, propylene glycol, and glycerol monoesters with fatty acids.

7. A monolayer film according to claim 1 containing a polyalcohol and at least one surfactant.

8. A monolayer film according to claim 1, wherein the surfactant is a polyoxyethylene sorbitan fatty acid ester, a α

-hydroxy-ω

hydroxypoly-(oxyethylene)poly(oxypropylene)poly(oxypropylene) block copolylmer, a polyoxyethylene alkyl ether or a polyoxyethylene castor oil derivative or a mixture thereof.

9. A monolayer film according to claim 1, comprising sorbitol and/or polyvinylpyrrolidone together with water-soluble cellulose-derivative polymer.

10. A monolayer film according to claim 1, wherein the pharmaceutically active ingredient is selected from the group consisting of a hypnotic, a sedative, an antiepileptic, an awakening agent, a pyschoneurotropic agent, a neuromuscular blocking agent, an antispasmodic agent, an antihistaminic, an antiallergic, a cardiotonic, an antiarrhythmic, a diuretic, a hypotensive, a vasopressor, an antitussive expectorant, a thyroid hormone, a sexual hormone, an antidiabetic, an antitumor agent, an antibiotic, a chemotherapeutic, and a narcotic.

11. A monolayer film according to claim 1, wherein the cosmetically active agent is selected from the group consisting of a breath freshening compound, a favor or fragrance used or oral hygiene, an agent for dental and/or oral cleansing and mixtures thereof.

12. A molecular film according to claim 1 in a shape suitable for application into the mouth.