Water soluble film for oral administration with instant wettability

• US 6,284,264 B1
• Filed: 08/02/2000
• Issued: 09/04/2001
• Est. Priority Date: 11/11/1996
• Status: Expired due to Term

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme GmbH
• Inventors: Serino, Anthony, Guo, Jian-Hwa, Zerbe, Horst Georg
• Primary Examiner(s): Reamer, James H.
• Application Number:
  US09/630,562
• Time in Patent Office: 398 Days
• Field of Search: 424/435, 424/434
• 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 method for the release of a pharmaceutically or cosmetically active agent into the oral cavity, comprising

a) applying a mucoadhesive film which comprises a pharmaceutically or cosmetically active ingredient, into the oral cavity,

b) allowing said mucoadhesive film to dissolve within the oral cavity, and

c) releasing said pharmaceutically or cosmetically active agent into the oral cavity.

2. The method of claim 1, wherein the mucoadhesive film is formed from a mucoadhesive composition comprising at least one polymer.

3. The method claim 2, wherein the polymer used in the mucoadhesive composition is a hydrophilic and/or water-dispersible and/or water-soluble polymer.

4. The method of claim 2, wherein the mucoadhesive composition further comprises at least one polyalcohol.

5. The method of claim 2, wherein the mucoadhesive composition further comprises at least one plasticizer.

6. The method of claim 2, wherein the mucoadhesive composition further comprises at least one surfactant.

7. The method of claim 1, wherein the pharmaceutically active ingredient is selected from the group consisting of hypnotics, sedatives, antiepileptics, awakening agents, psychoneurotropic agents, neuromuscular blocking agents, antispasmodic agents, antihistaminics, antiallergics, cardiotonics, antiarrhythmics, diuretics, hypotensives, vasopressors, antitussive expectorants, thyroid hormones, sexual hormones, antidiabetics, antitumor agents, antibiotics, chemotherapeutics, and narcotics.

8. The method of claim 1, wherein the amount of the pharmaceutically active ingredient in the mucoadhesive film is at least 0.01% (w/w).

9. The method of claim 1, wherein the cosmetically active ingredient is selected from the group consisting of breath freshening compounds, flavors used for oral hygiene, fragrances used for oral hygiene, active agents used for oral cleansing, and active agents used for dental cleansing.

10. The method of claim 9, wherein additional flavor enhancers are used.

11. A method for the rapid release of a pharmaceutically active agent to a patient, comprising

a) applying a mucoadhesive film which comprises at least one pharmaceutically active ingredient, into the oral cavity of said patient,

b) allowing said mucoadhesive film to dissolve within the oral cavity, and

c) releasing said pharmaceutically active agent to the patient via the mucous membrane.

12. The method of claim 11, wherein the mucous membrane is the buccal mucosa.

13. The method of claim 11, wherein the pharmaceutically active ingredient is selected from the group consisting of hypnotics, sedatives, antiepileptics, awakening agents, psychoneurotropic agents, neuromuscular blocking agents, antispasmodic agents, antihistaminics, antiallergics, cardiotonics, antiarrhythmetics, diuretics, hypotensives, vasopressors, antitussive expectorants, thyroid hormones, sexual hormones, antidiabetics, antitumor agents, antibiotics, chemotherapeutics, and narcotics.

14. The method of claim 11, wherein the amount of the pharmaceutically active ingredient in the mucoadhesive film is at least 0.01% (w/w).

15. The method of claim 11, wherein the pharmaceutically active ingredient is selected from the group of therapeutic agents, which exhibit absorption problems due to solubility limitations.

16. The method of claim 11, wherein the pharmaceutically active ingredient is selected from the group of therapeutic agents, which are subjected to degradation in the gastro-intestinal tract.

17. The method of claim 11, wherein the pharmaceutically active ingredient is selected from the group of therapeutic agents, which are subjected to extensive metabolism.