WO1987003476A1

WO1987003476A1 - Composition for the treatment of periodontal disease

Info

Publication number: WO1987003476A1
Application number: PCT/US1986/002625
Authority: WO
Inventors: Christian Schwabe
Original assignee: Micro-Map, Inc.
Priority date: 1985-12-13
Filing date: 1986-12-05
Publication date: 1987-06-18
Also published as: EP0250547A1

Abstract

Periodontal disease is effectively treated by topical application of alkyldimethylbenzylammonium chlorides having as the alkyl group a straight chain of from 12 to 18 carbon atoms. The preferred therapeutic agent is an equimolar mixture of these compounds. Treatment can be effected using a mouthwash containing from 0.1% to 0.2% alkyldimethylbenzylammonium chloride. Prophylactic applications, particularly using a toothpaste carrier, are also effective.

Description

Composition for the treatment of periodontal disease

Background of the Invention

This invention relates to a method and composition for the non-invasive treatment of periodontal disease, including periodontitis and related forms of gingival disease by topical application of alkyldimethylbenzylammonium chlorides.

Periodontal disease involves inflammation of gingival tissues in response to the actions of oral bacteria. The gingiva appear red and swollen, and have a tendency to bleed when the teeth are brushed. As the disease progresses, the attachment between the gums and the tooth may be broken. This creates a space, or periodontal pocket, between the tooth and gum which can serve as a center for enhanced microbial growth. Such growth can lead to the formation of abscesses and bone loss in the alveolar crest. The consequence of advanced periodontal disease is a loosening of the teeth and ultimately extraction is required.

Current methods of treatment of periodontal disease depend on the severity of the disease. Mild cases are generally treated by the removal of mechanical irritants such as calculus. More severe cases are treated surgically by removal of gingival tissue, polishing of tooth roots, or occasionally by splinting of the teeth. Surgical intervention is a painful and costly procedure, however, and should be avoided if at all possible.

Prophylactic measures can be taken to forestall the occurrence, or reoccurrence of periodontal disease. Known prophylactic measures include the regular use of dental floss. Such measures are generally time consuming and involve a strict regimen of home care to be effective. For this reason, known prophylactic measures are rarely completely effective in preventing periodontal disease.

Anti-bacterial mouthwashes have been disclosed which are believed to be effective in the prevention or minimization of plaque. Among the known antibacterials are some quaternary amines including benzethonium chloride. These preparations are not known to be effective, however, in the treatment of periodontal disease, and are of only limited effectiveness as a prophylactic measure.

It is therefore, an object of this invention to provide a method and composition for the treatment and prevention of periodontal disease.

It is a further object of this invention to provide a method and composition for the treatment and prevention of periodontal disease which is easily and rapidly administered by the user.

Summary of the Invention

Periodontal disease can be effectively treated by topical application of alkyldimethylbenzylammonium chlorides, where the alkyl groups are straight chains of from 12 to 18 carbon atoms. Application of alkyldimethylbenzylammonium chlorides leads to a reduction in the number of live microorganisms present in the oral cavity and to a reduction of gingival inflammation.

Treatment of extant inflammations is accomplished using a mouthwash containing from 0.1% to 0.2% of the alkyldimethylbenzylammonium chloride, The mouthwash is preferably used twice daily, following lunch and after the last food of the day.

Toothpaste preparations containing alkyldimethylbenzylammonium chloride can be effectively used to prevent inflammation of the oral gingiva and periodontal disease. The alkyldimethylbenzylammonium chloride is preferably incorporated into the toothpaste at a concentration of about 0.1%. Detailed Description of the Invention

Alkyldimethylbenzylammonium chlorides are routinely available from drug stores and hospital supply companies for use in cold sterilization of surgical instruments. It has now been found that these compounds are effective in the treatment and prevention of periodontal disease.

According to the invention, alkyldimethylbenzylammonium chloride, where the alkyl group is a straight chain of from 12 to 18 carbon atoms, is applied topically to the gingival tissues to treat and prevent periodontal disease. Each of the alkyldimethylbenzylammonium chlorides is effective when used alone, and when used as a mixture. Preferably, the treatment involves application of an equimolar mixture of alkyldimethylbenzylammonium chlorides having an alkyl substituent of from 12 to 18 carbon atoms in length.

For treatment of existing periodontal disease, alkyldimethylbenzylammonium chloride is preferably applied as a mouthwash. For this purpose, the alkyldimethylbenzylammonium chloride is dissolved in water to form a mouthwash capable of killing oral bacteria on contact. Preferably, the mouthwash contains from 0.1% to 0.2% alkyldimethylbenzylammonium chloride. higher concentrations are not required for therapeutic effectiveness, and are not recommended due to the bitter taste of the active ingredient.

A mouthwash according to this invention may also contain other ingredients conventionally included in mouthwash formulations, including flavorants, colorants, and astringents. It will also be understood that a mouthwash according to this invention can be formulated as a gel, as well as a liquid.

A mouthwash according to this invention is used regularly to treat periodontal disease until redness and swelling of the gums are alleviated. Preferably, the mouthwash is applied twice daily, following lunch and after the last food of the day. A portion of the active ingredient adsorbs to the surface of the teeth, resulting in prolonged effectiveness. Reduction of gingival inflammation generally results within one week of the onset of treatment, and in some cases may be effected with only a single application.

Alkyldimethylbenzylammonium chloride can be applied to the gums and teeth by simply swishing the mouthwash around in the oral cavity. Preferably, contact with the mouthwash is maintained for from 5 to 15 seconds. The mouthwash may also be advantageously introduced into the lumen of a periodontal pocket or abscess using a blunt-needled syringe.

For prophylactic use, alkyldimethylbenzylammonium chloride may be applied either in a mouthwash or in a toothpaste. A toothpaste according to this invention Preferably contains 0.1% alkyldimethylbenzylammonium chloride in an otherwise conventional toothpaste formulation. Such a toothpaste used regularly will effectively prevent the onset of periodontal disease. The following case studies will serve to illustrate the use and effectiveness of compositions according to this invention. Example 1

The patient diagnosed as having progressive periodontal symptoms was scheduled for periodontal treatment involving local surgical intervention. The patient was given a mouthwash containing 0.2% alkyldimethylbenzylammonium chloride (40% C₁₂ ; 50% C_{1 4}; 10% C₁₆) according to this invention which was used once daily after the last meal for a period of one week prior to the scheduled appointment. The use of alkyldimethylbenzylammonium chloride as directed eliminated the need for any surgical intervention in the opinion of the periodontologist who had initially recommended surgery. Example 2

The patient had a longstanding history of chronic gingivitis which led to bleeding of the gums and considerable discomfort after every use of the toothbrush. Treatment with an 0.2% alkyldimethylbenzylammonium chloride mouthwash (40% C₁₂; 50% C₁₄; 10% C₁₆) at noon and following the last meal of the day eliminated the gingivitis completely. In three days, the patient could brush her teeth without causing any bleeding or discomfort. Example 3

This patient had a periodontal abscess in the region of the upper left molar. The patient was given a syringe with a blunt needle and advised to flush out the abscess with an 0.2% solution of alkyldimethylbenzylammonium chlorides (40% C₁₂; 50% C₁₄; 10% C₁₆). The symptoms disappeared within one hour, and have not recur red af ter three months during which time a prophylactic amount of the compound was used occasionally in the form of an 0.2% mouthwash once every three days.

Compositions according to this invention give excellent results when used in the treatment and prevention of periodontal disease. It will be understood, however, that in very advanced cases of periodontal disease surgical intervention may still be necessary. In these circumstances, compositions containing alkyldimethylbenzylammonium chloride are advantageously used to reduce gingival inflammation prior to surgery and as a prophylactic regimen following surgery.

The method and composition embodiments described above are intended only to be illustrative. It will be understood that modifications in form and detail may be made within the scope of the following claims.

Claims

1. A method for treating periodontal disease comprising topical application of one or more alkyldimethylbenzylammonium chlorides having as the alkyl group a straight chain of from 12 to 18 carbon atoms.

2. A method according to claim 1, comprising topical application of an equimolar mixture of alkyldimethylbenzylammonium chlorides having as the alkyl group a straight chain of from 12 to 18 carbon atoms.

3. A method according to claim 1 comprising application of a mixture of 40% C₁₂, 50% C₁₄, 10% C₁₆ alkyldimethylbenzylammonium chlorides.

4. A method according to claim 1, wherein the alkyldimethylbenzylammonium chloride is applied as a mouthwash.

5. A method according to claim 4, wherein the mouthwash comprises from 0.1% to 0.2% alkyldimethylbenzylammonium chloride in aqueous solution.

6. A method according to claim 5, wherein the mouthwash is applied twice daily.

7. A method according to claim 1, wherein the treatment is preventative.

8. A method according to claim 7, wherein the alkyldimethylbenzylammonium chloride is incorporated in a toothpaste.

9. A method according to claim 8, wherein the alkyldimethylbenzylammonium chloride is present in the toothpaste at a concentration of 0.1%.

10. A composition for treating periodontal disease comprising one or more alkyldimethylbenzylammonium chlorides having as the alkyl group a straight chain of from 12 to 18 carbon atoms in an amount effective to kill oral bacteria on contact, and a non-toxic carrier.

11. A composition according to claim 9 comprising an equimolar mixture of alkyldimethylbenzylammonium chlorides having as the alkyl group a straight chain of from 12 to 18 carbon atoms.

12. A composition according to claim 1 comprising a mixture consisting of 40% C₁₂, 50% C₁₄, 10% C_{1 6} alkyldimethylbenzylammonium chlorides and a nontoxic carrier.

13. A composition according to claim 10, wherein the carrier is water.

14. A composition according to claim 13, wherein the alkyldimethylbenzylammonium chloride is present at a concentration of from 0.1% to 0.2%.

15. A composition according to claim 13 additionally comprising one or more ingredients selected from the group consisting of flavorants, colorants and astringents.

16. A composition according to claim 10, wherein the carrier is a toothpaste.

17. A composition according to claim 16, wherein the alkyldimethylbenzylammonium chloride is present at a concentration of about 0.1%.