Oral composition

Drug – bio-affecting and body treating compositions – Dentifrices – Ferment containing

Patent

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Details

424 54, A61K 716, A61K 728, A61K 722

Patent

active

051087359

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to a composition for the oral cavity. More particularly, it relates to an oral composition such as dentifrice, dental rinse, mouthwash, dental paste or denture cleanser wherein mutanase which is a pharmacologically active agent for preventing dental caries is stably formulated.


PRIOR ART

Heretofore, as one of mechanisms for developing dental caries, it has been pointed out that Streptococcus mutans which is etiogenic bacteria of dental caries produces a water-insoluble and adhesive glucan having .alpha.-1,3-glucoside bond (mutan) from sucrose and strongly adheres to the surfaces of teeth to produce lactic acid thereon, which results in decalcification of teeth (Clinical Bacteriology, Vol. 1, page 24, 1974). Mutanase is an enzyme which breaks .alpha.-1,3-glucoside bond of the glucan produced by Streptococcus mutans and a trial to prevent dental caries has been made by utilizing the activity of the enzyme to decompose the glucan to inhibit adhesion of Streptococcus mutans to the surfaces of teeth (Journal of Dental Research, Vol. 5, supplement, page 394, 1972). Mutanase used therein is derived from Trichlderma harzianum. However, in addition to this, the enzyme derived from bacteria belonging to the genus Flavobacterium (Japanese Patent Kokoku No. 52-38113), Pseudomonas (Japanese Patent Kokoku No. 56-1070) or the like is also reported. Further, to formulate mutanase in dentifrices is also proposed (Japanese Patent Kokoku No. 55-50006 and Japanese Patent Kokoku No. 57-36890) and it is admitted that mutanase is useful for preventing dental caries. However, mutanase is extremely unstable in the presence of water and a surfactant and is labilized by alterations in pH and, therefore, its enzymatic activity is liable to be lost. On the other hand, for example, a surfactant is generally an essential ingredient as a foaming agent, dispersant and/or detergent in an oral composition and, therefore, it is very difficult to formulate mutanase in such a composition. Under these circumstances, in Japanese Patent Kokai No. 59-152314 and Japanese Patent Kokai No. 59-152315, there is proposed that mutanase is stably formulated in an oral composition by using a N-acyl sarcosinate or a combination of a N-acyl sarcosinate with a sucrose fatty acid ester.


OBJECTS OF THE INVENTION

In order to improve the stability of mutanase formulated in an oral composition, the present inventors have studied intensively by adding a nonionic surfactant as a foaming auxiliary to a N-acyl sarcosinate which shows "juice effect" and has excellent feeling of use to obtain an oral composition having excellent feeling of use, foaming properties and stability. As a result, it has been found that, by using a specific nonionic surfactant, the stabilization of mutanase can be obtained in the same degree as or more improved degree than that obtained by a combination of a N-acyl sarcosinate with a sucrose fatty acid ester.
Further, since a N-acyl sarcosinate may cause detachment of oral mucosa depending on its amount formulated, the amount thereof in a dentifrice is limited to not more than 0.5% by weight and therefore the use thereof is extremely limited. However, mutanase can be stabilized by using a N-acyl-L-glutamate instead of a N-acyl sarcosinate and using it in combination with the specific nonionic surfactant.
The present invention is baste on this knowledge and provides an oral composition wherein mutanase is stably formulated.


SUMMARY OF THE INVENTION

The present invention is characterized in that, in an oral composition containing mutanase, a N-acyl sarcosinate or a N-acyl-L-glutamate is formulated as a surfactant together with one or more of nonionic surfactants selected from the group consisting of polyoxyethylene sorbitol fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene lanolin derivative, polyoxyethylene nonyl phenyl formaldehyde condensation product, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene sorbitan

REFERENCES:
patent: 4466954 (1984-08-01), Ichikawa et al.
patent: 4469673 (1984-09-01), Ioka et al.
patent: 4576816 (1986-03-01), Suganuma et al.
patent: 4585648 (1986-04-01), Maeyama et al.
patent: 4645662 (1987-02-01), Nakashima et al.
patent: 4725428 (1988-02-01), Miyahara et al.
patent: 4911918 (1990-03-01), Kiyoshige et al.
Sunstar CA. 101:235407F (1984) of JPN. 59152314 Aug. 31, 1984.
Sunstar CA. 101:235408G (1984) of JPN 59152315 Aug. 31, 1984.
Sunstar CA. 101:235409H (1984) of JPN 59152316 Aug. 31, 1984.
Sunstar CA. 101:235410B (1984) of JPN 59152317 Aug. 31, 1984.
Otsuki CA. 112:240332J (1990) of JPN 02045415 Feb. 15, 1990.
Otsuki CA. 113:46142C (1990) of JPN 02045412 Feb. 15, 1990.
Otsuki CA. 113:46143D (1990) of JPN 02045414 Feb. 15, 1990.
Otsuki CA. 113:217823G (1990) of PCT/WO 9002544 Mar. 22, 1990.
Patent Abstracts of Japan, vol. 8, No. 283, Dec. 25, 1984, 59-152315.
Patent Abstracts of Japan, vol. 12, No. 209, Jun. 15, 1988, 63-8326.
Patent Abstracts of Japan, vol. 12, No. 47, Feb. 12, 1988, 62-195320.

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