HUP0303822A2 - Applicator for applying a benefit agent and its use - Google Patents

Abstract

The subject of the invention is a pre-dosed applicator for the application of beneficial agents to the teeth, in which the beneficial agent is selected from the group consisting of the following: agents for sensitive teeth, anti-caries agents, anti-calculus agents, fresh breath agents, vitamins, aromas, anti-plaque agents and their mixtures. HE

Description

99489-2227C STG

10303^22.

PUBLISHED

X.

Applicator is a beneficial agent for teeth

FOR IMPLEMENTATION AND ITS APPLICATION

The present invention relates to a pre-dosed applicator loaded with a beneficial agent that provides localized application of the agent to a targeted surface while minimizing contact with other oral tissues.

Dental plaque is a non-mineralized microbial accumulation that adheres tenaciously to tooth surfaces. Plaque is composed of an organic matrix derived from salivary glycoproteins and extracellular microbial products and cannot be removed by rinsing or water spray. It is commonly present in all human populations and, if not removed regularly and completely by adequate toothbrushing and allowed to accumulate on tooth surfaces, can lead to dental disease.

Plaque is translucent or tooth-colored and therefore not easily visible, so some individuals are often unaware of the presence of plaque itself, its amount, and its location in the mouth. One method of effectively controlling plaque20 is to make the individual aware of what plaque is and how it affects the surrounding tissues. This can be done by visibly displaying plaque on the individual’s teeth, which demonstrates to the individual that there is bacterial build-up on their teeth that could cause damage later, and therefore creates concern and motivation to practice good oral hygiene. Plaque markers are also used to

« *· . » · ·· because the use of dye indicators allows for such a visible demonstration of plaque.

Currently available markers include organic dyes such as erythrosine dyes, fluorescent synthetic dyes that are not visible to the naked eye under normal daylight conditions but become visible using light of the appropriate wavelength, two-color dyes that distinguish between new and old plaque, etc. Other typical markers include tartrazine yellow; patent blue V; crystal violet; ruthenium red;

5-cyano-2,3-ditolyltetrazolium chloride; amaranth; FDC red 40; Congo red; rosaniline; neutral red; safranin; FDC red 3; FDC blue 1; FDC green 3; Hercules green shade 3; fluorescein; betamin red; and vulgaxanthin yellow.

Such markers can be applied in solution or in tablet form, as is known. These methods have the disadvantage that they stain the gingival tissues and lips indiscriminately, and the color remains on the surface of the tissues even after rinsing and only gradually disappears. This is one of the reasons why people do not use markers routinely.

US Patent No. 4,992,256 (Colgate-Palmolive Co., 1990) discloses the use of FD & C Red No. 3 as an aqueous aerosol spray, chewing gum, wafers and tablets for the detection of dental plaque with the naked eye under visible light.

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US Patent No. 4,431,628 (Colgate-Palmolive Co., 1984) discloses the use of a natural red dye derived from sugar beets, formulated as a solution, tablet, gel, powder or aerosol, to selectively stain plaque on the tooth surface without staining adjacent oral tissues.

Other forms of the product, such as chewable tablets, tablets, powders, lozenges, aerosols, liquid concentrates, are also known; they incorporate various known plaque-marking agents.

However, there is no known effective teaching on how to apply plaque marker to the surface of teeth for the above purpose without staining the adjacent oral soft tissues and lips.

Our aim with the invention is to overcome the problem described above.

Our invention enables the application of selected amounts of plaque markers to the teeth using an applicator, thereby selectively staining plaque, plaque, microbes and bacteria without staining the adjacent soft tissues of the oral cavity and lips. The applicator provides a more effective solution than the commonly used method of applying the dye via marker tablets or liquid. It is convenient to use and extremely economical.

In order to achieve our goal, according to the first aspect of the invention, we have created an applicator for applying a beneficial agent, which applicator is a

The device comprises a device carrying a beneficial agent in liquid form, which device has liquid-absorbent properties. Preferably, the beneficial agent is selected from the group consisting of: agents for sensitive teeth, anti-caries agents, anti-tartar agents, breath fresheners, vitamins, flavors, plaque markers, and mixtures thereof.

The skill of the invention thus provides the consumer with a means to target an area of the oral cavity without having to use a large amount of the above agent. The applicator also provides the consumer with a means to specifically target the area that needs treatment. The known skills have only provided a means that were suitable for targeting the oral cavity as a whole.

Antimicrobial agents — which may also provide anti-tartar or anti-gingivitis effects — include: triclosan, chlorhexidine, copper, zinc and tin(II) salts such as zinc citrate, zinc sulphate, zinc glycinate, sodium zinc citrate and tin(II) pyrophosphate, blood poppy (Sanguinaria) extract, metronidazole, quaternary ammonium compounds such as cetylpyridinium chloride; bisguanides such as chlorhexidine digluconate, hexitidine, octenidine, alexidine; and halogenated bisphenol compounds such as 2, 2’ methylenebis-(4-chloro-6-bromophenol); anti-inflammatory agents such as ibuprofen, flurbiprofen, aspirin, indomethacin, etc.

Anti-caries agents such as sodium and stannous fluoride, amine fluorides, sodium monofluorophosphate, sodium trimetaphosphate and casein.

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The beneficial agent of the invention may further comprise any of the following ingredients:

plaque buffers such as urea, calcium lactate, calcium glycerophosphate, and strontium polyacrylates;

vitamins such as vitamins A, C and E; plant extracts;

desensitizing agents such as potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salts;

anti-tartar agents, such as alkali metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates and phosphocitrates, etc.;

biomolecules, such as bacteriocins, antibodies, enzymes, etc.;

flavorings, such as peppermint and spearmint oils;

proteinaceous substances such as collagen;

preservatives;

opacifiers;

coloring agents;

pH adjusting agents;

sweeteners;

pharmaceutically acceptable carriers, such as starch, sucrose, water or water-alcohol systems, etc.;

surfactants, such as anionic, nonionic, cationic and zwitterionic or amphoteric surfactants;

particulate abrasives such as silicas, aluminas, calcium carbonates, dicalcium phosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates, and the like, including agglomerated particulate abrasives, generally in an amount of from 3% to 60% by weight of the oral care composition;

humectants such as glycerin, sorbitol, propylene glycol, xylitol, lactitol, etc.;

binders and thickeners such as sodium carboxymethylcellulose, xanthan gum, gum arabic, etc. as well as synthetic polymers such as polyacrylates and carboxyvinyl polymers such as Carbopol®;

Polymer compounds which can improve the delivery of active ingredients, such as antimicrobial agents, may also be used. Examples of such polymers include copolymers of polyvinyl methyl ether with maleic anhydride, and other similar delivery enhancing polymers, such as those described in DE-A-3,942,643 (Colgate); and buffers and salts for buffering the pH and ionic strength of oral care compositions.

Preferably, the beneficial agent is present in an amount capable of providing the desired beneficial effect. However, this may be well below the level required for a toothpaste to achieve the same effect. Accordingly, the composition of the invention comprises the beneficial agent in an amount in the range of 0.0001% to 1%, preferably in the range of 0.001% to 0.5%, based on the weight of the liquid absorbing portion of the composition after application of the composition. Alternatively, the agent is present in an amount in the range of 0.01% to 1%, preferably in the range of 0.02% to 0.7%, based on the weight of the liquid to be introduced into the liquid absorbing portion of the head before the composition is stored either as a dried or as a wet composition which is suitably sealed.

According to a preferred aspect of the invention, an applicator is provided in which the liquid-absorbing material filled with a beneficial agent is arranged at at least one end of the applicator, and the liquid-absorbing material is preferably wetted before the applicator is brought into contact with natural or artificial oral prostheses.

The beneficial agent may be in a liquid form or may be in a dried form for easier storage. Dried applicators may be moistened immediately prior to use. Wet applicators may be stored in a sealed container to maintain their freshness for use.

According to a preferred aspect of the present invention, single or multiple use applicators are provided which are capable of applying the required amount of plaque marker to natural or artificial oral prostheses.

According to another preferred aspect of the invention, the applicator is provided with a liquid absorbent material which is filled with the plaque marker in liquid or dissolved form and then dried. It is particularly preferred that the drying is carried out by vacuum drying. Various plaque markers which can be used for the purposes of the invention are mercurochrome, bismarck brown, erythrosine, brilliant green, fluorescein, two-color dyes and basic fuchsin, of which erythrosine is the most preferred agent.

Preferred colorants include a combination of colorants that results in a blue color prior to use of the product. Consumers prefer blue to red for applications such as those to which the invention relates. It is also preferred to use a colorant that actually changes color upon contact with the beverage in the oral cavity, such that there is no doubt that use of the product results in a mere transfer of the colorant. The color change preferably results in a change from blue or green to pink.

One preferred combination of colorants comprises a combination of FDC Red 5 No. 3 and FDC Blue No. 3. Preferably the ratio of red to blue is in the range of 150:1 to 1:15, more preferably in the range of 50:1 to 1:5, and particularly preferably in the range of 8:1 to 1:1. The amount of FDC Red No. 3 is in the range of 0.1% to 1.5% by weight of the colorant applied to the product, more preferably in the range of 0.3% to 1.5%, and most preferably in the range of 0.6% to 1.3%. FDC Blue No. The amount of 3 is between 0.01% and 1.8% by weight of the dye applied to the preparation, more preferably between 0.05% and 1%, and most preferably between 0.1% and 0.5%. In such a combination of dyes, FDC Green No. 3 can also be used.

The applicator may be designed for single or multiple use. The tip of the applicator may be specially designed to be of a size and shape that allows application to the teeth. Its diameter may vary from 1 mm to 10 mm, preferably from 2 mm to 20 mm and 8 mm, and particularly preferably from 2 mm to 6 mm. The shape of the head may be circular, elliptical, teardrop-shaped, conical, disc-shaped, pear-shaped and semicircular. In the case of multiple use, it may be provided with a reservoir for plaque marker so that the same may be made suitable for application to oral prostheses as and when desired. The reservoir may be provided with plaque marker in solid or liquid form.

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In the case of single-use applicators, a known and required amount is provided as part of the liquid-absorbing material on the applicator. For a single application to the entire dentition, the required amount of dye may be in the range of 1 mg to 10 mg, preferably in the range of 1 mg to 5 mg. The tablets typically contain 12 mg of dye, a significant portion of which is wasted as the surrounding soft tissues of the oral cavity are also stained.

The absorbent material may be of natural or synthetic origin and may be selected from the following: cotton wool, sponge or textile or any other absorbent material. It preferably also contains an abrasive material, such as chalk, silica, perlite, pumice stone or any other abrasive material commonly used in oral care.

After the plaque marker has been loaded into the liquid absorbing portion of the applicator, the applicator is dried by any suitable means, preferably by vacuum drying. The drying time may vary and may be in the range of 3 hours to 4 hours, while the temperature during drying may be in the range of 60°C to 80°C.

The applicator can be conveniently packaged individually or in multiples.

If the amount of agent is reduced, there may not be enough available to stain the teeth, and therefore some overdosing will be necessary, which nevertheless leads to another problem of staining soft tissues. The applicator is primarily used on the teeth, and thus the amount of agent used will be adequate.

In addition, the applicator of the invention may be part of a kit that includes an oral care product in addition to the applicator. In such a kit, the user enjoys the benefits of whiter teeth, fresher breath, reduced caries, reduced plaque formation, and reduced gingivitis, as he/she has the incentive to receive the applicator in the same package as the oral care product. The oral care product may be a toothpaste, mouthwash, gel, powder, or any other form of oral care product commonly used in the given field.

The invention is illustrated below by means of non-limiting examples, with reference to the accompanying drawings. In the drawing, Figures 1a and 1b show a disposable applicator, the

Figures 2a and 2b show a variety of different shapes and forms of applicators, the

Figures 3a and 3b show further embodiments of the applicator,

Figure 4 shows an applicator with a reservoir, while

Figure 5 shows an applicator with a toothpick.

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Examples

The applicator and its production

Figures 1a and 1b show a disposable applicator. Figures 2a and 2b show a variety of other forms and shapes. Figures 1a and 1b show an ST handle having a liquid-absorbing LH head at one end as shown in Figure 1a and at both ends as shown in Figure 1b. A reservoir is provided to allow for multiple uses. The liquid-absorbing LH head is made of cotton wool and is filled with 0.2 ml of 2% erythrosine dye. The applicator was dried under vacuum at 80°C for 3 hours.

Figures 3a and 3b show an applicator according to the invention, which comprises a liquid-absorbing head LH and a handle ST, and is also provided with a ring-like part FS, which allows the insertion of a finger. Thus, the application can be solved using a single finger. In this way, the skill can be used in hard-to-reach parts of the oral cavity.

Figure 4 shows an applicator according to the invention which has a reservoir R for storing the liquid to be applied. In this way, multiple use can be ensured.

The applicator shown in Figure 5 comprises a handle ST, a liquid absorbing head LH and a toothpick. The toothpick in this case is located at the end opposite the liquid absorbing head LH, however, this is not strictly necessary, although it is advantageous.

Combined dyes

The swab is kept in contact with the first dye, FDC red, for 1 minute.

This is followed by the second dye, FDC blue, for 1 minute. The pad is then dried at 90°C for 1 hour.

FDC red No. 3 FDC blue No. 3 the color of the tuft marker color (pink?) 0.3% 0.3% violet okay 0.2% 0.25% dark blue okay 0.3% 0.2% blue violet okay 0.5% 0.25% blue okay 0.6% 0.2% blue good 1.25% 0.2% blue-green good 1.25% 0.4% greenish black okay

Conclusions

The color of the swab was blue, which was achieved by combining 0.6% FDC red and 0.2% FDC blue. The color obtained after application was blue and the marked plaque was pink.

Plaque marking was found to be best when 1.25% FDC red and 0.2% FDC blue were used. The color of the plaque was blue-green.

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Testing the effectiveness of the applicator

A panel of trained volunteers was divided into two groups. One group was asked to use the applicator, while the other group was asked to chew an erythrosine tablet before brushing their teeth for the first time each day. The applicator was provided with a liquid-absorbing head filled with erythrosine at both ends. The panelists were asked to wet one end of the applicator and move it along the surface of their teeth for approximately 1 minute while observing this activity in a mirror. The presence of plaque was immediately visible. The tablet also revealed plaque if it was present on the teeth. The panelists were then asked to brush their teeth in the usual way, using a dentifrice and a toothbrush. After brushing was finished and their mouths were rinsed with water, the other end of the applicator was used as before to mark plaque if it was present.

There was minimal or no discoloration of the oral soft tissue when the applicator of the invention was used, but a deep red discoloration was visible when the erythrosine tablet was chewed and persisted for approximately 2 hours. However, the marking of plaque on the teeth assisted brushing to the same extent in both cases.

Claims (6)

Patent claims 1. An applicator for applying a beneficial agent to teeth, characterized in that the applicator comprises a handle (ST) and a liquid absorbing portion. 2. The applicator of claim 1, wherein the beneficial agent is selected from the group consisting of: agents for sensitive teeth, anti-caries agents, anti-tartar agents, breath fresheners, vitamins, flavors, plaque inhibitors, and mixtures thereof. 3. The applicator according to claim 1 or 2, characterized in that the beneficial agent is a plaque marker. 4. The applicator according to claim 1, characterized in that the applicator comprises a handle (ST) and an applicator head (LH), the head (LH) comprising a liquid-absorbing material for absorbing the plaque marker solution. 5. An applicator according to claim 3, characterized in that the applicator head (LH) contains a dried plaque marker. 6. Use of an applicator according to any one of claims 1, 3 or 4 for applying a plaque marker to teeth, characterized in that the device is first moistened and then applied to the teeth.