WO2005041910A1

WO2005041910A1 - The oral product of the solidity which is stabilized a whitening ingredient

Info

Publication number: WO2005041910A1
Application number: PCT/KR2004/002748
Authority: WO
Inventors: Jae Ick Lee
Original assignee: Individual
Current assignee: Individual
Priority date: 2003-10-31
Filing date: 2004-10-29
Publication date: 2005-05-12
Anticipated expiration: 2006-04-30
Also published as: KR20050041807A; KR100561211B1

Abstract

A solid tooth whitening agent and a fabricating method thereof are disclosed, which agent includes peroxide as a stabilized tooth whitening component. The method comprises steps of mixing source materials in a liquid state, drying the same in a state of being thinly applied to a release liner, and extruding a semi-finished product dried. Another method comprising the steps of directly mixing source materials in an extruding machine, and extruding the same through a self-mixing. Still another method comprising the steps of placing a semi-finished product in solution state in a forming mold, and curing the same, fabricating a solid tooth whitening agent with its tooth whitening components stabilized. The peroxide is further stabilized in comparison with a conventional product so that upon being applied to the tooth, it does not flow but to be selectively and easily applied to the tooth, it does not flow but to be selectively and easily applied tooth desired without unpleasant feeling.

Description

The Oral Product of the Solidity Which is Stabilized a Whitening Ingredient

Technical Field

The present invention relates to a solid tooth whitening agent with its whitening components stabilized, and more particularly, to a solid tooth whitening agent which is prepared to be conveniently used as to be directly applied to tooth by stabilizing whitening components for tooth whitening.

Background Art

With the recent change of dietary habits, a tooth discoloration has been often generated so that it has been gradually concerned about tooth whitening. To meet this demand, various kinds of tooth whitening supplies have been fabricated, but consumers do not satisfy such tooth whitening supplies due to their own problems. In case of a traditional method using toothpaste and tooth brushes, although very effective tooth whitening agents are contained in the toothpaste, it is difficult to obtain a tooth whitening effect for a short time even by tooth brushing for 1 to 3 minutes.

For example, in case of a product of Professional Whitening Gel, a tray is manufactured corresponding to a size of patent's tooth and a certain amount of high concentration peroxide gel should be applied thereto. However, it causes a problems in inconvenience, high costs, and side effect such as gum irritation due to remaining high concentration peroxide gel and the tray.

EP Publication No. 0511782 A has proposed a coating agent for tooth whitening. Its viscosity is 30,000 to 50,000cps so that it causes a problem in that the coating agent may flow after application or should be dried with patent's mouse opened.

USP No. 5,824,291 has proposed a tooth whitening component contained in the gum base. Tooth whitening components are discharged from the gum base during chewing the gum base. The discharged tooth whitening components react with contaminant of tooth to generate tooth whitening. However, it has a simple tenuous effect because the discharged tooth whitening components are continuously diluted by saliva. USP Nos. 5,879,691, 5,891,453 and 5,989,569 and WO 98/55044 of Procter

& Gamble (P&G) have proposed a delivery system for tooth whitening agent. In this delivery system, instead of using a mouth tray, a thin, transparent and flexible polyethylene strip is pre-coated with the tooth whitening agent. Otherwise, before use, the tooth whitening agent is directly applied to tooth or the strip. It provides advantages in convenience in use due to without using mouth tray and daily life is not hindered even in wearing due to its transparency and thin thickness. However, it also provides disadvantages in that as shown in an embodiment and the like, the flexible polyethylene strip is thinly pre-coated with high viscosity gel using carbopol in quantity as gelling agent in wet type. Thus, upon attaching it to tooth, high concentration peroxide gel is subject to be adhered to finger, tongue or gum and the like to cause unpleasant feeling in using. Further, technologies for forming of two layers of tooth whitening components and strip and for stabilizing of peroxide in the layers are not sufficiently secured, it may cause a problem in reduction of tooth whitening effect due to high temperature or long term preservation. USP Nos. 5,310,563 and 5,639,445 of Colgate have proposed a drug delivery system in which effective components and Dow Corning 3179 of dilatant compound are mixed into one mass, which is pressed and attached to the tooth and is easily then detached. It has a double layered structure in which effective components are contained in polymer in a capsulated type so that stability of peroxide according to time lapse may be secured to a certain extent. However, effective components are hardly escaped from dilatant compound in a short time so that longer contact time should be required for tooth whitening.

Japanese Patent No. 10,017,448 of Lion has proposed a sheet type mouth plaster. This drug delivery system consists of tooth attachment layer and a support layer. Tooth whitening agent includes kojic acid and its derivatives, ascorbic acid and its derivatives, urea peroxide and the like. However, all tooth whitening agents have strong acidity so that irritation due to pH may be generated in the mouth. Also, since they have tooth whitening effect only under strong acidity, it is difficult to obtain a plaster with little irritation and good tooth whitening effect. Such double layered patch has a problem in that, if relatively reactive source material as tooth whitening agent is used, stability at high temperature can be reduced even upon stored with a release liner attached thereto.

Disclosure of the Invention

Accordingly, the present invention is directed to a solid tooth whitening agent that substantially obviates one or more of the problems due to limitations and disadvantages of the related art.

Herein, the 'solid' state means that agent has a hardness of 50 to 200 and a low fluidity as to be applied to a tooth in a state of being contained in a holder as shown in FIG. 1. The solid tooth whitening agent of the present invention is composed of a few kind of polymer to maintain constant hardness. Complex property of polymer such as viscosity and elasticity can be changed according to various external environments. Thus, given hardness is measured such that a product of agent stored in incubator at 25 ^°C for lhour is measured by UDS-200 Rheometer of Physica (U.S. A) as shown in FIG. 2 in such a manner that agent is seated on a support of the Rheometer, and that a string connected with an adapter is contacted with a product of agent and then cut the product completely.

There are two methods for fabricating solid phase. First method is provided in which source materials including tooth whitening components, polymer components for stabilizing the former, stabilizing agent, moisturizing components, solvent and so on are mixed in liquid phase, liquid phase component is dried, and a dried semi-finished product is made into a product like a lipstick using an extrusion manner (see FIG. 3). Second method is provided in which source materials as explained above are intruded into an extruding machine to be directly mixed therein and to be extruded to form a product like a lipstick.

In a construction of the extruding machine, a body of the machine is shaped as illustrated in FIG. 3 and includes a screw that is the most important element smoothly speed-changed in a revolution speed of at least 20 to 80rpm by automatic transmissions. The screw serves to sufficiently intrude the semi-finished product into the screw so that intruded product is advanced and accelerated in a direction of head while increasing an internal pressure homogeneously. The product which is homogeneously accelerated is extruded by a sufficient pressure thus to be sufficiently formed at the head and die.

The intrusion of the semi-finished product is also related with a shape of feed- hopper (see FIG. 4).

In the illustrated feed-hopper as shown in FIG. 4, A and B types are proper for granular product, and C type is generally used for a semi-finished product whose state is required for the present invention. In the C type, the product can be smoothly intruded because a revolution direction is positioned under a screw groove in a horizontal direction of the screw groove. The screw is structured such that a pressure applied to the semi-product should be gradually increased so as to intrude the same in the head direction. To this end, some methods can be adapted in which pitches of the screw groove are gradually shorten toward the leading end of the groove, the groove is gradually narrowered toward the leading end thereof while maintaining the pitches constant, and a width of the screw is gradually enlarged toward the leading end thereof while maintaining the pitches constant.

Accordingly, an object of the present invention is directed to improve a tooth whitening effect through the stabilization of tooth whitening components while improving a method for fabrication tooth whitening agent.

To achieve this and other advantages and in accordance with the purpose of the present invention, as embodied and broadly described, a solid tooth whitening agent with a new drug delivery system and a fabricating method thereof are provided which stabilize tooth whitening components and improve tooth whitening effect and usability.

Hereinafter, an embodiment of the present invention will be explained in detail.

According to the present invention, the tooth whitening component includes at least one selected from group including peroxide, chloric bleaching agent, polyphosphates, Vit-E, and enzyme such as dextranase and papain. The peroxide includes hydrogen peroxide, urea peroxide, sodium carbonate peroxide, sodium perborate, calcium peroxide, sodium pyrophosphate peroxide and the like. The chloric bleaching agent includes sodium hypochlorite. The polyphosphate includes potassium pyrophosphate, sodium pyrophosphate, sodium acid pyrophosphate, sodium meta phosphate, sodium polyphosphate, potassium sodium pyrophosphate and the like.

In order to stabilize tooth whitening components, polymer is used. Polymer includes at least one selected from the group including cellulosegum, bentonite, carbopol, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, polyvinyl alcohol, polyvinylacetate, pectin, starch, xanthan gum, polyalkyl vinyl ether-maleate copolymer (PVM/MA copolymer, Gantrez AN 149, AN 139, S-97), polyacrylate, poloxamer 407 (pluronic), polyvinyl pyrrolidone-vinyl acetate copolymer (PVP/VA copolymer; Luviskol VA, Plasdone S PVP/VA), poly vinyl pyrrolidone (PVP, K-15 ~ K-120), polyquaterium-11 (Gafquat 755N), polyquaterium- 39 (Merquat plus 3330), hydroxypropylmethylcellulose, gelatin, alginic acid (sodium alginate), polyvinyl acetate, ethyl cellulose, poly methyl methacrylate, methacrylic acid copolymer, methacrylic copolymer, amino alkyl methacrylate copolymer, cellulose acetate phthalate, polyethyleneglycol and the like. In order to further stabilize tooth whitening component irrespective to using polymer, a stabilizing agent is added. The stabilizing agent includes at least one selected from a group including candelilla wax, beeswax, paraffin wax, wooden wax, carbauna wax, ceresin, tri-2-ethylhexyl acid glycerin, liquid paraffin, caprylic/capric triglyceride, alkyl aryl sulfonate, alkyl sulfonate, alkyl carboxylate, alkyl diphenyl oxide disulfonate, span 20 (Sorbitan Monolaurate), span 40 (Sorbitan Monopalmitate), span 60 (Sorbitan Monostearate), span 80 (Sorbitan Monooleate), span 85 (Sorbitan Trioleate), TWEEN (POE sorbitan fatty acid ester).

Also, according to polymers, a flexibility and an application property thereof are poor. In order to compensate this, moisturizing element can be added. The moisturizing element which includes at least one selected from a group including glycerin, sorbitol, propyleneglycol, butyleneglycol, ceramide, castor oil, hydrogenated castor oil and the like.

Solvent may be at least one selected from a group including water, alcohol and the like.

Dosage of source materials is as follows : As the tooth whitening component, at least one element among the group explained above is mixed to use in 1-15%. As the polymer, at least one element among the group explained above is mixed to use in 1-25%. As the stabilizing agent, at least one element among the group explained above is mixed to use in 1-8%. As the moisturizing element, at least one element among the group explained above is mixed to use in 1-8%. As the solvent, at least one element among the group explained above is mixed to use in 40-75%.

In order to solidify liquid compound with above compositions, solvent should be dried. If it is dried at high temperature, stability of tooth whitening component is degraded. Thus, in order to dry the liquid compound fast, it is thinly applied to a release liner and is dried using a drying tunnel until l~10wt% of solvent remains in whole weight of compound.

To make a shape of the dried compound, dried semi-finished product is separated and extruded using an extrusion, fabricating a solid tooth whitening agent (see FIG. 2.). Also, a solid tooth whitening agent can be fabricated by placing given semi-finished product in solution state in a forming mold and curing it.

Alternatively, by making solvent ratio different and directly intruding source materials provided above in the extruding machine without subjecting a mixing process so as to extrude the source materials, lipstick as solid product can be fabricated using only extrusion without subjecting a drying process. Brief Description of the Drawings

The accompanying drawings, which are included to provide a further understanding of the invention and are incorporated in and constitute a part of this specification, illustrate embodiments of the invention and together with the description serve to explain the principles of the invention.

In the drawings:

FIG. 1 is a perspective view of a holder;

FIG. 2 is photographs showing rheometer for measuring hardness of a product fabricated by the present invention; FIG. 3 is a cross-sectional view of an extruding machine used for fabricating a solidified product of the present invention; and

FIG. 4 illustrates shapes of feed-hoppers of the extruding machine of FIG. 3.

Best Mode for Carrying Out the Invention Hereinafter, preferred embodiments of the present invention will be described in detail with reference to accompanying drawings, example and comparative examples.

As will be described below, tooth whitening agent was prepared according to examples 1 to 5 and comparative examples 1 to 3.

[EXAMPLE]

Table 1. Composition of Source Materials

The respective fabricating methods thereof are conducted as follow. The source materials according to their compositions above were mixed in liquid state and thinly wet-applied. The applied source materials were passed through a drying tunnel and dried. The dried semi-finished product were extruded using a extruding machine thus to fabricate a solid tooth whitening agent.

[COMPARATIVE EXAMPLE 1]

Toothpaste was prepared by mixing 2% of cellulose gum, 10% of peroxide (35% solution), 20% of silica, 30% of glycerin, and water to 100% and removing bubble from mixed compound.

[COMPARATIVE EXAMPLE 2]

Coating fomulation for tooth whitening was prepared by mixing 10% of PVP, 10% of peroxide (35% solution), 5% of glycerin, 4% of castor oil, and of blend solution (water:ethanol=l:l) to 100%.

[COMPARATIVE EXAMPLE 3]

Tooth attached type tooth whitening agent was prepared by mixing 10% of carbopol, 10% of peroxide (35% solution), 5% of glycerin, pH adjuster, and of blend solution (water:ethanol=l:l) to 100% to provide gel, and applying this gel to a thin polyethylene file.

[EVALUATION OF TOOTH WHITENING EFFECT]

The best method for evaluating tooth whitening effect is to evaluate the tooth whitening agent by practically adapting it to tooth. Persons to be evaluated were selected whose tooth indicated dark in comparison with level 8 with reference to Vita shade guide¹³. Changed value from initial color was recorded. Also, after use, questionnaire research was conducted to the persons to evaluate tooth whitening effect and usability they felt.

Table 2. Evaluation Sheet For Tooth Whitening Effect

Twenty evaluating persons of men and women were distributed to the respective groups, and a dosage for respective group was selected according to property of a product. The evaluation was conducted by following methods for two weeks.

Examples 1 to 5: apply 3 times a day on the tooth.

Comparative example 1 : tooth-brush 3 times a day using toothbrush.

Comparative example 2: apply 2 times a day on the tooth. Comparative example 3: attach 2 times a day on the tooth.

Vita Shade Guide: it is a tooth model internationally approved expressing an amount of tooth color change as 16 levels, which is used for tooth whitening effect by university, evaluating institution and dentist of dental hospital. The evaluating of their tooth whitening effect is conducted by following 5- points level.

1: poor level, 2: little level, 3: a little level, 4: good level, and 5: excellent level.

The evaluating of convenience and usability is conducted by following 5- points level.

1 : poor level, 2: slightly poor level, 3: middle level, 4: good level, and 5: excellent level.

The examples according to the present invention have a good tooth whitening effect in comparison with comparative examples. It is because that tooth whitening components in the examples do not flow upon being applied on the tooth, so that they continuously maintain a long time contacting with the tooth thus to be continuously delivered thereto. Similarly, comparative example 3 (tooth attached type tooth whitening agent) has a good effect due to a continuous delivery of tooth whitening component because it is continuously attached to the tooth. On the contrary, tooth whitening agent of toothpaste and coating fomulation for tooth whitening has a poor effect due to that upon application to the tooth, it is continuously diluted by saliva in mouth. In case that oil component as stabilizing agent is contained, oil component remains in the tooth to prevent a dilution due to saliva. [Evaluation of Product Stability]

Products fabricated in examples and comparative examples were packed with pouch and remaining amount of peroxide thereof was periodically evaluated with the products stored in a constant temperature and humidity chamber (high temperature 40 TJ).

Table 3.

Evaluation Sheet for Stability

Comparing examples 1,2 and 3 with comparative examples 1,2 and 3 on the table 3, peroxide stability at high temperature was different according to whether or not peroxide stabilizing agent was added and an added amount thereof provided that other compositions were same.

Also, comparing example 3 with comparative examples 1,2 and 3, a solid type product had an excellent stability in comparison to a wet type product although they all did not contain peroxide stabilizing agent. Industrial Applicability

As described before, the present invention is directed to improve a tooth whitening effect through the stabilization of tooth whitening components while improving a method for fabrication tooth whitening agent.

While the present invention has been described and illustrated herein with reference to the preferred embodiments thereof, it will be apparent to those skilled in the art that various modifications and variations can be made therein without departing from the spirit and scope of the invention. Thus, it is intended that the present invention covers the modifications and variations of this invention that come within the scope of the appended claims and their equivalents.

Claims

1. A solid tooth whitening agent, comprising polymer and a stabilizing element in order to stabilizing tooth whitening components for tooth whitening, wherein the solid state means that agent has a hardness of 50 to 200 which is measured such that a product of agent stored in incubator at 25 ^°C for lhour is measured by UDS-200 Rheometer of Physica (U.S. A) in such a manner that agent is seated on a support of the Rheometer, and that a string connected with an adapter is contacted with a product of agent until to cut completely.

2. A method for fabricating solid tooth whitening agent according to claim 1, comprising the steps of mixing source materials in a liquid state, drying the same, and extruding a dried semi-finished product in order to fabricate a solid tooth whitening agent with its tooth whitening components stabilized.

3. A method for fabricating solid tooth whitening agent according to claim 1 , comprising the steps of placing a semi-finished product in solution state in a forming mold, and curing the same in order to fabricate a solid tooth whitening agent with its tooth whitening components stabilized.

4. A method for fabricating solid tooth whitening agent according to claim 1, comprising the steps of directly mixing source materials in an extruding machine, and extruding the same in order to fabricate a solid tooth whitening agent with its tooth whitening components stabilized.

5. The solid tooth whitening agent according to claim 1, wherein the tooth whitening component includes at least one selected from group including peroxide, chloric bleaching agent, polyphosphates, Vit-E, and enzyme such as dextranase and papain wherein peroxide includes hydrogen peroxide, urea peroxide, sodium carbonate peroxide, sodium perborate, calcium peroxide, sodium pyrophosphate peroxide and the like, wherein chloric bleaching agent includes sodium hypochlorite, and wherein polyphosphate includes potassium pyrophosphate, sodium pyrophosphate, sodium acid pyrophosphate, sodium meta phosphate, sodium polyphosphate, potassium sodium pyrophosphate and the like.

6. The solid tooth whitening agent according to claim 1, wherein the polymer for stabilizing tooth whitening components includes at least one selected from the group including cellulosegum, bentonite, carbopol, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, polyvinyl alcohol, polyvinylacetate, pectin, starch, xanthan gum, polyalkyl vinyl ether-maleate copolymer (PVM/MA copolymer, Gantrez AN 149, AN 139, S-97), polyacrylate, poloxamer 407 (pluronic), polyvinyl pyrrolidone-vinyl acetate copolymer (PVP/VA copolymer; Luviskol VA, Plasdone S PVP/VA), poly vinyl pyrrolidone (PVP, K-15 - K-120), polyquaterium-11 (Gafquat 755N), polyquaterium-39 (Merquat plus 3330), hydroxypropylmethylcellulose, gelatin, alginic acid (sodium alginate), polyvinyl acetate, ethyl cellulose, poly methyl methacrylate, methacrylic acid copolymer, methacrylic copolymer, amino alkyl methacrylate copolymer, cellulose acetate phthalate, polyethyleneglycol and the like.

7. The solid tooth whitening agent according to claim 1, wherein the stabilizing agent for stabilizing tooth whitening component irrespective to using polymer includes at least one selected from a group including candelilla wax, beeswax, paraffin wax, wooden wax, carbauna wax, ceresin, tri-2-ethylhexyl acid glycerin, liquid paraffin, caprylic/capric triglyceride, alkyl aryl sulfonate, alkyl sulfonate, alkyl carboxylate, alkyl diphenyl oxide disulfonate, span 20 (Sorbitan Monolaurate), span 40 (Sorbitan Monopalmitate), span 60 (Sorbitan Monostearate), span 80 (Sorbitan Monooleate), span 85 (Sorbitan Trioleate), TWEEN (POE sorbitan fatty acid ester).