DE1792769A1 - USE OF PHOSPHORIC ACID ESTER SALT TO PREVENT DENTAL CARIES - Google Patents

Description

Patent Attorneys 51 Audwn, Jen Mar 15, 1974

DIPL-ING. BRUNO SCHMETZ Augu & kjstraßeH-lo -Tei. (0241) 508051

DIPL-ING. WERNER KÖNIG

THE COLONIAL SUGAR HEFINING COMPANY LIMITED in Sydney, New South Wales (Australia)

File number: P 17 92 769.4-4I

New description

Use of phosphoric ester salts for prevention of dental caries

The invention relates to the use of phosphoric acid ester salts to prevent dental caries.

About the effect and influence of the dental caries is already Various known. The main factors are:

1. Bacteria that produce acids (for example of the type of lactic acid bacilli that produce lactic acid) are found in the Oral cavity in large numbers when dental caries invasion occurs.

2. Carbohydrates provide a favorable substrate for formation of acids in the oral cavity. With the term "cariogenic" In the following, foods are referred to as foods that consist of or contain carbohydrates.

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3. Acids that are developed in the oral cavity attack and dissolve tooth components, thereby protecting the teeth for Dental caries and tooth wear become more susceptible.

4. Solutions that contain calcium and phosphate in dissolved form prevent acid attack and also harden through Acids re-softened human tooth enamel. Fluoride accelerates re-hardening.

The cariogenic effect of these acids arises from direct and usually longer contact between the acid and the tooth. Experts do not yet agree on the exact nature of the effect, but it is known that the acids in the mouth or cause softening and erosion of tooth enamel in vitro. The softening or destruction of tooth enamel then the dental caries follows.

It is also known that the cariogenic effect of these acids is due to the presence of certain soluble organisclei Phosphates such as sodium or ammonium phosphate is prevented. This cariostatic effect takes place in the mouth or in vitro, however, the process is not yet fully understood.

Because of its local effect, the phosphate inhibitor should be used at the same time with and in the same place as the cariogenic agent. The cariogenic effect of the acids must be on the tooth surface take place in the mouth, at the point where the

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Acid touches the tooth. Hence the cariostatic Agents are present on the tooth surface.

The invention is based on the idea of using the cariostatic agent in foods and beverages, and in particular those which tend to form cariogenic agents in the mouth. Only then will the cariostatic agent be able to produce the most effective result at the right time to effect.

Since it is desirable to incorporate the active ingredient in foods and beverages, almost all of them are for practical reasons or even all previously known cariostatic remedies are unsuitable. Soluble phosphates like sodium, ammonium or magnesium phosphates have a very strong peculiarity Taste, which in effective concentrations of the phosphate is detrimental to the inherent taste of the food or drink influenced. Fluorides have known cariostatic properties, but are generally toxic and their uses in food and beverages requires constant and careful control. The addition of drinking water Flour in negligible amounts has not become generally accepted, despite the fact that it does reduce dental caries has been proven because the fluorides are toxic. Stable calcium phosphates could possibly be under certain conditions are effective, but are generally only sparingly soluble and, like sodium phosphate, have a strong taste. These two

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Properties prevent the successful application of calcium phosphate in food and beverages.

It has now been found that calcium and magnesium salts of Esters of phosphoric acid with sucrose represent substances that are not toxic, only an insignificant taste have and an essential cariostatic in the oral cavity Have an effect.

The invention therefore also provides for the use of the calcium or magnesium salts of esters of phosphoric acid Sucrose for the manufacture or preparation of foods and beverages for the exercise of cariostatic Effect in the oral cavity.

When using the phosphoric ester salts according to the invention for the production or preparation of foods and drinks, the cariogenic effects of the acids formed there by these foods and drinks in the oral cavity neutralized and thus prevented. The cariostatic effect of the phosphoric ester salts according to the invention is apparently based on a chemical action, on the cariogenic substances in the mouth.

In the case of foods for the production or preparation of which the phosphoric ester salts according to the invention are used,

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it can also be prophylactic tablets, candies or lozenges.

About the cariostatic effect of the phosphoric acid ester salts in question to determine, the applicant has carried out extensive tests. It was found that the cariostatic effectiveness of the special type of compound as well as the concentration in which this compound comes to use, depends.

It has further been found that the calcium salts of the phosphate ester obtained from sucrose are particularly effective at contributing the reduction in caries incidence in test animals. The magnesium salts of sucrose phosphate esters also have one good cariostatic effectiveness. However, this is less than that of the calcium salt. Also are the taste characteristics these salts are not quite as beneficial.

The phosphoric acid ester salts according to the invention have the following properties which are necessary for their use as cariostatic Means required in food and beverages are:

1. They exert a cariostatic effect.

2. They are non-toxic.

3. They are soluble.

4. They are edible and largely tasteless.

5. They are compatible with food and beverages, especially carbohydrates.

6. They are relatively cheap.

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It is so that the under 2, 3, 4, 5 and 6 Properties mentioned refer to concentrations that are required to achieve the property specified under 1 to meet.

Studies of various of these substances, particularly calcium sucrose phosphate, are given below Examples explained:

Example A;

The calcium salt of the sucrose phosphate ester (Ca ^c i2 ^H 21 ° 14 ^P * ^2H 2 ⁰ ^ ^ ^{a non-} toxic, water-soluble white powder with a mild taste) prevented the corrosive effect when added to a test medium in vitro at a concentration of 0.5% of lactic acid on human tooth enamel at a pH as low as 3 | 8 · By weight, calcium _{sucrose phosphate acid ester is as effective as sodium phosphate (Na 9} HPO,) meaning that it is three times as effective as sodium phosphate in preventing on a molar basis the attack of lactic acid on the tooth enamel.

Example B;

A strain of Osborn-Mendel rats with tooth decay occurs when following a high-carbohydrate diet fed, was based on the effectiveness of various phosphoric acid ester salts in reducing the occurrence examined the caries when added in varying concentrations to the diet. An example of the

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Given the nature of the results obtained in such an experiment:

The basic diet of the animals examined consisted of:

Sugar (sucrose) 59 parts by weight

Skimmed milk powder '27 ""

Whole wheat flour 6 ""

Alpha 3 ""

Liver powder (from ox) 4 ""

None of the components of the diet contained significant amounts Fluoride. When a control group of rats from the Osborn-Mendel strain was treated for 6 weeks with this diet the animals tooth decay. Control groups were used in each series of experiments.

The experimental groups of animals were given the basic diet with the addition of varying proportions of phosphoric acid ester salts, which were well mixed with the dry food. The degree of dental caries in rats can be measured in 2 different ways can be expressed:

1. Number of rotten teeth regardless of the degree of injury.

2. Number and degree of injuries.

The results of 2 test series (each with its own control group) are given below, with an addition

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of calcium sucrose phosphoric acid ester to the basic diet in the specified amounts.

Addition to the diet

0.5% calcium sucrose phosphoric acid ester

1.0 % calcium sucrose phosphoric acid ester

6.0 fo calcium sucrose phosphoric acid ester

fo reducing the ^ reducing the

Number of degrees of caries in

Caries afflicted compared to

Teeth compared to the control group

55%

81

81 fo

89 %

84 %

The advantage of using cariostatic agents according to the Invention compared to inorganic phosphates and fluorides as agents for reducing the incidence of dental caries and Tooth decay in food and beverages is based on the following:

1. The salts according to the invention of the listed organic esters of phosphoric acid are suitable agents for stable Soluble forms of phosphates and metals, such as calcium, can be obtained, those in the form of inorganic phosphates hardly are soluble.

2. In contrast to inorganic fluorides are those according to the invention Phosphoric acid ester salts not toxic. Some of they even represent valuable food components that can be supplied in an easily soluble form and supply sugar, phosphate and calcium or magnesium, all of which are animal metabolites.

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3. In contrast to inorganic phosphates, the inventive Phosphoric acid ester salts have a not unpleasant mild taste and influence even in Concentrations above the taste of food required for maximum cariostatic effect not essential.

4. Due to the properties listed above, you can the phosphoric ester salts according to the invention within a wide concentration range, within which these effective to combat dental caries and tooth wear.

5. The phosphoric ester salts according to the invention can also be incorporated into prophylactic tablets or lozenges that are particularly suitable for travelers and those users to whom they are not used in any other form To be available.

When used for the production or preparation of foods and beverages, the inventive Phosphoric acid ester salts directly into sugar, grain products such as rye, wheat, oats and barley, rice, soy and flours as well Mixtures of the same are entered. One uses such products for the production of finished goods, such as bread or Cake, then the finished product has a cariostatic effect without affecting its taste or other properties.

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businesses would be noticeably changed. One can use the phosphoric ester salts but also directly in baked goods, confectionery, sugar confectionery, beverages, syrups, canned goods, ice cream, gelatine bring in and the like. Plant foods high in carbohydrates, such as potatoes, can use the phosphoric ester salts to be cooked. The phosphoric ester salts can also be added to table salt or other seasonings and can only be used at the table.

In addition, the phosphoric ester salts according to the invention can also be used in other ways with foods and beverages brought together and used. It is important, however, that they are distributed in the food and drink in this way is even as possible.

The formation of cariogenic substances such as lactic acid and the effect of lactic acid on the teeth evidently require a certain amount Time. In order to achieve an optimal effect, the cariostatic agents according to the invention should be present when the Cariogenic substances (acids) are formed so that their hindering effect meets the cariogenic effect.

The type and concentration of the phosphoric acid ester salts depends on the type of the desired composition of the to be prepared or products to be prepared.

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For the use according to the invention of the phosphoric ester salts Concentrations preferred for foods and beverages are in the range between 0.1 to 6% by weight of these products. Higher concentrations are usually not required to achieve the desired protection against tooth decay.

In the case of candies, lozenges and tablets, higher concentrations can also be used be applied. You can such sweets, pastilles and tablets in the usual way, using Manufacture natural or artificial sweeteners, flavors and binders.

The maximum effectiveness of the use according to the invention of phosphoric acid ester salts arises predominantly when they are introduced Foods containing carbohydrates that are cariogenic or when exposed to acids and usually im Bacteria occurring in the mouth become cariogenic.

The phosphoric ester salts can also be added to foods and beverages are added either as a solid or in solution during their manufacture or preparation. The calcium salt of sucrose-phosphoric acid ester is readily soluble in water.

The invention is illustrated in the following examples:

example 1

Sugar: Sugar crystals are mixed with calcium sucrose phosphorus

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acid ester coated. A product is obtained with a content of 1 wt.% Calciumsaccharosephosphorsäureester. The desired goal can be achieved in various ways, for example:

1. By spraying a solution of calcium sucrose ester in water onto a rotating dryer present sugar crystals.

2. By spraying on an aqueous solution of calcium hydroxide phosphoric acid ester on the crystals before they are removed from the centrifuge during sugar production.

3. By mixing dry sugar and dry calcium sucrose phosphoric acid ester in the presence of finely divided spray water.

Example 2

Flour: In a device for mixing dry substances is mixed 1% by weight powdered Calciumsaccharosephosphorsäureester with flour..

Example 3

Cereal products: A breakfast product made from so-called corn flakes is sprayed with a solution of calcium sucrose phosphoric acid ester in water. The flakes are then dried to produce a finished product with a content of 1 %

To obtain calcium sucrose phosphoric acid ester.

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Example 4

Bread. 2% by weight Calciumsaccharosephosphorsäureester are added to the flour during the mixing of ingredients for bread production.

Example 5

Cake mix. 1 wt% Calciumsaccharosephosphorsäureester is added to the dry materials for the cake mix.

Example 6

Liquid sugar: A liquid sugar is made, consisting of

Sucrose 65 wt. $

Calcium sucrose phosphoric acid ester 0.5 wt Water 34.5% by weight

Example 7

Confectionery production: In the production of a candy mix, 2% by weight calcium sucrose phosphoric acid ester is added to the sugar added.

Example 8

Biscuit: In the preparation of a biscuit mix the other dry ingredients are Gaiciumsaccharosephosphorsäureester $ 2 wt added during mixing..

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Example 9

Beverages:. Is dissolved from liquid sugar, in which 1 wt% Calciumsaccharosephosphorsäureester, a drink is prepared.

Example 10

Tablets: It is prepared as sugar, flavoring agents and binders, a tablet with a content of 10 wt% Calciumsaccharosephosphorsäureester and other substances..

The invention is only intended to be illustrated by the above examples. There are numerous others as well Combinations possible.

The invention relates in particular to the use of the phosphoric acid ester salts in the production or preparation of foods containing carbohydrates, such as bread, bread ingredients, Cakes, potatoes and the like.

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Claims (1)

Patent Attorneys 51 Aadwn, 15, Färs- 1974 DIPL-ING. BRUNO SCHMETZ Augustastraße 14-16 Tel. [0241) 508051 DIPL-ING. WERNER KÖNIG THE COLOMIAL SUGAR EEFIMING COMPANY LIMITED in Sydney, Mew South Wales, (Australia) File number P 17 92 769.4-41 New, patent claims: 1 · Use of the calcium or magnesium salts of esters of phosphoric acid with sucrose for the production or preparation of food and beverages to exert a cariostatic effect in the oral cavity. 2ο Use according to claim 1, characterized in that the proportion of the salts used is 0.1 to 6 wt .- ^ of the products. 509825V0363