Compressed form (options) and the means of improving its compressibility (options)

 

(57) Abstract:

The invention relates to the production of compressed forms in the food and pharmaceutical industries. Compressed form contains sweetener 1-O--D-glyukopiranozil-D-sorbitol (1,1-GPS), or a mixture of sweeteners from 6-O--D-glyukopiranozil-D-sorbitol (1,6-GPS), 1-O--D-glyukopiranozil-D-sorbitol (1,1-GPS) and 1-O--D-glyukopiranozil-D-mannitol (1,1-GPM). 1,1-GPS, or a mixture of sweeteners from 1,6-GPS, 1,1-GPS and 1,1-GPM is used in compressed form as a means of improving their compressibility. Compressed form, obtained by use of the above substances have increased sweetness, solubility and compressibility. 4 C. and 8 C.p. f-crystals, 1 Il.

The invention relates to compressed forms, which contain a mixture of sweeteners, including 1-O-a-D-glyukopiranozil-D-sorbitol. In particular, the invention relates to compressed forms, which contain a mixture of sweeteners from 6-O--D glyukopiranozil-D-sorbitol, 1-O--D-glyukopiranozil-D-sorbitol and 1-O--D-glyukopiranozil-D-mannitol, as well as the application of this mixture sweeteners in compressed forms.

Compressed forms are susteadmetton this, compressed forms contain, in General, a carrier or diluent, binder, lubricant or imparting lubricity (tablets) substance, as well as biologically active substances, such as flavorings, medicines or sweeteners. As carriers, respectively, diluents commonly used sucrose, lactose, glucose, starch or mannitol. The use of these media, respectively, diluents has the disadvantage that it is also necessary to use a binder to provide sufficient compressibility.

In the European patent EP-61-0 028 905 describes the use of tablets isomaltulose as a diluent. However, isomaltulose has only a relatively slight sweetness.

In the application for the European patent EP-a-O 625 578 describes sweetener of 6-O--D glyukopiranozil-D-sorbitol, 1-O--D-glyukopiranozil-D-sorbitol and 6-O--D-glyukopiranozil-D-mannitol, as well as strawberry jam, caramel and ice cream that contain this sweetener, Dorr and Willibald-Ettle in Pharm. Ind., 58 (10), 947-952 (1996) describe compressed form, which contain sorbitol, xylitol, lactic or IsomaltR. Described therein compressed form hem., 2372-2383 (1981) describe the crystal structure analysis of isomaltitol.

The objective of the invention is to obtain compressed forms that are devoid of the above disadvantages and have, in particular, increased sweetness, solubility and compressibility.

The solution to this technical problem is achieved by the preparation of compressed form, characterized in the main claim, containing 1-O--D-glyukopiranozil-D-sorbitol (hereinafter briefly referred to as 1,1-GPS), in particular, compressed forms, which contain a mixture of sweeteners from 6-O--D-glyukopiranozil-D-sorbitol (hereinafter briefly referred to as 1,6-GPS), 1-O--D glyukopiranozil-D-sorbitol and 1-O--D-glyukopiranozil-D-mannitol (hereinafter briefly referred to as 1,1-GPM). Proposed according to the invention compressed form, due to their content of 1,1-GPS, in particular, due to their content of a mixture of sweeteners from 1,6-GPS, 1,1-GPS and 1,1-GPM, have increased solubility and sweetness compared to containing sales IsomaltR(equimolar mixture of 1,6-GPS and 1,1-GPM, gidrirovanny isomaltulose) compressed forms. Proposed according to the invention compressed form region is STV and they have improved compressibility, that is, to achieve a certain hardness requires a relatively lower pressure. Further, associated with improved compressibility advantages according to the invention the compressed forms are in their extreme hardness, which is achieved through a relatively slight pressure of the main pressing.

Further preferred embodiments of the invention follow from the dependent claims.

According to a preferred variant implementation, the invention relates to compressed forms, which contain a mixture of sweeteners from 10-50 wt.% 1,6-GPS, 2-20 wt.% 1,1-GPS and 30-70 wt.% 1,1-GPM, based on the weight of the mixture sweeteners. In the following, a particularly preferred variant implementation, the invention relates to compressed forms, which contain a mixture of sweeteners from 5-10 wt.% 1,6-GPS, 30-40 wt.% 1,1-GPS and 45-60 wt.% 1,1-GPM, based on the weight of the mixture sweeteners. Last mentioned mixture of sweeteners, because of high content of 1,1-GPS and a low content of 1,1-GPM, gives compressed forms even more enhanced sweetness and Ruritania, compressed forms include 50-99 wt.%, in the calculation of the mass of compressed form, 1,1-GPS, or a mixture of sweeteners. Compressed form may additionally contain monosaccharides, disaccharides, monosacharides, disaccharidases, starch, derivatives of starch, cellulose, derivatives of cellulose, or inulin. Compressed form can also contain in particular sorbitol, mannitol, hydrogenated or digidrirovannye oligosaccharides, xylitol or sugar, such as sucrose, glucose or xylose. However, these substances are preferably contained in amounts of less than 30 wt.%, preferably less than 5 wt.%, in the calculation of the mass compressed form. According to a particularly preferred variant implementation, however, the proposed invention in compressed form does not contain sugar and therefore calories are lowered and they are suitable for diabetics.

According to a particularly preferred variant of the invention, compressed form additionally contain intensely sweet substances, as Acesulfame-K, aspartame, cyclamate, glycyrrhizin, thaumatin, saccharin or other similar substances. Proposed according to the invention compressed form, chrome is or peppermint. Proposed according to the invention compressed form can also contain acceptable edible acid, ascorbic acid or citric acid, as well as substances which impart lubricity compressed forms, fatty acids or their salts, such as magnesium stearate or sodium stearate. Finally, proposed according to the invention compressed forms can contain dyes and/or porophore as bicarbonate or carboxymethylcellulose.

In a particularly preferred embodiment provides for compressed forms that can make the oral cavity and pharynx pharmaceutically active substances and release them there. According to the present invention, under the pharmaceutically active substances need to understand the substances that have the desired prophylactic or therapeutic effect on the human or animal. These substances, therefore, are, in particular, for the prevention or treatment of conditions failure or disease. According to the invention, in the compressed form can include, for example, enzymes, coenzymes, mineral substances, vitamins, antibiotics, microbicide or fungicide act is citiesi active substances. Pharmaceutically active substance should be provided in such quantity that they caused the desired pharmaceutical effect. Processing compressed form under mild conditions, as well as their special behavior when dissolved make offer according to the invention compressed form especially suitable for introduction into the oral cavity and pharynx pharmaceutically active substances. Containing IsomaltRand sugar containing compressed form dissolve relatively worse, so the release of biologically active substances occurs only with delay. The release of biologically active substances from proposed according to the invention compressed form comes quickly and favorably continues constantly.

According to the following alternative implementation, the invention relates to compressed forms in tablets for sucking or chewing tablets.

Finally, the invention relates to the use of 1,1-GPS, respectively, mixtures of sweeteners from 1,6-GPS, 1,1-GPM and 1,1-HAP powder mixture, respectively, cooked it in compressed form to improve its compressibility.

In the following examples and sonatica dissolution proposed according to the invention compressed forms and conventional tablets.

Example 1

Preparation of tablets for sucking (chewing tablets)

The recipe:

The mixture sweetening matter, containing 2 wt.% - 1,1-GPS, 37 wt.% 1,6-GPS and 53 wt.% 1,1-GPM, based on the weight of the mixture sweetening matter - 19,54 kg

Acesulfame-K - 30 grams

Aspartame - 30 grams

Aromatic substance peppermint - 200 grams

Menthol - 100 g

Magnesium stearate - 100 g

Preparation of

The components are mixed and compressed in a rotary press Fette R 1200 in the following conditions: pressing force ranges from 20 to 70 kN.

To obtain tablets for sucking preferably use a mixture with a higher content of 1,6-GPS, and chews using a mixture with a higher content of 1,1-GPM. In both cases does not require auxiliary substances.

Get uniformly compacted, solid and soluble compressed form.

Example 2

The kinetics of dissolution of compressed forms

To compare the behavior when dissolved compressed forms, which contain, according to the invention, 1,1-GPS, and, compared with them, IsomaltRand sucrose, remove the kinetics of dissolution of different compressed forms. Include the> 200 g of flavouring substances peppermint, 100 g of menthol, 100 g of magnesium stearate, 30 g of Acesulfame-K, 30 g of aspartame.

Including sucrose compressed form also does not contain 1,1-GPS and have the following composition: 19,6 kg of sucrose, 200 g of eucalyptus menthol, 100 g of menthol, 100 g of magnesium stearate.

Compressed form according to the invention containing 1,1-GPS, prepared by the method of example 1.

Behavior when dissolved determine the solution, according to the Law on foodstuffs and consumer goods, paragraph 35, at a temperature of 37oC. the Amount of solvent and compressed form is chosen so that when the complete dissolution of the compressed forms was 10% solution. Depending on the time determine the increase in the density of the solution and from it determine the concentration in grams of dry matter per 100 g of the solution (S; see drawing).

From the drawing it is seen that containing 1,1-GPS compressed forms are more soluble compared to compressed forms that contain IsomaltR. Also compared to the compressed forms containing sugar is altered kinetics of dissolution, i.e. soderzhatrazlichnye according to the invention compressed form so favorably complement existing media for example, for administering drugs.

Example 3

Experiments on the compressibility

In order to compare the proposed according to the invention of compressed form with compressed forms of IsomaltRand sucrose in the ratio necessary to obtain pressure and attainable hardness, perform the following experiments on the compressibility:

The proposed composition according to the invention compressed form corresponds to the formula of example 1.

As a comparative compressed forms using a mixture of IsomaltoRand sucrose, as described in example 2 composition.

Experiments on the compressibility is carried out using a rotary press Fette R 1200, and the punch was round and faceted. The punch diameter is 20 mm Rotary press equipped with krugloozernaya disks.

For pressing IsomaltRshould the pressure forpressure 24,3 kN and the pressure of the main pressing of 65.4 kN, and receive compressed form with a hardness 76 N. For pressing sucrose necessary pressure forpressure 24,0 kN and the pressure of the main pressing 65,0 kN, and receive compressed form with hardness 128 N. In protivoprotosana to 28.3 kN and the pressure of the main pressing of 49.4 kN moreover, the obtained compressed forms have hardness 204 N. Therefore, proposed according to the invention the compressed form can be obtained by using a reduced pressure principal pressing, and favorable way the result is a more solid compressed form than known from the prior art.

1. Compressed form, containing the sweetener 1,1-GPS (1-O--D-glyukopiranozil-D-sorbitol).

2. Compressed form, containing a mixture of sweeteners from 1,6-GPS (6-O--D-glyukopiranozil-D-sorbitol), 1,1-GPS (1-O--D-glyukopiranozil-D-sorbitol) and 1,1-GPM (1-O--D-glyukopiranozil-D-mannitol).

3. Compressed form under item 2, characterized in that the mixture of sweeteners contains 10-50 wt. % 1,6-GPS, 2-20 wt. % 1,1-GPS and 30-70 wt. % 1,1-GPM calculated on the weight of the mixture sweeteners.

4. Compressed form under item 2, characterized in that the mixture of sweeteners contains 5-10 wt. % 1,6-GPS, 30-40 wt. % 1,1-GPS and 45-60 wt. % 1,1-GPM calculated on the weight of the mixture sweeteners.

5. Compressed form according to any one of paragraphs. 1-4, characterized in that the compressed form contains 50-99 wt. % based on the weight of the compressed form, 1,1-GPS, or see premirovany form further comprises monosaccharides, disaccharides, monosacharides, disaccharidases, starch, derivatives of starch, cellulose, derivatives of cellulose, or inulin.

7. Compressed form according to any one of paragraphs. 1-6, characterized in that the compressed form further comprises intensely sweet substance, in particular, Acesulfame-K, thaumatin, glycyrrhizin, saccharin or cyclamate.

8. Compressed form according to any one of paragraphs. 1-7, characterized in that the compressed form further comprises a flavouring compounds, particularly aromatic substance fruits or peppermint, dyes or porophore as bicarbonate or carboxymethylcellulose.

9. Compressed form according to any one of paragraphs. 1-8, characterized in that the compressed form further comprises a pharmaceutically active substance, in particular an enzyme, a coenzyme, an antibiotic, microbicide or fungicide active ingredient, nicotine, caffeine, menthol or eucalyptus.

10. Compressed form according to any one of paragraphs. 1-9, characterized in that the compressed form is in the form of a compressed form for sucking or chewing the tablets.

11. The use of 1,1-GPS (1-O--D-glyukopiranozil-D-sorbitol) in the powder mixture is.

12. The use of mixtures of sweeteners from 1,6-GPS (6-O--D-glyukopiranozil-D-sorbitol), 1,1-GPS (1-O--D-glyukopiranozil-D-sorbitol) and 1,1-GPM (1-O--D-glyukopiranozil-D-mannitol) in the powder mixture and respectively received from her compressed form as a means of improving its compressibility.

 

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