CZ33739U1 - Tablet coating material using natural polymer - Google Patents

Description

Tablet coating composition using a natural polymer

Field of technology

The technical solution relates to the field of coating tablets with natural substances, in particular polymers which, together with plasticizers and pigments, form soft films with a viscosity suitable for application, and can be advantageously used for coating tablets in pharmacy or for coating tablets of food supplements.

Prior art

Tablet coatings are often used to increase the stability of the active ingredients, i.e. as protection against oxygen, humidity or light, protection of the drug or preparation against stomach acids, better swallowing or delayed release of the substance. The aesthetic function of the films used is also important, including the color of the tablet, the possibility of embossing the name of the tablet or increasing the gloss.

Last but not least, it is about ensuring a better shape and taste of tablets that make it easier to swallow.

At present, there is also pressure to coat food supplements, but this may lead to changed requirements for the coatings used compared to pharmaceutical tablets, such as resistance to increased fineness or friability of the internal contents of the tablets. Due to the use of the coating in food supplements, the natural origin of these coatings is preferred.

An important type of tablet coating is a coating that dissolves quickly to allow rapid release of the active ingredient. For this purpose, sugar-coated tablets have previously been used, but this can only be used with tablets, and due to the time-consuming, need for trained personnel or problems with production automation, this coating method is usually already used to a small extent.

At present, film-forming polymers, such as cellulose ethers or acrylic polymers or copolymers, which are often applied in admixture with colorants and plasticizers, are a popular immediate-release coating material. The most commonly used polymer is hydroxypropylmethyl cellulose, which is synthesized from an alkaline solution of cellulose, polypropylene oxide and methyl chloride. However, the latter substance is extremely flammable, with chronic toxicity showing a negative effect on the liver, kidneys, spleen, nervous system. Its harmful effect on the environment for damaging the upper atmosphere is also significant. A similar synthesis using CH 3 Cl is also used for other used cellulose derivatives, such as hydroxypropylcellulose, hydroxyethylcellulose, methylcellulose or ethylcellulose.

Other types of polymers include polyvinylpyrrolidone, which is made from N-vinylpyrrolidone monomers. However, toxic effects after single exposure in the form of eye and gastrointestinal irritation and repeated exposure carcinogenicity have also been reported.

Another polymer often used in tablets or dietary supplements is polyvinyl alcohol (PVA), which is synthesized from vinyl acetate (VA). Although PVA has been approved by the European Food Safety Authority (EFSA) as safe for use in coating compositions, irritant effects on acute and chronic inhalation exposure have been reported for the starting monomer VA.

Due to the adverse effects of intermediates, the aim is to limit the use of these substances in production processes and thus to use materials that come from natural sources to coat tablets and food supplements.

Water-insoluble β-D-glucans may be a suitable natural alternative for tablet coating. whose advantage is, in addition to suitable film-forming properties in tablets, also the biological activity of their compounds with (1 -> 3) binding, which show significant immunomodulatory properties, beneficial effects in the treatment of cancer or a significant decrease in serum cholesterol by 7.5%.

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The immunomodulatory properties of β- (1 -> 3), (1 ^ 6) -D-glucans have also been used in the formation of a polysaccharide film useful as a healing and covering agent in the treatment of wounds and burns, as described, for example, in patent CZ 303500 B6. Β-Glucan derivatives, β-glucan-mannans and their preparation are addressed by the patent DE 69630455 T2, which proposes the potential use of the substance in coating. WO 2006024949 A2 discloses the use of β-glucan acetate as a possible component of a controlled release coating.

As part of the coating liquid, a neutral glucan of a natural poly saccharide, in particular pullulan, is disclosed in JP Patent No. JPS 60104011, which discloses coating liquids composed of a combination of pullulan and a water-dispersed coating agent containing a copolymer of methacrylic acid and acrylic acid, wherein the pullulan content is 10 up to 30% of coating liquid. In addition to the use / glucan as part of tablet coatings, solutions using other types of glucans are also known, such as PCT / EP99 / 02386, which describe so-called retarded tablets which contain a wholly or partially water-insoluble linear polysaccharide as retarding material. preferably a poly- (1,4-D-glucan) polysaccharide in the form of microparticles, wherein the tablet is adapted for controlled release of the active ingredient.

The essence of the technical solution

The aim of this technical solution is to present a composition for the use of a natural substance for coating tablets, i.e. / glugaments mixed with a plasticizer, with which, when applied in aqueous solution, it forms a soft film, preferably usable in coatings.

Tablet coating using a natural, soft-film-forming polymer, consisting of glucose obtained from the cell walls of baker's yeast (Saccharomyces cerevisiae) with an announced purity of at least 72%, containing 53 to 80% by dry weight of the coating, triethyl citrate in a content of 13 to 20% expressed on the dry weight of the coating, natural or synthetic dyes such as titanium dioxide or iron oxides, riboflavin or beet extract according to the specific color requirement of the coating in a content of 13 to 20% expressed on the dry weight of the coating.

The coating is applied to the tablets as a hot aqueous suspension, where 50 to 100 g of β-glucan are weighed to prepare 1 kg of a colorless coating mixture and the mixture is thoroughly homogenized. Subsequently, 10 to 20 g of triethyl citrate are added. The mixture is used hot to coat a film with a 2% weight gain of the total tablet weight. The coating conditions are given in Table 1.

Table 1: Coating conditions of β-glucan coated tablets

Equipment Pharming Labcoat Inlet air temperature 60 ° C Outlet air temperature 40 ° C Injection speed 10 g / min Nozzle diameter 1 mm

The advantage of tablet coating using a natural soft film-forming polymer, according to this technical solution, is the viscosity of the resulting film suitable for application, and especially the fast solubility, which can be used in drugs or dietary supplements with the necessary rapid onset of action. The soft film shows a tablet weight gain of 1 to 2%.

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Explanation of drawings

Giant. 1: Images from a DigiMicro Lab 5.0 microscope camera showing an uncoated and coated tablet using a transparent β-glucan coating. The uncoated tablet is shown on the left and the tablet coated with a transparent β-glucan film on the right.

Giant. 2: Images from a DigiMicro Lab 5.0 microscope camera showing an uncoated tablet and a tablet coated with a yellow β-glucan coating. The uncoated tablet is shown on the left and the yellow film-coated tablet with riboflavin and β-glucan on the right.

Giant. 3: Images from a DigiMicro Lab 5.0 microscope camera showing an uncoated tablet and a tablet coated with a red β-glucan coating. The uncoated tablet is shown on the left and the red film-coated tablet of beet extract and β-glucan on the right is shown.

Examples of technical solution

Example 1 - transparent film for coating tablets

To coat 1 kg of tablets, a total of 2 kg of coating suspension containing 160 g of β-glucan was prepared and added to 1800 g of boiling water. The mixture was thoroughly mixed, and 40 g of triethyl citrate was then added to the resulting coating suspension as a plasticizer. The well-mixed suspension was still used for coating while hot. A film with a 2% weight gain was formed in the coating machine after 45 minutes at a suspension application rate of 12.5 to 15.0 ml min ¹ , an inlet air temperature of 60 ° C, an outlet air temperature of 40 ° C and a spray air pressure of 250 kPa.

Tab. 2 Composition of the transparent coating material

Substance Function Weight content (%) β-glucan film-forming substance 8 triethyl citrate plasticizer 2 water solvent 90

Example 2 - Yellow film for coating tablets with riboflavin

To coat 1 kg of tablets, a total of 2 kg of coating suspension containing 160 g of β-glucan was prepared and added to 1800 g of boiling water. The mixture was thoroughly mixed, and 40 g of triethyl citrate and 4 g of riboflavin (E 101) were then added to the resulting coating suspension as a plasticizer. The well-mixed suspension was still used for coating while hot. A film with a 2% weight gain was formed in the coating machine after 45 minutes at a suspension application rate of 12.5 to 15.0 ml min ¹ , an inlet air temperature of 60 ° C, an outlet air temperature of 40 ° C and a spray air pressure of 250 kPa.

Tab. 3 Composition of the yellow coating material

Substance Function Weight content (%) β-glucan film-forming substance 8 triethyl citrate plasticizer 2 riboflavin, E 101 dye 0.2 water solvent 89.8

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Example 3 - red film for coating beetroot extract tablets

To coat 1 kg of tablets, a total of 2 kg of coating suspension containing 160 g of β-glucan was prepared and added to 1800 g of boiling water. The mixture was mixed thoroughly with a mixer. To the resulting coating suspension was then added 40 g of triethyl citrate (TEC) and 4 g of beet extract (E 162) as plasticizer. The well-mixed suspension was still used for coating while hot. A film with a 2% weight gain was formed in the coating machine after 45 minutes at a suspension application rate of 12.5 to 15.0 ml min ¹ , an inlet air temperature of 60 ° C, an outlet air temperature of 40 ° C and a spray air pressure of 250 kPa.

Tab. 4 Composition of the red coating material

Substance Function Weight content (%) β-glucan film substance 8 triethyl citrate plasticizer 2 beet extract, E 162 dye 0.2 water solvent 89.8

Industrial applicability

The compound of natural origin can be used together with the proposed natural plasticizers to coat tablets to obtain films of different colors and rapid solubility in the oral cavity for rapid release of the active substance. Due to the natural origin of all components used, it is also very advantageous to use these films when coating food supplements.

Claims (4)

CLAIMS FOR PROTECTION A coating composition of medicaments or dietary supplements tablets comprising a natural insoluble polymer, characterized in that it consists of natural / Aghikan mixed with a plasticizer dissolved in an aqueous solution to improve the properties of the coating medium, and a colorant to improve the appearance of the tablet coating. consists of β-D-glucose units obtained from the cell walls of baker's yeast Saccharomyces cerevisiae with a stated purity of at least 70%, a plasticizer to form a finer and more pliable film of triethyl citrate, and a colorant to improve the appearance of the tablet coating are metal oxides, vitamins or natural extracts. Coating composition of drug or food supplement tablets according to Claim 1, characterized in that the water-insoluble / Aglucan extracted from the cell walls of the baker's yeast Saccharomyces cerevisiae is present in the coating composition of the tablet in an amount of 5 to 10% by weight. Coating composition of tablets or food supplements according to Claims 1 and 2, characterized in that the triethyl citrate is present in the coating composition of the tablet in an amount of 1 to 2% by weight. Coating composition of tablets or dietary supplements according to Claims 1 to 3, characterized in that the metal oxides are titanium dioxide or iron oxides, and the tablet coating composition contains 1 to 2% by weight of vitamins or extracts from natural The substances are riboflavin or beet extract, and the tablet coating composition contains 0.2% by weight.