BG730Y1 - Effervescent medicamentous form - Google Patents

Abstract

The effervescent medicamentous form, in particular the effervescent tablets (candy type) provoke saliva secretion and ensure a controllable continuous and full-value contact of the actively effective substances with the mucous membrane of the oral cavity and the upper respiratory tracts. The tablet comprises, in wt.%: active effective substances of natural origin from 0.010 to 0.500 and optionally vitamins from 0.000001 to 0.400 and/or minerals from 0.000001 to 0.400; pharmaceutically acceptable organic acid from 0.090 to 0.300; alkaline carbonate and/or alkaline hydrogen carbonate and/or alkali glycine carbonate from 0.100 to 0.300; binder - glucidex from 0.100 to 0.500; diluent - mannitol from 0.100 to 0.350 and/or lactose from 0.050 to 0.450; and auxiliary substances from 0.020 to 1.500. The actively effective means of natural origin can be vegetative extract of Matricaria Chamomilla, Echinaceae rosea, Valeriana officinalis, Salvia officinalis, Aloe vera, Tilia grandifolia, Hypericum perforatum; Thymus serpyllum, Calendula officinalis, Plantago lanceolata, Achilea millefolium, Origanum vulgare, Rodiola rosea, Livsea, Artemisia absinthinum, Crataegus monogyna, as well as a mixture of essential oils or a honey-bee product.

Description

Technical field

The utility model relates to an effervescent dosage form, in particular to effervescent suction tablets that provoke salivation and to provide manageable prolonged and complete contact of the active substances with the oral mucosa and upper respiratory tract.

BACKGROUND OF THE INVENTION

Effervescent tablets are dosage forms which are dissolved in cold water with a gas release which is carbon dioxide and is the result of the reaction between an acid and a basic compound, most commonly citric or tartaric acid and carbonate or hydrogen carbonate. The effervescent compositions also contain lubricants such as sodium benzoate, sodium acetate, fumaric acid, polyethylene glycols, alanine, glycine. They may contain fillers: diluents; binders; buffers; sweeteners such as aspartate, saccharin, cyclamate; flavoring agents; dissolution aids and others.

The instability of effervescent formulations is known, which is why attempting to avoid technological difficulties is to use direct tabletting.

WO 20005/07858 discloses a pharmaceutical dosage form for enhancing oral absorption of a drug. The composition of the dosage form includes fentanyl and prochlorperazine as active agents, lactose monohydrate, cellulose, anhydrous sodium carbonate, sodium bicarbonate, anhydrous citric acid, polyvinylpyrrolidone, magnesium stearate, colloidal silica.

A pharmaceutical composition is known comprising an effervescent pair comprising an acid and an alkaline ingredient suitable for dissolution in water and for suction as described in BG 103253. The composition includes an active agent such as piroxicam-cyclodextrin complex or ambroxol or paracetamol or paracetamol / paracetamol or paracetamol / paracetamol or paracetamol nimesulide or ibuprofen or morniflumate or levodopa or carbidopa; alkaline ingredient sodium glycine carbonate; acid component - fumaric or maleic acid or their salts. The composition may contain excipients such as polyethylene glycol 6000, lactose, mannitol, sweeteners, flavoring agents. Upon contact with saliva, the tablets made by this composition disintegrate rapidly and form an aqueous dispersion which is easily swallowed.

The essence of the utility model

An object of the present invention is an effervescent dosage form, in particular an effervescent suction tablet, which has a pharmacological action according to the active ingredient and a strong refreshing effect. The tablet contains in mass parts an active agent of natural origin from 0.010 to 0.500 and, if necessary, vitamins from 0.000001 to 0.400 and / or minerals from 0.000001 to 0.400; pharmaceutically acceptable organic acid from 0.090 to 0.300; alkaline carbonate and / or alkaline hydrogen carbonate and / or alkaline glycine carbonate from 0.100 to 0.300; glucide binder from 0.100 to 0.500; diluents mannitol 0.100 to 0.350 and / or lactose 0.050 to 0.450; and conventional excipients such as lubricating, sweetening, coloring and flavoring agents from 0.020 to 1.500.

The active agent of natural origin according to the invention is a plant extract of Matricaria Chamomilla (chamomile), Echinaceae rosea, Valeriana officinalis (sapling), Salvia officinalis (sage), Aloe vera, Tilia grandifolia, Hypericum perforatum (St. John's wort), St. John's wort Thyme), Calendula officinalis (Calendula), Plantago lanceolata (Thistle), Achilea millefolium (White yarrow), Origanum vulgare (Regan), Rodiola rosea, Livsea, Artemisia absinthinum, Crataegus monogyna (Hawthorn).

The active agent of natural origin according to the utility model may be a mixture of essential oils, for example a mixture of menthol and eucalyptol.

In another embodiment, the active agent of natural origin is a bee product such as propolis extract, royal jelly, honey, bee pollen.

If necessary, the active ingredient contains vitamins as well as minerals. When using a vitamin, the upper limit of its content is up to 0.150 wt. hours, and with a combination of different vitamins their content can be up to 0.400 wt. h. The minerals that may be present in the effervescent form are known pharmaceutically acceptable compounds of zinc, copper, magnesium, iron, manganese, selenium, calcium, phosphorus and the like.

Glucidex is used as a binder, creating adhesion forces between the components of the tablet. It slows down the disintegration of the tablet into the oral cavity upon contact with the saliva, resulting in better absorption of the active agent of natural origin and also of vitamins and minerals when contained in the effervescent form.

The pharmaceutically acceptable organic acids of the invention are citric, tartaric, fumaric and malic acids.

Preferred alkaline carbonate compounds are sodium carbonate, sodium bicarbonate and sodium glycine carbonate. They may be contained in the effervescent form individually or in combination, depending on the purpose of the application and the nature of the active ingredient.

The effervescent tablet is prepared according to conventional technology for the preparation of effervescent compositions comprising sieving, homogenizing and sequentially mixing the active ingredients and diluents, the acidic and basic components, followed by the remaining fillers, and finally direct tableting is performed.

The quantitative ratios between the components vary depending on the effervescent effect sought in relation to the absorption of the active substance.

The breakdown of the tablets is from 2 to 5 minutes.

The effervescent form, according to the utility model, provokes salivation and provides manageable prolonged contact of the active substances contained in the products of natural origin with the oral mucosa and upper respiratory tract. This leads to greater absorption of the active substances through the circulatory system. The effervescent form provides an opportunity for refreshing the breath and has a refreshing effect by the effect of the flavor and olfactory analyzer, as well as the aromatherapy effect by the introduction of appropriate substances.

Examples of implementation of the utility model

Exemplary embodiments illustrate the utility model without limiting it. The quantitative ratios between the components are in mass parts.

Example 1.

Matricaria Chamomilla Extract -0,050; mycidex - 0,200; mannitol - 0,100; sodium bicarbonate - 0.260; tartaric acid-0,130; lactose 0.150; polyethylene glycol 6000 (PEG 6000) - 0.020; aspartame-0.025.

The method of producing the tablets involves sieving, homogenizing and sequentially mixing the active ingredient and the diluents, then the acidic and basic components and other fillers are added, followed by direct tableting.

The effervescent tablet has a pronounced refreshing and toning effect, as well as analgesic, antimicrobial, antiseptic, anti-inflammatory action in diseases of the digestive system and respiratory tract, as well as a softening and healing effect.

Example 2.

Echinaceae rosea extract - 0,200; mannitol - 0,200; pgcidex - 0.400; sodium glycine carbonate-0.180; citric acid-0,125; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent-0.003;

The tablets were prepared as in Example 1.

The pills have a refreshing and tonic effect, which has a stimulating effect on the immune system.

Example 3.

Echinaceae rosea -0,200 extract; selenium 0,00003; mannitol - 0,200; Glucidex -0.400; sodium glycine carbonate-0.180; citric acid - 0.125; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0,003;

The tablets were prepared as in Example 1.

The pills have a refreshing and invigorating effect, stimulating the immune system. Selenium has an immunostimulating effect, slowing down the aging process. It is an antioxidant (as a component of glutathione peroxidase).

Example 4.

Valeriana officinalis extract - 0.020; Glucidex - 0.500; sodium glycine carbonate - 0.280; fumaric acid - 0.200; PEG 6000 - 0.010; lactose 0.100; sodium cyclamate - 0.001; tangerine oil - 0.020.

The tablets have a pronounced antispasmodic and soothing effect, lower blood pressure.

Example 5.

Salvia officinalis extract - 0.100; mannitol

- 0.200; Glucidex - 0.400; sodium glycine carbonate 0.180; citric acid - 0.120; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have a pronounced coughing effect, have anti-inflammatory and antibacterial action. They are used in acute and chronic diseases of the digestive system, in diseases of the biliary tract and liver, in stones and sand in the kidneys and bladder.

Example 6

Aloe vera extract - 0.100; mannitol - 0.200; Glucidex - 0.400; sodium glycine carbonate - 0.180; fumaric acid - 0.140; PEG 6000 - 0.010; peppermint oil - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have a stimulating effect, strengthen the immune system, have a slight laxative effect.

Example 7.

Aloe vera extract - 0.100; vitamin A 0.0001; zinc - 0.005; mannitol - 0.200; glycidex 0.400; sodium glycine carbonate - 0.180; fumaric acid - 0.140; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have a stimulating effect, strengthen the immune system, have a slight laxative effect. Zinc helps regenerate the optic nerve, strengthen the cornea and the retina of the eye.

Example 8.

Tilia grandifolia extract - 0.200; mannitol 0.200; Glucidex - 0.400; sodium glycine carbonate 0.180; fumaric acid - 0.140; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have antimicrobial, antispastic and diaphoretic action, are used in acute upper respiratory tract and colds, have a calming effect.

Example 9.

Hypericum perforatum extract - 0.200; manigol - 0.200; Glucidex - 0.400; sodium glycine carbonate -0.180; fumaric acid - 0.140; PEG 6000

- 0.010; lemon essence - 0.030; coloring agent

-0.003.

The tablets were prepared as in Example 1.

The tablets have a regenerative, antispasmodic, capillary and antimicrobial effect, as well as anti-inflammatory action of the gastrointestinal tract. Improve and tone the heart, act antidepressant.

Example 10.

Thimus serpyllum extract 0.200; mannitol - 0.200; Glucidex - 0.400; sodium glycine carbonate 0.180; citric acid - 0.120; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have a highly refreshing effect due to the high content of essential oil. They have a cough, antibacterial, anti-inflammatory, antispasmodic and gas-burning effect. Soothe with a dry and supple cough.

Example 11.

Plantago lanceolata extract - 0.200; mannitol - 0.200; Glucidex - 0.400; sodium glycine carbonate - 0.180; fumaric acid - 0.140; PEG 6000 0.010; flavoring agent - 0.030; coloring agent 0.003.

The tablets were prepared as in Example 1.

The tablets have antiviral, anti-inflammatory, hemostatic and nourishing effects. They are used for gastrointestinal catarrh, stomach ulcer, inflammation of the respiratory tract.

Example 12.

Achilea millefolium extract - 0.200; mannitol - 0.200; Glucidex - 0.400; sodium glycine carbonate - 0.180; citric acid - 0.120; PEG 6000 0.010; flavoring agent 0.030; coloring agent 0.003.

The tablets were prepared as in Example 1.

The tablets have an anti-inflammatory effect on gastrointestinal diseases and inflammation of the kidneys, as well as a bile and haemostatic action; excite appetite.

Example 13.

Propolis extract - 0.200; mannitol - 0.200; Glucidex - 0.400; sodium glycine carbonate -0.180; fumaric acid - 0.140; PEG 6000 - 0.010; flavoring agent -0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets have a strong antiseptic and anti-inflammatory effect.

Example 14.

Calendula officinalis extract - 0.200; m4 nigol - 0.200; Glucidex - 0.400; sodium glycine carbonate 0.180; citric acid - 0.140; PEG 6000 0.010; flavoring agent - 0.030; coloring agent 0.003.

The tablets were prepared as in Example 1.

The tablets have a pronounced antimicrobial and anti-inflammatory effect; have a sedative effect on the central nervous system, enhance heart function, are used to treat stomatitis and periodontal disease. 10

Example 15.

Origanum vulgare extract - 0.050; Glucidex - 0.200; mannitol - 0.100; sodium bicarbonate - 0.260; tartaric acid - 0.130; lactose -0.150; PEG 6000 - 0.020; aspartame - 0.025. 15

The tablets were prepared as in Example 1.

The pills have antiseptic and nerve-stimulating effects, aid expectoration and soothe coughs, eliminate cramps in stomach and intestinal pain, improve digestion and increase appetite.

Example 16.

Extract from: Matricaria Chamomilla; vitamin C - 0.100; mannitol - 0.280; shutsidex - 0.300; sodium carbonate - 0.110; citric acid - 0.140; PEG 25 6000 - 0.020; dry flavoring agent - 0.030; coloring agent- 0.003; sodium cyclamate - 0.005; polyvidone - 0.010; ppocosa 0.085;

The tablets were prepared as in Example 1.

The effervescent tablet has a pronounced refreshing and invigorating effect, as well as analgesic, antimicrobial, antiseptic, anti-inflammatory action in diseases of the digestive system and respiratory tract, as well as a softening and healing effect.

Example 17.

Menthol - 0.090; eucalyptol - 0.010; Schutside 0.450; mannitol - 0.300; chicoryl sodium carbonate 0.200; malic acid -0.160; PEG 6000 - 0.030; orange oil 0.020.

The tablets were prepared as in Example 1.

The tablets have a pronounced refreshing and toning effect and anti-influenza and analgesic effect, dilate the blood vessels of the nasopharynx, which leads to improved breathing, have a revulsive effect.

Example 18

Rodiola rosea extract - 0.100; mannitol 0.200; Glucidex - 0.400; sodium glycine carbonate 0.180; fumaric acid - 0.140; PEG 6000 - 0.010; lemon oil -0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1. The tablets strengthen the immune system. Example 19.

Livsea extract - 0.100; mannitol - 0.200 glycidex - 0.400; sodium glycine carbonate - 0.180; fumaric acid - 0.140; PEG 6000 - 0.010; rosemary oil - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The pills strengthen the immune system. Example 20.

Crataegus monogyna-0.150 extract; MgO - 0.050; mannitol - 0.200; glycidex - 0.350; sodium glycine carbonate-0.190; fumaric acid-0.140; PEG 6000 - 0.010; flavoring agent - 0.030; coloring agent - 0.003.

The tablets were prepared as in Example 1.

The tablets are used in diseases of the cardiovascular system, improve the circulation of the heart and brain. The presence of Mg in the active component helps to regulate the heart rate.

Example 21.

Stability studies of effervescent tablets obtained according to Example 1 were conducted under different relative humidity conditions for 6 days.

Relative humidity (%) Initial value (0%) 25 35 55 75

Moisture (%) 2 ^ 2 £ 3.8 4.3 5.8

The estimation of the adsorbed moisture is determined by Karl Fischer.

Claims (4)

Claims An effervescent dosage form comprising an active agent, an acid-base pair, a binder, diluents mannitol and / or lactose and excipients, characterized in that the active agent includes a product of natural origin and, if necessary, vitamins and / or minerals, the binder is glycidex and the components are in the following quantitative proportions by weight: active ingredient of naturally occurring vitamins from 0.010 to 0.500 from 0.000001 to 0.400 minerals pharmaceutically acceptable organic acid alkaline carbonate and / or hydrogen carbonate and / or glycine carbonate glycidex mannitol from0.000001 to 0.400 from0.090 to 0.300 from 0.100 to 0.300 from 0.100 to 0.500 from 0.100 to 0.350 lactose from 0.050 to 0.450 excipients from 0.020 to 1.500 An effervescent form according to claim 1, characterized in that the active agent of natural origin is a plant extract of: Matricaria Chamomilla, Echinaceae rosea, Valeriana officinalis, Salvia officinalis, Aloe vera, Tilia grandifolia, Hypericum perforatum, Thymusulapypyllic, Thymisendpyllic, , Plantago lanceolata, Achilea millefolium, Origanum vulgare, Rhodiola rosea, Livsea or Artemisia absinthinum, Crataegus mono gyna. An effervescent form according to claim 1, characterized in that the active agent of natural origin is a menthol-eucalyptus mixture. 4. The effervescent form of claim 1, wherein the active agent of natural origin is a bee product.