LT3670B - Stimulating preparation with nicotine - Google Patents

Abstract

FIELD: medicine; toxicology; narcology. SUBSTANCE: preparation comprises active principle, namely, nicotin or alkaloid dispersed in gel-like pharmaceutically acceptable water-binding agent. EFFECT: higher efficiency. 15 cl, 1 dwg, 2 tbli

Description

The present invention relates to a saliva soluble stimulant preparation containing nicotine.

It is well known that both active and passive smoking of tobacco products such as smoking tobacco, cigars and cigarettes pose serious risks to human health and the social environment.

It is also well known that smoking cessation is a major problem for smokers.

These problems are mainly due to the habit of nicotine. Indeed, constipated smokers have been found to have a strong need for tobacco stimulation, with nicotine levels dropping to about 15 ng / ml.

In addition, it is known that various nicotine-containing, smokeless stimulants (i.e., non-airway) can be used to alleviate a strong tobacco cravings condition, thereby helping the smoker to overcome the harmful habit of smoking with as little discomfort as possible.

Nicotinic stimulants, which have long been known, are used in non-respiratory ways as smokeless tobacco products such as chewing tobacco and snuff and are constantly being improved.

U.S. Pat. 1.376.586 discloses a product consisting of fine-cut or chewing tobacco in the form of tablets or individual chewing gum, the entire surface of which is chewed; this makes it inaccessible to both air and moisture and is very effective in preventing the evaporation of tobacco juice.

U.S. Patent No. 4,545,392 discloses a smokeless tobacco product comprising cut or otherwise crushed tobacco and based on 1-35% by weight of water-insoluble non-saccharide mastic resin, based on dry tobacco; in addition, the composition comprises water-soluble resins, such as, for example, gum arabic, for stabilizing the resin composition. The preparation is in the form of pieces of tobacco, whether or not cut up, and the mastic resin is based on the composition

1 The film covers their surface. Thus, according to the description, the individual pieces of tobacco must remain dispersed in the mouth.

PCT patent application no. No. 81/02090 discloses chewing tobacco product as individual portions in which the chewing tobacco is either coated or dispersed in a fine or semi-solid carrier. Chewing gum blend is preferred when selecting the carrier material. However, it is noted below that starch hyalolysates, such as non-stick products, used in the manufacture of lollipops may be used as carrier material, although this is not illustrated by the corresponding examples. The carrier material may also contain additional substances such as flavor and aroma additives, and dry, water-soluble natural products such as coffee and tea extracts,

Sprays or aerosols with nicotine for oral use are described in DE-OS32 41 437 and GB-PS 15 28 391. However, administration of nicotine by injection or aerosol has only a short-term effect.

The nicotine-containing preparation for nasal administration is known from DE-OS 34 01 763. However, nasal administration is not very pleasant, since the nasal mucosa is more sensitive than the oral mucosa, and in addition, the use of the preparation also has a short-term effect. It follows that nasal administration should be regarded as less appropriate.

DE-OS 34 38 284 proposes applying a nicotine release patch, but with this method, nicotine uptake is very slow and uncontrolled. In addition, the desired sharp increase in nicotine concentration in the subjects' blood and the accompanying physiological state that is consistent with the inclusion of the first cigarette smoke is not achieved by the application of a patch.

U.S. Pat. No. 3,901,248 discloses a preparation based on smoking substitution for chewing and which is presented as a nicotine-containing chewing gum. The formulation comprises from about 15 to about 80% of a resinous substrate and a complex of nicotine with cationic resin dispersed in the substrate. The cationic resin complex contains about 10% chewing gum, so that the same amount of nicotine is released when chewing as is the case with ordinary cigarettes.

U.S. Pat. No. 3,845,217 discloses other optimized preparations based on the replacement of smoking with chewing, which do not exhibit an annoying effect on the palate. These improved formulations comprise from about 15% to about 80% of a resinous substrate, nicotine and at least one physiologically acceptable water-soluble buffer that maintains saliva pH above normal physiological pH, e.g. about 7.4.

Nicotine may be selected from the group consisting of a free nicotine base, a water soluble physiologically acceptable salt thereof, adsorbed on a physiologically acceptable sorbent nicotine, and a nicotine complex with an insoluble cationic substance.

The amount of nicotine, calculated on the free base, is from 1 to 10, preferably from 1 to 3 mg of nicotine per chewing gum.

It is recommended to use a nicotine complex with insoluble cation exchanger to create a controlled, non-rapid release nicotine substance.

In the FR patent application, publ. No. No. 2,608,156 discloses other chewing gum type preparations which are essentially the replacement of smoking with chewing. In these formulations, the nicotine is in the form of particles coated with a layer of water-soluble material, which, according to the authors, enables the control of nicotine release which is not too rapid.

Typically year-old tobacco products containing fine-cut tobacco and substrate materials, such as chewing tobacco, machorka, placed in water-soluble resins (chewing gum) or starch hydrolysates (rubber lozenges) are characterized by the presence of residues after use. tobacco and / or substrates which are difficult or negligible in saliva.

In addition, these byproducts can cause discomfort and may be socially unacceptable, and the high concentration of ingredients from the crushed tobacco needed to produce the nicotine stimulating effect causes stomach aches.

An unwanted sudden release of ingredients such as nicotine and various flavor components can occur through years of smoking tobacco products as these products are chewed. In this case, new surfaces of the product may be exposed and the smoker will receive high concentrations of ingredients, causing undesirable changes in the expected physiological stimulation effects.

Similar uncontrolled release of nicotine is also seen with nicotine chewing gum when chewed.

The primary object of the present invention was to provide a tobacco supplement or substitute tobacco product as a nicotine stimulant for oral administration, the controlled release of nicotine and auxiliary ingredients such as flavor and aroma additives.

It is a specific object of the present invention to provide a saliva-stimulating preparation with nicotine and nicotine stimulation to provide greater or at least adequate stimulation of conventional tobacco products such as cigarettes, cigars, pipe tobacco and the above tobacco substitutes while avoiding tobacco and / or substrate waste. adverse physiological effects and unpleasant tobacco products and their substitutes.

It is also an object of the present invention to provide a salivary-stimulating preparation which can be used orally in a variety of conditions, e.g., with beverages such as coffee, wine, beer, and in such a form that the nicotine dose in this preparation is equivalent to that of a cigarette or outbursts.

According to the invention, controlled release of nicotine and additional ingredients, such as flavor and flavor additives, without smoking can be achieved using a saliva-soluble stimulant containing a gel obtained by using a water-binding agent to obtain the gel; nicotine or other alkaloids with similar activity; additional ingredients such as flavoring and flavoring agents. The preparation has the defined structure profile described below, characterized by certain mechanical properties such as strength, hardness, brittleness, adhesion, cohesiveness, elasticity, as well as a certain concentration of nicotine or said alkaloids.

More broadly, the present invention is directed to a salivary soluble preparation comprising the active ingredient and additional ingredients, such as flavoring and flavoring agents, added to a gel prepared with a water-binding agent wherein the active ingredient is nicotine or another alkaloid having a similar effect; said preparation has the following properties:

I. The following parameter ranges have been derived from the structure profile analysis:

'2

(a) Robustness, i.e. modulus - greater than 100 n (Newton) / cm

b) Hardness, i.e. maximum force exerted at '2 in the first compression period - greater than 5 n / cm;

c) fragility, t, y. strain size required to disintegrate the gel, expressed as a percentage of about 30%;

d) Adhesion, i.e. the ratio of the negative peak area between the two compression stages to the area of the first peak between 0 and 70%;

e) Elasticity, i.e. the ratio 100x (D-d) / D, where D is the height (cm) before the first compression period and d is the residual deformation of the specimen (cm) before the second compression period - from 25 to 100%;

f) Cohesiveness, i.e. overall ratio between first and second compression periods, 25 to 100%.

II. Disintegration time at 37 ° C using a disintegration test apparatus (according to Ph. Eur. Second Edition) - 5 to 60 min. within.

III. The amount of nicotine is from 0.5 to 10 mg or the corresponding amount of said alkaloids.

Disintegration time is determined at 37 ° C using the apparatus described in the second Ph.Eur. in Journal, Vol.5. 1.1 under the conditions described below. It should be noted that in other cases the disintegration time found is about one third of the above.

Definitions of the term structure profile and structure profile analysis are given in J. Sanderson et al. Resins and Stabilizers Used in the Food Industry, Proceedings of the 4th International Conference, Wrexham, Cluyd, Wales, July 1987, IRL Press Ltd. (1988) and Sczesniak et al., J. Food Science, 28, 385-403 (1963). who are on the list of references. The structure profile analysis version used here measures the force-deformation curve by double compressing the sample to 70% of its initial height at a given compression rate. This curve provides an objective measure of the physical parameters closely related to the characteristics of firmness, hardness, brittleness, adhesion, cohesiveness and elasticity.

This way,

(a) stiffness is determined by the initial effect of the force on the curve - deflection angle and expressed in units of force / area;

(b) hardness is determined from the maximum force exerted on a unit of area at any point in time during the first compression period;

c) Fragility is determined by the first reliable effect of the curve force - strain drop during the first compression period, i.e. first point of inclination, expressed as a percentage of the deformation required to destroy the sample;

d) adhesion is determined (in this specification) as the ratio of the negative peak area between the two compression periods and the first peak area;

e) elasticity is defined as the ratio 100x (D-d) / D, where D is the height of the sample (cm) before the first compression period and d is the residual deformation of the sample (cm) before the second compression period; and

(f) Cohesiveness is defined as the ratio of the peaks in the first and the first compression periods, expressed in%.

It has been found that the structure of the invention results in a controlled release of nicotine from the formulation:

- since the exposed surface area of the stimulant preparation remains practically stable during chewing, i.e. gradually dissolving the surface layers of the stimulant preparation;

- as the preparation does not significantly deform during chewing; and

- since the ingredient in the volume unit of the stimulant is only released when the part of the preparation is on the surface and its matrix is dissolved by the action of saliva.

Selected limits:

- hardness and brittleness - guarantees that the exposed surface area will not increase sharply due to degradation of the stimulant;

- strength, elasticity and cohesiveness - guarantees that the stimulator will not be crushed during chewing; and

- Adhesive - guarantees that the stimulant is non-sticky, which means it will not stick to the teeth.

Preferably, the structural profile parameter values and disintegration times are in accordance with claims 2 and 3 of the invention.

Buffer or agent

Salivary uptake of nicotine in plasma is dependent on saliva pH, plasma pH and nicotine pK (= 8.02).

With a plasma pH of 7.4 and saline of 7.0, only 30% of the nicotine will be in free base form. Thus, saliva pH should be increased to improve nicotine uptake. At pH 8.5, about 80% of the nicotine is in the free base form and the plasma nicotine concentration, calculated as:

| l + 10 ^{_ (pH} p ^pK a ⁾ In / l + 10 ^{_ (pH} s ^pK a ⁾ In by Martin et al., Clin. Pharmacol. Ther., 16, 1052-1058 (1974), is 3.8 times higher than the concentration in saliva.

Thus, most desirably, the stimulant formulation contains, as additives, physiologically acceptable buffering agents or agents, and their concentrations are selected to maintain saline pH within the range of 8-10 during preparation disintegration. Generally, the buffering agent or agent in the stimulant formulation will be in the range of 5 to 50 mg.

Nicotine doses

Stimulants are manufactured to provide a dose of nicotine that has a stimulating effect equivalent to e.g. for the effect of smoked cigarettes.

Thus, most desirably, the amount of nicotine in the stimulant is in the range of 0.5 to 5.0 mg nicotine per unit preparation. The amount of nicotine in the stimulant may be selected so as to provide, under certain conditions, stimulation of nicotine which is sensitive to light, environment, concentration, etc. The optimum concentrations are within the following ranges: 1.0-1.5 mg, 1.5-2.5 mg, 2.5 3.0 mg nicotine per unit.

Nicotine release profiles

Stimulants are formulated to achieve the desired nicotine release profiles. Continuous release. Where necessary, continuous release of nicotine is achieved by homogeneously distributing the nicotine throughout the formulation.

Generally, the release profile of nicotine depends on the effective surface area of the preparation during disintegration. In the first approximation, irrespective of the edge effects, nicotine is considered to be steadily released as the formulation degrades, with the rate of release gradually decreasing as the formulation weight decreases.

Initial, primary and sustained release of nicotine. Alternatively, a two-step release of nicotine release, which includes the initial and maintenance stages of nicotine release, is accomplished by the uneven distribution of nicotine in a multilayer stimulant:

(1) the outer layer is manufactured to have a short disintegration time and high nicotine content, and that the nicotine plasma concentration in the smoker's plasma is above the minimum effective concentration at the initial stage;

II) The inner layer is manufactured to provide a longer disintegration time and to release nicotine plasma levels of nicotine in the smoker above the lowest effective concentration for the desired time period.

Forms of stimulant preparations.

The nicotine released from the nicotinic stimulant formulations according to the invention is best absorbed in the oral cavity, when the formulation is placed under the tongue, cheek, or palate. Thus, the form of the nicotine stimulating preparation may be such that it can be stored in the aforesaid sites.

In addition, in certain forms, the preparation is fixed and can be taken orally.

It is desirable that the stimulant preparation has a shape which corresponds wholly or partially to the shape of the palate.

Method of administration.

According to the invention, nicotinic stimulant preparations can be used to obtain the effect of nicotine stimulation without smoking, similar to that obtained during smoking or consumption. tobacco products; the corresponding stimulant is administered orally by placing it at the desired desired site in the oral cavity with the tongue, slightly sucking or applying the preparation at the site of the oral cavity, depending on the stimulus effect of the individual and the nicotine.

(a) Analysis of structure profile

In this description, the term material structure is used to define the material consistency characteristics. The structure of the material can be objectively described by a set of six physical parameter sizes, and the structure profile is determined by the structure analysis described in Sanderson et al., As noted above.

The following explains the magnitude of these parameters, i.e. the structure profile calculation method based on the force-deflection (20 ° temp.) curve analysis presented in the corresponding drawing, obtained by testing a sample of a stimulating cylindrical preparation having a diameter of 15.4 mm and a height of 12.3 mm, which consistently the two steps are compressed to 70% of the original banners height using a compression speed of 50 mm / min.

The structure profile comprises the first, compression period 10 and the second compression period 20. In the first, compression stage 10, the 2 '' stiffness (modulus), 16S η / cm, is determined as the initial inclination angle of curve 11 at its beginning 12 when the deformation process begins. multiplied by the height of the specimen before compression and divided by the final surface area of the specimen.

Further, the hardness, 58 n / cm 2, is determined as the maximum force exerted 13 (height of the first peak) at any time during the first compression phase 10, i.e. strain at level 14 divided by the final surface area of the specimen.

Fragility, greater than 30%, is determined as the first bend point (failed in this test), i.e. this sample has a brittleness greater than 30% since the given sample was compressed before 30% of the deflection (a higher value indicates a low brittleness of the structure).

Adhesion, about 4%, is determined as the ratio of the area of the negative peak 17 after the first compression step 10 to the peak area of the first compression step. If the material has adhesive properties, it adheres to the pressing plates and stretches the plates in a different direction than they move.

The elasticity, 85%, is determined by the ratio of sample height D (12.3 mm) prior to first-stage compression for 10 min strain d (1.8 mm), i.e.. distance 22-18 and sample height before the first compression stage. The initial value 18 for the second compression step is found as a double distance of 30% of the strain 14-12.

The cohesiveness, 57%, is determined as the ratio between the peak areas of the first and second compression stages. First of all, this ratio is calculated by multiplying ··. ' . .peak ratios of heights 23 and 13 from the ratio of their bases, i.e. of distances 26-22 and 16-12 ratio. Peak areas can also be calculated in other ways, such as using a computer digitally, graphically, using a planimeter, or by weighing out clipped copies of defined areas.

(b) Active ingredient

According to the invention, any of the following compounds may be used as active ingredient:

nicotine (3- (1-methyl-2-pyrrolidinyl) pyridine) including synthetic nicotine and nicotine extracts from tobacco plants such as the nicotiana family; and other alkaloids of a similar activity type, including nornicotine and lobelin, for example, from lobeliaceae and lobelia species; methylanabazine and anabazine.

A single compound or combination thereof may be used; as the free base or its salts with acids. Also, various oxidation products of these compounds, such as nicotine-1'-N-oxide, may be present as the active ingredient.

(c) Water-binding gel forming agent

An important factor in obtaining the required structure of the stimulant preparation according to the invention is the selection of a suitable water-binding gel-forming agent.

According to the invention, the water-binding gel-forming agent may be selected from the group consisting of:

organic gelling agents, including gelatin, modified starch and unmodified starch; and resins such as: agar, alginate, gum arabic, carob gum, carrageenan, gati gum, karaya gum, pectin, tragacanth gum, pseudo-locus strain, xanthine gum.

The most suitable gel forming agents are gum arabic, starch, gelatin, agar and pectin. The most suitable of these is gum arabic, which accounts for 50-70% of the total solids. Another gel-forming agent, such as gelatin, is recommended for softer stimulant preparations; in addition, multiple agents can be used together.

(d) Optional (additional) ingredients

Optional, additional ingredients include sweetening, flavoring, coloring, stabilizing, vitamins, mineral salts, buffering agents or agents to provide the necessary pH for saliva to successfully pass into the bloodstream.

Sweetening. One or more synthetic or natural sugars, e.g. any carbohydrate suitable for sweetening confectionery.

According to the invention, the sweetening agent may be selected from the group consisting of:

individual sugars, which include: cane and beet sugar (sucrose), dextrose (also called glucose), fructose (also called levulose) and lactose (also called lactose); sorbitol, mannitol, glycerin, xylitol ·, saccharin sodium; and sugars such as glucose syrup, for example starch hydrolysates containing a mixture of dextrose, maltose and other complex sugars, invert sugar syrup such as sucrose invertase invertase containing a mixture of dextrose and fructose, , such as molasses and honey, which are predominantly a mixture of levuiose, dextrose, maltose, sucrose, dextrin and more complex sugars.

You got it. because of. taste_and aroma. Flavoring and aroma additives may contain one or more synthetic or natural substances with a suitable taste and odor.

According to the invention, the additives for taste and aroma can be selected from the following materials:

essential oils obtained by distillation, solvent extraction, cold pressing of a blend of flowers, leaves, peel or fruit purée, containing a mixture of alcohols, ethers, aldehydes and lactones;

essences that include either dilute solutions of essential oils or blends of synthetic materials, which are blended to give a natural taste of fruits such as strawberries, raspberries, blackcurrants, artificial and natural jams and beverages such as cognac, whiskey, rum, gin, sherry, wine, wine, additives; tobacco, coffee, tea, cocoa, mint; fruit juices derived from washed, peeled fruits such as lemons, oranges; licorice root, menthol, eucalyptus, anise, nuts (for example, peanuts, coconut, hazelnuts, chestnuts, walnuts) almonds, raisins; and powders, flours or milled vegetative parts of plants, including tobacco, e.g. nicotiana species, parts of the plant, ku * and curry content does not change the nicotine content of the preparation, ginger.

The most suitable additives for taste and aroma are derived from essential oils, essences, powders, flours, and crushed tobacco plant parts that are added in amounts that do not significantly affect the nicotine content.

Especially suitable for flavor and aroma are essential oils, tobacco, coffee, tea, cocoa and mint extracts.

jPr.slides_ on_ s_pa_lvo_s. According to the invention, color additives may be derived from paints having a light-absorbing chemical moiety, e.g. paints with no reducing properties such as sugar and confectionery acids; light and heat resistant paints, paints that do not decompose into individual primary colors; particularly suitable inks are mixtures of tartrate and indigo carmine, which give the pea its green color; blends of erythrosine and indigo carmine to give a purple color and mixtures of tartracin, amaranth and indigo carmine to give a chocolate color; caramel containing burnt sugar powder or liquid giving a brown color; carbon giving black color and titanium dioxide giving white color,

Stabilizers. According to the invention, the stabilizing additives may be selected from the following materials:

antioxidants including vitamin E, ascorbic acid, sodium pyrosulfate, butyloxytoluene, and preservatives such as citric acid, tartaric acid, lactic acid, acetic acid, benzoic acid, sorbic acid. Vitamins ^ JLr_mirieraljjj S-Mediums ^ It has been found that smoking reduces the amount of minerals and vitamins, especially vitamin C. These losses can be offset by stimulants containing vitamins and mineral supplements.

Therefore, according to the invention, one or more vitamins and minerals may be present in the preparation as additional additives.

The most suitable vitamins are selected from the group consisting of vitamins A, B1, B2, B5, C, D2, D3, E, F, K and P, especially vitamin C.

Preferred minerals are selected from the group consisting of magnesium, iron, zinc, copper, iodine, manganese, chromium, selenium, molybdenum, cobalt, vanadium, nickel, tin, fluorine, silicon. However, according to the invention, besides the addition of vitamins and minerals to the preparation, it is still necessary to create conditions for the said substances not to break down; this is monitored by exposure of the vitamins A, B, C and E to the air and all vitamins at high temperatures. In addition, vitamins and minerals can give the preparation an unwanted, difficult to remove spice and adversely affect other ingredients, such as acids. In addition, vitamins are highly photosensitive and are degraded, albeit slowly, when stored.

Buffer medž_ia £ s £ arba_a eritai_ _r According to the invention, buffer substances or agents can be selected from the group consisting of physiologically acceptable buffering agents and agents capable of stabilizing the pH between 6.5 and 9, such as an alkali metal carbonate and bicarbonate or phosphate systems; particularly suitable are sodium carbonate and sodium bicarbonate, potassium carbonate and potassium bicarbonate, trisodium phosphate, sodium hydrophosphate, sodium dihydrophosphate, potassium phosphate, potassium hydrogen phosphate, potassium dihydrogen phosphate, and mixtures thereof.

(e) Preparation of stimulant preparations

Key parameters that determine the structure of the stimulant formulation, the formulation of the ingredients, the pH value and the temperature of the premix or solution, and the individual process steps for converting the premix / solution into semi-finished products to condense and preserve to the stimulant . In the case of rubber, jelly or lozenge products made by concentration in molds, starches or resins, care should be taken to ensure that the final product contains a moisture content not exceeding 20%, depending on the gel-forming material chosen. Stimulants according to the invention can be prepared according to a number of methods commonly used in the art (see Sugar, Confectionary and Chocolade Manifacture, R. L. and EB Jackson, Leonard Hill Books, 1973), such as gum arabic, agar gel, gelatin gel, starch jelly. and methods of obtaining pastilles; starch jelly can be like orange slices, marmalade and jelly beans; fruit pastilles., in the form of chewing gum, gel in the form of tablets, tablets, scones, licorice paste and pectin jelly.

Formulations and Methods for Gel-forming Water-Binding Agents (Known in the Art) (a) Gum Arabic gum

Recipe: Gum Arabic Cold Water Sugar

Glucose syrup Water

Weight Parts 100 120 90

The amounts of dyes, materials due to taste and aroma and acid depend on the desired taste and shade.

Method of obtaining

Slices of gum arabic slowly dissolve in water.

Carefully pass the solution through a dense sieve or cloth to remove impurities and other foreign matter.

3. Dissolve the sugar in water, add glucose syrup, and heat to 124 ° C (257 ° F).

4. Pour the warmed solution into the gum arabic solution and mix thoroughly.

5. Stir and leave to stand for at least one hour (during this time the mixture begins to clear and foams appear on the surface which must be removed before the next stage of the procedure).

6. Add paints, substances for color and odor and acid solution.

7. Mix.

8. Pour into starch molds.

9. Transfer the pressed product to the drying oven until it has the required strength.

10. The product is thoroughly cleaned and glazed.

(b) Agar Gel Recipe Agar Water

Sodium Citrate Sugar

Glucose syrup

Additives for taste and smell, paints and acid

Parts of Weight 2.0

70.0 0.7

60.0

40.0 by taste

Method of obtaining

1. Agar should be soaked in cold water for 3 to 12 hours, depending on its origin.

2. Slowly heat the mixture in an open steam boiler until a solution is formed.

3. Sodium citrate is added.

4. Pass through a fine sieve.

5. Add the sugar and glucose syrup to the agar solution and heat to 107 ° C (225 ° F).

6. Cool to a temperature not exceeding 76 ° C (170 ° F) and add any acid solution.

7. Add paints and substances for taste and smell.

8. Pour into warm dry starch molds.

9. In starch molds, the jelly is kept for 12-24 hours.

10. The total soluble solids content of the already prepared jelly should be checked to exceed 76% before removal of starch. The forming starch should have a humidity of 5-7% and be stored at 26-43 ° C (73-110 ° F).

(c) Gelatin jelly

Recipe Weight Loss Parts

Gelatine.180 Bloom Powder 25

Hot water 50

Sugar 80

Glucose syrup

Water 40

Method of obtaining

1. Prepare a gelatin solution by mixing the required amount of gelatin powder slowly in warm water to make a solution and leaving until clear.

2. The sugar is dissolved in water and glucose syrup is added. Heat to 116 ° C (241 ° F).

3. At this stage, it is recommended to cool the solution to about 70 ° C (158 ° F) before adding the gelatin solution.

4. Pour the heated solution into the gelatin solution and mix.

5. Add dissolved paint and acid solution and mix. Add the right amount of substances for taste and smell and mix.

6. Dip into starch molds.

7. Transfer the pressed product to the drying oven until it has the required strength.

If gelatine in leaf or granular form is used, it must be soaked in a volume of water equal to the weight of gelatin for at least three hours. Most factories usually soak overnight.

(d) Dextrin jelly and lozenge

Recipe

Ingredients A B {parts by weight} dextrins Hard pastilles Soft fruity pastilles Medium hardness pastilles sugar 40.0 34.0 30.0 40.0 Glucose syrup 40.0 54.0 48.0 48.0 Diluted cooked starch 12.5 12.0 12.0 11.0 Water 100.0 120.0 110.0 100.0 Jam 10.0

Paints, odors, acids on demand

The main method of obtaining

1. Sugar and glucose syrup are heated in a two-thirds water-pot with double-walled steam.

2. Make a starch suspension in the remaining amount of water.

3. The starch suspension is slowly added to the boiling sugar mass at such a rate that the sugar mass stops boiling. Vigorous stirring is recommended at this stage.

4. Boiling to the required consistency.

5. Add paints, substances for taste and smell and acid solution.

6. Pour into starch molds and dry in a hot room for 24 hours.

Jam can be prepared by boiling 50% sugar and 50% fruit pulp. For diluted cooked starches the acidification recommended is 20, 30, 40 and 50.

(e) Starch jelly (continuous manufacture)

Starch jelly as a base

sugar

Glucose syrup 42 DE

Water

Diluted cooked starch with a yield of 7 5

Paints, aromatics, acid

Weight Parts 25 25 19 as required

Method of production

1. Add water to the bowl with mixer (refrigerated)

2. Add sugar and mix (refrigerate)

3. Add the starch and mix (refrigerate).

4. Add glucose syrup and mix.

5. Raise the temperature to 80-90 ° C (176-194 ° F).

6. Check the total solids content of the pre-mixed mass at 20 ° C (68 ° R) using a refractometer. The jelly should have this size within the 76-82% range.

7. Transfer the Offlfl to the oven for cooking.

8. Check the total solids content after boiling; it must not change more than 2% water.

9. Pour into starch molds and keep in a hot place for 24 hours.

Orange slices (based on starch)

Parts of weight

Glucose syrup 200,0 Sugar 200,0 Glucose 104,0 Starch (flowability 85) 60,0 Water 100,0

Total solids content 76-80%. Boiling point 278285 ° F.

Structure: fragile / delicate.

Marmalade

Parts of weight

Glucose syrup 200.0 Sugar 160.0 Starch (flowability 75) 64.0 Glucose 80.0 Water 80.0

Total solids content 78%. Boiling point 275-285 ° F Structure: Fragile / Harder.

Jelly beans

Parts of weight

Water 132.0 Starch (yield 70) 60.0 Glucose syrup 330.0 Sugar 130.0

Total solids content 68-70%. Boiling point 285-295 ° F.

Structure: Durable / chewing gum type.

(f) Fruit pastilles

A: Starch based lozenge

Recipe:

sugar

DE glucose syrup

Water

Diluted boiled starch (Flowability 60) Gelatin (Bloom medium)

Fruit pulp Tartaric acid

Paints and flavorings

Parts of Weight 90.0 90.0 35.0 20.0 12.0 16.0

3,5 to taste dali

Method of production

1. Add the sugar to the water and bring to the boil.

2. Add pre-boiled glucose syrup.

3. Slowly add the starch suspension in 50 cold water and boil for 10 minutes.

4. Folding oašildoma fruit pulp and up to 110 ° C (230 _Q

5. Cool to 93 ° C (200 ° F).

6. Gelatin is added, dissolved in 24 parts of hot water.

7. Addition of paints, aromatic substances and acid dissolved in 5 parts of water.

8. Put in warm dry starch.

9. Store in an oven at 54 ° C (130 ° F) for 48 hours.

10. Starch is removed and crystallized with sugar or wet-sugared.

B: Resin based lozenge

Parts of weight

Sugar 100.0

Glucose Syrup 75.0

Water 30.0

Reconstituted gum arabic solution 100.0

Gelatin 10.0

Water 20.0

Paints, aromatics, acid to taste

Method of production

1. Dissolve the sugar in the water, add the glucose syrup, and warm to 127 ° C (260 ° F).

2. Mix the prepared gum arabic solution.

3. Gelatin is dissolved in twice the volume of hot water.

4. Pour into a batch at 82 ° C (180 ° F).

5. Addition of paints, flavoring agents and acid dissolved in the same weight as water.

6. Add to dry warm starch.

7. Dry in oven at 54 ° C (130 ° F) until required.

(g) Jelly Tiles

Recipe: Parts of weight

Cane and beet sugar

Inverted sugar syrup (70%) 245.0

Water 70.0

Batch yield 595.0

Method of production

1. Pour the required amount of hot water into a large heated boiler.

2. Heat to 90 ° C (.194 ° F).

3. An appropriate quantity of cane or beet sugar shall be added and dissolved.

4. Add the appropriate quantity of invert sugar syrup and mix.

5. Filter under suction through a filter.

6. Store · as needed at 60 ° C (140 ° F). Welding

7. Suction 590 parts of syrup.

8. Heat quickly to 123 ° C (252 ° F). Alternatively, it is passed through a hot heat exchanger, concentrating the syrup to a total soluble solids content of 90%. Chilling

9. Stop heating $ 2 and allow the temperature to reach below 100 ° C (212 ° F).

Preparation of other ingredients

Gelatin

10. Slowly add 80 parts of gelatin to 145 parts of hot water at 90 ° C (194 ° F) in a mixing tub.

11. The mixing pads should rotate at low speed until all the syrup has been poured into the tub.

Acid

12. Dissolve 12 parts of citric acid in 12 parts of water.

Buffer

13. Dissolve 2.5 parts of sodium citrate in 2.5 parts of water.

Additives for taste and smell (if desired)

14. Measure 45 parts of the aromatic additives and batch them.

15. Dissolve 0.025 parts by color in 0.25 parts water and make up the batch.

Mixing

16. At the end of Step 8, the syrup is fed by self-circulation or by pump into the Step 11 gelatin mass.

17. Stir for 3-5 minutes.

18. Up to 5% jelly waste may be added at this stage

19. Buffer solution, aromatic additives, dyes and finally acid are added.

20. Upon completion of mixing, stop the scoops and transfer the mixture to a loading funnel, from which it is passed through a large-mesh sieve.

Settling down

21. Giving the opportunity for 'foams' to occur.

22. Check that the backing plates or dies are well covered with a release material.

23. Allow to settle at relatively low speeds to avoid air bubbles.

(h) Tablets

Recipe:

Weight Parts 100 0.75 1.25 0.75 0.5 4.0 0.125

Sugar glaze

Stearic acid

Isopropanol

Gelatin

Glucose syrup

Water

Aromatic additives Method of production. Wet granulation

1. Stearic acid is dissolved in isopropanol.

2. Dissolve the gelatin in a sufficient quantity of warm water and mix with the glucose syrup.

3. Put the sugar glaze into a mixing bowl.

4. Add liquid components and form a batch.

5. Check that the mixture becomes a ball by holding it in the hand.

6. If the mixture has a satisfactory consistency, it is granulated and sieved through appropriate sieves (norm. 6) to obtain a mixture of fine granules.

7. Spread the pulp onto a pallet and transfer to a drying oven.

8. Dry at 60 ° C (140 ° _F ) for 10 hours.

9. Transfer to switch mixer and add lubricant and aromatic additives. Mix.

10. Transfer to tablet and press to appropriate shape.

(i) Buns

Sugar glaze Resin A solution

Gum arabic

Water

Gelatin solution

Gelatin (100 Bloom)

Water

Resin B solution

Tragacanth

Water

Aromatic additives

Weight Parts 300

0.03

0.5

Method of production

1. Put the sugar glaze into a blender.

2. Prepare a gelatin mixture with water at a temperature not exceeding 80 ° C (176 ° F).

3. Resin solutions (made the day before) are added to the gelatin mixture. This gelatin-resin mixture is filtered and mixed before use.

4. The aromatic additives shall be mixed with part of the sugar coating and added to the remainder of the lot.

5. Gelatin-resin mixture is added to the sugar glaze.

6. Slowly and thoroughly mix the mixture for the time required for the given mixer.

7. Dispense into containers and transfer to loading funnels for punching equipment.

Size: large rolls - 200/1 pack (440 / kg); Cachons 1000 / i Pack. (2200 / kg), small buns 500/1 pack. (1100 / kg).

Variants

Centers with room boilers

Stage I adds 10 parts of rice flour to produce buns with greater strength and less disintegration in rotating boilers.

Painted and fragrant buns (Kachons). It is recommended that 0.05 parts of paint be used to obtain the desired pastel shade and 0.02 parts of lanterns, peach blossoms, rose or lily oils are added to give the desired scent.

(j) Licorice paste

Recipe

Open Boiler Lot _T Leaflet Innovations 'Continuous Cooking Ingredients ^J '

ΙΪ1 no ί * *

Leaflets.

weight d. weight d. weight d.

Suspension in water wheat flour 50 150 50 150 125 Mixture in water 130 160 80 Yellow fine sugar 125 100 60 Green molasses 7 5 150 140 Hydrol 25th - 25th Glucose syrup (high elasticity (DE) 12.5 10th A block of juice 20th 25th 18th Water as a solvent 15th 20th 10th Liquid caramel 15th 25th 10th Hardened Palm Dice Oil 2.5 2.5 2.5 Anise seed oil 0.25 0.25 0.25 Black Color 1 1 1 Salt 0.5 0.5 0.5 Water 5 5 - Gelatin 5 5 - JMS 0.5 0.5 0.5

Cooking time (min. ) 80 150 Feeding speed and temperature need to control according to required- dropping rates. Waste overhead more than 25th 50 25

Red licorice can be made by replacing liquid caramel with golden molasses syrup. Add 1 part red paint to get a bright red tint replacing black ·.

Method A is a continuous process

1. Pour the glucose syrup and water into a container with a disintegrator or steam wall and add the yellow granulated sugar, mix.

2. Raise the temperature to 104 ° F (40 ° C)

3. Brush the block with juice and dilute to 1 gallon with hot water; warm to dissolve and pour into the previous mixture.

4. Add the remaining ingredients and, using a 20 min. recirculation to form a homogeneous suspension.

5. Raise the temperature to 60 ° C (140 ° F) and recirculate for 2 minutes.

6. Using a pump, the mixture is fed to the rotary unit at a constant speed (the mechanism is determined by the structure of the product to be obtained).

Method B - Batch Process

1. Pour the aqueous suspension into a mixing bowl and add the wheat flour; mix.

2. Pour the mixture in water into a saucepan, bring it to the boil and add hydrol, yellow sugar, salt and a block of juice dissolved in boiling water.

4. Molasses, glucose syrup and black molasses are added to produce licorice leaves.

5. Continue heating and bring the mixture to the starch slurry after boiling.

6. When all the starch suspension has been added, bring to a boil and boil for a specified period.

7. You need 30 minutes to get the innovation and stopper. until the end of boiling, add the necessary amount of glucose syrup and black molasses.

8. When cooked, heat off and add liquid caramel, flavored aniseed, iBlack Color and ready-made gelatin solution.

8. Mix until a constant color is obtained.

?. the cooked mass is removed and transferred to the forming apparatus. Method C - Plant with VSN NK conveyor fluid

1. Mix the ingredients of a batch of unmodified formula ⁷ and pour into a pre-prepared suspension

2. Turn on the mixer and add the remaining solid ingredients; recirculate to obtain a homogeneous mass.

3. Enable:

(a) vapor in the Fm maker,

(b) extractor fan to remove water vapor,

(c) water flow in the condenser installed in the steam outlet.

4. Pour the mixture into the kettle and start cooking.

5. Monitor the condensate level in the measuring vessel and the current reading. (It should be noted that the amount of condensed water is an indicator of the increase in solids, while the increase in energy consumption indicates an increase in the degree of gelatinization).

6. As soon as the amount of condensed water reaches the desired humidity level of the liquorice paste at the end of cooking, turn off the steam, the fan and the cooling water.

7. The cooked paste is loaded onto a conveyor and transported to the forming apparatus. Formed at 70-82 ° C (158-180 ° F).

8. The squeezed sheet is passed through a 40-foot chilling tunnel in 1.5 to 5 minutes (depending on shape) and the gelatin is cut into individual pieces by a cutting machine.

(k) Pectin Jelly

Recipe:

(A) Buffer slow-curing pectins

Parts of weight

Pectin 1.25

Citric acid, monohydrate 0,4

Sugar 51

Glucose syrup 42 DE 29

Water 40

Dyes and Flavorings as Required Yield 100 (B) Buffer Slow Curing Pectins (Using 63 DE Glucose Syrup)

Pectin

Citric acid, monohydrate

Parts of weight

1.25

0.4

sugar

Glucose Syrup 63 DE Water

Dyes and fragrances Yield per demand 100

0.82

0.28

0.25 by necessity 100

Formula (A) gives a sufficiently hard gel, while formula (B) produces a softer product.

(C) Non-buffering slow-curing pectins

Parts of weight

Pectin

Citric acid, monohydrate

Potassium citrate

sugar

Glucose syrup

Water

Paints and flavorings

Yield

The amount of citric acid monohydrate used depends on the type of pectin. Some non-buffered slow-setting apple pectins require 0.28 parts and non-buffered slow-setting citrus pectins require 0.4 parts citric acid.

(D) Non-Buffered Slow Curing Pectins (Using 63 DE Glucose Syrup)

Parts of weight

Pectin 0.82

Citric acid, monohydrate 0.28

Potassium citrate 0.25

Sugar 38

Glucose syrup

Water 37

Paints and fragrances on request

Yield 100

Continuous production methods

For continuous production, first and foremost, a stable pectin solution must be prepared. Slow curing buffer and low methoxyl (buffer) pectins are most suitable. High weight and type of pectin manufacturer requires and used pectin buffer salts

Pectin

sugar

Water

Method of production

1. Dry pectin is mixed and it is important to make sure that the pectin is completely dissolved before use. Failure to do so may result in the formation of a weak gel and under-utilization of the gel's full capacity. It is recommended that solutions be prepared in such a way that their concentrations are obtained in accordance with the instructions for solubility.

Parts of weight

88 dry sugar.

2. Pour water into the mixing vessel and heat to 70-77 ° C (158-170 ° F).

3. Turn on the mixer and add the pectin / sugar mixture to the water.

4. Heat to boiling and stir for 1 minute.

5. Cool the solution to 50-60 ° C (122-140 ° F).

Chilling is required to prevent degradation of the pectin. If the solution is used immediately, it may not be refrigerated.

Further descriptions of the various types of rubber products, jelly, lozenges can be found in a series of articles, rubber-jelly lozenges, parts 1-6, in the Sweetmaker confectionery industry, beginning in 1983. June to June 1983 November; references to these articles in the references.

The invention is further illustrated by a number of examples.

Examples

The following examples provide a number of formulations that may be used in the preparation of the stimulant formulations of the present invention.

The production of the stimulant is based on obtaining a homogeneous liquid formulation containing sugar, water, carbohydrates or carbohydrates selected on a case-by-case basis, and, if necessary, additional, untreated, poorly purified animal material such as gelatin.

Dyes, aromatics, preservatives and other additives are used in this formulation. According to the recommendations, an active ingredient such as nicotine is added to the mixture shortly before the formulation process. This procedure is needed to strictly control the amount of the very chemically active compound, nicotine. It must be ensured that the total amount of active substance used in the manufacturing process plus the amount of the active ingredient in any of the added substances must correspond to the amount of active ingredient in the final product. in production; if this is not possible, the material should be carefully collected and disintegrated, for example by heating. Any suitable method known to those skilled in the art can be used to prepare the formulations of the invention. Methods such as the production of polysaccharides and / or starch and gelatine solutions and their further mixing with sugar (including other carbohydrates such as dextrose syrup) solutions must be selected according to the raw materials selected; this will allow products of the appropriate structure having the above parameters to be obtained.

A commonly used method of production is based on the formation of the liquid form in the corresponding cavities made of starch of appropriate purity and moisture, in which they are stamped in the size and shape required before forming. Other molding techniques may also be used, for example using molds made of elastic materials such as elastomers. In particular cases, the stimulant formulations of the present invention may be obtained by known techniques, such as extrusion extrusion, or by compressing tablets from a suitable mixture of powder or granular ingredients.

When stored at a controlled temperature and relative humidity for an appropriate period of time, the hardening stimulant is removed from the starch by known methods, and the starch is removed from the preparation by brush or air blast; after these operations, it is recommended that the product be glazed or polished using oils, either alone or in solution in a volatile solvent; the resulting thin film gives the surface an attractive shine, removes it. adhesive and protects the preparation from fluctuations in water content in an environment that is too dry or too humid.

Although the examples in the batch formulation process more or less use manual work whereby the formulation is made in starch-shaped trays, a partially or fully automated production method such as the 'Modul' device may also be used, but replacement with this type of high speed technique is obvious. will require some adjustment to the formulation of the molding material.

The following materials were used in the samples:

Raw materials, raw materials:

Dextrose Syrup, Glycosum Liquidum (Lot No. 302 589), Mecobenson, Denmark;

Sugar (preferably Formal) Dannsukker Blue, DDS, Denmark;

Gum Arabic (purified), Gummi Arabicum (Chemically Powder) Lk (E414), (lot no 233 200) Nordisk Droge Handels A / S, Denmark;

Gelatin (preferably Bloom 215), Gelatin Powder 215 (lot No. 232 883), Nordisk Droge Handel A / S, Denmark;

Tap water;

Tobacco dust, half granular and half pipe tobacco, American Branch;

Citric acid;

Peppermint essence;

Aniseed;

Almond essence; and

Cocoa.

Materials for drying

Cornstarch, Maydis Amylum (Lot No. 257 329), Mecobenson, Denmark;

Wheat Starch, Tritici Amylum (lot No. 257,535), Mecobenson, Denmark;

Before use, the starch must be dried at 150-200 ° C for at least 2 hours, i.e. as long as the moisture content does not exceed 10%.

Gum Arabic Solutions Solution (50% Gum Arabic)

With stirring, 3.5 kg of water, heated to 30 ° C, is slowly added to 3.5 kg of gum arabic, shaken vigorously and left to stand for approximately 20 hours. Remove foam from the surface of the solution and leave to stand for 1 hour. The solution surface is cleaned again before use.

solution (50% gum arabic)

Slowly add 3,5 kg of gum arabic to the mixture, stirring constantly

3.5 kg of water preheated to 30 ° C; this solution is then treated in the same way as solution 1.

solution (33.3% gum arabic) kg warm water (30 ° C), slowly stirring, pour into 1 kg gum arabic and then treat in the same way as solution 1.

Pre-soaked gelatin solutions solution (33.3% gelatin)

900 g of gelatine is slowly added to water (12 ° C) with constant stirring, then 900 g of warm water (70 ° C) is added to this solution with stirring and left to stand for 20 hours.

Note: Solution 4 must not be used without re-heating and filtering.

solution (33.3% gelatin)

900 g of gelatine is slowly added to 1800 g of warm water (70 ° C) with constant stirring, shaking vigorously and left to stand for 20 hours.

solution (33.3% gelatin)

1800 g of warm (50 ° C) water, slowly stirring, slowly dissolve 900 g of gelatin, shake vigorously and leave to stand for 20 hours.

solution (33.3% gelatin)

Transfer 150 g of gelatine and 300 g of water to a slowly heated dish at 95 ° C and, after dissolving, cool the solution to 50 ° C and use immediately.

θ solution (25% gelatin)

Slowly add 1800 g of warm water (70 ° C), stirring constantly, to 600 g of gelatine, shake vigorously and leave to stand for 20 hours.

Examples

Dry weight% in parentheses.

The recipe

210g sugar (25%)

210 g dextrose (25%) g water

420 g of gum arabic (50%) (1260 g of solution 3)

The sugar is mixed with water and heated until completely dissolved Dextrose is added and the mixture is slowly heated to 125 ° C (boiling time 23 minutes). Add the gum arabic and boil over low heat for 80 minutes, then leave to stand for 3 hours. At 35 ° C. The final pH of the mixture is 4.0-5.0.

The surface of the mixture is thoroughly cleaned, then the mixture is poured into individual wells of maize starch and dried at 50 ° C until the moisture content is 5-10%.

Recipe B

210g sugar (19%)

365 g dextrose (32%) g water

560 g of gum arabic (49%) (1 solution)

The sugar is mixed with water and heated until completely dissolved. After the addition of dextrose, the mixture is heated to 125 ° C (heating time 55 minutes). Stirring constantly, add the gum arabic and heat to 75 ° C. The mixture is then maintained for 1.5 hours. At 35 ° C. The final pH of the mixture is 5.0-5.5.

The surface of the mixture is thoroughly cleaned and then the mixture is poured into cornstarch molds and dried at 50 ° C until the moisture content is 5-10%.

C Recipe

210g sugar (24%)

350 g dextrose (41%) g water

300 g of gum arabic (35%) (1 solution)

The mixture of sugars, etc., prepared according to recipes A and B, is heated to 117 ° C (heating time 20 minutes). Add the gum arabic and bring to a boil. The mixture is left to stand for about 1 hour. At 35 ° C. The final pH of the mixture is 4.5-5.5.

After thoroughly wiping off the surface of the mixture, the mixture is poured into starch pits in a mold and dried at 50 ° C until the humidity is 5-10%.

Recipe D

210g sugar (23%)

210 g dextrose (23%) g water

480 g of gum arabic (53%) (solution 2)

The sugar mixture is heated to 118 ° C for 23 minutes. Stirring constantly, add the gum arabic to the mixture, leave the mixture to stand for 1.5 hours. At 35 ° C. The final pH of the mixture is 3.5-5.0.

After thoroughly wiping off the surface of the mixture, the mixture is poured into molds containing cornstarch and dried at 50 ° C until the moisture content is 5-10%.

Recipe E

210g sugar (17%)

360 g dextrose (30%) g water

640 g of gum arabic (53%) (solution 2)

The sugar mixture is heated to 122 ° C (heating time 20 minutes), then cooled to 115 ° C. Add the gum arabic and leave the mixture to stand for 1.5 hours. At 35 ° C. The final pH of the mixture is 3.0-5.0.

The surface of the mixture is thoroughly cleaned of foam. The mixture is then poured into cornstarch pots and dried at 50 ° C until the moisture content is 5-10%.

The F recipe

210g sugar (23%)

280 g dextrose (31%) g water

400 g gum arabic (44%) (solution 2) g gelatin (solution 8)

The sugar mixture is heated to 140 ° C (heating time 25 minutes). Add the gum arabic and cool to 80 ° C. The gelatin is heated to 70 ° C and added to the mixture. The mixture is left to stand for 1.5 hours. At 35 ° C. The final pH of the mixture is 4.0-5.0.

After thoroughly wiping off the surface of the mixture, the mixture is poured into molds containing cornstarch and dried until the moisture content is 5-10%.

G recipe

210g Sugar (33%)

280 g dextrose (44%) g water

150 g of gelatin (23%) (solution 5)

The sugar mixture is heated to 120 ° C (heating time - 25 minutes). The mixture is cooled to 90 C. The gelatin is heated to 70 ° C and poured into the mixture. Leave to stand for 35 min. The final pH of the mixture is 4.0-5.0.

After thoroughly wiping off the surface of the mixture, the mixture is then poured into molds containing cornstarch and dried at room temperature until 5-10% moisture remains.

H recipe

210g sugar (32%)

350 g dextrose (53%) g water

100 g of gelatin (15%) (solution 6)

The sugar mixture is heated to 116 ° C (heating time 15 minutes). The mixture is then cooled to 80 C. The gelatin is heated to 60 ° C and added to the mixture with constant stirring. Leave to stand for 35 min. At 35 ° C. The final pH of the mixture is 4.0-5.0.

The surface of the mixture is thoroughly cleaned of foam. The mixture is then poured into cornstarch pits and dried at room temperature until 5-10% moisture remains.

J recipe

210g sugar (23%)

290 g of dextrose (31%) g of water

350 g gum arabic (38%) (solution 2) g gelatin (8%) (solution 6)

The sugar mixture is heated to 120 ° C (heating time - 25 minutes). While stirring, add the gum arabic and cool to 90 ° C. The gelatine is heated to 60 ° C and stirred into the mixture. The mixture is left to stand for 80 minutes. At 35 C. The final pH of the mixture is 3.0-5.5.

After thoroughly wiping off the surface of the mixture, the mixture is poured into starch pits and dried at room temperature until 5-10% moisture remains.

The K recipe

210g sugar (20%)

350 g dextrose (34%) g water

400 g gum arabic (39%) (solution 2) g gelatin (7%) (solution 7)

The sugar mixture is heated to 120 ° C (heating time - 20 minutes). Gum arabic is added, then the mixture is cooled to 100 ° C and then preheated to 60 ° C with gelatine. The mixture is left to stand for 100 minutes. At 35 ° C. The final pH of the mixture is 4.5-5.0.

After thoroughly wiping off the surface of the mixture, the mixture is then poured into starch pits and dried at room temperature until 5-10% moisture remains. Additional ingredients

The examples labeled I have no attachments.

Citric acid was added to the samples labeled II (pH values are given in various recipes).

Examples III-VII include citric acid and flavoring agents as shown below:

I have no attachments

Citric acid II

III Peppermint Essence

IV anise (powder)

V Almond Essence

VI cocoa

VII Tobacco Powder

Gum Arabic Solutions Solution (50% Gum Arabic)

Add 2000 g of gum arabic to 2000 g of warm (50 ° C) water. Shake vigorously and leave standing for 24 hours, shaking vigorously from time to time. Mix two identical portions.

Gelatin solutions solution (33.3% gelatin)

100 g of gelatin are mixed with 100 g of warm (70 ° C) water to form a homogeneous mixture. An additional 100 g of warm water (70 ° C) is added to the mixture, which is then allowed to stand for 5 hours.

The L recipe

400 g sugar (33%) g water

100 g dextrose (8%)

100 g of gelatin (8%) (solution 10)

600 g of gum arabic (50%) (solution 9)

The sugar is mixed with water and heated until completely dissolved. After the addition of dextrose, the mixture is heated to 120 ° C (heating time 15 minutes). The gelatin is then heated to 70 ° C and added to the mixture. Add gum arabic to it, stirring constantly to distribute it evenly. Drain half the mixture (in /) and keep at 35 ° C for 30 minutes. The other half is boiled for another 35 minutes, then left to stand at 35 ° C for 80 minutes. The final pH of the mixtures is 3.5-5.0.

The surfaces of both mixtures are carefully scraped off with foam

The L · 'mixture is then poured into cornstarch molds

V O wells and dry at 50 ° C until moisture remains 5-10%. Subsequently, the L · mixture is poured into wells of wheat starch molds and dried at 50 ° C until 5-10% moisture remains.

M recipe

400 g sugar (29%) g water

100 g dextrose (7%)

900 g of gum arabic (64%) (solution 9)

Mix the water and sugar and heat until the sugar is completely dissolved. Add dextrose and heat to 117 ° C (heating time 15 minutes). Add the gum arabic and stir until a homogeneous mixture is obtained. One side (M ') is decanted and held for 65 minutes. At 35 ° C. The other half is boiled for another 45 minutes and then left to stand for 70 minutes at 35 ° C. The final pH of the mixtures is 3.0-5.0.

The two mixtures (M and M ') are carefully scraped off with foam, then poured into cornstarch pits and dried at 50 ° C until 5-10% moisture remains.

N recipe

400 g sugar (27%) g water

100 g dextrose (7%)

1000 g of gum arabic (67%) (solution 9)

Mix the water and sugar and heat until the sugar is completely dissolved. Dextrose is added and the mixture is then heated to 118 ° C (heating time 12 minutes). Add the gum arabic and mix until homogenous. Drain one half (Ν ') and hold for 70 min. At 35 ° C. The other half is boiled for another 50 minutes, then left to stand for 120 minutes. At 35 ° C. The final pH of the mixture is 4.0-5.0.

The surfaces of both mixtures (N and N ') are carefully scraped off with foam. The mixture N 'is then poured into the cornstarch pits and dried at 50 ° C until 5-10% moisture remains, and the mixture M' is poured into the pellets of the wheat starch and dried at 50 ° C for 5 minutes. -10% moisture.

Additional ingredients used in L-N recipes

The examples labeled I were prepared without any additional ingredients. The samples labeled II were obtained by the addition of nicotine after the initial gel formation (pH unchanged). The examples labeled III are prepared by the addition of nicotinic and citric acid.

In the following examples, the formulas of Q and R can be formulated with the base of various stimulant formulations to which a certain amount of active ingredient is added and flavored by the addition of tobacco. The base of these stimulants is a solution of 11 gum arabic.

solution (50% gum arabic)

1500 g of gum arabic is mixed with 1500 g of warm water (50 ° C). The mixture is left to stand for about 40 hours.

Q recipe

200 g sugar (25.6%) g water g dextrose (10.3%)

500 g of gum arabic (6; 1%) (solution 11)

Ingredients included:

I 4 ml of 10% nicotine base

II 1 ml 50% tobacco as flavoring agent Ig

III 5 g Na ₂ CC> ₃ + 5 g NaHCO ₃

Mix water and sugar and heat until completely dissolved. Add dextrose and heat to 116 ° C (heating time 14 minutes). Add the gum arabic and mix until uniformly distributed in the mixture. Bring the mixture to a low heat for 26 minutes until clear. The mixture was then allowed to stand for 155 min. at about 30 ° C and then foam is scraped off its surface.

Annexes I and II

Nicotine content: 0.5-1.0 mg / g Flavoring tobacco content 1.0-1.5 mg / g pH 5.0

Like ę ¹ and Q ² + III

Nicotine content: 0.5-1.0 mg / g

Flavoring tobacco content: 1.0-1.5 mg / g

Well, C0.

'2 3

NaHCO

3 'pH:

about about about

1,

1.

9,

R prescription

200 g sugar (25.8%) g water g dextrose (9.8%)

500 g of gum arabic (64.4%) (solution 11) Ingredients:

I:

II:

IV:

V:

VI:

VII ml 10% nicotine base 1 ml 50% flavored tobacco lg 7.5 g Na2CC> 3 dissolved in 15 ml water

7.5 g of NaHCO3 dissolved in 15 ml of water g of Na2CO3, dissolved in 5 ml of water g of NaHCO3, dissolved in 5 ml of water

The mixture is boiled as described in recipe Q for the following parameters:

at

Boiling point: 120 ° C Welding time 12 min Slow boiling time: 28 mins Settling time: 150 min "1 ·" 2 R and R Add I + II + IV + V Nicotine content: 0.5-1.0 mg / g Quantity of flavoring tobacco: 1.0-1.5 mg / g Na ₂ CO ₃ : about 0.9% NaHCO ₃ : about 0.9% pH: about 8.0

2

Equivalent to R + R + VI + VII

Nicotine content:

Quantity of flavoring tobacco:

0.5-1.0 mg / g 1.0-1.5 mg / g

Na ₂ CO ₃ : NaHCO-,:

about about pH:

3

Mixture R + Q Nicotine content: Flavoring tobacco content: Na ₂ CO ₃ :

NaHCO

_3'P H:

All examples labeled Q i

2.3%

2.3%

9.0 with starch at 50.

0.5-1.0 mg / g 1.0-1.5 mg / g about 1.8% about 1.8% about 9.0 r R dried in molds

Note: In all cases, the amount of various compounds in the total mixture calculated on a dry basis. In addition, the solutions must not be reheated to avoid the formation of CO 2 after the addition of carbonate buffer and before drying in starch molds.

Determining the structure profile

The determination of the structure profile according to the above method of Sanderson et al., Ibid, was carried out according to the following methodology;

(a) Methodology:

A cylindrical sample is made 15 mm in diameter and 7-10 mm high and placed between two plates of a material testing device (J.J. Instrument M3OK, Lloyd Instrument, PZC). Around the plates there is a heating element that maintains a constant desired temperature.

The sample is compressed twice at 50 mm / min up to 70% of its original height and at the same time the material-dependent resistance force of the sample is measured and recorded.

After the first compression, the pressure plates are returned to their original position and the second compression stage is started immediately.

(b) Production of sample

For structure analysis, the samples are prepared by incorporating one or more stimulant formulations into a mold having a 15 mm inside diameter and a pressure piston. This mold, together with its contents, is placed in an oven at 80 ° C for 10 to 15 minutes. Once removed from the oven, the piston is pressed with a force of about 3 kg until a stable, room-temperature form is obtained. The mold and its contents are then cooled with liquid nitrogen and a sample of a particular structure is removed from the mold.

(C) Test Conditions

Samples for structure analysis are packed in a waterproof polyethylene package and stored at the required temperature, eg 35 ° C, for 24 hours.

Measurement of disintegration time

In some cases, the disintegration time was measured according to Ph. Eur. 2 Ed., V.5.1.1, using the following methodology:

(a) Methodology. Samples of 10 mm x 10 mm x 5 mm tested and weighing 0.5 to 1.5 g are placed in cylindrical glass tubes, stored in a special rack, and suspended in clean water at 37 ° C using a Pharma Disintegrator PT 21 apparatus.

Disintegration time is expressed as the time required for complete disintegration of the sample.

(b) Measurement of pH The pH is measured with a pH meter, such as Metrom 691.

Results

The results are given in Tables 1 and 2.

table

Structure The parameter BU Manufacture O'I CII Fl M'II M'III 2 Strength (n / cm) 690 170 1960 450 310 12βθ 2 Hardness (n / cm) 100 20th 270 80 60 210 Fragility (%) > 30 > 30 > 30 > 30 > 30 > 30 Adhesion (%) Λ. 0 -0 -0 ~ 0 ~ 0 Elasticity (%) 88 83 88 86 87 91 Cohesiveness (%) 50 44 54 68 70 61

Note: The structure parameters were measured at 35 ° C.

table

Disintegration

Manufacture BI CI FU O'II O'III Disintegration time (min) 31.6 32.0 28.0 33.6 —-Y = —e— - 38.5

Note: Disintegration time was set at 37 ° C.

The structure parameters and disintegration time of stimulant formulations prepared according to A-R formulations were within the ranges specified in claim 1 of the invention.

The buffering capacity of the stimulant formulations of the present invention is illustrated by measuring the pH of 1.0773 g of the sample prepared according to the recipe R having a disintegration time of 25-26 minutes. The following pH values were obtained:

Time (min) pH

8.66

8.84

8.95

9.01

8.89

DEFINITION OF INVENTION

Claims (15)

DEFINITION OF INVENTION 1. A salivary soluble preparation, characterized in that it contains an active ingredient containing 5 to 10 mg of nicotine or other alkaloids of a similar action and auxiliary components in a gel prepared in the presence of a water-binding gel-forming agent having the following structural profile. parameter values obtained from structural analysis: (a) Robustness, i.e. module greater than 100 n / cm; b) Hardness, i.e. maximum force applied in first compression stage greater than 5 η / οπΛ c) Fragility, i.e. size of deformation required for gel disintegration, expressed as a percentage - more than 30% ·, d) Adhesion, i.e. the ratio of the negative peak area between the two compression stages and the first peak is between 0 and 70%. e) Elasticity, i.e. the ratio 100x (D-d) / D, where D is the height (cm) before the first compression step and d is the residual deformation of the specimen (cm) before the second compression step within the range of 25-100%; f) Cohesiveness, i.e. overall operating ratio between the first and second compression stages within the range of 25-100%; and having a disintegration time set at 37 ° C using a disintegration tester according to European Pharmacopoeia II, 5-60 min. within. 2. Stimulant preparation according to claim 1, characterized in that the values of its structural profile parameters are within the following limits: '2 (a) strength greater than 200 n / cm; (b) hardness greater than 25 n / cm; (c) more than 30% brittleness; (d) Adhesion, 0 to 40%; (e) elasticity within the range 50-100%; (f) cohesiveness within the range 40-100%; and disintegration time 6-45 minutes. within. 3. Stimulant preparation according to claim 1 or 2, characterized in that the values of its structural profile parameters are within the following limits: a) strength - higher 2 for 400 n / cm b) hardness - 80 to 300 n / cm -1; c) fragility - more for 30%; d) adhesion - from Q up to 20%; e) elasticity - 30-100 within%, and disintegration time - 15-45 minutes. within. 4. Stimulant preparation according to any one of claims 1 to 3, characterized in that the gel-forming agent is gelatin or one or more synthetic or natural polysaccharides, preferably used in the confectionery industry. of polysaccharides. 5. A stimulant according to any one of claims 1 to 3, wherein the gelling agent is selected from the group consisting of: agar, algin, carrageenan, garlic, gum arabic, gum resin, tragacanth gum, karaya gum. , pseudo-locust strain, xanthine resin, preferably gum arabic and carrageenan, and in particular gum arabic. 6. A stimulant according to any one of claims 1 to 5, characterized in that one or more synthetic or natural flavoring compounds derived from essential oils, essences, fruit juices as well as flavoring agents are added thereto. ground vegetative parts of plants such as tobacco, coffee, tea, mint. 7. Stimulant preparation according to any one of claims 1 to 6, characterized in that it contains one or more vitamins and minerals as additives. 8. Stimulant preparation according to any one of claims 1 to 7, characterized in that it contains physiologically acceptable buffering substances or agents as additives. Stimulant preparation according to claim 8, characterized in that the amount of buffer or agent in the preparation is such that the saliva pH is maintained within the range of 8-10 during the disintegration of the preparation. 10. A simulation preparation according to claim 8 or 9, wherein the amount of buffer or agent in the preparation is from 5 to 50 mg. 11. Stimulant preparation according to any one of claims 8 to 10, characterized in that it comprises a buffering agent or an agent consisting of alkali metal carbonates, bicarbonates, phosphates and / or hydrophosphates. 12. Stimulant preparation according to any one of claims 1 to 11, characterized in that it comprises nicotine in an amount ranging from 0.5 to 5.0 mg, preferably from 1.0 to 1.5 mg, from 1 to 10 mg. 5 to 2.5 mg or 2.5 to 3.0 mg to achieve nicotine stimulation. 13. Stimulant preparation according to any one of claims 1 to 12, characterized in that release of a sufficiently constant amount of nicotine from the preparation is achieved by uniformly distributing it throughout the weight of the preparation. 14. The stimulant formulation according to any one of claims 1 to 12, wherein the differentiated release of nicotine from the formulation, comprising initial, basic and sustained release of nicotine, is obtained by unevenly distributing it in the multilayer structure of the formulation. 15. Stimulant preparation according to any one of claims 1 to 14, characterized in that it is very convenient to attach to the hard palate.