Ball-shaped lipoic acid composition

FIELD: medicine, pharmaceutics.

SUBSTANCE: composition for treating oxidative stress comprises ball-shaped lipoic acid or one of salts thereof, and at least one lipophilic medium. The lipoic acid balls represent particles consisting of an inert core (a nucleus) coated with lipoic acid which is coated with a first layer of an isolating polymer, and with a second polymer layer resistant (stable) at gastric pH. What is also described is a preparation for treating oxidative stress with an unified dose containing the above composition. The preparation is presented in the form of a soft gelatin capsule.

EFFECT: compositions according to the invention are stable in the lipophilic medium.

22 cl, 15 ex

 

The technical field to which the invention relates.

The present invention relates to a new composition based on balls (granules) lipoic acid in a lipophilic medium, optionally in combination with other active ingredients.

The level of technology

Lipoic acid, 1,2-ditiolan-3-pentane acid, also known as thioctic acid, is the active ingredient with antioxidant activity, it is used in the treatment of various pathologies, for example, diseases of liver and biliary diseases, neuropathies of different origin, hypercholesterolemia, dyslipidemia, poisoning by mushrooms, cancer and other diseases. There are significant problems in the manufacture of the drug lipoic acid because of its chemical-physical characteristics: it is a yellow powder with a melting point of 60-61°C and with a distinctive and aggressive smell and taste and has a tendency to polymerization by means of bond-S-S - education glue; it is practically insoluble in water and relatively soluble in ethanol.

Therefore, it is difficult to produce a stable pharmaceutical composition containing lipoic acid.

Patent application EP 1325747 relates to biologically active additive to food on the basis of numerous components, including lipoic acid. This document does not decree is by pre-treatment of lipoic acid and therefore, it is used without processing, in the form of powder. As already mentioned, the processing lipoic acid is difficult due to the above serious problems, and the stability of the compositions that contain it, it is not guaranteed. In addition, due to the numerous components in addition to the above applications, the interaction between lipoic acid and various components, and these interactions not only affect the stability of the composition, but also lead to the destruction of a significant part of lipoic acid and subsequent reduction of its title. The titer of lipoic acid in the composition was evaluated on the market that performs the sale of the product described and claimed in EP 1325747 and found that the quality of present lipoic acid is worse than the declared quality, this is proof of the fact that the composition is not stable and that it is present in the lipoic acid undergoes decomposition. Neither nature nor the pharmacological effects of these degradation products is not known.

In the above patent EP 1325747 also described the combination of lipoic acid to gamma-linolenic acid and selenium or its derivatives. Selenium or its derivatives are important components for the stability of the composition in the stomach. It was also noted that at the concentrations used gamma-linolenic acid is not specified, and since we know that this acid is commercially available as mixtures containing acid at various concentrations, for example, from 9 mass./wt.% to about 40 wt./wt.%., the number of gamma-linolenic acid is actually used in the described compositions is not installed.

Disclosure of inventions

Recently, the author of this application was registered with the patent application (MI2006A001024-PCT/EP2007/055124), claiming the new bulbs on the basis of lipoic acid, and these balls are covered so that they are stable and easy to manufacture, and therefore they are suitable for receiving, for example, pharmaceutical compositions or food and/or diet products.

The present invention is the provision of new compositions based on lipoic acid, which eliminate the disadvantages of the known prior art, are easily produced and are stable for a long time.

The next task of the present invention is the provision of compositions based on combinations of lipoic acid and other active ingredients, stable lipophilic environment.

It was found that the beads containing lipoic acid, according to the patent applications MI2006A001024 and RSTER/055124, are particularly stable in the lipophilic environment. These results and the following led the authors of this patent application to research in the development of compositions for oral administration, contains lipoic acid, which is stable, which is easy to manufacture and which is suitable for combining multiple active ingredients, thereby eliminating interactions and chemical reactions between them and thus increasing the stability of the composition.

The implementation of the invention

Thus, according to one of its aspects, the invention relates to compositions containing balls lipoic acid or one of its salts, introduced in at least one lipophilic environment.

The expression "balls lipoic acid" means, according to the present invention, the particles comprising an inert core (kernel), covered lipoic acid, in turn, further covered with the first layer of insulating polymer material and the second polymeric layer may be resistant to gastric pH.

These balls are described in detail in patent applications MI2006A001024 and PCT/EP2007/055124, registered on may 25, 2006 and may 25, 2007, respectively, and is included in context by reference. Some details of these balls nevertheless provided also in the following description.

Lipoic acid according to the present invention is in racemic form or enantiomeric R - and/or S-form with any degree of purity. The use of mixtures of the two enantiomers in any vzaimootnoshenii also included in the present invention.

According to the present invention, it is also possible to use salts of lipoic acid. In the present description reference lipoic acid also includes a salt thereof, provided that they are acceptable from a pharmaceutical and/or nutritional point of view. Specified in the context of the amount of lipoic acid refers to an acid form and not the form of its salts.

"Lipophilic environment" in the context means at least one filler or at least one lipophilic component, pharmaceutically acceptable or in any way edible. You can also apply a mixture of fillers or lipophilic components.

According to a preferred aspect of the present invention, a lipophilic environment is a lipophilic component having favorable properties for the human body or an animal, for example, the antioxidant properties or properties that regulate the metabolism of fats. Alternatively, a lipophilic environment can be inert environment, which should be pharmaceutically acceptable, or in any way edible, the sole purpose of which is to act as a carrier for the balls lipoic acid and any other active ingredients and additives. If lipophilic environment is inert lipophilic component, for example, edible oil composition of the invention Bud is t, it is preferable to contain at least one other active ingredient.

"Active ingredient" in the context means the component is understood as one molecule or mixture of molecules with activity, favorable for the organism, for example, drug or food Supplement.

According to a preferred variant implementation, the lipophilic environment contains EPA ((5Z, 8Z, 11Z, 14Z, 17Z) - 5,8,11,14,17-eykozapentaenovuyu acid) and DHA ((4Z, 7Z, 10Z, 13Z, 16Z, 19Z) - 4,7,10,13,16,19-docosahexaenoic acid). In this case, the lipophilic environment can be either inert lipophilic component, in any case pharmaceutically acceptable and edible or lipophilic environment, which by its nature contains EPA and DHA.

According to a preferred variant implementation, lipophilic environment is fish oil or fat, cod liver. These fats can be purchased in purified form and shape, enriched with omega 3, particularly EPA and DHA.

Fish oil or fat, cod liver contain polyunsaturated fatty acids called omega 3 and including EPA and DHA.

According to a preferred variant implementation, lipophilic environment is fish oil or fat, cod liver in purified form and shape, enriched with omega 3, especially enriched in EPA and DHA.

According to a particularly preferred variant implementation, the lipophilic environment contains EPA, DHA, or in General, omega 3 in purified form.

According to another preferred variant implementation, lipophilic environment contains linolenic acid, especially gamma-linolenic acid. Gamma linolenic acid is an essential fatty acid, also known as ALA, 18:3;

ALA is also a member of the family of omega 3. According to another variant implementation, the lipophilic environment contains gamma-linolenic acid as the only other active ingredient (in addition to lipoic acid) or in combination with other active ingredients mentioned above (EPA, DHA, or in General, omega 3, fish oil or fat, cod liver).

The terms "lipophilic environment, which contains gamma-linolenic acid"includes oil derived from plant extracts, rich in gamma-linolenic acid, such as borage oil and evening primrose oil and other oils.

According to another preferred variant implementation, lipophilic environment also contains benfotiamin.

According to another preferred variant implementation, the lipophilic environment contains gamma-linolenic acid and also contains benfotiamin.

The composition of the invention may also contain other active ingredients specified above. These additional active agents can be in liquid or solid form.

With regard to prior art, the invention has very valuable to becoming the PTO in preventing interaction between lipoic acid, very reactive component, which is difficult to handle, and lipophilic environment and any other components present. In fact, the balls separate lipoic acid other ingredients creating a physical barrier.

In addition, the use of balls and the resulting physical separation lipoic acid from the rest of the composition allows the use of the drug components in high purity and concentration.

In fact, the physical separation provided by the balls, allows you to apply one or more lipophilic components with a high degree of purity, i.e. without the necessity of dispersing components within an inert solid and/or liquid mass, in order to limit the interaction between them within the composition.

For example, in the case of gamma-linolenic acid, selected for the composition of the invention can be applied gamma-linolenic acid oils (usually natural extracts, for example, borage or evening primrose), at concentrations equal to the maximum purity, currently available on the market (from 20% to 40% or more) with or without adding traces of stabilizers, such as vitamin E and vitamin C.

Balls lipoic acid are also very applicable in special cases, in which the possible combinations provide for the use of the group of active ingredients, available only in liquid form and at relatively high concentrations. As the only example, the authors could specify (in addition to the above lipophilic components, i.e. fish oils, DHA, EPA and gamma-linolenic acid), evening primrose oil, a natural source of gamma-linolenic acid, conjugate linoleic acid, Flaxseed oil, gamma-tocopherol, hemp oil, tocotrienols and some vitamins.

It should be clear that the use of components with high purity is the basis for restricting the size of the dosage form, the actual size of the capsules should always be considered as a critical parameter of the application of the compositions of the invention, the greater the possibility of use in the preparations of the active ingredients with high purity in terms of comparable stability, the smaller the size of the capsules, which can be used as the liquid components in high purity allow you to apply the capsules are smaller than the size of the capsules that you want to ensure that they contained the same number of components when applied on inert carriers.

As indicated, is preferably used balls lipoic acid balls are described in MI2006A001024 and PCT/EP2007/055124. These balls are preferably balls, consisting of an inert core coated with lipoic acid,in turn, then covered with the first layer of insulating polymer material and the second polymeric layer may be resistant to gastric pH.

Specified inert core preferably consists of sucrose, microcrystalline cellulose or other inert substances. The first polymer layer is preferably formed from hydroxypropylmethylcellulose or hydroxypropylcellulose, while the second layer contains one or more compounds selected from cellulose ethers, polivinilatsetatftalat, copolymers of methacrylic acid and methylacrylate esters, acetate-cellulose phthalate, phthalate of hydroxypropylmethylcellulose, acetate-phthalate of hydroxypropylmethylcellulose, acetate-succinate of hydroxypropylmethylcellulose, Eudragit® and shellac. Details of the method of obtaining beads described above, and various types of balls that you can get presented in the above patent applications.

Balls predominantly contain from 5 to 60% lipoic acid, preferably about 50% (wt./mass.).

The size of the balls is also quite critical parameter, since it is preferable to work with average diameters of less than one millimeter (1000 microns)in order to minimize the risk of accidental capture bead in the wall of the gelatin during the phase of closure, resulting in what is rupture or loss of contents. Mainly used balls with diameters between 100 and 1000 microns, preferably between 300 and 600 microns.

Compositions of the invention are predominantly made in the form of standardized doses, for example, in the form of gelatin capsules, hard or soft, the latter are particularly preferred.

Soft gelatin capsules can contain in a sealed environment protected all the components that can be included in the matrix, forming a capsule. In General, gelatin capsules can be filled, as is well known in this field, using one or several filling systems simultaneously. In the first case, the usual practice is the preparation of suspensions and/or emulsions, which are uniformly dissolved or suspended all the ingredients, before taking a volumetric filling and dosing, i.e. apply one pump, which loads the suspension of balls and a lipophilic environment plus any other substances, prior and mixed to ensure homogeneity, thereby allowing you to obtain the desired volumetric dose of the active ingredients.

Alternatively, when using several filling systems, you can use two separate lines, which synchronously load the oil component and a solid component (beads or granules), sootvetstvenno is, to provide the desired dose.

Drugs with standardized doses according to the invention can contain, for example, from 10 to 1000 mg lipoic acid, preferably from 100 to 800 mg, for example, approximately 200, 300, 400, 500 or 600 mg

Lipophilic environment can contain these drugs with standardized doses in variable quantities, for example, in the case of capsules in accordance with the size of the capsules, if the lipophilic environment is inert, or in accordance with the concentration of the active ingredients contained therein to obtain the desired dose inside the capsule. Therefore, when a lipophilic environment is a lipophilic component having favorable properties for human or animal specified component is present in amounts typically used in the conventional practice, nutritional and therapeutic areas. These quantities can be entered as one unified dose or more uniform dose throughout the day.

As indicated above, the use of balls prevents interaction lipoic acid with a lipophilic component(s), which can thus be applied practically in a clean and efficient manner. For example, when a lipophilic environment is fish oil or fat, cod liver, this component may be present in quantities is between 100 and 1000 mg, preferably between 500 and 800 mg, for example, 400-600 mg of Fish oil or fat, cod liver mainly can contain not less than 60% EPA and DHA in a variable mutual respect, for example, in respect of approximately 2:1.

When the lipophilic environment consists of omega-3 essentially of a mixture of EPA and DHA, it is present in quantities between 100 and 3000 mg or even more. When the lipophilic component contains gamma-linolenic acid, this component is used in such amounts to approximately 300-1000 mg, for example, approximately 400-600 mg, for example, approximately 500 mg of pure gamma-linolenic acid, to enter on the day. This number can be contained in one unified dose or can be divided into several uniform doses. Such drugs with standardized doses are preferably administered orally, once or several times a day.

In the composition of the invention balls lipoic acid dispersed in a lipophilic environment while maintaining their physical integrity, and the resulting composition is particularly stable. The resulting composition, therefore, is a mixture of balls lipoic acid and lipophilic environment (consisting of one or more lipophilic components).

According to a particularly preferred aspect, the invention relates to compositions in the form of gelatin is apsel, preferably soft, containing balls lipoic acid or a salt thereof, as defined above, and a lipophilic component selected from fish oil, omega 3, and mixtures thereof.

According to the following particularly preferred aspect, the invention relates to compositions in the form of gelatin capsules, preferably soft, containing balls lipoic acid or its salts indicated above, and the lipophilic component, which is gamma-linolenic acid, if necessary, in combination with benfotiamine. Benfotiamin and any other solid active ingredients can be added directly mixing the composition of the invention. However, according to a preferential option for the implementation of the present invention, benfotiamin and any additional solid active ingredients used after granulation, if necessary, in combination with inert additives, well known in this field. According to a preferred variant implementation, produce balls that have physical properties (bulk density, flowability, etc.), similar to the physical properties of the balls lipoic acid used in the compositions of the invention. This allows you to get even more stable composition, which can be easier to homogenize.

The composition of the invention possesses antioxidant action is receiving and is applicable for the treatment of oxidative stress and in any case, all pathologies, which shows lipoic acid.

The use of a composition of the invention for obtaining a medicinal product for the treatment of oxidative stress is the next subject of the present invention. It is proved that the composition of the invention is effective and well tolerated in the absence of selenium or its derivatives.

The composition of the invention may also contain other active ingredients in liquid or solid form, mostly one or two additional active ingredient, provided that they are stable in a lipophilic environment.

Due to the presence of lipophilic environment, the interaction between the balls lipoic acid and any other present active ingredients significantly reduced with a huge advantage for the stability of the composition. That lipoic acid is in the form of coated beads, therefore, further reduces the risk of interactions and destruction of components. This clearly represents an important technical step in the direction of the manufacture of preparations of the active ingredients, which, for example, have low stability, low solubility and/or are very reactive.

Said additional active ingredients, in solid or liquid form, is selected, for example, asbolutely funds drugs active in the treatment of diabetic neuropathy, hepatoprotective tools, medicines, active in the prevention of alcohol abuse, drugs, active supportive treatment for oxidative stress caused by chemotherapy, antagonists of angiotensin II, ACE inhibitors, antiviral drugs, anticancer drugs, and antidepressants, provided that, as stated above, they are stable in a lipophilic environment.

The active ingredients can be, for example, selected from gabapentin, pregabalin, olmesartan captopril, interferon, acamprosate and megestrol.

Compositions of the invention may include components with antioxidant activity, such as acetylcysteine, acetyl-1-carnitine, acetate, alpha-tocopherol (vitamin E), beta-carotene, Biotin, boron, chlorophyll, chrysin, Lycopodium and its extracts, cocoa flavonoids, coenzyme Q10, conjugated linoleic acid, copper, Coptis chinensis, also known as huang lian, curcuminoid, daidzein, licorice, including its extracts, deprived of glycyrrhizic acid, a sulfoxide, fish fats in General (cod, herring, tuna, salmon etc), oil evening primrose (Oenothera Biennis, a natural source of gamma-linolenic acid), Flaxseed oil, folate, gamma-tocopherol, garlic, genistein, Germany is, ginseng, glucosamine, peptide derivatives, glutamine, glutathione, glycine, glycitein, grape seed oil, proanthocyanidins grape, green tea catechins, extracts or parts of Viola tricolor, hemp oil, hesperetin, hesperidin, hydroxyethylrutoside, indole-3-carbinol, hexaphosphate Inositol, lactoferrin, lactulose, 1-arginine, 1-carnitine, 1-cysteine, 1-cystein, 1-methionine, 1-theanine, lycopene, magnesium, melatonin, extracts or part of the artichoke (Sylibum marianum), nicotinamide, one, Pantothenic acid, propolis, pumpkin seeds, Pycnogenol ® (extract of pine bark), pyruvate, quercetin, resveratrol, Riboflavin vitamin B2, rutin, secoisolariciresinol, diglucoside (sdg), shark cartilage, soy isoflavones, soybean protein, spirulina, sulforaphane (derived glucoraphanin), taurine, thiamine (vitamin B1), tocotrienols, Vinpocetine, vitamin A, vitamin B6, vitamin C, vitamin D, vitamin E, vitamin K, wheat malt and its derivatives, whey proteins and zinc. Compositions of the invention can include the following components: L-alanine, L-arginine HCl, L-cystine, L-creatine, DL-phenylalanine, L-phenylalanine, L-glutamine, L-isoleucine, L-histidine, L-histidine HCl, L-leucine, L-lysine HCl, L-melatonin, L-ornithine, alpha-Ketoglutarate, L-ornithine HCl, L-Proline, L-serine, L-tyrosine, L-tryptophan, L-valine, azetilcarnitin, propionylcarnitine, folic acid, lutein, zeaxanthin, rice oil, t is ceny, Tocopherols, tocotrienols, ginseng, gamma orizanol, policosanol, ceramide, sennoside, multivitamin complexes, sugar, maltodextrins, flavonoids, hesperidin, naringin, diosmin, hesperidin, metalhalide, troxerutin, lycopene, resveratrol, geromin and propolis.

Compositions of the invention may also contain conventional additives and excipients known in this field, for example, stabilizing agents and suspendresume agents. Drugs with standardized doses containing composition of the invention comprise the following object of the present invention.

Compositions and preparations with standardized doses of the invention receive according to methods known to the expert in this field.

Compositions of the invention can be obtained by mixing the various components, for example, by adding different components to the selected lipophilic environment.

Drugs with standardized doses according to the invention are obtained from the use of a composition of the invention according to methods well known in the field.

Experimental part

Getting 1

Getting balls lipoic acid

Balls lipoic acid get, as described in MI2006A001024 and PCT/EP2007/055124.

In short, the balls get through the following stages:

(i) lipoic acid is applied to the inert core, the floor is tea active core;

(ii) on specified inert core, put a layer of polymer insulating substance;

(iii) in an active, covered with a layer of the core, obtained in stage (ii), put the second polymer layer and

(iv) thus obtained core is dried and removed.

Details of the used substances and methods presented in the previous description and the above-mentioned patent applications.

The following examples use the balls lipoic acid, containing 50 wt./wt.% active ingredient (lipoic acid).

Example 1

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
fish oil500 mg

Example 2

Get a soft gelatin capsule containing

lipoic acid in the form of a ball500 mg
fish oil800 mg

Example 3

Get a soft gelatin capsule containing

lipoic acid in the form of a ball400 mg
Omega 32000 mg

Example 4

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
fish oil700 mg
gabapentin300 mg

Example 5

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
fish oil700 mg
pregabalin120 mg

Example 6

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
fish oil700 mg
gabapentin300 mg
coenzyme Q1030 mg

Example 7

Get a soft gelatin capsule containing

lipoic acid in the form of a ball200 mg
coenzyme Q1030 mg

vegetable oil (to balance)

The following examples use the balls lipoic acid containing 50% active ingredient (lipoic acid), and lipophilic environment that contains gamma-linolenic acid at a concentration of 20-40% of the active ingredient (all concentrations are expressed in wt./wt.%).

Example 8

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
gamma-linolenic acid, 40%312.5 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 4 times a day.

Example 9

Get a soft gelatin capsule containing

lipoic acid in the form of a ball400 mg
gamma-linolenic acid, 40%416 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 3 times a day.

P is the iMER 10

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
gamma-linolenic acid, 20%625 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 4 times a day.

Example 11

Get a soft gelatin capsule containing

lipoic acid in the form of a ball400 mg
gamma-linolenic acid, 20%832 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 3 times a day.

The following examples use the balls lipoic acid containing 50% active ingredient (lipoic acid), a lipophilic medium containing gamma-linolenic acid at a concentration of 20-40% of the active ingredient, and the balls benfotiamine having a concentration of 50-80% of the active ingredient (all concentrations are expressed in wt./wt.%).

Example 12

Get a soft gelatin capsule containing

lipoic acid in the form of the e ball 300 mg
gamma-linolenic acid, 40%312.5 mg
benfotiamin, 80%62.5 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 4 times a day.

Example 13

Get a soft gelatin capsule containing

lipoic acid in the form of a ball400 mg
gamma-linolenic acid, 40%416 mg
benfotiamin, 80%83 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 3 times a day.

Example 14

Get a soft gelatin capsule containing

lipoic acid in the form of a ball300 mg
gamma-linolenic acid, 20%625 mg
benfotiamin, 50%100 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 4 times a day.

Por what measures 15

Get a soft gelatin capsule containing

lipoic acid in the form of a ball400 mg
gamma-linolenic acid, 40%832 mg
benfotiamin, 80%133 mg

stabilizing and suspendresume agents (to balance),

which preferably is administered 3 times a day.

1. Composition for treating oxidative stress, containing balls lipoic acid or one of its salts, which are particles consisting of an inert core (kernel), covered lipoic acid, which in turn is covered with a first layer of insulating polymer material and second polymer layer, resistant (stable) gastric pH value entered at least one lipophilic environment.

2. The composition according to claim 1, characterized in that the specified lipophilic environment is pharmaceutically acceptable and/or edible lipophilic component, inert or having advantageous properties for human or animal.

3. The composition according to claim 2, characterized in that the lipophilic environment has antioxidant properties.

4. Composition according to claims 1-3, otlichayushiesya, that said lipophilic environment contains EPA and DHA.

5. Composition according to claims 1 to 3, characterized in that the lipophilic environment selected from fish oil or grease cod liver.

6. The composition according to claim 5, characterized in that the lipophilic environment selected from fish oil and grease cod liver in purified form and enriched with omega 3.

7. The composition according to claim 6, characterized in that the lipophilic environment selected from fish oil and grease cod liver in purified form and enriched with EPA and DHA.

8. The composition according to claim 1, characterized in that the lipophilic environment contains gamma-linolenic acid.

9. Composition according to claims 1 to 3, characterized in that the lipophilic environment contains gamma-linolenic acid.

10. The composition according to claim 1, characterized in that it also contains benfotiamin.

11. The composition according to claim 1, characterized in that it is in the form of drugs with standardized doses.

12. The composition according to claim 11, characterized in that it is in the form of gelatin capsules.

13. Composition according to any one of § § 11 or 12, characterized in that it contains from 10 to 1000 mg of lipoic acid.

14. The composition according to item 13, characterized in that it contains from 100 to 800 mg of lipoic acid.

15. The composition according to claim 11, characterized in that it contains between 100 and 1000 mg of fish oil or grease cod p is Cheney in purified form.

16. The composition according to claim 10, characterized in that it contains between 100 and 1000 mg of a mixture of EPA and DHA.

17. The composition according to claim 11, characterized in that it contains 100-1000 mg of gamma-linolenic acid.

18. The composition according to claim 1, characterized in that it also contains an active ingredient selected from gabapentin, pregabalin, olmesartan, captopril, interferon, acamprosate and megestrol.

19. The composition according to claim 1, characterized in that it also contains the active ingredient with antioxidant action.

20. The use of a composition according to any one of the preceding paragraphs to obtain drugs for the treatment of oxidative stress.

21. Drug for the treatment of oxidative stress with a uniform dose containing composition according to any one of claims 1 to 19.

22. The drug in item 21, which is a soft gelatin capsule.



 

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1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly, the use of human lactoferrin apo-form as an antihypoxant and a hypoxia inducible factor-1 alpha stabiliser.

EFFECT: invention provides the use of the natural iron chelator lactoferrin, no toxicity, hypoallergenicity, an ability to penetrate through the bowel into the blood flow and through the blood-brain barrier.

2 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: method involves the introduction of lead acetate and a calcium-containing substance. For this purpose, 10% calcium chloride 0.3 ml per 200 g is introduced in rats once a day daily through a probe into a stomach for 20 days. In 4 days from the beginning of the experiment, it is combined with the subcutaneous introduction of lead acetate 40 mg/kg at a metal basis for 16 days.

EFFECT: method is easily reproducible, cost-saving and moreover provides relieving toxic action of lead effectively.

5 tbl, 2 dwg, 1 ex

Sorption container // 2452450

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely to sorption container, which includes zeolite sorbent, located in cavity of membrane from flexible inelastic porous material - dialysis film, whose pore size is smaller than size of sorbent particles, characterised by the fact that sorbent dispersity constitutes 0.15-10 mcm, in addition, as sorbent, used are natural zeolites of volcano-sedimentrary type deposits, selected from Vanginskoye and/or Vanchinskoye and/or Vodorazdelnoye and/or Lyutogskoye and/or Chekhovskoye and/or Shivertuiskoye and/or Khonguruu deposits, with content of clay component not more than 30% of volume, and mineral admixtures, volcanic glass and/or, feldspar and/or quartz not more than 5%, said zeolites being used in mixture with zeolite of Lyulinkoye deposit, whose part constitutes not less than 5% of mixture volume.

EFFECT: specific surface area of sorbent increases (due to providing possibility of finer reduction), which makes it possible to reduce number of used sorption containers, in addition, labour-consumption of treatment process is reduced (due to reduction of number of container replacements, eliminating necessity to wound cleaning operations) and acceleration of their healing.

3 cl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing interferon-coated cephalosporin microcapsules. The declared method is characterized by mixing 1% aqueous solution of human leukocyte α- or β-interferon, cephalosporin powder and preparation E472c as a surfactant. The prepared mixture is stirred until the reaction components are fully dissolved, and after a transparent solution is generated, methanol 1 ml as a first non-solvent and then isopropyl alcohol 5 ml as a second non-solvent are slowly added drop-by-drop, then filtered, washed in acetone and dried.

EFFECT: invention provides preparing the high-yield cephalosporin microcapsules and ensuring the loss reduction.

8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, and represents a method for preparing medicine microcapsules by non-solvent addition differing by the fact that the medical preparations are presented by the cephalosporin preparations, while a coating is polyvinyl alcohol that is precipitated by the addition of non-solvents that are carbinol and acetone at -25°C.

EFFECT: invention provides simplifying and accelerating the process for preparing the water-soluble cephalosporin microcapsules in polyvinyl alcohol, providing loss reduction in preparing the microcapsules (higher yield-mass).

16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a microcapsules for preventing or treating hepatic disorders. The microcapsules for preventing or treating hepatic disorders containing a capsule coating, an encapsulating suspension of a therapeutically effective hepatocyte count in a physical contact with a hepatocyte-stimulating amount of erythropoietin. A method for preparing microcapsules involving preparing the suspension of the therapeutically effective hepatocyte count and the hepatocyte-stimulating amount of erythropoietin to bring them in physical contact with each other, and encapsulating the suspension of hepatocytes and erythropoietin in a biologically compatible capsule shell so that to form a microcapsule. A method for preventing or treating a hepatic disorder in an individual in need thereof involving administering the microcapsules in the individual in need thereof. The method for introducing the hepatocytes in the individual involving administering the microcapsules in the individual. A method for hepatocyte culture in a culture medium involving hepatocyte culture in the microcapsules in the appropriate culture medium.

EFFECT: microcapsules are effective for preventing or treating the hepatic disorders.

20 cl, 1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to capsule suspensions prepared by coacervation, and to methods for reducing leakage of the capsule content in such suspensions during storage. Substance of the method for reducing leakage of the capsule content consists in storage of the capsules prepared by coacervation, in the capsule suspension containing min. 20 wt %, a moisturiser, which is at least a moisturiser specified in sorbitol, glycerol, polyethylene glycol, propylene glycol, xylitol, erythritol or betaine. What is also presented is the above capsule suspension containing at least one capsule prepared by coacervation and at least 20 wt % of the above moisturiser.

EFFECT: using the above moisturiser in the amount of min 20 wt % provides reducing the leakage rate of the capsule content.

21 cl, 4 tbl, 2 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to iron-enriched food product, which contains iron source in form of solid particles, where particles include core, containing iron alginate, and external layer, which contains calcium alginate, where particles are obtained by method which includes the following stages: (i) formation of core, which contains iron alginate, by contact of bioavailable water-soluble salt of iron and one water-soluble alginate salt, (ii) contact of core with water solution of calcium salt, in concentration, which constitutes from 0.025 M to concentration of lower than solution saturation point, and (iii) separation of obtained solid product. Iron-enriched food product is applied for prevention and treatment of iron deficiency conditions of people.

EFFECT: solid particles are applicable for enrichment of food products with iron and is characterised by improved load ability, as well as possesses good stability under standard storage and application conditions.

11 cl, 9 dwg, 13 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and pharmaceutical industry, particularly to creating a pharmaceutical composition of a submicron emulsion for parenteral administration, having anticonvulsant activity. The composition contains 5-carbamoyl-5H-dibenz-(b,f)-azepine, and additionally it contains soya been oil and sodium deoxycholate in the following proportions, wt %: 5-carbamoyl-5H-dibenz-(b,f)-azepine - 18.5-23.2, soya been oil - 2.1-2.3, sodium deoxycholate - 74.5-79.4. The composition has an average size of the deagglomerated microparticles of 108-132 nm.

EFFECT: composition enables the intravenous intraperitoneal administration of a low therapeutic dose with a high efficacy of the preparation, and reduction of dose-dependent adverse reactions, and extends the range of such preparations.

4 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents microspheres for treating schizophrenia, having a nucleus/coating structure and a spherical shape wherein the nucleus contains ariliprazol in the solid state, and the coating covers the entire surface or most of the nucleus and contains a biodegradable polymer.

EFFECT: invention provides producing the microspheres of ariliprazol characterised by the high content and sustained release of the active substance, and preparing an injectable aqueous suspension of the above microspheres.

17 cl, 18 ex, 14 dwg

FIELD: nanotechnology.

SUBSTANCE: invention relates to the use of nanoparticles for prevention and/or treatment of cancerous diseases, when the nanoparticles are injected with anti-cancer therapeutic agent, and the nanoparticles and anti-cancer agent are simultaneously present in the patient's body. The nanoparticles are free from binding with the anti-cancer medicinal product and have a coating which contains polycondensated aminosilanes.

EFFECT: simultaneous presence of nanoparticles and the anti-cancer therapeutic agent in the body of patients enables to increase the activity of the said anti-cancer agent with simultaneous reduction of the side effects.

12 cl, 1 tbl, 13 dwg, 196 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine. A biocidal capsule for treating and diagnosing in vagina to be used in the biocidal preparation wherein at least one active ingredient is encapsulated with a wall insoluble or minimally soluble in an aqueous environment within the pH range lower than a threshold pH value, but soluble within the pH range higher than a threshold pH value wherein the threshold pH value is found between 4.6 to 6.0 and at least one of the walls and the content contains a tracer substance suitable for colour-coded indication. A tampon contains the biocidal preparation which in case of a vaginal tampon comprises a hygroscopic cylinder (1) preferentially swelling in a cross section under action of fluid, having a longer back flange (2) on an inner end inserted to a posterior vaginal vault, and a peritoneal flange (3) shorter than the back flange; and in between, there is a saddle (4) receiving a vaginal portion of neck of uterus.

EFFECT: invention provides using the preparation for medical and hygienic purposes, preferentially for elimination of pathogens of body surface, body openings, open and closed body cavities.

13 cl, 1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely to pharmaceutical industry and deals with disulfiram preparations. Medical form of disulfiram with prolonged action contains, at least, one microsphere from disulfiram, covered with first stabilising nanosize coating from neutral polysaccharides or gelatin, enclosed in second, spatially linked coating in form of microcapsule from neutral polysaccharides. Invention also deals with method of obtaining medical form of disulfiram with prolonged action.

EFFECT: application of claimed inventions ensures durative effect of prolonged action of disulfiram, stabile kinetics of drug release into tissues, sparing procedure of drug introduction and excludes possibility of its independent removal.

7 cl, 9 ex, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to biotechnology and immunology. What is presented is a method for preparing a vaccine with using reverse latex. The first stage involves preparing an adjuvant composition by dispersion of reverse latex or polymer powder prepared by reverse latex spraying, in a physiologically acceptable solution. The second stage involves mixing the prepared adjuvant composition with an antigen-containing medium for preparing the vaccine composition.

EFFECT: reverse latex adjuvant is characterised by higher safety and possesses the high adjuvant effect both at the level of the humoral response, and at the level of the cell response.

8 cl, 2 dwg, 3 ex

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