Pharmaceutical composition of choline alphocerate expressing nootropic activity and cholinomimetic action, method for making thereof

FIELD: medicine.

SUBSTANCE: invention concerns chemical-pharmaceutical industry, more specifically to a pharmaceutical composition expressing nootropic activity and cholinomimetic action. There is offered original pharmaceutical composition containing choline alphoscerate as an active ingredient in therapeutically effective amount and pharmaceutically acceptable carriers, differing that as pharmaceutically acceptable carriers it contains macrogol (polyethylene glycol 400) and povidone (Plasdone or collidone). There is also offered method for making thereof that enables making a high-yield end product. The pharmaceutical composition produced by the declared method exhibits minimum by-effects, improved bioavailability and prolonged storage stability.

EFFECT: invention can be used for treatment or prevention of CNS diseases and consequences of craniocereberal injuries.

11 cl, 1 tbl

 

The invention relates to the field of pharmaceutical industry, particularly to a pharmaceutical composition having neuroprotective activity and cholinomimetic action.

Today there is an acute problem of mortality from cerebrovascular disease. According to the world health organization mortality from cerebrovascular disease is second only to deaths from heart disease. Prevention of ischemic cerebrovascular disease - relevant medico-social problem due to its prevalence, high incidence of morbidity and mortality in patients with ischemic stroke and vascular dementia. Acute disorders of cerebral circulation (cerebral vascular accident) is one of the leading causes of morbidity, mortality and disability. In the Russian Federation and the CIS countries have a progressive increase in the incidence of this pathology: approximately every 1.5 min at someone from the Russians for the first time evolving stroke. The incidence of stroke in Russia amounts to 450,000 cases per year: only in Moscow the number of acute stroke ranges from 100 to 120 cases per day. Total mortality from stroke in 2001 amounted to 1.28 per 1000 people (men - 1,15 for women to 1.38). Mortality from stroke in our country one of the highest in the world: only in 2000 standardized pokazatel who was 319,8 per 100,000 people. These figures continue to grow steadily. In different countries the mortality of stroke varies from 0.61 to 2.43 per 1,000 population. In Russia onmk take second place in the overall mortality. In the acute period of stroke die 30%, and in the next year after 45-48% of patients. High and indicators of morbidity patients who have had a stroke: 75-80% of survivors lose their ability to work and require long and expensive medical and social assistance.

Modern requirements for therapy of these States determine the need for search and introduction of new highly effective neuroprotective agents with minimal side effects and improved bioavailability.

Among the drugs with neuroprotective activity, special attention is given to drugs that enhance cholinergic processes. This group of nootropics is the most promising because the use of these drugs for the treatment of cerebrovascular diseases experiencing the greatest positive effect. In addition, unlike anticholinesterase drugs this group of nootropics is almost devoid of side effects.

However, the share of such drugs on the Russian pharmaceutical market is small. Currently widespread for the treatment of vascular brain diseases of various origins, the latter is out of traumatic brain injury and cognititive disorders received the original drug Gliatilin® (manufacturer of Italfarmaco/Pharmacor (Italy/Russia)and its generic version of Cerepro® (manufacturer Veropharm(Russia)), containing as active substance alfostserat. In this regard, currently faces the challenge of expanding Arsenal of these funds and the implementation of new highly effective neuroprotective agents.

Alfostserat has a cholinomimetic effect, stimulates mainly the Central cholinergic receptors. The body is split into choline and glycerol. Provides a synthesis of acetylcholine and phosphatidylcholine neuronal membranes, improves the function of receptors and membranes in cholinergic neurons. The drug activates cerebral blood flow, stimulates the metabolism of the Central nervous system, stimulates the reticular formation. Improves mood, stimulates mental activity, improves concentration, ability to memorize and reproduce the received information, optimizes cognitive and behavioral responses, eliminates apathy (Register of medicines of Russia (RLS 2007 (15)). M: "radar", 2007, s).

The author of the present invention has set itself the task to develop a new generic version of the drug Gliatilin® with minimal side effects and improved bioavailability. The set of essential characteristics of the drug Gliatilin® is the closest to the proposed drug and adopted as a prototype.

Put the does is solved by what the author of the present invention was developed to obtain the original pharmaceutical composition having neuroprotective activity and cholinomimetic action and containing as the active ingredient alfostserat in a therapeutically effective amount and a pharmaceutically acceptable carriers, characterized in that as pharmaceutically acceptable carriers it contains macrogol (polyethylene glycol 400) and povidone (plasdone or kollidon). This pharmaceutical composition preferably has the following ratio of components based on 100 wt.% the entire composition:

Alfostserat55,6-75%
Macrogol (polyethylene glycol 400)20-40%
Povidone (plasdone or kollidon)1,6-4,2%
Purified waterto 100 wt.%

According to the invention the inventive pharmaceutical composition is made in the form of soft gelatin capsules. The capsule is a soft gelatin preferably consist of medical gelatin, glycerin, methylparaben, propyl paraben, titanium dioxide, iron oxide yellow (dye), purified water

Selection of components for the claimed dosage form was carried out experimentally.

To give special technological properties of the inventive pharmaceutical composition by the author of the invention was chosen original value (qualitative and quantitative) of auxiliary substances.

In this composition as auxiliary substances used macrogol (polyethylene glycol 400) and povidone (plasdone or kollidon).

Polyethylene glycol 400 (preferably in the amount of 20-40% to 100 wt.% the whole composition is used in the form of pharmaceutical compositions as a filler and gives the flexibility and mobility of the mass, thereby decreasing losses kapsulirovanie.

Povidone (plasdone or kollidon) (preferably in the amount of 1.6 to 4.2% per 100 wt.% the whole composition is used as a stabilizer and helps to preserve the properties of the pharmaceutical composition during long-term storage. In addition, povidone promotes better dissolution of the active substance (choline alfoscerate) in water due to the formation of soluble complex of povidone with choline by alfoscerate.

The technical result of the claimed invention consists, first, in expanding Arsenal of drugs with neuroprotective activity and cholinomimetic action, as well as in the teachings stable over a long period of time the dosage form of the above medicines (4 years, unlike capsules in accordance with the prototype, the retention of which was about 3 years old) with minimal side effects and improved bioavailability.

The following example illustrates (without limitation of the scope of claims), the most preferred embodiments of the invention, and also confirms the possibility of obtaining the claimed pharmaceutical compositions.

In volumetric flask of 1000 ml was placed a polyethylene glycol 400, preferably in the amount of 20-40%, and add the calculated amount of purified water (to 100%).

In clean containers weighed:

alfostserat, preferably 55,6-75% (active substance and all auxiliary components are used for formulations I, II and III in quantities in accordance with table);

- povidone (plasdone or kollidon) (preferably 1.6 to 4.2 per cent);

Into the reactor under stirring consistently placed povidone (plasdone or kollidon), stirred for 5-10 min until complete dissolution. To the resulting solution was added alfostserat, stirred for 10 min until complete dissolution of the components.

Get a pharmaceutical composition in the form of a solution which is passed through encapsulation. The encapsulation process is carried out according to the standard procedure.

Ratio of all components are given in terms of 100 wt.%the whole composition. The output stage is 99.0%. Thus, the method allows to obtain the claimed pharmaceutical composition with the highest possible output.

Part IPart IIPart III
Alfostserat mg200480800
Macrogol (polyethylene glycol 400)144130216,8
Povidone (plasdone or kollidon), mg61544,8
Purified water, mg10155,1

A comparative Toxicological study of encapsulated dosage form of choline alfoscerate obtained by the present pharmaceutical compositions, and standard sample (the original drug Gliatilin® (manufacturer of Italfarmaco/Pharmacor (Italy/Russia).

Subacute experiment conducted on 50 nonlinear rats male with an average body weight of 226±6, Cf is viveme the drugs were injected intragastrically at doses of 10.0 (therapeutic) and 100.0 mg/kg once a day for 2 weeks.

According to the results of the experiment revealed no irritant effect on the mucous membrane of the gastrointestinal tract in laboratory animals when exposed to both drugs. Compare the drugs had no significant effect on weight gain and other integral indicators. Experimental data shows no differences from peripheral blood, lipid and carbohydrate in the liver, and renal excretory function.

Thus, in the studied doses experimentally confirmed the safety of the claimed pharmaceutical composition having neuroprotective activity and cholinomimetic action (drug-prototype Gliatilin®).

In addition, as a result of research it has been unexpectedly discovered that claimed in the present invention the pharmaceutical composition has improved, compared with the drug-prototype bioavailability. The bioavailability of choline alfoscerate included in the inventive pharmaceutical composition, as measured by labeled14C-isotope of carbon, amounted to 88-91%, 7-10% above preparation of the prototype. If ingestion is rapidly and completely absorbed in the gastrointestinal tract, Tsah - 1 hour Therapeutic plasma concentration of 10-20 ng/ml parenteral amount of races shall determine - 5.3 l/kg, T_1/2 - 4,74-5 hours Easily penetrates the blood-tissue interfaces barriers.

The author of the present invention notes that probably a higher bioavailability of the inventive pharmaceutical composition is caused by the original excipients. Due to the presence in the inventive pharmaceutical composition of polyethylene glycol 400 (preferably in the amount of 20-40% to 100 wt.% the whole composition) and povidone (plasdone or kollidon) (preferably in the amount of 1.6 to 4.2% per 100 wt.% the whole composition) provides better penetration of active substances (choline alfoscerate) and thereby increasing its bioavailability.

The pharmaceutical composition claimed in accordance with the present invention may be used for the treatment and prevention of diseases of the Central nervous system and the effects of traumatic brain injury according to the following indications: traumatic brain injury with a predominantly stem the level of the lesion (acute period), cerebrovascular insufficiency, discirculatory encephalopathy, psychoorganic syndrome on the background of degenerative diseases and involutional processes in the brain, multi-infarct dementia, Alzheimer's disease, brain infarction, loss of memory.

Introduction to the person of the claimed pharmaceutical compositions provide intramuscularly or intravenously.

1. Maintain the new pharmaceutical composition, with nootropic activity and cholinomimetic action, containing as the active ingredient alfostserat in a therapeutically effective amount and a pharmaceutically acceptable carriers, characterized in that as pharmaceutically acceptable carriers it contains 20-40% of macrogol (polyethylene glycol 400) and 1.6-4.2% povidone (plasdone or kollidon).

2. The pharmaceutical composition according to claim 1, characterized in that the content of choline alfoscerate is 55,6-75 wt.%.

3. The method of obtaining the encapsulated pharmaceutical composition having neuroprotective activity and cholinomimetic action and containing as the active ingredient alfostserat in therapeutically effective amount, wherein implementing the following stages:
a) in a volumetric flask of 1000 ml was placed a polyethylene glycol 400 and add the calculated amount of purified water (to 100%);
b) weighed alfostserat and povidone;
C) in the reactor under stirring consistently placed povidone (plasdone or kollidon), stirred for 5-10 min until complete dissolution;
g) obtained in stage C) solution added alfostserat and stirred for 10 min until complete dissolution of the components;
d) carry out the stage of encapsulation and get pharmac wtiches composition according to any one of claims 1,2.

4. The method according to claim 3, characterized in that stage a) in a volumetric flask polyethylene glycol 400 in an amount of 20-40 wt.%.

5. The method according to claim 3, characterized in that stage b) is weighed 55,6-75 wt.% choline alfoscerate and 1.6-4.2 wt.% of povidone;

6. Treatment/prevention of diseases of the Central nervous system and the effects of traumatic brain injury, characterized in that exercise ingestion of the pharmaceutical composition according to any one of claims 1, 2.

7. Treatment/prevention of diseases of the Central nervous system according to claim 6, characterized in that the Central nervous system diseases include cerebrovascular insufficiency, discirculatory encephalopathy, psychoorganic syndrome on the background of degenerative diseases and involutional processes in the brain, multi-infarct dementia, Alzheimer's disease, brain infarction, loss of memory.

8. The method of treatment or prevention according to claim 6, characterized in that traumatic brain injury is a traumatic brain injury with a predominantly stem the level of the lesion (acute period).



 

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SUBSTANCE: there is described thiomorpholine compound presented by formula (I) wherein the ring A represents benzene ring; the ring B represents benzene ring; R1 represents hydrogen atom, R2 represents C1-6-alkyl group; R3a and R3b are identical or different, each representing hydrogen atom or C1-6-alkyl group, and n represents an integer equal to 2, or its pharmaceutically acceptable salt. There is also described method for making the compound of formula (1), a pharmaceutical composition and application of the compound of formula (1) for making a medical product used for treatment and prevention of the disease chosen from inflammation, allergic diseases, pain, migraine, neuralgia, itch, cough, central nervous system diseases, alimentary organ diseases, nausea, vomiting and urological disorders.

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Gsk-3 inhibitors // 2379300

FIELD: medicine.

SUBSTANCE: invention concerns GSK-3 inhibitors of general formula (I), method for making thereof and based pharmaceutical compositions which can be used in medicine: formula I, where R1 means an organic group containing at least 8 atoms, chosen of C or O, including aromatic ring of phenyl, naphthyl or methylene dioxypjenyl, which is not bound directly with N through -C(O)- or oxygen; Ra, Rb, Rz, R3, R4, R5 and R6 represent hydrogen.

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28 cl, 13 ex, 3 tbl

FIELD: chemistry.

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53 cl, 4 tbl, 253 ex

FIELD: medicine.

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35 cl, 22 ex, 15 tbl

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7 cl, 2 tbl

FIELD: pharmacology.

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20 cl, 6 dwg, 4 tbl, 8 ex

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12 cl, 1 dwg, 4 tbl, 9 ex

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9 cl, 1 dwg, 3 tbl, 18 ex

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11 cl, 4 tbl

FIELD: medicine.

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6 cl, 2 tbl, 19 ex

FIELD: medicine.

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3 ex

FIELD: medicine.

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3 ex

FIELD: medicine.

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EFFECT: efficiency for diabetes treatment.

14 cl, 3 tbl, 18 ex

FIELD: medicine.

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EFFECT: new dosed out forms are stable throughout all period of storage.

15 cl, 17 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: present invention concerns area of medical products, in particular, to the capsule of a medicinal preparation made in the form of an elastic, soluble in a human body, monolithic body with a cavity for placing of a liquid medicinal preparation, having an inflow with a notch on an outer side, with the through aperture executed in it; the capsule is fixed on clothes. Such performance of the capsule excludes leak of a liquid medicinal preparation at an abruption from it, it is convenient for the patient as allows receiving a medicinal preparation in time.

EFFECT: exclusion of leak of a liquid medicinal preparation at an abruption from it, it is convenient for the patient as allows receiving a medicinal preparation in time.

1 dwg, 1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and medicine, namely to oral gindarine medicine characterised as a tranquilizer. Said medicine contains gindarine hydrochloride as an active material and auxiliary components and represents a solid gelatinous capsule. Gindarine is included as a compound of the mass filling capsules as mixed powders of gindarine and auxiliary components or as a granulated material. As the auxiliary components, the medicine contains bulking agent either alone, or combined with a disintegrant or antifriction material or with their mixture. There is also provided method of production of specified oral medicine.

EFFECT: invention provides simplified technological process for making the gindarine medicine, reduction of defective goods, reduced production cost, higher bioavailability of gindarine in comparison with a tableted medical product.

4 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns medical products and concerns capsules for delivery of biologically active agent, containing: a water-soluble, washed away, blasted and-or bulking up cover; and b) the water filling composition including one or more active agents, the water which is in quantity from at least approximately 10% of masses/masses, to less than approximately 70% of masses/weights; and water-soluble derivative cyclodextrin, present at quantity of at least 30% of mass/mass, in recalculation on a total weight of water and derivative cyclodextrin in a filling composition where the quantity derivative cyclodextrin is enough for suppression of dissolution, washing out, destruction and-or a swelling of the cover, caused by water in a filling composition and where the capsule has a period of storage at least one week. Also the way of stabilisation of a capsule is opened.

EFFECT: creation of capsules with steady against dissolution, washing out, destruction and swelling covers.

51 cl, 11 dwg, 11 tbl, 10 ex

FIELD: medicine.

SUBSTANCE: present invention concerns lysine compounds of formula (I) or its pharmaceutically acceptable salts, a based pharmaceutical compositions and application for treatment or prevention of HIV-infection. The compounds of formula (I) where n is equal to 3 or 4, where X and Y identical or different are chosen from the group consisting of H, F, Cl, Br, I and -NR4R5, where R6 is chosen from the group consisting of unbranched alkyl group, containing 1 to 6 carbon atoms, and branched alkyl group containing 3 to 6 carbon atoms, where R3 is chosen from the group consisting of the group of formula R3A-CO-, and R3a is chosen from the group consisting of unbranched or branched alkyl group containing 1 to 6 carbon atoms, alkyloxygroup containing 1 to 6 carbon atoms, and 4-morpholinyl, where R4 and R5 are identical and represent H, where R2 is chosen from the group consisting of diphenylmethyl group, naphthyl-1-CH2-group, and naphthyl-2-CH2-group, where X' and Y' are identical and represent H, and where R1 is chosen from the group consisting of from (HO)2P(O) and (MO)2P(O), where M represents alkaline metal.

EFFECT: lysine compounds representing effective inhibitors of aspartyl-protease.

15 cl, 3 tbl, 1 ex

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