Hypotensive means

FIELD: medicine.

SUBSTANCE: invention represents a hypotensive means, which contains felodipinum as an active component, as well as target additional components: mesoporous silicon dioxide, lactose, hypromeloza. Realisation of the invention ensures the high technological efficiency of the claimed medical means production with the provision of a prolonged release of an active substance with the application of available components. Felodipinum is included into spherical particles with a highly developed mesoporous structure of silicon oxide.

EFFECT: increase of stability in storage and protection from unfavorable environmental factors.

4 cl, 4 ex

 

The invention relates to medicine, in particular to pharmaceutical preparations used for the treatment of arterial hypertension.

Arterial hypertension (AH) remains a serious health problem in many countries. For example, in Russia 23-30% of the population suffers from this disease. Hypertension is also a risk factor for other diseases of the cardiovascular system. The results of epidemiological studies showed a significant Association between hypertension and coronary heart disease (CHD), stroke, chronic heart failure and chronic renal failure.

Currently for the treatment of hypertension, use of different classes of antihypertensive drugs. These include thiazide and casinomodule diuretics, beta-blockers, angiotensin converting enzyme inhibitors (ACEI), calcium antagonists (AK), blockers of AT1-angiotenzinovyh receptor blockers α1-adrenergic receptors, agonists I1-imidazoline receptor agonists Central α2-adrenergic receptors.

Calcium antagonists, which include derivatives of dihydropyridine (nifedipine, amlodipine, isradipine, nisoldipine, nitrendipine, felodipine, etc.) have long been used in cardiology, due to the high efficacy and good tolerability.

One of the derivatives dihydropyrido�and is felodipine (utilmately ester 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridine-dicarboxylic acid). He is considered the most secure in the treatment of hypertension in patients, especially those with overt or latent systolic dysfunction of the left ventricle. The drug has a significant impact on the contractile function of the myocardium. However, when using it, physicians are faced with the problem of low bioavailability. According to some, she is 12-16%. The half-life felodipina for retardnoy form - 10-36 hours and the time to reach maximum concentration in plasma is 2 to 8 hours (the drug THERAPY of HYPERTENSION. PART 4. CALCIUM ANTAGONISTS AS ANTIHYPERTENSIVE DRUGS, A. Sidorenko, D. V. Preobrazhensky, http://www.rmj.ru/articles_2313.htm).

Known drugs Plendil (AstraZeneca AB, Sweden) and Feldip ("IVAX Pharmaceuticals sro, Czech Republic) are composed of hypromellose and lactose [Regulatory documentation "Plendil. Tablets prolonged action, film-coated 2.5 mg, 5 mg, 10 mg AstraZeneca Sweden; radar, electronic directory, [access Mode: http://www.rlsnet.ru]; MASHKOVSKY M. D. Medicines. - M., 2007, p. 432]]. The use of lactose as excipients improves the dissolution felodipina, the introduction of hypromellose slows the release of active substance. The use of microcrystalline cellulose and other insoluble components makes the release felodipina �more uniform. However, these formulations have drawbacks associated with inadequate allocation felodipina in the early hours.

Known patents, in which attempts were made for the development of improved forms felodipina with a slow action.

Patent RU 2363464 (C2), publ. 2009-08-10 describes a composition for the manufacture of tablet dosage forms with modified release for oral administration of the drug containing felodipine or its salt, HPMC, sodium alginate, lactose, Gagne stearate, calcium hydrogen phosphate dehydrate, kollidon 30, Aerosil.

CN 101953837, publ. 2011.01.26 describes tablets with slow release Felodipina containing cyclodextrins clathrate compound, a filler, microcrystalline cellulose, grease, and glidant.

CN 102552200, publ. 2012.07.11 describes tablets with slow release felodipina containing a methylcellulose with a high viscosity hydroxypropyl methylcellulose low viscosity, and water-soluble filler.

CN 101744786, publ. 2010.06.23 reveals tablets felodipina with a slow release, which include the core, soteriades felodipine, polyoxyethylene (20) sorbitan monooleate, hydroxypropyl methylcellulose, microcrystalline cellulose, magnesium stearate, fine powder of silicon dioxide and the solution �of canola.

As can be seen from the presented prior art, to slow release profile preferably in systems using hydroxypropyl methylcellulose (HPMC).

It is known that the ideal release profile is a zero-order dependence when the transition of the active substance from the dosage form in the solution described in the form of a linear function.

However, the constant speed of separation of the zero-order from solid dosage forms such as tablets or capsules, powders, is not something that immediately would be expected from moderately and poorly soluble ingredients, and it is difficult to achieve because you must consider many parameters.

As shown by experimental studies, it cannot be expected a priori, the kinetics of zero-order allocation with moderately soluble calcium antagonists of the dihydropyridine type, such as felodipine, HPMC systems. The kinetics of zero-order allocation should be considered as a special case, which can only take place in certain forms of dispensing.

In recent years, are increasingly being studied ordered porous materials with the possibility of their application as drug delivery system. Depending on the size of the pores, inorganic materials can be classified as microporous, mesopore�tide or macroporous.

There are attempts to create forms with controlled selection based on such media. For example, published applications CN 103007290 (A) Nano-carrier particle controllable in drug release and preparation method thereof, GB 2507983 (A) Mesoporous silica particles and their use in drug delivery, etc. However, these technical solutions have paid zero attention to the order of layoff and biodatabase antihypertensive agents.

As the closest analogue may be specified in the international application WO 2006026840 (A2). The application discloses a controlled release delivery system containing a biologically active compound and a carrier matrix, which is an amorphous microporous non-fibrous silicon or titanium oxide loaded the specified biologically active compound and where the micropores of the specified matrix carrier have an average size in the range from 0.4 to 2.0 nm. At least 50% of the biologically active compound has a molecular dispersed in the pores of the said matrix carrier. As a possible active compounds mentioned in the list felodipine. A concrete example no. Not discussed its pharmacokinetics and bioavailability.

The problem to be solved by the invention, consists in obtaining new ready prolonged dosage forms felodipina meeting all Pharmacopoeia requirements, quality�idents and quantitative composition of which will provide a high manufacturability of the drug, while guaranteeing disintegration and complete release from drugs using the available components.

To solve this problem is proposed to include felodipine in the structure of silicon oxide with mesoporous structure, from which the active substance is released delayed, and the additional extension is achieved by introducing into the composition of hypromellose. The composition also contains lactose, which performs a number of functions, including a binder, a dispersant, a sweetening effect.

Thus, the object of the invention is a hypotensive agent in the form of solid dosage forms for oral administration, containing particles of silicon oxide with mesoporous structure, the pores of which having a mean diameter of 2 to 50 nm filled felodipina, lactose and hypromellose when the ratio of components in wt%:

Felodipine - 0,48-10,0

Lactose monohydrate - 0,25-39,0

Polymer-0,25-50,0

Colloidal silicon dioxide (Syloid) - 1,0-99,0.

Preferably, the particles of silicon oxide with mesoporous structure, the pores of which are filled with felodipina get by dissolving felodipina in ethanol when heated to 40-45°C with subsequent introduction into the solution of silicon dioxide colloidal mesoporous, stirring for 3-5 minutes and drying in vacuum.

The final form may not contain or may contain up to 30 wt.% ethanol.

Substance felodipina can be�ü obtained by any known means, for example described in patent EP 0007293 (B1) - 1982-06-23, the application WO 9725313 (A1) - 1997-07-17, US 5310917 (A) 1994-05-10.

Oxide particles of flint with mesoporous structure have a pore size from 2 to 50 nm. Use colloidal silicon dioxide, in particular, such as Syloid (https://grace.com/pharma-and-biotech/en-us/Documents/Syloid/M417_Syloid%20Anti-Caking%20App%20NoteFINAL.pdf).

The polymer has a large molecular weight (of 86000 Dalenov) and, thus, is slowly absorbed.

Lactose can represent both the monohydrate and anhydrous lactose. You can use parts of lactose (30%) in the form of micronized lactose with a particle size D50 of less than 5 microns.

Solid dosage form is preferably a tablet or a granulate, which can be packaged in capsules or sachets.

The invention can be illustrated by the following the following examples.

Example 1. Get a tablet weight of 200 mg, containing 20 mg felodipina and 1% mesoporous silicon dioxide. Ethyl alcohol is measured into a flask and added felodipine. If necessary, the solution is heated to 40-45°C. To the resulting solution is injected silicon dioxide mesoporous and stirred for 3-5 minutes. Formed a mass that retains all the properties of flowability with slight agglomeration. In the drying process, the signs of agglomeration disappear. Received�th sorption complex was dried in vacuum or on pallets in a layer thickness of 1-1,5 cm. Thus there is a decrease in the number of alcohol up to 30% relative to the total mass of the sorption complex. Further polymer is added and lactose. From the obtained granulate is compressed tablets weighing 200 mg.

Felodipine - 20

Lactose monohydrate - 78

Polymer - 100

Colloidal silicon dioxide (Syloid) - 2

Weight of tablet 200 mg.

Used pharmaceutical composition with the stated ratio of the components provides optimum physico-chemical and technological properties of dosage form and high bioavailability of the drug substance. According to the "dissolution test", felodipine released on Wednesday dissolution in an hour 10% 2 hours 30% after 5 hours, 60% after 7 hours at 80% [USP: USP 29. National formulary: 2 t: [per. s angl.]. - M.: GEOTAR-Media, 2009. - T. 2. - 1800 S.], a description of the methodology CFC "Dissolution".

Example 2. Gain capsules weight 411 mg, containing 1 mg felodipina and 49% of mesoporous silicon dioxide. The granulate obtained analogously to claim 1, and then the granulate is Packed in a capsule.

Felodipine - 1

Colloidal silicon dioxide (Syloid) - 200

Lactose anhydrous - 10

Polymer - 200

Weight capsules 411 mg.

Used pharmaceutical composition with the stated ratio of the components provides optimum physico-chemical and technological properties�and dosage form and high bioavailability of the drug substance. According to the "dissolution test", felodipine released on Wednesday dissolution in an hour 10% 2 hours 30% after 5 hours, 60% after 7 hours at 80% [USP: USP 29. National formulary: 2 t: [per. s angl.]. - M.: GEOTAR-Media, 2009. - T. 2. - 1800 S.], a description of the methodology CFC "Dissolution".

Example 3. Get capsules weighing 200 mg and containing 1 mg felodipina and 99% of mesoporous silicon dioxide. The granulate obtained analogously to claim 1, Stephanus Packed in capsules.

Felodipine - 1

Colloidal silicon dioxide (Syloid) - 198

Polymer - 0,5

Lactose anhydrous - 0,5

Weight capsules 200 mg.

Used pharmaceutical composition with the stated ratio of the components provides optimum physico-chemical and technological properties of dosage form and high bioavailability of the drug substance. According to the "dissolution test", felodipine released on Wednesday dissolution in an hour 10% 2 hours 30% after 5 hours, 60% after 7 hours at 80% [USP: USP 29. National formulary: 2 t: [per. s angl.]. - M.: GEOTAR-Media, 2009. - T. 2. - 1800 S.], a description of the methodology CFC "Dissolution".

Example 4. The granulate obtained analogously to claim 1, and then Packed in sachet of 4.12 g with the addition of a measuring spoon to 200 mg

Felodipine - 20

Colloidal silicon dioxide (Syloid) - 2000

Lactose - 100

Polymer - 2000

Used pharmaceutical composition with the stated ratio of the components provides optimum physico-chemical and technological properties of dosage form and high bioavailability of the drug substance. According to the "dissolution test", felodipine released on Wednesday dissolution in an hour 10% 2 hours 30% after 5 hours, 60% after 7 hours at 80% [USP: USP 29. National formulary: 2 t: [per. s angl.]. - M.: GEOTAR-Media, 2009. - T. 2. - 1800 p.].

Derived drug used in hypertension.

The positive effect is that in addition to prolonging one additive (hypromellose) introduces nanostructured surfactant - mesoporous silicon oxide. The drug is prolonged due to the slow diffusion from the pores of the oxide of silicon. When taken orally, the liquid contents of the intestine included in the space of mesoporous structure of silicon oxide and dissolves felodipine. When this environment is a granulate or tablet. Next, the drug diffuses inside the granules or tablets, after which it enters the suction area of the intestine, thus, the extension is achieved due to the mesoporous structure of the oxide of silicon, and due to the slow patterns of soluble tablets or granules. Selected softwaresocial higher bioavailability and effective release kinetics. The new form increases resistance felodipina during storage and protects from adverse environmental factors.

1. Hypotensive agent, characterized by the fact that it is made in the form of solid dosage forms for oral administration, containing particles of silicon dioxide with colloidal mesoporous structure, the pores of which having a mean diameter of 2 to 50 nm filled felodipina, lactose and hypromellose in the following ratio of components in wt.%:
Felodipine - 0,48-10,0
Lactose - 0,25-39,0
Polymer - 0,25-50,0
Colloidal silicon dioxide - 1,0-99,0.

2. Hypotensive agent according to claim 1, characterized in that it contains up to 30 wt.% ethanol.

3. Hypotensive agent according to claim 1 or 2, characterized by the fact that the particles of silicon dioxide with colloidal mesoporous structure, the pores of which are filled with felodipina get by dissolving felodipina in ethanol when heated to 40-45°C with subsequent introduction into the solution of silicon dioxide colloidal mesoporous, stirring for 3-5 minutes and drying in vacuum.

4. Hypotensive agent according to claim 1 or 2, characterized in that the solid dosage form is a tablet or granules, which can be packaged in capsules or sachets.



 

Same patents:

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SUBSTANCE: invention refers to a compound of structural formula I

which can be used for protecting cardiomyocytes or for preventing or treating a disease or a disorder related to cardiomyocyte apoptosis. In formula I A represents =S, -SR4 or =O, X represents F, Cl, Br or I, R1 represents phenyl, R2 and R3 are connected to form morpholine, and R4 represents C1-C6-alkyl.

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8 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

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21 cl, 4 tbl, 26 ex

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Vasopressor agent // 2552529

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2 cl, 2 dwg, 8 tbl, 4 ex

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4 tbl, 2 ex

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12 cl, 3 tbl, 21 ex

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65 cl, 1 dwg, 1 tbl, 7 ex

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1 dwg, 2 ex

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53 cl, 6 ex, 5 dwg, 4 tbl

FIELD: chemistry.

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3 ex

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2 ex

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3 dwg, 3 ex

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2 ex

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EFFECT: simplification and acceleration of the process of producing microcapsules, reduction of loss in production of microcapsules.

1 dwg, 2 ex

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SUBSTANCE: method represents physico-chemical of precipitation with non-solvent, in which as microcapsule envelope xanthan gum, as core - ADS 2 fraction, and as precipitating agent - benzene are used.

EFFECT: simplification and acceleration of the process of obtaining microcapsules and increase of output by their weight.

3 dwg, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical composition in the form of a tablet with an erodible matrix, which contains one or more fumaric acid ethers, as well as a rate-controlling agent, representing hydroxypropylcellulose and a binding agent, representing lactose, with the decomposition of the said degradable matrix providing the controlled release of the said fumaric acid ether (ethers).

EFFECT: provision of the controlled release of fumaric acid ether (ethers).

19 cl, 43 ex, 2 tbl, 2 dwg

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