UA12210U - Effervescent argimag, cardiologic drug - Google Patents

Abstract

The cardiologic drug consists of L-arginine-related component and the additive. L-arginine or L-arginine hydrochloride is used as L-arginine-related component. Magnesium-containing substance, namely magnesium oxide, magnesium carbonate basic, magnesium gluconate, magnesium citrate or magnesium aspartate, is used as the additive. The formulation also comprises sodium bicarbonate and anhydrous citric acid.

Description

Description of the invention

The useful model belongs to pharmacy, to drugs of cardiac action, namely, for the treatment of 2 atherosclerosis, ischemic heart disease, angina pectoris, arterial hypertension, as well as the correction of endothelial dysfunction.

An urgent problem of modern medicine is the treatment of diseases of the cardiovascular system, which are the most common and lead to disability and mortality of the population of industrialized countries.

The arsenal of drugs with cardiac action is quite significant, but the search for effective and non-toxic drugs of 70 cardiac action continues.

It is known that I-arginine is used for the treatment of atherosclerosis of coronary and peripheral arteries, as well as in the prevention of restenosis after stenting. Siiipis! apa ipyattayogu ePesiv oi adiebagu I-agdipipe ip rayepiv m/y ipigassiarie oapdipa resiogiv. That Ategisap |oigpa! oh

Sagaioiodu.- 1997.- Mo1I.-80.-R. 1488-1490). In the process of treatment with I-arginine, 10 patients participated, 12 of whom suffered from stable angina pectoris of MI FC (MI of functional class). Previously, all of them underwent operative treatment of CHD (ischemic heart disease) - stenting or shunting. Arginine was prescribed at a dose of 9 g per day for three months. Before the use of I-arginine, patients received classical combined therapy (P-blockers, calcium antagonists, nitrates, aspirin, statins). The introduction of arginine into their treatment regimen produced the following results: seven patients switched to FC II, one to FC II, and two remained in

IM FC. Already a month after the start of treatment, favorable changes in the well-being of the patients were noted.

Unfortunately, this effect was not long-lasting. Three months after the end of the course of treatment, all patients returned to the IM FC.

Common features with the claimed useful model are the presence of I-arginine in the composition of the medicinal product.

As a prototype, a drug with cardiological action was chosen, which is described in the patent of Ukraine (Mo 66456, IPC / Z

Ab1KZ1/00, publication date 05/17/2004, Bull. Mo. 5/20041. Cardiological medicinal product contains riboxin and

And arginine at a 1:1 ratio of components: riboxin 49-51 wt. 95, Fr

And arginine 49-51 wt. 95. yes

Riboxin in the composition of the drug stimulates the synthesis of adenyl nucleotides, which leads to an increase in CAMP (cyclic adenyl monophosphate) in the vascular wall. Introduction to the composition of the drug I! -arginine, which is a He substrate for MO-synthetase, increases the content of nitric oxide (MO), activating guanylate cyclase, which leads to an increase

From the content of CGMP (cyclic guanyl monophosphate) in vascular smooth muscle cells. --

The authors of the Ukrainian patent No. 66456 claim that the synergistic effect of riboxin on TsAMP-dependent metabolic processes and I-arginine on cGMP-dependent metabolic processes causes the vasodilating and metabolic effect of the drug. The drug is offered in the form of tablets to be taken internally, 1-2 tablets 3 times a day before meals. One tablet contains 0.09-0.11 mg of riboxin and 0.09-0.11 mg of I-arginine. However, our 37Z 70 studies have shown that the drug with cardiological action under the patent of Ukraine Mob6456 has a low therapeutic effect. "with common features with the claimed useful model is the presence in the composition of the medicinal product of cardiological action of a component based on I-arginine and additives.

The reasons that prevent the achievement of the desired technical result are the insufficiently balanced qualitative and quantitative composition of the medicinal product of cardiac action.

The basis of a useful model is the task of improving the prognosis and quality of life of patients, as well as pleasant organoleptic properties, by changing the qualitative and quantitative composition of the drug with cardiac action. o The task is solved by the fact that the medicinal product of cardiac action "Argimag effervescent", containing - 20 components based on I-arginine and an additive, according to a useful model, the component based on I-arginine is selected from the group consisting of I-arginine hydrochloride, pure I-arginine, as an additive it contains a compound with magnesium selected from the group consisting of magnesium oxide, basic magnesium carbonate, magnesium citrate, magnesium gluconate, magnesium aspartate, and also additionally contains sodium hydrogen carbonate and anhydrous citric acid with such ratio of components: c component based on I-arginine 1.5-3.Og, magnesium compound 5-15 mmol of magnesium, sodium bicarbonate 0.75-1.Og, because citric acid anhydrous 0.8-1.2g.

The first additional difference is that the drug with cardiological action "Argimag effervescent" additionally contains anhydrous sodium carbonate, as well as a sweetening component selected from the group consisting of mannitol, sorbitol or sodium saccharinate, with the following ratio of components: -Д-

component based on I-arginine 1.5-3.0g suitable magnesium compound 5-15 mmol magnesium with sodium bicarbonate 0.75-1.0g citric acid anhydrous 0.8-1.2g sodium carbonate anhydrous 0.1-0, 3 g of sweetening component 70 0.005 - 0.85 g

The second additional difference is that the drug with cardiological action "Argimag effervescent" additionally contains flavoring and food coloring with the following ratio of components: component based on I-arginine 1.5-3.0g suitable magnesium compound 5-15 mmol magnesium sodium hydrogen carbonate 0.75-1.0g citric acid anhydrous 0.8-1.2g sodium carbonate anhydrous 0.1 - 0.3 sweetening component 0.005 - 0.85g flavoring 0.01 - O.O8g - food coloring 0.2-0 .8 mg

For the manufacture of the medicinal product with cardiological action "Argimag effervescent", which is claimed, the following were taken: - I-arginine according to the State Pharmacopoeia of Ukraine (DFU), 1 ed., p. 319 or I-arginine hydrochloride according to DFU, 1st edition, p. 320; - anhydrous citric acid according to DFU, 1 ed., p. 3950; h - sodium bicarbonate according to DFU, supplement 1, p. 410; y - y c - anhydrous sodium carbonate according to DFU, supplement 1, p. 413; - magnesium oxide according to DFU, 1 ed., p. 409; sa - basic magnesium carbonate according to DFU, 1 ed., p. 390; - - magnesium citrate according to the US Pharmacopoeia OBR27-ME22 Rade 1122; - magnesium gluconate according to the US Pharmacopoeia OBR27-ME22 Rade 1123; - magnesium aspartate according to the European Pharmacopoeia, article 1445. - sorbitol according to TU 9325-021-05800314-98 produced by the company "ISM Marbiopharm", Russian Federation; « du - mannitol according to the European Pharmacopoeia, article 0959; z - sodium saccharinate according to the European Pharmacopoeia, article 0787, produced by the private enterprise "Khim s Ton", Kyiv; :z" - flavoring agent: aromatic edible orange essence according to TU 9154-270-00008064-98 or aromatic edible raspberry essence according to TU 9154-008-00334557-97; 15 - food dye tartrazine; - - dye red light purple E 121 company "AKOSO", Czech Republic;

Cardiological drug "Argimag effervescent", which is claimed, was prepared by mixing calculated quantities of components. o Table 1 - 50

The composition of the medicinal product of cardiac action "Argimag effervescent" 2 Moprikladu | -arginine |And--arginine| Magnesium )/ Magnesium Magnesium Magnesium Magnesium Lemon Sodium Sodium hydro "g oxide carbonate citrate gluconate )|aspartate |acid hydrocarbonate, g |carbonate chloride, g basic anhydrous anhydrous, g anhydrous, g her in r yuga 1-11-11-111о8 11 c 212v 1 July 1-1 1-1 1-1 1-1 July 101 8 July 1-1 July 1-11 1-1 mov 1861 v ov 1-11 11121211 ayu vo - 2-1 1-1 6116111 1-5 r 1-1 11110811 tyu 11111011 01206821 01ov1m 812611 1-1 | rvav 12 81861 riv ra 1-1 111212 |from vya0029111- 116 101-105 ov 0o8 1081 - - -1 - - 11 - | 5 21) - - 0.8 0.8 -

pa 7.110175 17. 1.17. 1.17. 1.170115 is ov iov |.

The manufactured drug with cardiological action "Argimag effervescent" was packaged in plastic bags or sent to a device for pressing tablets. Further, the implementation of the claimed utility model 95 is confirmed by the following layouts.

Example 1. 1.5g of I-arginine hydrochloride, 0.2g of magnesium oxide, 0.8g of anhydrous citric acid and 0.75g of sodium bicarbonate are mixed in a mortar. The resulting powder is poured into a plastic bag and hermetically sealed.

Examples 2 - 12. Cardiological drug "Argimag effervescent" was prepared as described in example 1, except that the composition of the components was changed. Information about the components and their ratio is given in examples 2-12 of table 1 and examples 7-12 of table 2. rvav 11111 8717-6111 81931111 byu 00001030000100100801030010803 vom 111110 pa 111о8 117.11 .1004 181111

Cardiological drug "Argimag effervescent", which is claimed, increases tolerance to dosed physical activity, reduces the manifestations of endothelial dysfunction, reduces the frequency of attacks of 8 tension angina pectoris, as well as manifestations of arterial hypertension. In addition, the drug "Argimag effervescent" with cardiological action can have a pleasant taste and smell, which is convenient for consumption. The contents of one sachet or tablet of "Argimag effervescent" cardiology medicine are diluted in a glass of boiled water. At the same time, citric acid in the solution reacts with sodium hydrogen carbonate, basic magnesium carbonate, and sodium carbonate with the formation of carbon dioxide, which saturates the solution and bubbles are released from the solution, giving it pleasant organoleptic properties reminiscent of a carbonated drink, for example, lemonade.

The claimed "Argimag effervescent" cardiology medicinal product can be manufactured on standard industrial equipment without additional capital costs. with h-

Claims (2)

The formula of the invention 1. Cardiological medicine containing a component based on I-arginine and an additive, which differs in that the component based on I-arginine is selected from the group consisting of I-arginine hydrochloride and pure 50 I-arginine as an additive it contains a magnesium compound selected from the group consisting of magnesium oxide, magnesium 3s carbonate basic, magnesium citrate, magnesium gluconate, magnesium aspartate, and additionally contains sodium 3s" hydrogen carbonate and anhydrous citric acid in the following ratio of components: component based I -arginine 1.5-3.0 g magnesium compound 5-15 mmol magnesium - sodium bicarbonate 0.75-140 g citric acid anhydrous 0.8-1.2 g 2. Cardiological medicinal product according to claim 1, which is characterized by the fact that it additionally contains sodium carbonate -l 20 anhydrous, as well as a sweetening component selected from the group consisting of mannitol, sorbitol or sodium saccharinate, with the following ratio of components: (42) component based on I-arginine 1.5-3.0 g magnesium compound 5-15 mmol magnesium sodium bicarbonate 0.75-1.0 g citric acid anhydrous 0.8-12 g sodium carbonate anhydrous 0.1 -03 g of sweetening component 0.005-0.85 g. 60 Z. Medicinal product of cardiological action according to claims 71 and 2, which is distinguished by the fact that it additionally contains flavoring and food coloring with the following ratio of components: component based on I -arginine 1.5 -3.0 g magnesium compound 5-15 mmol magnesium 65 sodium bicarbonate 0.75-1.0 g citric acid anhydrous 0.8-12 g sodium carbonate anhydrous 0.1-03 g sweetening component 0.005-0.85 g flavoring 0.01-0.08 g food coloring 0.2-0.8 mg. - "c) "-- s s o - with . and? shk name) name) shk 20 (42) c bo b5