Combined hypotensive agent

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a combined medicinal agent used in treatment of arterial hypertension. The proposed agent comprises the combination of enalapril maleate and hydrochlorothiazide as an active component, and also sodium hydrocarbonate, starch, lactose, iron oxide and stearate as accessory substances. The proposed agent is stable in storage and releases the active component easily.

EFFECT: improved and valuable properties of agent.

8 cl, 1 tbl, 5 ex

 

The invention relates to medicine, specifically to compound medicines, and can be used for the treatment of hypertension.

Studying the role of angiotensins and angiotensin-converting enzyme (ACE) inhibitors in the regulation of blood pressure served as the scientific basis for the creation of antihypertensive drugs based on ACE inhibitors. Among the drugs from the group of ACE inhibitors is important enalapril maleate (or (S)-1-[N-[1-(etoxycarbonyl)-3-phenylpropyl]-L-alanyl]-L-Proline maleate (1:1)) [Mashkovsky PPM Medicines, vol. 1, ed. 14-e, M.: Publishing house New Wave, 2001, s]. therapeutic action of enalapril maleate is due to its metabolism in the body to enalaprilat, which leads to the suppression of the formation of angiotensin II is a powerful vasoconstrictor agent. The result is lower blood pressure and thus does not increase the heart rate. The presence of these effects was a prerequisite widespread use of enalapril maleate in medical practice as an antihypertensive.

To enhance therapeutic action is preferable to make use of enalapril maleate in combination with other antihypertensive agents, preferably diuretics. Thus, the literature describes the use for the treatment cauliform hypertension means, which contains a combination of enalapril maleate and diuretic - hydrochlorothiazide [Mashkovsky PPM, s]. However, information about specific excipients in the preparation are not available.

It is known that the enalapril maleate has a low stability and easily undergoes degradation in pharmaceutical preparations, especially in combination with other active ingredients.

In European patent No. 12401, 1980, described antihypertensive composition containing as active principle a combination of enalapril and hydrochlorothiazide is used as auxiliary substances Pregelatinised starch, microcrystalline cellulose and magnesium stearate. However, the known composition is characterized by low stability and, accordingly, a small shelf life.

The present invention is to create a combined antihypertensives, stable during storage and at the same time characterized by a high degree of release of the active agent.

The technical result obtained by implementing the present invention is that the proposed combined hypotensive agent has stability during storage and has a shelf life of more than 2 years and easily releases the active principle is the combination of enalapril maleate and hydrochlorothiazide, h is about provides high bioavailability of active ingredients.

This technical result is achieved by the claimed means of hypotensive action contains as active principle - the combination of enalapril maleate and hydrochlorothiazide is used as excipients sodium bicarbonate, starch, milk sugar, iron oxide and salt of stearic acid.

The optimal ratio of ingredients is, wt.%:

The active principle4,5-35,0
Sodium bicarbonatethe 2.0-10,5
Starchfrom 1.0 to 22.5
Iron oxide0,01-0,5
Salt of stearic acid0,4-1,5
Milk sugarRest

The claimed ratio of ingredients found experimentally and allows you to retrieve the specified technical result.

The active beginning of the proposed drug is the combination of enalapril maleate and hydrochlorothiazide (chemical name is 7-sulfamoyl-6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide). Enalapril reduces the amount of angiotensin II in blood serum and hydrochlorothiazide causes a diuretic effect, with enalapril maleate and hydrochlorothiazide reinforce the hypotensive effect of each other. Preferred mA is its ratio of enalapril maleate and hydrochlorothiazide is about 1:1.25 or 1:2,5.

The goal, namely the stability of the dosage form, and accordingly increase the shelf life and a high degree of release of the active principle, is achieved at the stated interval content of the active principle.

Because the mixture of enalapril maleate and hydrochlorothiazide in its pure form is not able to direct pelletizing and, in addition, enalapril maleate compatible with many auxiliary substances which accelerate its decomposition to create a combined preparation with the hypotensive action was necessary to find a combination of excipients and the ratio between them from the beginning. Introduction to composition as the target additives of sodium bicarbonate, lactose and iron oxide along with the use in the claimed limits of the other auxiliary ingredients allows not only to achieve stability of the proposed composition during storage, but also provides a high degree of release of the active principle. So, after 45 minutes on Wednesday dissolution becomes more than 90% of enalapril maleate and more than 85% of hydrochlorothiazide (the State Pharmacopoeia XI edition (GF XI) - not less than 75% in 45 min) (table 2).

As a salt of stearic acid can be used stearates of calcium, magnesium, zinc or other metals, preferably magnesium and/or the calcium salt.

Used according to the invention, the starch may be potato and/or corn and/or rice and/or modified starch, such as, for example, nitroglycerol brand "Primogel" or "Explotab", preferably a mixture of potato and modified starch. Suitable mass ratio of the modified potato starch in the mixture is 1:(7-20).

The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in the form of tablets that allows for maximum adaptability subsequent packaging and precision dosing of the active agent.

Obtaining the claimed composition can be carried out basically in accordance with known techniques, such as wet granulation of a mixture of enalapril maleate and hydrochlorothiazide is used with the auxiliary substances and subsequent pressing of dry granules. Salt of stearic acid and/or starch can be entered partially or completely immediately before the pressing of the granules. These methods obtain are not exhaustive, and may use other known mainly techniques, for example, the method of dry granulation, or a combination of the above methods.

In more detail, the present invention is illustrated by the following examples (see table 1).

P is the iMER 1. Mix the sifted powders of enalapril maleate (13,0 g; 5.0 wt.%), of hydrochlorothiazide (32,0 g; 12.5 wt.%), 176,3 g of milk sugar (67,8 wt.%), of 11.7 g of sodium bicarbonate (4.5 wt%), to 17.6 g of dry potato starch and iron oxide (0.52 g; 0.2 wt.%) moisturize 3%starch paste, mix to a uniform distribution of moisture, granularit on the device for producing granules and dried. After dry granulating the resulting mass optivault-stearate (1.0 wt.%) and modified starch brand Primogel (the total amount of starch in the composition of 9.0 wt.%, the ratio of modified potato starch is 1:7). The mixture is compressed on a tablet machine. Get tablet light yellow color with an average weight of 0.2 g, the content of enalapril maleate 0.01 g, hydrochlorothiazide - 0,025 g (the ratio of hydrochlorothiazide and enalapril maleate is 1:2,5), the release of the active substance (test "dissolution") - 100% of analapril maleate and 98% of hydrochlorothiazide after 45 min (GF XI - not less than 75%). The obtained tablets meet the requirements of the global Fund XI and have a shelf life of more than 27 months.

Example 2. Perform analogously to example 1 with the difference that in the part of the starch (2.5 wt.%) injected directly prior to pelletizing together with calcium stearate and modified starch (ratio modificarea the nogo and potato starch is 1:20). Get tablets with an average weight of 0.13, the Content of enalapril maleate 0.01 g, hydrochlorothiazide 0.0125 g (the ratio of hydrochlorothiazide and enalapril maleate is 1: 1,25), the release of the active substance (test "dissolution"), 99.5% of analapril maleate and 96.5% of hydrochlorothiazide after 45 minutes of Pharmaceutical remedy meets pharmacopoeial requirements and has a shelf life of more than 27 months.

Examples 3-5. Perform analogously to example 1 with the difference that in example 3 as a salt of stearic acid used calcium stearate, and apply corn starch, and in examples 4, 5 as starch used potato starch. Obtained in examples 3-5 tablets comply with pharmacopoeial requirements and have a shelf life of over 2 years.

12,5)
Table 1
IngredientsContent, wt.%
Examples
12345
The active principle, includingof 17.5the 17.34,535,07,0
the enalapril maleate(5,0(7,7(2,0(10,0(2,0
- hydrochlorothiazide9,6)2,5)25,0)5,0)
Sodium bicarbonate4,58,02,010,52,5
Starch9,022,59,08,01,0
Milk sugar67,851,782,9945,088,45
Iron oxide0,20,10,010,50,05
Salt of stearic acid1,00,41,51,01,0
Only100,0100,0100,0100,0100,0

Table 2
ExampleThe ratio of enalapril maleate and hydrochlorothiazide, parts by weight/parts by weightRelease

analapril maleate/hydrochlorothiazide, % after 45 min
The expiry date, the month
11:2,5100,0/98,0> 27
21:1,2599,5/96,5> 27
31:1,25of 97.8/a 94.2over 24
41:2,590,7/85,5over 24
51:2,595.3 per 90,6over 24

1. The tool with the hypotensive action, containing as active principle a combination of enalapril maleate and hydrochlorothiazide is used as excipients sodium bicarbonate, starch, milk sugar, iron oxide and salt of stearic acid in the following ratio of ingredients, wt.%:

The active principle4,5-35,0
Sodium bicarbonatethe 2.0-10,5
Starchfrom 1.0 to 22.5
Iron oxide0,01-0,5
Salt of stearic acid0,4-1,5
Milk sugarRest

2. The tool according to claim 1, characterized in that it contains enalapril maleate and hydrochlorothiazide in the ratio of 1:1,25.

3. The tool according to claim 1, characterized in that it contains enalapril maleate and hydrochlorothiazide in the ratio of 1:2,5.

4. The tool according to claim 1, characterized in that it contains as a salt of stearic acid magnesium stearate or calcium.

5. The tool according to claim 1, characterized in that it contains as starch mixture of the modified potato starch is.

6. The tool according to claim 5, characterized in that the ratio of modified potato starch is 1:(7-20).

7. A tool according to any one of claims 1 to 6, characterized in that it is made in the form of solid dosage forms.

8. The tool according to claim 7, characterized in that it is made in the form of tablets.



 

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