Dosage form having antihypertensive, vasodilator, anti-atherosclerotic inflammatory action, and method of its manufacture

 

(57) Abstract:

The invention relates to the field of pharmaceutical industry and relates to solid dosage forms of drugs that have a protective effect against the development of atherosclerosis and coronary heart disease, and is effective for the treatment of benign prostatic hyperplasia. The invention consists in that the dosage form contains the following components: doxazosin, calcium stearinovokisly, calcium phosphate, polyvinylpyrrolidone, sodium dodecyl sulphate, talc, sugar, dairy. Also disclosed a method of manufacturing a dosage form. The invention provides no loss of doxazosin in the process of getting in shape, improving the physico-chemical parameters and increase the biological availability of the active component. 2 AD. and 2 C.p. f-crystals, 3 tables.

The invention relates to medicine, in particular to a pharmacy, can be used in the manufacture of solid dosage forms of drugs that have a protective effect against the development of atherosclerosis and coronary heart disease, and effective for the treatment of benign prostatic hyperplasia.

Known dosage form with antihypertensive, sossoudorasshirate substance - doxazosin in doxazosin nelfinavir, auxiliary substances: mixture of exopolysaccharide and Aerosil, magnesium stearate, sodium sodium dodecyl sulphate, polyvinylpyrrolidon and lactose (milk sugar) (EN 2190392, publ. 10.10.2002).

The way to obtain this form provides for the mixing of Aerosil with exopolysaccharide, adding doxazosin, stirring, followed by hydration of the mixture polyvinylpyrrolidone and granulation of the obtained hydrated mixture. Then the granulate is dried, optivault the stearate and tabletirujut.

The disadvantages described dosage form, and method of its manufacture is that there are losses of doxazosin in the process of getting in shape, therefore, the variation of the content of active ingredient in the dosage form increases, deteriorating physical-chemical characteristics and reduced bioavailability of the active component.

The objective of the invention is the elimination of all the above drawbacks.

The problem is solved dosage form with antihypertensive, vasodilator, anti-atherosclerotic and antispasmodic effect, containing as an active deystvuyushey sugar, characterized in that it additionally contains as excipients calcium stearinovokisly, calcium phosphate and talc in the following ratio, wt.%:

Doxazosin 0,3-8,0

Calcium stearinovokisly 0,1-2,0

Calcium phosphate 10,0-26,0

Polyvinylpyrrolidone 0,2-2,5

Sodium dodecyl sulphate 0,1-3,0

Talc 0,1-3,0

Sugar dairy Else

In private embodiment of the invention the problem is solved in that the dosage form contains doxazosin in the form of doxazosin nelfinavir.

As polyvinylpyrrolidone form contains Kollidon-30.

The task is also solved by a method of manufacturing the above-described dosage forms, in accordance with which is mixed doxazosin with calcium phosphate, add milk, sugar and sodium dodecyl sulphate, the resulting mixture is moistened with a solution of polyvinylpyrrolidone, re-mix, damp granulation, subsequent drying, dry granulation, the powder mixture of calcium stearinovokisly and talc and tableting.

The invention consists in the following.

The active ingredient doxazosin predstavlyaeyym (monoethanolamine).

The active ingredient doxazosin lowers blood pressure, which reduces the total peripheral vascular resistance, and also has an antispasmodic effect, reducing a tonus of smooth muscle cells.

Doxazosin also reduces the level of total cholesterol, LPN-cholesterol and triglycerides and increases levels of HDL-cholesterol in the serum, which exerts a protective effect against the development of atherosclerosis and coronary heart disease. Doxazosin is used for treating patients with non-insulin-dependent diabetes, because it has a neutral or even a positive effect on insulin and blood glucose.

Doxazosin inhibits platelet aggregation. With prolonged treatment doxazosin reduces the mass of the left ventricle. Doxazosin safe for patients with renal insufficiency, chronic obstructive pulmonary disease, peripheral angiopathy and gout.

Its content in the dosage form is 0.3-8.0 wt.%. Recalculation shows that such content doxazosin is achieved by the introduction of 0.4-10% doksazosin nelfinavir.

As accessories the sodium dodecyl sulphate, talc and milk sugar.

Data supplements easily granularity to the desired size and non-toxic for the organism.

The contents of all of the components are selected in such a way as to achieve the best results when using the well-known auxiliary materials.

Additional introduction to dosage form calcium stearinovokisly, calcium phosphate and talc provides solid tablet with high bioavailability.

The set of operations in the way and their modes are selected in such a way as to simplify the method of manufacturing dosage forms without compromising their quality.

The invention is carried out as follows.

Pre-sifted calcium phosphate and doxazosin mesilate mix thoroughly. To the resulting mixture, with stirring, add pre-sifted sodium dodecyl sulphate and sugar of milk. Thoroughly mixed, the mass of the hydrate 3% solution of kollidon-30, again stirred until a uniform moisture and granularit.

The wet granules are dried at a temperature of 45 to 50°C to a residual moisture of 10,5%. The dried pellets are cooled to room temperature and Provo is logo and talc. The mixture is stirred until a homogeneous tablet mass.

Then tablets weight tabletirujut, receiving tablets biconvex shape with a diameter (0.001 g) 60.2 mm (0.002 g) 70.2 mm (0.004 g) 90.3 mm and a weight of 0.1 g to 0.13 g, 0,26,

Example 1 production of a dosage of 0.001,

Pre-sifted calcium phosphate 35,19 kg and 2,525 kg doxazosin mesilate mix thoroughly. To the resulting mixture, with stirring, add pre-sifted sodium dodecyl sulphate 0,414 kg milk and sugar 165,975 kg. Thoroughly mixed, the mass of the hydrate 3% solution of kollidon-30 number of 27.6 kg, once again stirred until a uniform moisture and granularit.

The wet granules are dried at a temperature of 45 to 50°C to a residual moisture of 10,5%. The dried pellets are cooled to room temperature and conduct a dry granulation. Dry the granulate in the number 201,96 kg optivault adding pre-sifted calcium stearinovokisly 1.02 kg and talc 1,02 kg the Mixture is stirred until a homogeneous tablet mass.

Then tablets weight tabletirujut, receiving tablets biconvex shape with a diameter (0.001 g) 60.2 mm and a weight of 0.1 g in the amount of 201,0 kg

Example 2 doxazosin mesilate mix thoroughly. To the resulting mixture, with stirring, add pre-sifted sodium dodecyl sulphate 0,3105 kg milk and sugar 93,315 kg. Thoroughly mixed, the mass of the hydrate 3% solution of kollidon-30 in number 20,7 kg, once again stirred until a uniform moisture and granularit.

The wet granules are dried at a temperature of 45 to 50°C to a residual moisture of 10,5%. The dried pellets are cooled to room temperature and conduct a dry granulation. Dry the granulate in the number 131,07 kg optivault adding pre-sifted calcium stearinovokisly 0,51 kg and talc 0,51 kg the Mixture is stirred until a homogeneous tablet mass.

Then tablets weight tabletirujut, receiving tablets biconvex shape with a diameter (0.002 g) 70.2 mm (0.004 g) 90.2 mm and a weight of 0.13 g and 0.26 in the number 130,65 kg

In tables 1-3 shows the compositions obtained in accordance with the present invention pills.

In medicinal form, completed in accordance with the claimed group of inventions, not loss doxazosin in the process of getting in shape, improving the physico-chemical parameters and increases the bioavailability of active is acclerations and antispasmodic effect, containing as active doxazosin, and as excipients sodium dodecyl sulphate, polyvinylpyrrolidone and milk sugar, characterized in that it additionally contains as excipients calcium stearinovokisly, calcium phosphate and talc in the following ratio, wt.%:

Doxazosin 0,3-8,0

Calcium stearinovokisly 0,1-2,0

Calcium phosphate 10,0-26,0

Polyvinylpyrrolidone 0,2-2,5

Sodium dodecyl sulphate 0,1-3,0

Talc 0,1-3,0

Sugar dairy Else

2. Dosage form under item 1, characterized in that it contains doxazosin in the form of doxazosin nelfinavir.

3. Dosage form under item 1 or 2, characterized in that as polyvinylpyrrolidone contains Kollidon-30.

4. The method of manufacture of dosage forms with antihypertensive, vasodilator, anti-atherosclerotic and antispasmodic effect, namely, that mix doxazosin with calcium phosphate, add milk, sugar and sodium dodecyl sulphate, the resulting mixture is moistened with a solution of polyvinylpyrrolidone, re-mix, damp Gras is the key.



 

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