Preparation for interrupting and treating ischemic cardiac disease and method for its manufacturing

FIELD: pharmaceutics, medicine.

SUBSTANCE: the present innovation deals with cardiotherapy for treating and preventing coronary deficiency. The preparation is designed as a plate (film) consisted of three layers, each of them is manufactured out of co-polymer of vinyl pyrrolidone, acrylamide and nitroglycerin-containing ethylacrylate; moreover, internal layer additionally contains solid fat - cacao oil, and weight ratio for the sum of external layers to internal corresponds to 1 : 1. The suggested preparation could additionally contain brilliant green dyestuff. The preparation should be manufactured out of pre-obtained mixture of nitroglycerin and copolymer in solution of alcohol and water followed by layer-by-layer forming three-layer film due to spreading the mixture onto solid bottom plate and drying at 30-50 C. The innovation provides higher adhesion to gingival mucosal surface, decreased side action, improved bioavailability and stability of therapeutic effect.

EFFECT: higher efficiency of therapy.

3 cl, 3 ex

 

The invention relates to pharmaceutical medicine, more specifically to the development and study of prolonged dosage forms used in cardiotherapy for the treatment and prevention of coronary insufficiency.

It is known that the effect of prolongation is obtained by applying a polymer membranes, soluble in the environments of the gastrointestinal tract, such as “Sustak”, “Nitrong and others (Mashkovsky PPM “Drugs”, M. 1993, vol. 1, str). Such funds may be used for oral administration only for the prevention of coronary heart disease and do not provide immediate relief of angina.

Closest to the present invention is a tool for control and treatment of coronary heart disease, containing copolymer, nitroglycerin and dispersion of solid fats, that provides a long lasting selection of cardiorespiratory (RF Patent No. 806037, publ. 23.02.81, Byulluteni inventions No. 7).

However, the known tool has a significant drawback. Introduced in the means of dispersion of fats along with the positive effect of giving the desired liquid greatly reduces the adhesion means to the surface of the gums, resulting in deteriorating the bioavailability and stability of therapeutic effect observed adverse cases migration cf is DSTV on the mouth, grinding and swallowing, which is accompanied by an overly large nitroglycerin in the blood and severe side symptom headache (Blizzard VI Handbook on clinical pharmacology of cardiovascular drugs”, M. 2002, p.86-87).

The technical object of the present invention is to increase the adhesion means to the mucosal surface of the gums, preventing their migration through the mouth, possible chewing and swallowing, reduced side effects, improved bioavailability and stability of therapeutic effect.

The technical result is achieved in that the means for control and treatment of coronary heart disease, containing nitroglycerin, the copolymer dispersion of solid fat made from three layers, each of which copolymer contains a copolymer of vinylpyrrolidone, acrylamide and acrylate, and the dispersion of the solid fat - cocoa butter is distributed only in the inner layer, the ratio of the components in the layers ranges (wt. -%):

the outer layers

- copolymer of vinylpyrrolidone

acrylamide, acrylate 92.0-96.0

- nitroglycerin 4.0-8.0,

the inner layer

- copolymer of vinylpyrrolidone

acrylamide, acrylate 75.0-88.0

- nitroglycerin 4.0-10.0

- cocoa butter, 8.0-15.0

when the mass ratio of the sum on uinyh layer to the inner layer 1:1.

To identify the dose of nitroglycerin the tool may additionally contain dye brilliant green in the number (1-3) of 10-2wt. -%

Means get using the dissolution of the copolymer of nitroglycerin in a coincidental solvents or in a common solvent, and forming is conducted sequentially in three layers from solutions with a concentration of from 12 to 30% wt. on solid substrates, followed by drying at a temperature of 30-50°C. the resulting tape or plate is formed into a tool of the required size and shape.

The proposed method is illustrated by examples.

Example 1

Prepare the composition by means of the following composition:

for the formation of the outer layers

- nitroglycerin - 2.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 46.0

210 g of distilled or demineralized water dissolve 46 g of a copolymer of vinylpyrrolidone, acrylamide, ethyl acrylate. The copolymer solution is mixed with 50 g of 4%alcohol solution of nitroglycerin. Get solution of 17.8% concentration, which is subjected to deaeration;

for forming the inner layer

- nitroglycerin - 2.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 42.0

- cocoa butter - 8.0

42 g of a copolymer of vinylpyrrolidone, acrylamide, ethyl acrylate are dissolved in 190 g of distilled or Demin is alizirovannoj water, receiving a solution of 21%concentration 8 g cocoa butter put 50 g of 4%alcohol solution of nitroglycerin, heated to 35-40°until complete melting of cocoa butter, intensively stirred for 5-10 min and cooled to 18-20°C. Receive a suspension, which with constant stirring is introduced into the copolymer solution prepared previously.

Solutions consistently by any known method applied in layers on an inert substrate, dried at a temperature of from 30 to 50°With and formed from strip or plate is formed of a plate of the required size and shape, providing a given dosage of the drug substance is nitroglycerin.

Example 2

Prepare the composition by means of the following composition:

for the formation of the outer layers -

- nitroglycerin - 4.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 44.0;

for forming the inner layer

- nitroglycerin - 4.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 36.0

- cocoa butter - 12.0

Then proceed as described in example 1.

Example 3

Prepare the composition by means of the following composition: for the formation of the outer layers -

- nitroglycerin - 8.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 88.0

- brilliant green - 0.01 (over 100);

for forming the inner layer

<> - nitroglycerin - 8.0

- copolymer of vinylpyrrolidone

acrylamide, acrylate - 81.0

- cocoa butter - 15.0

- brilliant green - 0.02 (over 100)

During mixing of the solutions of the copolymer and nitroglycerin in the preparation of compositions for the outer layers and an inner layer of the composition is administered accordingly 0.01 g to 0.02 g of brilliant green.

Then proceed as described in example 1.

In contrast to the known means of the proposed remedy does not contain lipophilic particles in the outer layers of the hydrophilic carrier, provides good adhesion to the mucous membrane of the gums, promotes a more even allocation of the drug substance, reduces side effects such as headache and eliminates the possibility of abrupt changes in blood pressure, improves the bioavailability and stability of therapeutic action of the drug.

1. Means for control and treatment of coronary heart disease, containing copolymer, nitroglycerin and dispersion of solid fats, characterized in that it is made in the form of plates (film) three layers, each of which copolymer contains a copolymer of vinylpyrrolidone, acrylamide and acrylate, the inner layer further comprises as a dispersion of solid fats cocoa butter, while the ratio of the components in the layers is, m is S.%:

outer layers -

- copolymer of vinylpyrrolidone

acrylamide, acrylate 92,0-96,0

nitroglycerin 4,0-8,0,

the inner layer

- copolymer of vinylpyrrolidone

acrylamide, acrylate 75,0-88,0

nitroglycerin 4,0-10,0

cocoa butter 8,0-15,0

when the mass ratio of the sum of the outer layer to the inner layer 1:1.

2. The tool according to claim 1, characterized in that it additionally contains a dye brilliant green in the number (1-3)·10-2wt.%.

3. Method for the production of tools for kopirovni and treatment of coronary heart disease, comprising the combination of copolymer and nitroglycerin with subsequent formation of plates (film), characterized in that the formation carried out in layers on an inert substrate of the two outer and inner layers of the water-alcohol solutions with a concentration of 12 to 30 wt.% followed by drying at a temperature of 30-50°C.



 

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