A method of obtaining a solution of aminocaproic acid injection

 

(57) Abstract:

The invention relates to the field of pharmaceutical industry and relates to a method of obtaining a solution for injection, aminocaproic acid, an inhibitor of fibrinolysis, i.e. the dissolution of a blood clot own enzymes of the body. The invention lies in the fact that the solution of Epsilon-aminocaproic acid injection, obtained by preparation of a solution of sodium chloride with aminocaproic acid, taken in therapeutically permitted quantities in the gradual heating the resulting solution to a temperature of 50-60°C under stirring for 20-40 min, followed by exposure of the solution at a temperature of 98-102°C for 20-25 min, pre-filtration of coarse solids and sterile membrane filtration. The invention ensures the production of high quality injection solution. 1 PL.

The invention relates to Epsilon-aminocaproic acid for injection, namely, to a method for solution for injection, aminocaproic acid, an inhibitor of fibrinolysis, i.e. the dissolution of a blood clot own enzymes of the organism.

Epsilon-aminocaproic acid - kristalli the ora of isotonic sodium chloride solution (Mashkovsky M. D. Drugs, 2001, T. 1, page 470).

Known use in combined preparations, for example in a mixture with Dimedrol for the treatment of rhinitis (U.S. Pat. Of the Russian Federation No. 2082405), mixed with fibrinogen in surgery (U.S. Pat. Of the Russian Federation No. 2089248).

A method of obtaining solution for injection, which consists in the direct dissolution of the active substance, usually in powder form immediately before use. To do this in a bottle with the drug, which was sealed with a rubber stopper and balcova aluminum cap, enter the necessary amount of isotonic sodium chloride solution. If necessary, the bottle can be warmed in a water bath up to 60-70°C, cooled and then administered intravenously to the patient (U.S. Pat. Of the Russian Federation No. 2060031).

The method has the following disadvantages:

- lack of assurance of sterility of the drug,

- the impossibility of ensuring a sufficient degree of mechanical purity of the drug intended for intravenous injection

- the absence in domestic practice, filters, nozzles disposable to ensure mechanical purity solutions and sterility in the clinical setting.

In addition, it tripreport in industrial production aminocaproic acid, which is also very hygroscopic. Factories are reluctant to undertake the production of such drugs.

To ensure sterility, and liberation from mechanical impurities company Wellcome, England, offers a solution preparations before entering the patient to filter through a special syringe-nozzle disposable.

A method of obtaining solutions for injection, including the dissolution of the active substances and auxiliary components in water for injection at a temperature of 30 to 60°C with constant stirring, filtering the resulting solution through a sterilizing filter (pore size 0.22 μm), filling in aseptic conditions solution in sterile vials, closing rubber plugs under running aluminum caps (U.S. Pat. Of the Russian Federation No. 1819613).

The closest technical solution to the declared object is a method of obtaining injectable solutions, including dissolved in isotonic Epsilon-aminocaproic acid under stirring, followed by sterilization known method (U.S. Pat. Of the Russian Federation No. 2128030). The method is used to obtain the drug Wisecup used in ophthalmic surgery for the prevention of hemorrhagic complications.

Weeks the tion by autoclaving may cause partial decomposition of aminocaproic acid.

The purpose of this invention is to improve the reliability of sterile filtration, which will allow to achieve high quality injection solution of aminocaproic acid.

This goal is achieved through the use of the method of obtaining the solution of Epsilon-aminocaproic acid for injection, which consists in the preparation of a solution of sodium chloride with aminocaproic acid, taken in therapeutically permitted quantities in the gradual heating the resulting solution to a temperature of 50-60°C under stirring for 20-40 min, followed by exposure of the solution at a temperature of 98-102°C for 20-25 min, pre-filtration of coarse solids and sterile membrane filtration at a filtration rate of(0,2-0,3)·10-3m·s-1.

The bottling and sterilization of the finished product is carried out at a temperature 120-122°C and a pressure of 0.20 MPa for 13-17 minutes, then produce the sealing rubber plugs, compressed aluminum caps.

When heated aminocaproic acid leads to the formation of 7-membered lactam (-caprolactam), which was determined with analytical control polarographic method. When rastvorosmesiteljah quantities since temperatures above 130°C. the Resulting admixture is possible to filter on a sterile membrane filters with a filtration rate of(0,2-0,3)·10-3m·s-1.

When the claimed filtration rate was able to completely clean the solution from impurities. Membrane filtration is carried out with the use of the disc holder of the company “Millipor”. The filter holder is placed in a membrane with a pore diameter of 0.2 μm “Vladipor” type FMAC. For sterilizing filtration use capsules made of polypropylene with hydrophilic membrane 0.22 μm Sartobran P company “Sartrius”.

The method is as follows

Example 1. In capacitive heated apparatus, equipped with a stirrer, a pre-prepared solution of sodium chloride concentration of 0.9% at room temperature, add a therapeutic amount of aminocaproic acid. Then the resulting solution was gradually heated to a temperature of 50°C, stirred for 20-40 minutes To the solution add a buffer to a pH of 7.0 to 8.0 with the calculated amount of water. Maintain the solution at a temperature of 98°C for 20 minutes Carry out a preliminary filtering of coarse solids. Sterile membrane filtration in / min net is the. The filter holder is placed in a membrane with a pore diameter of 0.22 μm “Vladipor” type FMAC. For sterilizing filtration use capsules made of polypropylene with hydrophilic membrane 0.22 μm Sartobran P company “Sartrius”. The bottling is carried out according to GOST 10782-85 dose of 100 ml Capping produce tubes of rubber compound 52-369/1, compressed aluminum caps. After filling sterilized finished product at a temperature of 120°C and a pressure of 0.20 MPa for 15 minutes

Example 2. In capacitive heated apparatus, equipped with a stirrer, a pre-prepared solution of sodium chloride concentration of 0.9% at room temperature, add a therapeutic amount of aminocaproic acid. Then the resulting solution was gradually heated to a temperature of 60°C, stirred for 20-40 minutes To the solution add a buffer to a pH of 7.0 to 8.0 with the calculated amount of water. Maintain the solution at a temperature of 102°C for 20 minutes Carry out a preliminary filtering of coarse solids. Spend a sterile membrane filtration at a filtration rate of 0,3·10-3m·s-1. Further as described in example 1. After filling sterilized finished product when temperam stirrer, pre-prepare a solution of sodium chloride concentration of 0.9% at room temperature, add a therapeutic amount of aminocaproic acid. Then the resulting solution was gradually heated to a temperature of 55°C, stirred for 20-40 minutes To the solution add a buffer to a pH of 7.0 to 8.0 with the calculated amount of water. Maintain the solution at a temperature of 100°C for 20 minutes Carry out a preliminary filtering of coarse solids. Spend a sterile membrane filtration at a filtration rate of 0,25·10-3m·s-1. Further as described in example 1. After filling sterilized finished product at a temperature of 121°C and a pressure of 0.20 MPa for 15 minutes

A method of obtaining a solution of Epsilon-aminocaproic acid for injection, which consists in the preparation of a solution of sodium chloride with aminocaproic acid, taken in therapeutically permitted quantities, with stirring and subsequent sterilization in a known manner, characterized in that gradually heat the resulting solution to a temperature of 50-60°C under stirring for 20-40 minutes, maintain the solution at a temperature of 98-102°C for 20-25 min, filtered from ·10-3-1.



 

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