The way prolonged physiological effect of timolol to lower the intraocular pressure

 

(57) Abstract:

The invention relates to the field of medicine, particularly, to a method of prolonging therapeutic effect of timolol drug belonging to the group nekardioselektivnym beta - blockers used to reduce intraocular pressure and treating glaucoma. The invention solves the problem of reducing the dose of timolol and prolongation of its ability to reduce intraocular pressure, this result is achieved in a method of prolonging therapeutic effect of timolol, including the use of timolol in combination with compounds that enhance its ability to reduce intraocular pressure, as compounds that enhance a specific effect of timolol, use hyaluronic acid, with timolol and hyaluronic acid take in a mass ratio of 1:2-4, and the concentration of the solution containing this combination is 0.01 to 0.05%. table 1.

The way prolonged physiological effect of timolol to lower the intraocular pressure.

The invention relates to the field of medicine particularly, to a method of prolonging therapeutic effect of timolol drug belonging to the group of nocardiosis>/P>It is known the use of timolol in the treatment of chronic open-angle glaucoma /2,3/. However, this drug, which is a chemical structure of (-)-1-(tert. -butylamino)-3-(4 - morpholino-1,2,5-thiadiazol-3-oxy)-2-propanol,

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itself slightly decreases the intraocular pressure elevated intraocular pressure and this effect is seen only for 1-2 hours

In this regard, attempts were made to enhance and prolong the action of timolol by using it in combination with various miotikami (pilocarpine), agonists and carbonic anhydrase inhibitors (e.g., diakarbom) /4/. However, such combinations include the use of sufficiently high doses of ingredients that allows you to cause bronchospasm and other side effects /5/, and the duration of their therapeutic effect does not exceed 2-4 PM

Closest to the claimed adopted for the prototype, is a method of prolonging therapeutic effect of timolol /6/ based on the purpose of various dosage forms containing a combination of 0.5-20 wt.h. timolol n-1 wt.h. 13,14-dihydro-15-keto-prostaglandins.

The disadvantages of this method are associated with nemennym (not more than 5-6 h) decrease intra-ocular pressure.

The invention solves the problem of reducing the dose of timolol and prolongation of its ability to reduce intraocular pressure.

This result is achieved in a method of prolonging therapeutic effect of timolol, including the use of timolol in combination with compounds that enhance its ability to reduce intraocular pressure, as compounds that enhance specific pressure timolol use hyaluronic acid, with timolol and hyaluronic acid take in a mass ratio of 1:2 to 4, and the concentration of the solution containing this combination is 0,01-0,05%

The inventive method has advantages over known in part to the fact that the duration of intraocular pressure reduction with the introduction of the combination of timolol and hyaluronic acid (used the drug timolol company "Sigma", USA and domestic hyaluronic acid on THE 9185-00317204830-93) is 24-48 h after a single instillation in the eye. To achieve this effect, use 1-2 drops of 0.01 to 0.05% solution, i.e., 0.005 - 0.01 g of the drug per reception, while used in the known method dose of timolol 0.05-10 mg, i.e., are 10-100 times higher.

The invention is illustrated by the following examples of its implementation.

1. A mixture of 1 g (1 wt.h.) of timolol and 2 g of hyaluronic acid (2 wt.h.) dissolve in a small amount of water, the solution is filtered through a sterile filter paper and diluted under aseptic conditions with sterile water to a 0.01% solution (about 30L of water, which is poured into the tube-dropper 10 ml Instillation into the eyes of 1-2 drops of this solution leads to a sustainable reduction of intraocular pressure in 24-48 hours

2. A mixture of 1 g (1 wt.h.) timolol 3 g hyaluronic acid (3 wt.h.) dissolve in a small amount of water and then proceed as in example 1 to obtain of 0.025% solution (about 16 liters of water), which has a similar effect.

3. A mixture of 1 g of timolol (1 wt.h.) and 4 g of hyaluronan acid (4 wt.h.) dissolve in a small amount of water and then proceed as in example 1 to obtain a 0.05% aqueous solution (about 10 l of water), which has a similar effect.

Comparative analysis of technical and economic indicators of the well-known SP is th dose of timolol compared with the known method and significant (5-10 times) prolongation of its ability to reduce intraocular pressure.

The way prolonged physiological effect of timolol to lower the intraocular pressure, which consists in adding to the aqueous solution of timolol excipients, characterized in that as an auxiliary substance use hyaluronic acid, which is taken at the rate of 2 to 4 wt. including acid 1 wt.h. timolol, and the process is continued until reaching the concentration of the solution calculated for both components 0,01 0,05%

 

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