Means for treating patients for articulation diseases

FIELD: medicine.

SUBSTANCE: means is found to be lyophilisate containing glycosamine salt and tromethanol taken in known proportions.

EFFECT: high active ingredient concentration in the preparation; high speed and effectiveness of diffusion into articulation zone.

2 cl,1 tbl

 

The invention relates to medicine, namely preparations for the treatment of diseases of the joints.

Disease affects about 70% of the population older than 45 years. They are manifested as pain in the joint, aggravated by motion, sensation of tightness. Inflammatory processes are accompanied by swelling, change in shape of the joints.

In addition, when astrologicheskih diseases of the joints gradually destroys the cartilage covering the articular surfaces, as well as bone tissue and the inner surface of the articular capsule.

Currently widespread in the world of medical practice for the treatment of diseases of the joints (arthritis, arthrosis, osteochondrosis, etc.) received drugs on the basis of saccharides (chondroitin sulfate, glucosamine salt), mainly in the form of tablets, capsules and injections. Treatment with these drugs not only reduce inflammation and pain in the joints, but also produces the restoration of damaged cartilage tissue [Nasonov EL Clinical guidelines and algorithms for clinicians, Rheumatology, M., 2004; K.Pavelka, Archives Internal Medicine, №10, 2002, №7, 2003].

Closest to the claimed composition is an injectable preparation containing as an active ingredient saccharide-glucosamine hydrochloride (acidic saccharide with a pH of an aqueous solution of 1.2 to 2.5), neutralizing the medium is in the on the contrary, a local anesthetic agent - trimekain and excipients [RF patent №2118156]. Its disadvantages are as follows:

- the drug is a two-component solution containing a vial with a solution of glucosamine hydrochloride and a vial with a solution of Ethylenediamine. The preparation for the introduction of patient consists in mixing the contents of two vials in the syringe immediately before injection of;

neutralizing agent is Ethylenediamine - liquid with a boiling point 116°and, therefore, cannot be used to prepare one-component preparation (HA + neutralizing agent) in the form of a lyophilisate;

- the use of Ethylenediamine in the product in relatively high concentrations (>3 wt.% in relation to glucosamine) requires a supplemental part of the preparation of local anesthetic products - trimekainom that, in turn, causes a number of undesirable side effects.

The problem solved by the invention is the development of single injection of the drug for the treatment of diseases of the joints in the form of a lyophilisate, combining chondroprotective action with high pharmacokinetic parameters and bioavailability with the exception of the disadvantages of the prototype.

The technical result from the use of the image is to be placed is to increase the specific concentration of active ingredient in the drug and, as a consequence, increase the speed and efficiency of diffusion of the active substance in the joint area.

For the achievement of the proposed remedy for the treatment of diseases of the joints, representing a lyophilisate containing saccharide - glucosamine salt and neutralizing agent is an aliphatic amine - trometamol in the following ratio, wt.%:

glucosamine salt - 98,0-99,9

trometamol - 0,1-2,0

As salts of glucosamine can be used a known pharmaceutical substance (registered in the Russian Federation or imported, the relevant requirements of United States Pharmacopeia 27 editions): glucosamine hydrochloride, sodium or potassium salts of glucosamine sulfate. Preferred is the use of disodium salt of glucosamine sulfate and glucosamine hydrochloride. Low molecular weight of these saccharides (573,3 and 215,0 daltons, respectively) and their high pharmacological activity [Eszteca, Scientific-practical rheumatology, No. 2, 2003] in the treatment of diseases of the joints ensure the creation of effective chondroprotective drugs.

The neutralizing agent is trisamin (trade name), registered as a pharmaceutical substance in Russia №78/702/1. International name - trometamol. The chemical name is 2-Amino-2-(hydroxymethyl)-1,3-propandiol

The number added to the glucosamine trisamina is determined by the acidity of the commercial sample used salt and installed in each experiment specifically to obtain before filling the original solution with physiological pH value of 5.0 to 8.0.

It was established experimentally that the introduction of the injectable antacid systemic action - trisamina with buffer properties and local anesthetic action, which significantly accelerates the transport of the active substance into the bloodstream of a living organism. Trisamin, penetrating through the cell membrane, increases the transport, bioavailability and specific content of glucosamine in the joint area. These increases bioavailability of the active ingredient and increased anti-inflammatory properties of the drug is also associated with the ability of supramolecular structures created in the claimed pharmaceutical compositions, to change the state of the environment in the microenvironment of the saccharide.

Pharmacological group - 8.8. Concealer metabolism of bone and cartilage (Register of medicines of Russia, 2005 edition).

The preparation is carried out by known methods lies in the dissolution of the active ingredients in water, sterile filtered, followed by filling into ampoules and freeze accourate.

Control the quantitative content of the active ingredients (glucosamine, trisamin) in the preparations is carried out by known methods adopted for similar legform registered in the Russian Federation and contains the active ingredients (spectrophotometry, titration values).

Example 1. 100 g of glucosamine sulfate ×2NaCl dissolved at a temperature not exceeding 40°With 400 ml of distilled water, add with stirring for about 0.5 g of trometamol (to pH 6,0-7,5). The solution is sterile filtered through a sterile 0.22 μm filters and pour into sterile ampoules of 2 ml Mode lyophilic drying of the drug includes its freezing at -80°and drying in vacuum at room temperature for 10 hours. In the final preparation of 1 ampoule contains 400 mg of glucosamine sulfate ×2NaCl and 2.0 mg (0.5 wt.%) trisamina.

Example 2. 100 g of glucosamine sulfate ×2l dissolved at a temperature not exceeding 40°With 400 ml of distilled water, add with stirring to about 0.1 g of trometamol (to pH 6,0-7,5). The solution is sterile filtered through a sterile 0.22 μm filters and pour into sterile ampoules of 2 ml Mode lyophilization of example 1. In the final preparation of 1 ampoule contains 400 mg of glucosamine sulfate ×2l and 2.0 mg trisamina (0.1 wt.%).

Example 3. 100 g of glucosamine hydrochloride is dissolved when temperaturee above 40° With 400 ml of distilled water, add with stirring, about 2 g of trometamol (to pH 6,0-7,5). The solution is sterile filtered through a sterile 0.22 μm filters and pour into sterile ampoules of 2 ml Mode lyophilization of example 1. In the final preparation of 1 ampoule contains 400 mg of glucosamine sulfate ×2l and 8.0 mg trisamina (2.0 wt.%).

The drug efficacy was studied in models of post-traumatic osteoarthritis, the collapse of the ears of rabbits and aseptic inflammation of the limbs of rats.

When the subchondral defects of the femoral head in rats caused by surgical injury of the articular cartilage, the proposed drug significantly reduces the size of the defect compared to control animals.

When intravenous papain in rabbits there is a collapse of the ears - sagging their peripheral end. The use of the proposed drug allows you to restore turgor ears, which indicates the inhibition of the destruction of the cartilage of the ears.

Comparative evaluation of chondroprotective action of drugs Glucit-1 (obtained in example 1 description of the application) and Glucat-2 (obtained in example 1 description of the prototype) was studied in experiments on rabbits rentgenograficheski to change the size of the joint space according to the established procedure (see table).

The rst is by biological research harmlessness of the drug showed that single administration of the drug in doses of 100-200 times higher than the minimum therapeutic for a person, it is practically non-toxic. The preparation is stable for at least 2 years of observation.

Preliminary clinical tests have confirmed its high chondroprotective activity and good tolerability in the treatment of arthritis and degenerative disc disease.

Table
MedicationIndicators (n=20)Reducing the size of the joint space
Very good and good effectModerate effectNo
Glucit-166268
Glucat-2402040

1. For the treatment of diseases of the joints, with chondroprotective and anti-inflammatory action, representing a lyophilisate containing a salt of glucosamine and aliphatic amine, characterized in that as the aliphatic amine is used trometamol, in the following ratio, wt.%:

Salt of glucosamine98,0 to 99.9
Trometamol0,1-,0

2. The tool according to claim 1, characterized in that salts of glucosamine uses glucosamine hydrochloride or sodium or potassium salts of glucosamine sulfate.



 

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