Pharmacological composition with anti-tuberculosis action

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and medicine, in particular to composition, which possesses bacteriostatic and bactericidal action and is intended for treatment of tuberculosis diseases. Pharmacological composition with anti-tuberculosis action contains active substances - anti-tuberculosis medications (ethambutol, isoniazid, rifampicin, pirazinamide) and as potentiating agent of synergetic action, enhancing impact of chemical preparations, stabilised nanoparticles of silver.

EFFECT: invention possesses properties allowing to inhibit medication-resistant strains of tuberculosis mycobacteria.

5 ex, 1 tbl

 

The invention relates to medicine and can be used to create drugs combined form with bactericidal and bacteriostatic properties for use in the treatment of patients with drug-resistant forms of tuberculosis.

Known means for the treatment of tuberculosis (plain products)that suppress the bacterial population. The use of such drugs (isoniazid, rifampicin) does not terminate the persistence part of mycobacteria, which are stored mainly intracellular (inside phagocytes). It should also be noted that in the treatment of one anti-TB drug (monotherapy) is rapidly emerging drug resistance of Mycobacterium tuberculosis (MBT) (for example, the drug "Akrikhin").

There is a method of treatment of tuberculosis isoniazid with silver water (EN 2003335, AK 33/38). It should be noted that the silver is present here in the form of ions, and this form of particles are very unstable over time, which significantly reduces the useful life of the medicinal product. The disadvantage of this drug is that it is prepared immediately before use, which is not always convenient for treatment.

In the patent RU 2240806 AC 33/38 also describes the use of silver water as a Supplement to the treatment of tuberculosis is traditional chemotherapeutic drugs. There's preparation, including the silver water, is introduced into the trachea or bronchi in the form of aerosols or through a catheter, or via the thoracic intercostal puncture. This method of treatment is quite difficult, and in some cases even dangerous for the patient. Also the disadvantages of this drug is the instability of silver that is present in the form of ions.

Closest to the proposed pharmaceutical composition is combined antituberculosis drug myrin P (MYRIN P, manufacturer Lederle Laboratories, UK)adopted for the prototype, providing antibacterial anti-TB activity at different stages of disease development. It contains in its composition ethambutol - 32 wt.%, isoniazid is 8.5 wt.%, rifampicin -17 wt.%, pyrazinamide - to 42.5 wt.%.

Ethambutol, penetrating into the growing bacteria, inhibits cellular metabolism, stopping the development of pathogens. Rifampicin has a bactericidal effect by inhibiting RNA polymerase office. Isoniazid active against intracellular M. tuberculosis. Pyrazinamide improves the penetration of chemotherapy into the private pockets of infection.

Myrin P sufficiently effective for the treatment of intensive phase treatment of pulmonary tuberculosis and tuberculosis of other organs.

However, the disadvantage of this drug is the number of spin-off de the action on the digestive system, nervous system and blood system. It is also known that treatment of tuberculosis marinom P in some cases leads to the emergence of drug resistance.

The task of the claimed invention is to provide pharmaceutical compositions TB action long shelf life, high effectiveness of the treatment, with the exception of side effects on the patient's body and improving therapeutic effect due to attenuation, and exclude the factor of drug resistance.

The task is solved in that the pharmacological composition of TB action, containing as active substance anti-TB drugs (ethambutol, isoniazid, rifampicin, pyrazinamide), additionally contains as a potentiating component synergistic actions aqueous solution stabilized silver nanoparticles with a size of 20-100 nm. The invention consists in a synergistic potentiating effect of stabilized silver nanoparticles, leading to a significant or complete recovery of sensitivity to drug-resistant forms of the office.

The inventive pharmaceutical composition comprises as active substances of anti-TB drugs: ethambutol, isoniazid, rifampicin, pyrazinamide (all PR the production JSC JFK "Akrikhin") and potentiating component synergistic effects - the silver nanoparticles in the following ratio, wt.%:

Ethambutol25,0-35,0
Isoniazid8,0-10,0
Rifampicin15,0-20,0
Silver nanoparticles0,2-0,6
Pyrazinamideto 100.0

Despite the fact that the components of the inventive pharmaceutical compositions TB actions are used as drugs (or are members of various dosage forms), however, the composition having the claimed combination of features by a certain proportion, was not previously known.

The inventive pharmaceutical composition of TB action was prepared as follows.

In the aqueous medium containing the stabilized silver nanoparticles, with stirring successively introduced the estimated number of drugs in powder form. After complete dissolution were vacuum at 40-50C to constant mass.

Example 1

In a flask equipped with a stirrer, was loaded with 500 ml of water, containing the nd 0.1 wt.% silver nanoparticles (0.5 g), include mixing, sequentially add powdered drugs: ethambutol - 30.0 g, isoniazid - 8.0 g, rifampicin - 20,0 g, pyrazinamide - 41,5, After the complete dissolution of the contents of the flask vacuum at 40-50C to constant weight. Get a 100.0 g composition.

Example 2

Analogously to example 1, but with the following downloads components:

300 ml of aqueous medium containing 0.3% of silver nanoparticles, ethambutol - 25,0 g, isoniazid - 10,0 g, rifampicin - 15.0 g, pyrazinamide - 49,7, Get a 100.0 g composition.

Example 3

Analogously to example 1, but with the following downloads components: 200 ml aqueous medium containing 0.2% of silver nanoparticles, ethambutol - 35,0 g, isoniazid - 10,0 g, rifampicin - 20,0 g, pyrazinamide of 34.8, Get a 100.0 g composition.

Example 4

Analogously to example 1, but with the following downloads components:

600 ml of an aqueous medium containing 0.6% of silver nanoparticles, ethambutol - 25,0 g, isoniazid - 9.0 g, rifampicin - 18.0 g, pyrazinamide, with 47.4, Get a 100.0 g composition.

Example 5 - prototype.

The study of inhibition of growth of drug-resistant Atlantov the office held by the absolute concentration method using nutrient dense Lowenstein-Jensen medium. The research material was obtained in the laboratory goose Yao "Regional TB hospitals is from 30 patients with various forms of pulmonary tuberculosis. All selected strains office (740 PCs) had drug resistance to various anti-TB drugs (from monostichous to extensive drug resistance). The potential synergistic effect of silver nanoparticles was demonstrated by the fact that drug-resistant strains of the restored sensitivity to chemotherapy and was determined suppression of the growth of the office. The evaluation of the results of research conducted by counting colonies in the experimental samples (examples 1-4) compared with the control (example 5-prototype), where he distinguished four degrees of inhibition of growth of the office (full, significant, moderate suppression and no suppression).

The table presents summary results for the study of the ability of the claimed pharmaceutical compositions of anti-TB activity (examples 1-4) and drug-prototype to suppress the growth of drug-resistant (LU) strains of the office.

Pharmacological composition of the TB action, containing as active substances of anti-TB chemotherapy - ethambutol, isoniazid, rifampicin, pyrazinamide, characterized in that it further comprises a potentiating component synergistic effects - the silver nanoparticles, in the following ratio, wt.%:

Ethambutol25,0-35,0
Isoniazid8,0-10,0
Rifampicin15,0-20,0
Silver nanoparticles0,2-0,6
Pyrazinamideto 100.0



 

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