Rifampicin-based medication with prolonged action for treatment of resistent forms of tuberculosis

FIELD: medicine.

SUBSTANCE: invention relates to field of pharmacology and medicine and represents rifampicin-based medication of prolonged action for treatment of resistant tuberculosis forms, which is different because it represents stable nanoparticles and contains rifampicic, biodegradable polymer of lactic acid or copolymer of lactic and glycolic acid, as well as surface active substance, cryoprotector, components in medication being in specified ratio in wt %.

EFFECT: invention ensures reduction of risk of toxic effects, prolonged action and reduction of intake factor in treatment.

6 cl, 3 ex, 1 tbl, 1 dwg


The invention relates to the field of pharmacology and medicine, specifically to a new generation of antimicrobial and anti-TB drugs are regulated actions on the basis of 3-[[(4-methyl-1-piperazinil)imino]-methyl]rifamycin or 5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[N-(4-methyl-1-piperazinil)-formimidoyl]-2,7-epoxyphenolic[1,11,13]trientine)oil-[2,1-b]furan-1,11(2H)-dione-21-acetate (rifampicin).

According to the who in 2006 was 9.2 million new cases of tuberculosis (139 per 100,000). It is 100 thousand more than in 2005, In 2006, died of tuberculosis 1.7 million people. In Russia in 2007, the number of patients with multidrug resistance among new cases was 4149 people (9.8% of the total number of newly diagnosed). Just consists on the account at the end of 2007 - 24445 people per 100 thousand population.

A similar pattern is observed with the incidence of gastrointestinal tract, upper and lower respiratory tract, etc. caused by various microorganisms, resistant to most contemporary antibiotics.

One of the modern antibiotic with a broad antibacterial and germicidal action spectrum is a semisynthetic drug rifampicin. Rifampicin is active against M. tuberculosis and therefore widely uses the I for the treatment of tuberculosis in combination with other drugs. The antibiotic is also used for infections of skin, soft tissue, the treatment of pneumonia, lung abscesses, cholecystitis, etc.

The resistance of mycobacteria to rifampicin is developing rapidly, which is a big drawback of antibiotics in this series.

Another negative property of rifampicin is its poor absorption when administered, consequently, it is necessary to apply parenteral.

Rifampin and other antibacterial and bactericidal drugs, has low selectivity of action and with the introduction of the antibiotic patients only a small dose gets into the target cell. A large part of biotransformation and excreted from the body, not having therapeutic effect. In this regard, during treatment with rifampicin, especially its long-term use, recorded numerous adverse effects: allergic reactions (skin rash, eosinophilia), nausea, vomiting, increased liver transaminases in the blood, headache, arthralgia, tubular necrosis, impaired vision, the development of thrombophlebitis and other Rifampin is contraindicated in patients with impaired liver and kidney, pregnant women and during lactation [1].

To solve the problems associated with the toxicity of drugs, contraindications, resistance and so on, it is necessary to solve for the ACI to improve the effectiveness of drugs and therefore, reducing therapeutic dose and toxic effects. The most significant of the possible ways of achieving this goal is the development of drugs or dosage forms which are focused on delivering and localization of drugs in target cells in effective therapy doses. While it is desirable that this property combined with a long gradual release of substances (prolongation of action)that allows you to create a more comfortable environment for patients, displaced regularly and long-term use of drugs.

A new technical result is achieved by the totality of all existing signs created medicines on the basis of rifampicin to achieve positive pharmacodynamic activity of the drug at lower doses and thereby reduce the risk and the degree of occurrence of toxic effects, while achieving the effect of prolongation of the action, reducing the multiplicity of admission for treatment.

The technical result of the invention is achieved through the inclusion of a new drug on the basis of rifampicin, commercially available biodegradable polymers approved for medical use, for nanoparticles. As such used: polylactic acid (PLA), copolymers of glycol is eve and lactic acid (PLGA) and a copolymer of glycolic and lactic acid with a free carboxyl end group (PLGA-COOH).

For nanoparticles used polymers with a molecular mass of from 10 to 300 kDa and a molar ratio of the residues of lactic and glycolic acids from 25:75% to 50:50%. To obtain a stable dosage forms, representing the nanoparticles size of 200-500 nm and having a slow release of antibiotic, are also used surfactants include Polysorbate 80, polyvinyl alcohol (PVA), poloxamer 188, serum albumin and cryoprotectants: mannitol, lactose, glucose and other sugars. The proposed tool get known method simple (single) emulsification (water/oil) [2]. Sorption of rifampicin nanoparticles inside the polymer occurs when the removal of organic solvent from the resulting emulsion, and in the process of formation of the suspension.

It should be noted that earlier similar studies were conducted with Indian, Japanese and Iranian researchers [3-7]. In the works of Indian scientists [3, 4] described getting nanopreparations on the basis of PLGA enabled in the polymer matrix rifampicin, isoniazid, protionamide and ethambutol by ultrasonic emulsification. Preparations showed in vivo high antituberculosis activity within 10 days, while in our case the high activity was maintained and 21 days after the beginning of the experiment. In [3, 4] the absence of Tvout data on the toxic properties of drugs and therefore it is difficult to judge the prospects of their further use.

In the article the Iranian authors [5] provides data to obtain nanoparticle preparations (209÷260 nm) on the basis of PLGA with rifampicin and the study of their physico-chemical properties. Brief description of the data for the study of in vitro antibacterial activity in cell cultures. The in vivo experiments, not shown.

In [6] described experiments for obtaining particulate matter (less than 3 µm) on the basis of PLGA and antituberculosis drugs (isoniazid, rifampicin and pyrazinamide) by the method of double emulsification. The studied LV distribution in various organs of experimental animals after administration of these drugs over time. It is shown that the concentration of rifampicin and its activity was decreased after 9 days after injection. Information about the long-term effects of the drugs is not given. Similar information is presented in the work of Barrow E.L.W. and others [7], which describes a method of obtaining microspheres (7,5÷15 μm) of polymers of PLGA different composition adsorbed rifampicin. Data on the presence of activity on Mycobacterium tuberculosis for 6 days [7].

Thus, the aggregate of all existing signs created medicines: the presence of prolonging effect, the presence of high specific activity in vivo in animal experiments, infected with drug-resistant forms of TB, even after 3 weeks, yienna toxicity, achieved a new technical result.

The invention is illustrated by the following examples.

Example 1. Obtaining polymeric nanoparticles incorporating rifampicin method simple emulsions

A mixture consisting of a solution of 5÷60% polymer (PLA, PLGA or PLGA-COOH) and 1÷10% of rifampicin in an organic solvent (chloroform, methylene chloride), and 0.5÷2% aqueous solution of polymeric stabilizer emulsion in a volume ratio to the organic solvent of 5:1 homogenized at about 24 thousand./min on the homogenizer Ultra-Turrax T-25 (IKA®(Germany) 3 times for 1 min with intervals for 1 min Emulsion is stirred for 1 h at 40°C (if used chloroform) or 1.5 h at room temperature (if using methylene chloride) to complete removal of the organic solvent. This operation should be done when working exhaust ventilation. The resulting suspension is filtered through a coarse glass filter (pore. 40÷110 μm), added to the filtrate 1÷3% (vol.) cryoprotectant (D-mannitol), frozen and lyophilizers. The average particle size, determined by the method of autocorrelation spectroscopy on submicron laser spectrometer Coulter N4MD (USA), ranges from 250 to 500 nm, which facilitates the efficient absorption in the gastrointestinal tract [8]. The size of the particles depends on the type of polymer is, stabilizer emulsion, their concentration, and homogenization. The degree of inclusion of rifampicin in the polymer particles is from 15 to 75%.

Composition 1 (example 1)wt.%
Polyvinyl alcohol : 15,2
Particle size378±84 nm
Part 2 (of example 1)wt.%
PLGA 50: 5058,3
Polyvinyl alcohol : 16,6
Particle size281±73 nm
Part 3 (example 1)wt.%
PLGA 50:5058,5
D-Mannitolthe 17.3
Particle size324±57 nm

The optimal dilution means in the water corresponds to the ratio of from 1:20 to 1:10 that may be used to adjust the dosing of the drug depending on the individual patient.

The medicinal product is obtained according to claim 1, may be made in the form of tablets, capsules, granules, powder or other oral forms on the basis of known technologies [9, 10].

Example 2. Comparative pharmacological efficacy of the original drug prolonged action on the basis of rifampicin

Impact studies developed medicines on the basis of rifampicin on the survival and inoculation .tuberculosis in the lungs was conducted on a model of acute tuberculosis by injecting a lethal dose (.tuberculosis strain H37Rv at a dose of 5·106/mouse). Introduction drug prolonged action on the basis of rifampicin (PH), obtained in example 1, was started one day after playing TB. The drug was administered for 3 days. As a comparison, the por is performed experiments under similar conditions, where instead of a new drug rifampicin used or saline () or substance rifampicin (R). After completion of the experiment, animals were subjected to euthanasia by action geksenala, were removed and homogenized lungs were sowing to determine the number of viable .Tuberculosis. The data obtained are presented in table 1 and in the drawing.

Table 1
Comparative pharmacological efficacy of a drug action prolonged action on the basis of rifampicin
MedicationStated valueDoseInoculation .tuberculosis in the lungs, the number of bacilli, CFU*/mouse
7 days14 days21 days
Control (physiologic solution)To1.0 ml(3,7±1,22)×105(1,6±0,06)×107(2,6±0,68)×109
Rifampicin substance P20 mg/mouse(7,3±0,06)×103(1,7±0,17)×105(4,6±0,56)×107
Medicinal product on the basis of rifampicinPH20 mg/mouse(1,2±0,2)×103(7,9±0,9)×103(2,03±0,08)×105
Rifampicin substanceP10 mg/mouse(2,3±0,08)×104(1,3±0,16)×106(1,8±0,65)×109
Medicinal product on the basis of rifampicinPH10 mg/mouse(6,3±0,07)×103(5,3±0,16)×104(1,06±0,06)×106
Note. the controls were injected with saline in a volume, equal to the volume of the injected drug; *CFU - colony forming unit.

From table 1 and the drawing data shows that obtained in example 1 preparation on the basis of rifampicin with prolonging effect, also has superior activity of the parent substance - rifampicin. This is particularly evident through the 14th and 21st day after the start of the experiment, and when the drug concentration of 10 mg/mouse, when rifampicin (substance) almost ceases to act on the 21st day. This may allow to reduce therapeutic dose of rifampicin and thereby reduce the level of toxic side effects. Treatment of acute experimental tuberculosis in mice given the drug by the developed scheme allows to reduce the content of mycobacteria in the lung tissue is more than 100 times in comparison with the free rifampicin, reduce dosing frequency to 3 introductions by prolongirovannomu actions developed drug.

Example 3. Toxicological characteristics of the original drug prolonged action on the basis of rifampicin

A comparative study of the acute toxicity of the substance of rifampicin and developed polymeric drug based on it (the composition of example 1) were performed on mice male Balb weight 19÷21 GK the moment of testing. Mice were kept in standard cages No. 4, under conditions of unlimited access to water and food when natural changes in illumination. To test the toxic effect of the drugs was launched after a two-week quarantine of animals. The drugs were injected in a saline solution to warm-blooded animals orally into the stomach using an atraumatic tip. Monitor the effects of drugs had been produced for 14 days from the moment of introduction. As a control, were injected corresponding to the mass of the polymer compositions obtained without active substance, in equiano number of physiological solution.

Determination of the value of median lethal dose LD50(when n=7 for each of the tested doses, calculations were made according to the method of Litchfield and Wilcoxon signed [11]) showed that the value LD50for developed based drug rifampicin prolonged action of example 1 was 700 mg/kg, and for substance rifampicin 500 mg/kg Therefore, the average toxic dose for a new drug form of rifampicin was significantly higher (40%), and toxicity, respectively, lower than the original rifampicin.

Thus, the obtained nanoparticles means on the basis of rifampicin with prolonged action, exhibits high specific Akti the activity against Mycobacterium Tuberculosis with reduced toxicity compared to the original drug substance. This result allows us to conclude about the growth of therapeutic latitude and increasing therapeutic index when the reduction ratio of taking the drug due to prolongirovannomu his actions.

Developed a drug proposed for release in the form of enteric-soluble tablets or capsules.

Sources of information

1. Radar - encyclopedia of medicine / CH. edit Ufraw, 8th ed. M: "radar-2001", 2000. S-767.

2. Fang D., Singh M, O Hagan D., Hora M. Composition of microparticles and methods for their production // Patent RF №2257198 C2. - Publ. 27.07.2004,

3 Pandey R., Khuller G.. Oral nanoparticle-based antituberculosis drug delivery to the brain in an experimental model // Journal of Antimicrobial Chemotherapy 2006, V.57 (6). P.1146-1152.

4. Pandey, R., Sharma, A., Zahoor A. et al. Poly (DL-lactide-co-glycolide) nanoparticle-based inhalable sustained drug delivery system for experimental tuberculosis // Journal of Antimicrobial Chemotherapy 2003. V.52 (6). P.981-986.

5. Esmarili F., be started-Nasr M, Rad-Malekshahi M. et al. Preparation and antibacterial activity evaluation of rifampicin-loaded poly lactide-co-glycolide nanoparticles // Nanomedicine: Nanotechnology, Biology and Medicine 2007, V.3 (2).P. 161-167.

6. Ul-Ain Q., Sharma s, Khuller G.K. Chemotherapeutic Potential of Orally Administered Poly(Lactide-Co-Glycolide) Microparticles Containing Isoniazid, Rifampin and Pyrazinamide against Experimental Tuberculosis // Antimicrobial Agents and Chemotherapy 2003. V.47 (9). P.3005-3007.

7. Barrow E.L.W., Winchester G.A., Staas J.K. et al. Use of microsphere was Technology for Targeted Delivery of Rifampin to Mycobacterium tuberculosis-Infected Macrophages // Antimicrobial Agents and Chemotherapy 1998. V.42 (10). P.2682-2689.

8. Vranckx A., Demote M, Delaer M Headlight is aseptically composition, containing nanocapsules, and method thereof // Patent RF № 2145498 C1. - Publ. 20.02.2000,

9. Pharmaceutical technology: the technology of medicinal forms: Textbook for high schools / Under the editorship Cry and Gvieaway. Ed. 3-E. Rev. and ext. M.: Publishing house "Academy", 592 S.

10. Microencapsulation: Methods and Industrial Applications / Ed. S. Benita. 2nd ed. Taylor & Francis Group. 2006. 747 p.

11. Belenky, M. elements of a quantitative evaluation of the pharmacological effect / 2nd ed. revised and enlarged additional HP: Medgiz, 1963. S-106.

1. The drug prolonged action for the treatment of drug-resistant tuberculosis on the basis of rifampicin, characterized in that it is a stable nanoparticles and contains rifampicin, a biodegradable polylactic acid or a copolymer of lactic and glycolic acids, and surfactant, cryoprotector in the following ratio of components, wt.%:

a biodegradable polylactic acid
or a copolymer of lactic and glycolic acids20-60
surfactant and cryoprotectorrest

2. Les is arctonoe tool according to claim 1, characterized in that the biodegradable polymer contains a polymer of lactic acid or a copolymer of lactic acid and glycolic acid or a copolymer of lactic and glycolic acid with a free carboxyl group.

3. The drug according to claim 1, characterized in that as a cryoprotectant contains D-mannitol or lactose, or glucose.

4. The drug according to claim 1, characterized in that as the surfactant contains polyvinyl alcohol or Polysorbate 80, or poloxamer 188, or serum albumin.

5. The drug according to claim 1, characterized in that represents the nanoparticles ranging in size from 250 to 500 nm.

6. The drug according to claim 1, characterized in that it is made in the form of tablets or capsules, or granules, or powder, or other oral forms.


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