Tb rectal suppositories

 

(57) Abstract:

The invention relates to pharmaceutical industry. The invention consists in that the dosage form is a suppository, contains as active ingredients ethionamide 0,175 g, isoniazid 0,175 g, pyridoxine hydrochloride 0.03 g, as well as comprehensive fat basis - 2,62, the Invention allows to avoid the inactivation of the drug by enzymes of the gastrointestinal tract metabolism in the liver and unwanted effects on the body. The combination in the form of the drug isoniazid, high bacteriostatic activity, ethionamide, enhancing therapeutic effect of isoniazid and acting on refractory and atypical forms of Mycobacterium tuberculosis, can reduce therapeutic dose. table 1.

The invention relates to pharmacy and medicine, to the soft medicinal forms and can be used as a means of TB.

In Russia registered a solid dosage of anti-TB drug form of isoniazid, ftivazide, Metasite, ethionamide, protionamide, sodium paraaminosalicylic, pyrazinamide, ethambutol, thioacetazone (Reference Vidal. Lek is a, being highly efficient, can have various side effects: cardiotoxic, neurotoxic, hepatotoxic, and dyspeptic symptoms. For their prevention assign different protectors: pyridoxine hydrochloride, cyanocobalamin, and others.

Modern chemotherapy of tuberculosis is in the use of new anti-TB drugs acting on drug-resistant Mycobacterium tuberculosis (MW) and with a wide range of effects on non-specific pathogenic flora. To this end, apply the combination of anti-TB drugs prescribed for different dosage forms and at different times, such as isoniazid with pyrazinamide, isoniazid with ethambutol and others. (Sokolova, B. Effective and gentle treatment regimens of patients with pulmonary tuberculosis. - A manual for TB doctors. - M.: Publishing house IMMA them. Sechenov, 1998, S. 3-17).

Currently abroad produce finished dosage forms containing isoniazid in combination with other anti-TB drug substances and protectors. Thus, the firm “fatal (Germany) produces film tablet “Saaremaa” containing isoniazide the drug). Film tablet “Isozid include isoniazid and pyridoxine hydrochloride.

In Russia synthesized domestic drug ethionamide, advantage of which is its effect on atypical and isoniazid-resistant strains of Mycobacterium (Mashkovsky M. D. Medicines. - M.: New wave, 2001, T. II, S. 309).

In Russia up to the present time are not made of composite dosage form containing isoniazid in combination with other antituberculosis drugs, including rectal dosage forms. Closest to the proposed rectal suppositories on essential features are the tablets of ethionamide, selected as a prototype.

Tablets ethionamide contain drug substance and excipients in the following ratio of 1 tablet:

Ethionamide 0,2500 g

Polyvinylpyrrolidone 0.0125 g

Dry starch with moisture content of 2% 0,0150 g

Calcium stearate 0.0025 g

However, tablets ethionamide have not pronounced TB action as a reserve drug II series.

The aim of the invention is to increase therapeutic effectiveness of PR is achieved through the development of rectal TB suppositories, medicated: isoniazid, ethionamide, pyridoxine hydrochloride and various foundations in the following ratio of components on a single suppository mass 3 g:

Isoniazid 0,175 g

Ethionamide 0,175 g

Pyridoxine hydrochloride 0,030 g

The basis 2,620 g

The main feature of the claimed composition is the use of the most effective anti-TB drug isoniazid drug II series ciprofloxacin, which enhances anti-TB effect of isoniazid, affects isoniazid-resistant forms of Mycobacterium, can reduce therapeutic dose. In addition, the suppositories are also included pyridoxine hydrochloride, which, as a protector, prevents possible side effects of drugs. The rectal route of administration of drugs avoids inactivation of drugs in the gastrointestinal tract, liver metabolism and unwanted effects on the body. In the prototype as an active ingredient applied only ethionamide.

We offer comprehensive fat basis consists of the following components: paraffin, fat konditerskii powder, odorless, bitter taste. Easily soluble in water, sparingly soluble in 95% alcohol, very little in chloroform, practically insoluble in ether.

Ethionamide (2-ethyl-4-thiocarbamoylation) - small yellow crystals or yellow crystalline powder with a slight odor. Practically insoluble in water, soluble in 30 hours 95% ethanol, soluble in methanol, slightly soluble in chloroform and ether.

Pyridoxine hydrochloride (2-methyl-3-hydroxy-4,5-di-(oxymethyl)-pyridine hydrochloride) is a white crystalline powder, odorless, bitter-sour taste. Easily soluble in water, it is difficult in 95% alcohol, practically insoluble in ether.

The combination in the form of the drug isoniazid (a drug with a high bacteriostatic activity) with the same number of ethionamide, which enhances therapeutic effect of isoniazid and acts on the outside - and intracellular located Mycobacterium tuberculosis (including refractory and atypical forms), can reduce therapeutic dose. The use of medicinal substances in the form of rectal dosage forms in combination with the protector pyridoxine hydrochloride avoids inactivation of the drug by enzymes of the gastro-Kish is itories.

Pre-prepared base. To do this, in the melter put the required amount of paraffin, serially add the emulsifier, and then the confectionery fat, then cocoa butter and thoroughly homogenized.

Part of the basis of pre-dispersed powdered medicinal substance. Then the softened concentrate is loaded into the reactor and mix thoroughly with the rest of the basics at a temperature of 40-50C.

The prepared mass is fed to the molding. In the molding process the mass is constantly stirred. The manufacture of suppositories perform on machines with the necessary technological modes.

Suppositories are yellow, torpedo-shaped form. The shelf life of suppositories for 2 years.

The study of specific tuberculostatic efficacy of medicinal substances was conducted in the Ural research Institute of Phthisiopulmonology, Ekaterinburg. For an objective assessment of the proposed activity suppositories were used to define tuberculostatic activity on solid nutrient medium by the method of G. N. Pershina. The results of biological tests in vitro on solid medium are presented in table.1.

The conducted research is itories the effectiveness of superior tablets ethionamide and show activity against laboratory strains of H37RV similarly, the composite tablets, but doses of medicinal substances in the suppositories are greatly reduced.

As follows from the obtained results, the proposed suppositories are effective anti-TB drug form and allow us to expand the range of drugs used to treat tuberculosis.

The advantage of the proposed composition while maintaining equivalent to prototype pharmacological action is

1. strengthening the primary pharmacological effects of anti-TB activities;

2. use as active components of the combination of two anti-TB drugs - isoniazid and ethionamide - while reducing their therapeutic dose and the prevention of possible side effects.

Anti-tuberculosis drug containing as an active ingredient ethionamide, characterized in that it is a suppositories, additionally containing as active ingredients isoniazid, pyridoxine hydrochloride and the basis of the following ratio of components on a single suppository, g:

Isoniazid 0,175

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