RU96117257A - GALENA FORM DERIVATIVES OF 5-NITROIMIDAZOLE - Google Patents

Claims (1)

1. The galenic form of 5-nitroimidazole derivatives, characterized in that it contains a combination of microgranules of 5-nitroimidazole derivatives, consisting, on the one hand, of gastroresistant microgranules and, on the other hand, of microgranules with a prolonged release of the drug.  2. The galenic form according to claim 1, characterized in that the weight ratio between gastroresistant microgranules and microgranules with prolonged release of the drug is from 6/4 to 1/9.  3. The galenic form according to claim 2, characterized in that the weight ratio between gastroresistant microgranules and microgranules with a slow release of the drug is from 25/75 to 15/85. 4. Herbal form in one of the paragraphs. 1-3, characterized in that the combined microgranules must meet the following dissolution characteristics, expressed in wt.% Dissolved microgranules of the total weight before dissolving:
- gastroresistant microgranules:
2 h in 0.1 n. HC1 - less than 15%
1 hour at pH 6.0 - more than 75%
microgranules with a prolonged release of the drug:
2 h in 0.1 n. HC1 - less than 15%
1 hour at 6.8≤RH≤7.5 - less than 50%
4 hours at 6.8≤pH≤7.5 - 40-90%
6 h at 6,8≤рН≤7,5 - more than 70%
5. Herbal form in one of the paragraphs. 1-4, characterized in that the gastroresistant microgranules consist of a neutral granular carrier coated with an active layer consisting of a mixture of 5-nitroimidazole derivative and a binding agent and a gastroresistant outer layer.  6. The galenic form according to claim 5, characterized in that the gastroresistant outer layer contains fillers that guarantee the resistance of the coating at pH values 4.5-5.5, which are preferably chosen from poly (meth) acrylic esters, hydroxypropylmethylcellulose, and mixtures thereof, and, optionally, talc and / or one or more plasticizers.  7. Herbal form in one of the paragraphs. 1-4, characterized in that the microgranules with a slow release of the drug consist of a neutral granular carrier coated with an active layer consisting of a mixture of 5-nitroimidazole derivative and a binding agent, and an outer layer of prolonged release.  8. The galenic form according to claim 7, characterized in that the outer layer of sustained release contains the usual fillers, which are used in the manufacture of slow-release microgranules, not dependent on the pH of the medium in which the microgranules act, and which are selected from poly (met ) acrylic esters, ethyl cellulose, and mixtures thereof, and, optionally, talc and / or one or more plasticizers.  9. The galenic form according to claim 8, characterized in that the gastroresistant outer layer contains at least one filler that depends on the pH of the medium through which the microgranules pass, in particular, pH-dependent poly (meth) acrylic esters, and Optionally, talc and / or one or more plasticizers.  10. Herbal form in one of the paragraphs. 5-9, characterized in that the neutral carrier consists of particles of starch or a mixture of starch and sucrose, which have an average diameter of 400 - 800 microns.  11. Herbal form in one of the paragraphs. 5-10, characterized in that the binding agent is a common agent known for the preparation of microgranules, which is preferably selected from polyvinylpyrrolidone of various molecular weights, hydroxypropylmethylcellulose of various molecular weights, hydroxypropylcellulose of various molecular weights, poly (meth) acrylic esters, and mixtures thereof.  12. Herbal form in one of the paragraphs. 1-11, characterized in that the gastroresistant microgranules and microgranules with a slow release of the drug have an average diameter of 0.4-1.5 mm, preferably 0.8-1.1 mm.  13. Herbal form in one of the paragraphs. 1-12, characterized in that the 5-nitroimidazole derivative is selected from metronidazole, secnidazole, tinidazole, and mixtures thereof.  14. Pharmaceutical composition, characterized in that it contains a herbal form according to any one of paragraphs. 1-13, in particular in the form of tablets, instant tablets or gelatin capsules.  15. Hydro-protected microgranules of 5-nitroimidazole derivatives, which are particularly suitable for the preparation of galenical form according to one of claims. 1-13.  16. Microgranules derived 5-nitroimidazole with a slow release, which are particularly suitable for the preparation of galenical form according to one of claims. 1-13.  17. Combined product containing microgranules of gastro-protected 5-nitroimidazole derivatives and microgranules with a prolonged release of 5-nitroimidazole derivatives, for use as a combination at the same time, separately or separated in time for the treatment of parasitic and infectious diseases of the gastrointestinal tract, in particular, amebiasis and infections associated with the presence of He1obacter p11ori.