Patent EA-003863-B1 (EA)
Title: Pharmaceutical composition, the use of it and method of preparing
IPC: A61K31/047
Filed: 2001-08-20
Abstract: 1. Pharmaceutical composition for preparation of tablets of durable action, comprising microcapsules, containing non-sintered particles of water-soluble pharmaceutical agent, covered by bed from film-forming agent, and also a lubricating agent and a loosener, characterized in that it further comprises water, content of pharmaceutical agent and of film-forming agent in microcapsules makes correspondingly 96.0-99.2 w/% and 0.8-4 w/%, and said pharmaceutical agent is used as loosener at the following component ratio, w/%: microcapsules 96.0-99.8 lubricating 0.1-1 water 0.1-3 at adding of loosener in an amount of 0.1-10 w/% of resulting mixture. 2. Pharmaceutical composition according to claim 1, characterized in that the sizes of non-sintered particles of the pharmaceutical agent are 200-700 mkm. 3. Pharmaceutical composition according to claim 1 or 2, characterized in that the quantity of non-sintered particles wit size up to 200 mkm doesn't exceed 10 w/%. 4. Pharmaceutical composition according to claim 1 or 2, or 3, characterized in that a pharmaceutically acceptable swellable agent is used as film-forming agent. 5. Pharmaceutical composition according to claims 1 or 2, or 3, or 4, characterized in that amino acetic acid is used as pharmaceutical agent. 6. Pharmaceutical composition according to claims 1 or 2, or 3, or 4, characterized in that xylite is used as pharmaceutical agent. 7. Pharmaceutical composition according to claim 1 or 2, or 3, or 4, or 5, or 6, characterized in that the cellulose ester soluble in water and in mixture of water and organic solvent is used as film-forming agent. 8. Pharmaceutical composition according to claim 1 or 2, or 3, or 4, or 5, or 6, or 7, characterized in that stearic acid or a pharmaceutically acceptable salt thereof, or mixture of them, is used as lubricating agent. 9. Use of pharmaceutical composition according to claims 1-8 as a mixture for pressing the tablets, used sublingually. 10. Method of preparing of pharmaceutical composition for production of mixture for pressing the tablets of durable action, comprising preparing of microcapsules by applying the bed from film-forming agent on non-agglomerated particles of water-soluble drug, adding of lubricating agent and loosener, characterized in that at preparing of microcapsules and/or their intermediate storage, moisture content in bed is taken up to concentration of at less 0.5w/%, before adding of lubricating agent and loosener, the microcapsules are wetted by water up to 0.1-3 w/% until the swelling of bed, and after introducing of lubricating agent into a mixture, the loosener is added as a fine-dyspersated fraction of said drug. 11. Method according to claim 10, characterized in that non-agglomerated particles of drug with size of 200-700 mkm are used. 12. Method according to claim 10, or 11, characterized in that the quantity of used for covering with bed non-agglomerated particles of drug with size of 200 mkm don't exceed 10 w/%. 13. Method according to claim 10, or 11, or 12, characterized in that the applying of polymeric bed on non-agglomerated particles of drug is realized in apparatus with air-fluidized bed. 14. Method according to claim 10, or 11, or 12, or 13, characterized in that the film-forming agent is pharmaceutically acceptable swellable agent. 15. Method according to claim 10, or 11, or 12, or 13, or 14, characterized in that the film-forming agent is cellulose esters, soluble in water and in mixture of water and organic solvent. 16. Method according to claim 10, or 11, or 12, or 13, or 14, or 15, characterized in that the lubricating agent is stearic acid or pharmaceutically acceptable salt, of mixture thereof. 17. Method according to claim 10, or 11, or 12, or 13, or 14, or 15, or 16, characterized in that the amino acetic acid is used a drug. 18. Method according to claim 10, or 11, or 12, or 13, or 14, or 15, or 16, or 17, characterized in that xylite is used as a drug.