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Publication of SI8710407BpublicationCriticalpatent/SI8710407B/en
13 Patentni zahtevki 1. Postopek za pripravo trdnega pripravka s podaljšanim sproščanjem aktivne spojine, ki ima topnost manj kot 0,1 mas.% v vodi, označen s tem, da aktivno spojino raztopimo ali dispergiramo v pol-trdnem ali tekočem ne-ionskem sredstvu za raztapljanje, izbranem izmed estrov in/ali etrov polietilenglikolov, v vsaj enaki masni količini glede na aktivno spojino, nakar zmes vključimo v sistem hidrofilnega gela, ki nadzoruje sproščanje in oblikujemo v farmacevtsko dozirno enoto.A process for the preparation of a sustained release solid preparation of an active compound having a solubility of less than 0.1% by weight in water, characterized in that the active compound is dissolved or dispersed in a semi-solid or liquid non-ionic agent. for dissolving selected from esters and / or ethers of polyethylene glycols in at least the same weight by weight according to the active compound, after which the mixture is incorporated into a hydrophilic gel system which controls the release and formed into a pharmaceutical dosage unit.2. Postopek po zahtevku 1, označen s tem, da ne-ionsko sredstvo za raztapljanje izberemo izmed polietoksiliranih maščobnih kislin, hidroksiliranih maščobnih kislin ali maščobnih alkoholov.Process according to Claim 1, characterized in that the non-ionic dissolving agent is selected from polyethoxylated fatty acids, hydroxylated fatty acids or fatty alcohols.3. Postopek po enem ali obeh zahtevkih 1 in 2, označen s tem, da ne-ionsko sredstvo za raztapljanje izberemo izmed polietoksiliranega ricinovega olja, polieto-ksiliranega hidrogeniranega ricinovega olja, polietoksilirane maščobne kisline iz ricinovega olja ali polietoksilirane maščobne kisline iz hidrogeniranega ricinovega olja.Process according to one or both of Claims 1 and 2, characterized in that the non-ionic dissolving agent is selected from polyethoxylated castor oil, polyethoxylated hydrogenated castor oil, polyethoxylated fatty acid from castor oil or polyethonexylated hydrogenated fatty acid. .4. Postopek po zahtevku 3, označen s tem, da so ne-ionska sredstva za raztapljanje estri maščobnih kislin hidrogeniranega ricinovega olja z oksietiliranim glicerinom, zlasti z zmesjo trihidroksistearatnega estra etoksiliranega glicerola in majhnih količin makrogol trihidroksistearata in ustreznih prostih glikolov.Process according to Claim 3, characterized in that the non-ionic solubilizing agents are fatty acid esters of hydrogenated castor oil with oxyethylated glycerol, in particular a mixture of ethoxylated glycerol trihydroxystearate ester and small amounts of macrogol trihydroxystestarate.5. Postopek po zahtevku 1, označen s tem, da so razmerja med aktivno spojino in sredstvom za raztapljanje v obsegu od 1:1 do 1:10, prednostno v obsegu od 1:2 do 1:6.Process according to Claim 1, characterized in that the ratios between the active compound and the dissolving agent are in the range from 1: 1 to 1:10, preferably in the range from 1: 2 to 1: 6.6. Postopek po enem ali več zahtevkih od 1 do 5, označen s tem, da je topnost spojine v vodi od 1:1000 ali manj, masno, in da se aktivna spojina raztaplja v ne-ionskem sredstvu za raztapljanje ali v kombinaciji vode in ne-ionskega sredstva za raztapljanje. 14Process according to one or more of Claims 1 to 5, characterized in that the water solubility of the compound is 1: 1000 or less, by weight, and that the active compound is dissolved in a non-ionic solvent or in combination with water, and non-ionic dissolving agent. 147. Postopek po enem ali več zahtevkih od 1 do 6, označen s tem, da aktivno snov izberemo izmed enega ali več substituiranih dihidropiridinov, zlasti nifedipina in/ali felodipina.Process according to one or more of Claims 1 to 6, characterized in that the active substance is selected from one or more substituted dihydropyridines, in particular nifedipine and / or felodipine.8. Postopek po kateremkoli izmed zahtevkov 1 do 7, označen s tem, da je sproščanje aktivne snovi nadzorovano s sistemom hidrofilnega gela, zlasti sistemom, v katerem znaša komponenta, ki tvori sistem hidrofilnega gela 20-80 mas.% pripravka.Process according to any one of Claims 1 to 7, characterized in that the release of the active substance is controlled by a hydrophilic gel system, in particular a system in which the component forming the hydrophilic gel system is 20-80% by weight of the preparation.9. Postopek po patentnem zahtevku 8, označen s tem, da je komponenta, ki tvori sistem hidrofilnega gela, hidroksipropil metilceluloza, zlasti sisteme, v katerih je hidroksipropil v razmerju od 4 do 12 mas. % samega pripravka.Process according to Claim 8, characterized in that the component forming the hydrophilic gel system is hydroxypropyl methylcellulose, in particular systems in which the hydroxypropyl is in a ratio of 4 to 12% by weight. % of the preparation itself.10. Postopek po zahtevku 8, označen s tem, da vsebuje sistem hidrofilnega gela kar-boksipolimetilen. Za AKTIEBOLAGET HASSLE:Process according to Claim 8, characterized in that the hydrophilic gel system contains carboxypolymethylene. For AKTIEBOLAGET HASSLE:LL
SI8710407A1986-04-111987-03-12Process for obtaining solid pharmaceutical preparation with extended release of active compound
SI8710407B
(en)
INTRODUCED BY THE ORAL WAY OF THE GALENOV FORM WITH FAST DELIVERY AND WITH A PROLONGED DIVISION, INCLUDING THE AMPLIFIED ABSORPTION AGENT, AND THE APPLICATION OF THIS STRENGTHENING ABSORPTION AGENT.