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Priority claimed from DK604286Aexternal-prioritypatent/DK604286D0/en
Priority claimed from DK370087Aexternal-prioritypatent/DK370087D0/en
Application filed by Novo Nordisk A/SfiledCriticalNovo Nordisk A/S
Priority claimed from YU228487Aexternal-prioritypatent/YU46978B/en
Publication of SI8712284ApublicationCriticalpatent/SI8712284A/en
Publication of SI8712284BpublicationCriticalpatent/SI8712284B/en
Medicines That Contain Protein Lipid Enzymes And Other Medicines
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Medicinal Preparation
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Claims (15)
1 Patentni zahtevki 1. Pripravek za intranazalno uporabo, označen s tem, da vsebuje farmacevtsko aktivno sredstvo in sistem, ki pospešuje absorbcijo, ki vsebuje vsaj en fosfolipid s splošno formulo I H-CH-OR’ (I) CH-OR" I H-CH-O-P(O) (OH)-OR"' v kateri sta R’ in R” enaka ali različna in vsak predstavlja vodik, alkil, alkenil, alkilkarbonil, alkenilkarbonil, alkadienilkarbonil, alkatrienilkarbonil ali alkatetraenilkarbonil, ki ne vsebuje več kot 14 ogljikovih atomov, pod pogojem, da niti R’ niti R” nista vodik in R”’ predstavlja hidrofilno skupino dobljeno iz skupine, ki obsega 2-(trimetilamonio)etil, 2-aminoetil, 2,3-dihidroksipropil.CLAIMS 1. A preparation for intranasal use, characterized in that it contains a pharmaceutically active agent and an accelerating absorption system comprising at least one phospholipid of the general formula I H-CH-OR '(I) CH-OR " And H-CH-O-P (O) (OH) -OR " in which R 'and R "are the same or different and each represents hydrogen, alkyl, alkenyl, alkylcarbonyl, alkenylcarbonyl, alkadienylcarbonyl, alkatrienylcarbonyl or alkatetraenylcarbonyl, containing no more than 14 carbon atoms, provided that neither R' nor R" hydrogen and R "'represents a hydrophilic group obtained from the group comprising 2- (trimethylammonio) ethyl, 2-aminoethyl, 2,3-dihydroxypropyl.2. Pripravek po zahtevku 1, označen s tem, da R’” predstavlja 2-(trimetilamonio)etil.A preparation according to claim 1, characterized in that R '' represents 2- (trimethylammonio) ethyl.3. Pripravek po zahtevku 2, označen s tem, da je tako R’ kot R” alkil ali alkilkarbonil, ki vsebuje od 4 do 12 ogljikovih atomov ali prednostno alkilkarbonil.A preparation according to claim 2, characterized in that both R 'and R "are alkyl or alkylcarbonyl containing from 4 to 12 carbon atoms or preferably alkylcarbonyl.4. Pripravek po zahtevku 3, označen s tem, da tako R’ kot R” predstavljata nonilkarbonil.A preparation according to claim 3, characterized in that both R 'and R "represent nonylcarbonyl.5. Pripravek po zahtevku 2, označen s tem, daje ali R’ ali R” vodik.A preparation according to claim 2, characterized in that either R 'or R "is hydrogen.6. Pripravek po zahtevku 1, označen s tem, da sistem za izboljšanje absorbcije vsebuje maščobno olje.A preparation according to claim 1, characterized in that the absorption improvement system comprises a fatty oil.7. Pripravek po zahtevku 6, označen s tem, da je maščobno olje - rastlinsko olje, prednostno dobljeno iz skupine, ki sestoji iz sojinega olja, arašidovega olja, kokosovega olja, koruznega olja, olivnega olja in sončničnega olja. 2A preparation according to claim 6, characterized in that the fatty oil - vegetable oil, preferably obtained from the group consisting of soybean oil, peanut oil, coconut oil, corn oil, olive oil and sunflower oil. 28. Pripravek po zahtevkih 1-5, označen s tem, da je vsebnost fosfolipidov s formulo I v obsegu od 0,5-5% (m/v) pripravka.A preparation according to claims 1-5, characterized in that the content of phospholipids of formula I is in the range of 0.5-5% (w / v) of the composition.9. Pripravek po zahtevkih 6-7, označen s tem, da je vsebnost maščobnega olja v obsegu od 0,01 do 50% (m/v), ali prednostno 0,1-10% (m/v) pripravka.A preparation according to claims 6-7, characterized in that the fat content is in the range of 0.01 to 50% (w / v), or preferably 0.1-10% (w / v) of the composition.10. Pripravek po zahtevkih 1-9, označen s tem, da je farmacevtsko aktivno sredstvo polipeptid.A preparation according to claims 1-9, characterized in that the pharmaceutical active agent is a polypeptide.11. Pripravek po zahtevku 10, označen s tem, da je polipeptid insulin ali insulinski derivat ali njuna zmes.A preparation according to claim 10, wherein the polypeptide is an insulin or an insulin derivative or a mixture thereof.12. Pripravek po zahtevku 11, označen s tem, daje vsebnost insulina v obsegu od 5 do 1000, prednostno od 50 do 500 mednarodnih enot na ml pripravka.A preparation according to claim 11, characterized in that the insulin content is in the range of 5 to 1000, preferably from 50 to 500 international units per ml of the preparation.13. Pripravek po zahtevku 10, označen s tem, da je polipeptid glukagon.A preparation according to claim 10, characterized in that the polypeptide is a glucagon.14. Postopek za pripravo pripravka po zahtevku 6, označen s tem, da metoda obsega dispergiranje vsaj ene zmesi fosfolipidov z maščobnim oljem, v tekočem ali trdnem razredčilu, skupaj s farmacevtsko aktivnim sredstvom v raztopljenem ali prahastem stanju, pri čemer razredčilo v danem primeru vsebuje pomožno sredstvo za pH-pufranje, zaščitno sredstvo in sredstva za nadzorovanje osmotskega tlaka.A process for the preparation of the preparation according to claim 6, characterized in that the method comprises dispersing at least one mixture of phospholipids with a fatty oil in liquid or solid diluent, together with a pharmaceutically active agent in a dissolved or inert state, wherein the diluent optionally contains an auxiliary agent for pH-buffering, a protective agent and means for monitoring osmotic pressure.15. Uporaba pripravka po zahtevku 6 v napravi za odmerjanje doze, ki je prilagojena za intranazalno dajanje. Za NOV$W^NM...·. |y«iuA^.ftč0P0VA uUse of the preparation according to claim 6 in a dosage unit adapted for intranasal administration. For NOV $ W ^ NM ... ·. | y «iuA ^ .ftč0P0VA u
SI8712284A1986-12-161987-12-16Preparations for nasal application and procedures for their production.
SI8712284B
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