초록 ▼

The invention relates to novel pharmaceutical compositions for the systemic administration of pharmacologically active ingredients. The invention relates in particular to an injectable pharmaceutical composition comprising (a) a pharmacologically active ingredient in a solid phase, (b) a vehicle co

The invention relates to novel pharmaceutical compositions for the systemic administration of pharmacologically active ingredients. The invention relates in particular to an injectable pharmaceutical composition comprising (a) a pharmacologically active ingredient in a solid phase, (b) a vehicle consisting substantially of polyol fatty acid esters with a degree of esterification of over 80%, and (c) a wetting agent consisting substantially of polyol fatty acid esters with a monoester proportion of over 60%. The inventive composition is used for the systemic administration of numerous pharmacologically active ingredients, whereby the ingredients are released from the pharmaceutical composition over a period of at least 12, preferably at least 24 hours.

대표청구항 ▼

The invention claimed is: 1. An injectable pharmaceutical composition comprising: (a) at least one pharmacologically active agent in its solid phase; (b) a vehicle essentially consisting of polyol fatty acid esters with an esterification level of over 80%; and (c) a wetting agent comprising polyol

The invention claimed is: 1. An injectable pharmaceutical composition comprising: (a) at least one pharmacologically active agent in its solid phase; (b) a vehicle essentially consisting of polyol fatty acid esters with an esterification level of over 80%; and (c) a wetting agent comprising polyol fatty acid esters with a monoester content of over 60%, wherein the active agent is an antiparkinsonian agent which is released in the body from the injectable pharmaceutical composition in a therapeutically effective amount over a time period of at least 24 hours. 2. The injectable pharmaceutical composition of claim 1, wherein the vehicle is more than 70% (w/w) of the total composition. 3. The pharmaceutical composition of claim 1 or 2 wherein the pharmaceutical composition is anhydrous. 4. The pharmaceutical composition of claim 1 or 2 wherein the pharmacologically active agent is substantially insoluble in the pharmaceutical composition. 5. The pharmaceutical composition of claim 1 or 2 wherein the vehicle consists essentially of polyol fatty acid esters containing as the polyol component 1,3-propanediol, 1,3-butanediol or glycerol. 6. The pharmaceutical composition of claim 1 or 2 wherein the vehicle consists essentially of polyol fatty acid esters containing over 90% saturated fatty acids. 7. The pharmaceutical composition of claim 1 or 2 wherein the vehicle consists essentially of polyol fatty acid esters containing fatty acids with a chain length of 6 to 14 C-atoms. 8. The pharmaceutical composition of claim 1 or 2 wherein the vehicle consists essentially of medium-chain triglycerides. 9. The pharmaceutical composition of claim 1 or 2 wherein the wetting agent consists essentially of polyol fatty acid esters containing as the polyol component 1,3-propanediol, glycerol, 1,2,3-butanetriol, 1,2,4-butanetriol, 1,3-butanediol, sorbitan or isopropanol. 10. The pharmaceutical composition of claim 1 or 2 wherein the wetting agent consists essentially of polyol fatty acid esters containing over 90% saturated fatty acids. 11. The pharmaceutical composition of claim 1 or 2 wherein the wetting agent consists essentially of polyol fatty acid esters containing fatty acids with a chain length of 6 to 14 C-atoms. 12. The pharmaceutical composition of claim 1 or 2 wherein the wetting agent consists essentially of glycerol monolaurate or glycerol monocaprylate. 13. The pharmaceutical composition of claim 1 or 2 wherein the wetting agent is present at a concentration of 0.1-5% (w/w). 14. The pharmaceutical composition of claim 1 or 2 wherein the pharmaceutical composition is free of any phosphatides. 15. The pharmaceutical composition of claim 1 or 2 wherein the pharmacologically active agent is present in crystalline form. 16. The pharmaceutical composition of claim 1 or 2 wherein the pharmacologically active agent is present in an amorphous form. 17. The pharmaceutical composition of claim 1 or 2 wherein the pharmacologically active agent is present in salt form. 18. The pharmaceutical composition of claim 1 wherein the active agent is present at a concentration of from 0.01 to 20% (w/v). 19. The pharmaceutical composition of claim 1 wherein the active agent is present at a concentration of from 0.02 to 5% (w/v). 20. The pharmaceutical composition of claim 3 wherein the active agent is selected from the group consisting of N-0923 (rotigotine), levodopa, cabergoline, ropinirole, pergolide and pramipexole. 21. The pharmaceutical composition of claim 1 or 20 wherein the composition consists of (a) the at least one pharmacologically active agent in its solid phase; (b) the vehicle consisting essentially of polyol fatty acid esters with an esterification level of over 80%; and (c) the wetting agent comprising polyol fatty acid esters with a monoester content of over 60%. 22. The pharmaceutical composition of claim 1 or 20 wherein the composition does not contain a fatty acid aluminum salt. 23. A kit comprising: (a) a pharmaceutical composition of claim 1 or 2; and (b) an injection device. 24. The pharmaceutical composition of claim 2 wherein the active agent is present at a concentration of from 0.01 to 20% (w/v). 25. The pharmaceutical composition of claim 2 wherein the active agent is present at a concentration of from 0.02 to 5% (w/v). 26. The pharmaceutical composition of claim 2 wherein the active agent is selected from the group consisting of N-0923 (rotigotine), levodopa, cabergoline, ropinirole, pergolide and pramipexole. 27. The pharmaceutical composition of claim 2 wherein the composition consists of(a) the at least one pharmacologically active agent in its solid phase; (b) the vehicle consisting essentially of polyol fatty acid esters with an esterification level of over 80%; and (c) the wetting agent comprising polyol fatty acid esters with a monoester content of over 60%. 28. The pharmaceutical composition of claim 2 wherein the composition does not contain a fatty acid aluminum salt. 29. The pharmaceutical composition of claim 1 wherein the active agent is selected from the group consisting of N-0923 (rotigotine), levodopa, cabergoline, ropinirole, pergolide and pramipexole.