Novel pharmaceutical composition

• US 20030180332A1
• Filed: 02/11/2003
• Published: 09/25/2003
• Est. Priority Date: 08/24/2000
• Status: Active Grant

• Current Assignee: UCB Pharma GmbH (UCB SA)
• Original Assignee: Schwarz Pharma Ag (Schwarz Pharma)
• Inventors: Rimpler, Stephan, Thelen, Markus, Krein, Cliff, Grapatin, Sabine
• Granted Patent: US 7,309,497 B2
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Abstract

The invention relates to novel pharmaceutical compositions for the systematic 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%, (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 systematic 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.

Claims

1. 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%

(c) a wetting agent essentially consisting of polyol fatty acid esters with a monoester content of over 60%.

2. Pharmaceutical composition as in claim 1, characterized in that the pharmaceutical composition is anhydrous.

3. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmacologically active agent is largely insoluble in the pharmaceutical composition.

4. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmacologically active agent is released from the pharmaceutical composition in a therapeutically effective amount over a time period of at least 24 hours.

5. Pharmaceutical composition as in one of the preceding claims, characterized in that the vehicle consists essentially of polyol fatty acid esters containing as the polyol component 1,3-propanediol, 1-3-butanediol or glycerol.

6. Pharmaceutical composition as in one of the preceding claims, characterized in that the vehicle consists essentially of polyol fatty acid esters containing over 90% saturated fatty acids.

7. Pharmaceutical composition as in one of the preceding claims, characterized in that the vehicle consists essentially of polyol fatty acid esters containing fatty acids with a chain length of 6 to 14 C-atoms.

8. Pharmaceutical composition as in one of the preceding claims, characterized in that the vehicle consists essentially of medium-chain triglycerides.

9. Pharmaceutical composition as in one of the preceding claims, characterized in that 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. Pharmaceutical composition as in one of the preceding claims, characterized in that the wetting agent consists essentially of polyol fatty acid esters containing over 90% saturated fatty acids.

11. Pharmaceutical composition as in one of the preceding claims, characterized in that the wetting agent consists essentially of polyol fatty acid esters containing fatty acid residua with a chain length of 6 to 14 C-atoms.

12. Pharmaceutical composition as in one of the preceding claims, characterized in that the wetting agent consists essentially of glycerol monolaurate or glycerol monocaprylate.

13. Pharmaceutical composition as in one of the preceding claims, characterized in that the wetting agent is present at a concentration of 0.1-5% (w/w).

14. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmaceutical composition is free of any phosphatides.

15. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmacologically active agent is present in crystalline form.

16. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmacologically active agent is present in an amorphous form.

17. Pharmaceutical composition as in one of the preceding claims, characterized in that the pharmacologically active agent is present in salt form.

18. Pharmaceutical composition as in claim 17 or 18, characterized in that the active agent is present at a concentration of 0.02-5% (w/v).

19. Pharmaceutical composition as in one of the preceding claims, characterized in that the active agent is an antiparkinsonian agent, an anti-epileptic or a substance for treating neuropathy.

20. Pharmaceutical composition as in one of the preceding claims, characterized in that the active agent is selected from among N-0923, levodopa and proinsulin C-peptide.

21. Kit, comprising

(a) a pharmaceutical composition per one of the preceding claims

(b) an injection device.