Preparation of selective epoxide hydrolase II inhibitor

A cyclooxygenase and inhibitor technology, applied in the field of new pharmaceutical preparations, can solve problems such as the inability to provide cyclooxygenase 2 inhibitors

Inactive Publication Date: 2005-01-05
迪内希·尚蒂拉尔·帕特尔 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Therefore, because of the above-mentioned solubility and toxicity problems, the prior art cannot provide cyclooxygenase 2 inhibitors that can be administered directly by injection

Method used

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  • Preparation of selective epoxide hydrolase II inhibitor
  • Preparation of selective epoxide hydrolase II inhibitor
  • Preparation of selective epoxide hydrolase II inhibitor

Examples

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Effect test

example 1

[0049] While stirring, 3.976 mmol of rofecoxib was added to 100 ml of 2,5-bis-O-methyl-1,4:3,6 dianhydro-D-glucitol. The solution was stirred for an additional 15 minutes under aseptic conditions. The sterile-filtered solution is sealed in vials / ampoules.

example 2

[0051] While stirring, 3.976 mmol of rofecoxib was added to 80 ml of 2,5-bis-O-methyl-1,4:3,6 dianhydro-D-glucitol. Continue to stir the solution under aseptic conditions and add 20ml of water for injection. The solution (diluted to 100 ml with 2,5-bis-O-methyl-1,4:3,6 dianhydro-D-glucitol) was sterile filtered and sealed into vials / ampoules.

example 3

[0053] While stirring, 7.952 mmol of rofecoxib was added to 80 ml of 2,5-bis-O-methyl-1,4:3,6 dianhydro-D-glucitol. The solution was continuously stirred under aseptic conditions and 20ml of water for injection was added. The solution (diluted to 100 ml with 2,5-bis-O-methyl-1,4:3,6 dianhydro-D-glucitol) was sterile filtered and sealed into vials / ampoules.

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Abstract

A transparent stable injection preparation of a new selective epoxide hydrolase II(cyclooxygenase II) inhibitor, is used for the treatment of pain and the inflammation that causes by cyclooxygenase II, especially the preparation is prepared by dissolving the selective active cyclooxygenase II inhibitor such as cyclooxygenase II inhibitor selected from example choose from celebrex, vioxx and their homologous compounds, into solvent such as isobide ester isosorbide as shown by the chemical formula I, wherein, R[1] and R[2] are hydrogen atom or the alkyl or acetic acid ester of 1 - 3 carbons; also disclosed is a simple and cost-rational preparation method of tha said new medicine preparation.

Description

Technical field: [0001] The invention relates to a novel pharmaceutical preparation of a transparent and stable selective cyclooxygenase 2 (CYCLOOXY GE NASEII, abbreviated as COX2) inhibitor, which is suitable for injection to treat pain and inflammation symptoms caused by cyclooxygenase 2. Background technique: [0002] Selective cyclooxygenase 2 inhibitors such as Celecoxib, Rofecoxib and their homologues are widely used to treat musculoskeletal disorders such as rheumatoid arthritis, bone Osteoarthritis, ankylosing spondylitis, and acute pain. They are also used as the medicine of choice for dysmenorrhea. Long-term treatment with celecoxib and rofecoxib can effectively suppress inflammation without the gastric toxicity of conventional non-selective non-steroidal anti-inflammatory drugs (NSAIDs) (Simon et al., 1998, 1999; Bensen et al., 1999; Emery et al. 1999; Howaky et al. 2000; Schintzer et al. 1999; Ehlidrich et al. 1999; Laine et al. 1999 through Goodman & Gilman's ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/415A61K31/42A61K47/26
Inventor 迪内希尚蒂拉尔·帕特尔萨钦迪内希·帕特尔沙希坎特普拉布达斯·库拉尼
Owner 迪内希·尚蒂拉尔·帕特尔
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