Process for preparing a ginger fraction and the use thereof for inhibiting human CYP enzymes
AssigneeBoehringer Ingelheim International GmbH
InventorsThomas Ebner, Eva Ludwig-Schwellinger, Stefan Blech
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Abstract
The present invention relates to a process for preparing a ginger fraction, the fraction prepared by this process and the use thereof on its own or combined with drugs for inhibiting human cytochrome P450 (CYP) enzymes (particularly cytochrome P450 3A4, CYP3A4) for positively influencing the oral bioavailability and pharmacokinetics of active substances.
Claims31
Process for isolating a ginger fraction while separating off the ethereal oil, comprising the steps of
- (a) extracting an oleoresin with a non-polar organic solvent;
- (b) extracting the combined residues from step (a) with warm water and discarding the supernatant.
A pharmaceutical composition effective to inhibit cytochrome P450 1A2, 2C9 and 2C19, wherein the pharmaceutical composition comprises one or more compounds having at least one of the general formulas:
- wherein
- n denotes the number 1, 2 or 3,
- R1 denotes one of H and CH3,
- R2 denotes one of H and CH3,
- R4 denotes one of H, O, OH, OCH3 and OC(O)CH3 and
- R5 denotes H, O, OH, OCH3 and OC(O)CH3, and
- the enantiomers or diastereomers thereof.
Pharmaceutical formulation comprising one or more compounds having at least one of the general formulas:
- wherein
- n denotes the number 1, 2 or 3,
- R1 denotes one of H and CH3,
- R2 denotes one of H and CH3,
- R4 denotes one of H, O, OH, OCH3 and OC(O)CH3, and
- R5 denotes H, O, OH, OCH3 and OC(O)CH3, and
- the enantiomers or diastereomers thereof;
- wherein the pharmaceutical formulation further comprises one or more inert carriers and/or diluents.
Pharmaceutical formulation comprising one or more compounds having at least one of the following formulas:
- the enantiomers and the diastereomers thereof;
- wherein the pharmaceutical formulation further comprises one or more inert carriers and/or diluents.
Dependencies are inferred from the claim text.