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| Composition for the treatment of cutaneous mycosis |
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Pharmaceutical compositions and preparations thereof
| Details |
Inventors: Snyckers, Friedrich O.; Fourie, Theunis G.;
Assignee: 501 Noristan Limited (ZA)
Primary Examiner: Waddell; Frederick E.
Assistant Examiner:
Attorney, Agent or Firm: Berman, Aisenberg & Platt
The invention provides oleanolic acid and/or a physiologically acceptable salt thereof for use in treating a patient prophylactically and/or therapeutically for ulcerogenic-type disorders of the stomach and/or intestines. The ulcerogenic disorders can be of the type chemically induced and/or stress-induced. The invention also provides a pharmaceutical composition comprising an active amount of oleanolic acid and/or a physiologically acceptable salt thereof in combination with an analgesic compound and/or an anti-inflammatory compound. The invention further provides for use of oleanolic acid in preventing and/or significantly reducing and/or therapeutically treating ulcerogenic-type disorders of the stomach and/or intestines. |
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DETAILED DESCRIPTION OF THE INVENTION The invention and its various aspects will now be described hereunder.
Examples 1 and 2 are not to be regarded as part of the invention but are intended rather for information and background.
EXAMPLE 1 Preparation of Oleanolic Acid Suitable plant material, for example grape husks (preferably dried and milled), is exhaustively extracted with such solvents in which oleanolic acid is soluble.
These include: aromatic solvents, such as benzene; esters, such as ethyl acetate; ketones, such as acetone; halogenated hydrocarbons, such as chloroform and dichloromethane; alcohols, such as methanol and ethanol; ethers, such as diethyl ether or dioxane; and mixtures thereof.
Preferably the extractions are performed with chloroform, dichloromethane, ethanol, or methanol, or mixtures thereof.
From these extracts, the oleanolic acid can be separated by any method known in the art.
Preferably the extracts are treated with sufficient aqueous base to effect conversion into a water soluble salt of oleanolic acid.
Preferably a diluted sodium hydroxide solution is used for this purpose.
The aqueous solution of this salt is now treated with a suitable water immiscible solvent (such as dichloromethane or diethyl ether) to remove the bulk of the non-acidic components from the aqueous phase.
The purified aqueous solution containing the salt of oleanolic acid is now acidified with a suitable acid (preferably hydrochloric or sulphuric acid), to reconvert the salt to oleanolic acid.
The crude oleanolic acid can now be recovered by filtration or sedimentation, but preferably by extraction with a solvent which is not water miscible but which is a good solvent for oleanolic acid (preferably dichloromethane or diethyl ether), and subsequent evaporation of that extract.
Purification of the crude oleanolic acid can be achieved by recrystallisation or chromatography.
EXAMPLE 2 Preparation of Sodium Oleanolate A 10% aqueous solution of sodium hydroxide is added to an almost saturated solution of oleanolic acid in a water immiscible solvent, for example dichloromethane or diethyl ether
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