Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2000-01-19
2002-11-26
Robinson, Allen J. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C424S464000, C426S425000, C426S429000, C426S431000, C426S472000, C426S478000, C426S655000, C514S822000, C514S925000, C514S960000
Reexamination Certificate
active
06486205
ABSTRACT:
This invention relates to a new mixture of primary fatty acids with straight chains of 26, 28, 29, 30, 31, 32, 33, 34, 35 and 36 carbon atoms. This mixture shows a relative composition of the fatty acids that is highly reproducible from batch to batch and it is extracted from sugar cane (Saccharum officinarum L.) wax, and can be used for the treatment of type II hypercholesterolemia, as antiplatelet agent, as anti-thrombotic, as anti-ischemic agent as well as protective and/or curative agent against gastric ulcers.
There are other mixtures of fatty acids that has reported biological properties, such is the case of the one reported in U.S. Pat. No. 5,284,873 in which is claimed a pharmaceutical composition for combatting prostate affections, in which the active principle is a fraction of fatty acids obtained from the fruits of Sabal Serrulata, with oleic acid as the main one, followed by lauric and palmitic acids, being the one with the greater number of carbon atom eicosenoic. In the U.S. Pat. No. 5,502,045 is claimed a method of reducing the cholesterol levels in serum using an ester formed by a-sitostanol and a 2 fatty acid from 2 to 22 carbon atoms. Also, claims a method of formation of such esters, being the effective daily dose of 0.2 to 20 g of the ester. Although, in the U.S. Pat. No. 5,444,054 is reported a method of treating ulcerative colitis in which one of the fractions used is an oil that contains certain fatty acids from 18 to 22 carbon atoms, but unsaturated. Not close to this patent application are the U.S. Pat. Nos. 4,505,933 and 4,687,783 in which are claimed mixtures of fatty aldehydes derived from fatty acids, for the treatment of patients with multiple sclerosis as well as neurological and dermatological diseases, the inventors claims a daily dose of 100-400 mg/kg of body weight of the patients.
In the last decade, numerous patent have appeared which report the omega-3-poly-unsaturated fatty acids have an effect on serum cholesterol and blood platelet aggregation, such is the case of U.S. Pat. No. 4,526,902 where it is claimed a pharmaceutical composition for the treatment of thrombo-embolic conditions in which the active principle are unsaturated eicosapentaenoic and docohexacnoic fatty acids together with linoleic acid, linolenic acid and its derivatives. Also, in the U.S. Pat. No. 5,502,077 is claimed a composition of fatty acids for the treatment or prophylaxis of multiple risk factors for cardiovascular diseases, where the 80% in weight corresponds with omega-3 fatty acids, its salts or derivatives thereof, being the main ones eicosapentaenoic and docohcxacnoic acids. In EPO patent 0 422 490 A2 it is claimed a pharmaceutical composition for inhibiting the absorption of cholesterol, containing triglycerides formed, preferably, by a mixture of saturated fatty acids from 20 to 24 carbon atoms, but they should be administered in a daily dose of 2 to 10 g. Also, in the Japanese patents 55092316 A and 56115736 A. of Tokiwa Shizeru et al, is reported the demonstration as well as the isolation and purification of an agent for diminishing cholesterol composed by a mixture of highly unsaturated fatty acids, especially eicosatrienoic and docosatertraenoicacids. In other Japanese patents (publication # 1290625 A, 02053724 A, 02243622 A and 04169524 A) claimed different pharmaceutical formulations, such as an improver of cerebral function or for the treatment of degenerative disease, or for lowering cholesterol in blood and for having Serum lipid-improving activity in which are presents as active principle, mixtures of fatty acids, especially eicosapentaenoic and docosahexacnoic acids, in a daily dose that varies from 500 mg/kg of body weight to 0.5-30 g.
As it has been shown, these patents claims mixture of fatty acid with specific biological properties, some of them closely related with the ones claimed in the present patent application. But, the composition of these mixtures significantly differs from the one claimed in these patent application and, also, the proposed daily dose to be used in these treatments in higher than the one claimed in the present patent application.
The present invention is related mainly with the pharmaceutical industry, particularly with the development of pharmaceutical formulations with specific properties, because them could be used as hypocholesterolaemic and hypolypoproteinaemic, anti-platelet anti-thrombotic, anti-ischemic drugs as well as in the prevention of gastric and duodenal ulcers induced by different agents.
These formulations contains, as active principle, a natural mixture of primary fatty acids of high molecular weight ranging from 24 to 38 carbon atoms, especially those ranging from 26 to 36 carbon atoms and more especially those of straight chain of 26, 28,29,30,31,32,33,34,35 and 36 carbon atoms, obtained from sugar cane wax (named MFASCW).
Drugs with specific pharmacological properties, based in the uses of primary fatty acids of high molecular weight (from 26 to 36 carbon atoms) obtained from, vegetable or animal waxes as active principles has not been reported previously, but it is known that primary fatty alcohols of high molecular weight obtained from sugar cave wax shows the same pharmacological properties. In EPO patent 0 488 928 A2 is claimed a mixture of fatty alcohols of high molecular weight for the treatment of hypercholesterolaemia and hyperlypoproteinaemia, type II that., also, in patent WO 94/07830 is claimed the use of the same mixture as antiplatelet agent, anti-ischemic, anti-thrombotic as well as in the prevention of gastric and duodenal ulcers induced by different agents.
The procedure for the obtention of this mixture of primary fatty acids of high molecular weight in the present invention is based in an homogeneous saponification of sugar cane wax with concentrated solutions of alkaline and earth-alkaline hydroxides, especially those of low molecular weight and more especially those of sodium, potassium and calcium. The concentration of the alkaline solution must be such that the ratio in weight of the corresponding hydroxide with that of the wax to be processed must be over 5% on, especially from 8 to 25% and more specifically from 15 to 25%. Saponification process lasts for a period over 30 min and more especially between 1 to 5 hours. The solid, obtained in this step, is processed using a conventional solid-liquid extractor, where the M.F.A.S.C.W., in salt form, is isolated from the rest of the components by extracting these components using the adequate organic solvent choose among ketones from 3 to 8 carbon atoms, alcohols from 1 to 5 carbon atoms, hydrocarbons from 5 to 8 carbon atoms, haloforms as well as aromatic compounds including mixtures of them. Some preferred solvents used in the present invention are the following: acetone, methyl-ethyl ketone, pentanone, hexanone, terbutanol, ethanol, methanol, 2-propanol, butanol, hexane, pentane, isopentane, ciclohexane, heptane, chloroform, 1,2 dichloroethane, dichloromethane, trichloroethane, trichloromethane, 1,2,3 trichloropropane, benzene, toluene, phenol, p-methyl toluene and others.
The mixture of primary fatty acids of high molecular weight in salt form is purified by succesive recristalizations in an adequate organic solvents or in aqueous solutions, choosen among ketones from 3 to 8 carbon atoms, alcohols from 1 to 5 carbon atoms, hydrocarbons from 5 to 8 carbon atoms, as well as aromatic compounds, including mixtures of them. Some preferred solvents used in this step of the process acetone, methyl-ethyl ketone, pentanone, hexanone, terbutanol, ethanol, methanol, 2-propanol, butanol, hexane, pentane, heptane, octane, ciclohexane, benzene, toluene, phenol, p-methyl toluene and water between others.
An step in the purification of this mixture of primary fatty acids of high molecular weight consist in refluxing the components in an adequate organic solvent, choose among ketones from 3 to 8 carbon atoms, alcohols from 1 to 5 carbon atoms, hydrocarbons from 5 to 8 carbon atoms as well as aromatic compounds including mixtures of them
Carbajal Quintana Daysi
Cora Medina Mirian
de Lourdes Arruzazabala Valmana Maria
Gonzáles Bravo Luis
Laguna Granja Abilo
Choi Frank
Laboratorios Dalmer SA
Lorusso & Loud
Robinson Allen J.
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