Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex
Patent
1988-08-24
1991-03-26
Rollins, John W.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Conjugate or complex
514458, 514558, 514822, 514863, 514882, 514886, 514887, 514930, A61K 3578, A61K 31355, A61K 3120
Patent
active
050027670
DESCRIPTION:
BRIEF SUMMARY
The invention concerns the field of drugs, especially antiinflammatories.
It relates to a therapeutic composition which contains, as the active principle, at least .alpha.-linolenic acid and at least one compound capable of promoting the passage of the acid through the cell membrane, in association with a physiologically acceptable excipient.
It further relates to the plant extracts containing the active principle.
.alpha.-Linolenic acid by itself has no therapeutic activity.
According to the present invention, it has been found that the active principle described above has totally unexpected therapeutic properties, especially antiinflammatory properties. Alcohols of vegetable origin, such as tocopherols (.alpha., .beta., .gamma. and .delta.) or sitosterols like .beta.-sitosterol, may be mentioned among the compounds which are capable of promoting the passage of .alpha.-linolenic acid through the cell membrane. Apart from these two types of product, the active principle can contain other compounds, especially C.sub.16 and C.sub.18 fatty acids such as palmitic acid, stearic acid, oleic acid and linoleic acid. Moreover, the presence of these other compounds often results from the process for the preparation of the active principle, as will be understood below.
Thus, preferably, the active principle will have the following composition in percentages by weight:
______________________________________ linolenic acid 10-80 and preferably 15-60
compound 10-80 and preferably 15-60
C.sub.16 and C.sub.18 fatty acids
0-65 and preferably 15-55
other than .zeta.-linolenic acid
______________________________________
The active principle is preferably an aqueous or organic extract of plants which contain .alpha.-linolenic acid and a compound capable of promoting the passage of the acid through the cell membrane.
The expression "aqueous or organic extract" refers to the product which results from the action of an aqueous or organic solvent on ground plants, i.e. the process involves extracting the products which are soluble or miscible in these solvents.
Among the plants which are suitable for the present invention, preference will be given to those belonging to the Resedaceae family, such as Reseda lutea, Reseda luteola, Reseda glauca L., Reseda suffruticosa, Reseda alba, Reseda jacquini Rehb, Reseda odorata, Reseda complicata, Reseda bory, and Reseda phyteuma.
It is possible to use the whole plants harvested when flowering or fruiting, or seeds. They are then dried in the absence of light under a stream of air.
The aqueous extract advantageously results from extraction of ground plants or seeds with water, followed by recovery of the dry solute by an appropriate means.
Appropriate means which may be used are lyophilization or nebulization (after the addition, in the latter case, of an agent for imparting viscosity or an adsorbent, such as hydroxypropyl methyl cellulose (HPMC) or silicic acid).
It is also possible to extract the resulting aqueous solution with an organic solvent and then to concentrate the organic phase and finish, if appropriate, with a chromatographic fractionation of the concentrate. Advantageously, the fractionation will be such as to enable the fractions containing the fatty acids to be recovered. Preferably, the aqueous extract will result from a solid-liquid chromatographic fractionation, the eluent being a 50/50 benzene/methanol mixture, the support being silica and elution being carried out in 10 ml fractions, and from recovery of the fractions between forty-three and sixty.
The organic extract results from extraction of ground plant or seeds with an organic solvent such as ether, hexane or methanol, or with liquid CO.sub.2 in the supercritical phase, followed by recovery of the dry solute by evaporation. However, preferred solvents will be ether, hexane or petroleum ether and especially methyl tert-butyl ether, or liquid CO.sub.2 in the supercritical phase, either in the pure state or, if appropriate, with traces of water, ethanol or the like (to extract the compounds of greater or
REFERENCES:
Weissberger, Technique of Organic Chemistry, vol. III, Part I, Separation and Purification, pp. 302, 307, 817-823, 830-832, (1956).
Steinmetz, Codex Vegetabilis, 950-951, (1957).
Lust, The Herb Book, First Edition, p. 218, (1974).
"Unlisted Drugs", vol. 15, Jan. 1963, No. 1.
"Rote Liste", 1961, Verzeichnis pharmazeutischer Spezialpraparate.
Laboratories Natura Medica
Rollins John W.
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