Bioactive concentrate, its producing method and certain drug com

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert

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Details

424433, 424443, 424DIG15, A61F 202, A61F 1302

Patent

active

059651512

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

This invention relates to a bioactive concentrate, a method of producing same and pharmaceutical compositions containing the bioactive concentrate for treatment of degenerative diseases, including rheumatism, arthropaties and other related diseases.


BACKGROUND OF THE INVENTION

A complex of anti-hyaluronidase substances has been derived from several natural products, such as small fish containing amino acids, whole glucides, glycogen chondroitinsulphate, phenol, hypotensive substances, with an antihyaluronidase activity of a minimum of 50 I.U/ml.
The method whereby the complex is produced consists of a two-phased treatment of se fish with 0.5% phenol solution, over a period of 24 h, the extracts brought together are vacuum concentrated at a maximum 40.degree. C., then they are treated with an equal ethanol 96.sup.c volume; the precipitate is removed and the supernatant obtained is treated with celite, filtered, vacuum-concentrated at a maximum 40.degree. C., then solvent-extracted--treated and after removing the solvent the supernatant is treated with phenol up to a value of 4.5-5.5%.
Drug compositions containing an anti-hyaluronidase bioactive extract, phenol and sodium metabisulphite, have been developed too.
These drugs rely on a complex of substances, natural active principles, associated in proportions close to the normal, functional ones, produced by extraction from animal tissues or biosynthesized in cells and microorganism cultures, the role of this complex being to replace, to substitute for or even to allow recovery of the naturally existing complex in connective tissues, that had been unbalanced for various reasons and which caused the disease.
The extraction and conditioning processes have been established so that losses and degradation of active substances should be as low as possible and when the ratio of raw material constituents is different from that one required to treat disease in human being, it may be set off by a proper compounding of extracts or by a treatment schedule.
Now, the disease-inducing mechanisms are known to result from a disequilibrium in the biosynthesis and breakdown of normal constituents on which the proper movement of joints depends.
Cells in the tissues of the living body are embedded and evolve within basic substances. This basic substance--a general compound of living structures-pervades every interspace and isolates every stationary cell from its neighbors. Variations in the composition of the extracellular environment exert a profound influence on cell behavior and in turn the cells possess a powerful means of modifying their immediate environment.
The intercellular substance is a complex gel containing water, electrolytes, metabolites, dissolved gases, enzymes, trace elements, fats, proteins, carbohydrates. This substance is rendered highly viscous by an abundance of certain long-chain acid mucopolysaccharide polymers, particularly glycosaminoglycans and the related proteoglycans, reinforced at the microscopic level by a three-dimensional network of collagen fibrils (Cameron, E. and Pauling, L--The Encyclopedia of Ignorance, p. 377-385, Pergamon Press, Oxford, 1982).
The role of synovial fluid, found in all joints, is not only to lubricate the moving structures but also to dissipate the energy.
This function is performed by the synovial fluid composition where the glycosaminoglycans (GAC) and proteoglycans (PG such as hyaluronic acid and chondroitinsulphate inducing a high viscosity with their spiral structure, behave viscous-like when the moving frequencies are low and elastic--like when the moving frequencies are high (Ogston, A. G. and Stanier, J. E. (1953)--J. Physiol, 199, 124).
Elasticity is due to the presence of the highly concentrated hyaluronic acid, at a pH=2.5 which forms a viscous-elastic paste in a salt solution (Balasz, E. A., Chemistry and Molecular Biology of the Intercellular Matrix, Vol. II and III, Academic Press, New York, 1970).
At different ages, the synovial fluid behaves similarly as it concerns viscosity, but

REFERENCES:
patent: 4411988 (1983-10-01), Toth et al.

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