Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
2000-01-18
2001-02-20
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
C424S489000, C424S490000, C424S499000, C424S195110, C427S213310
Reexamination Certificate
active
06190687
ABSTRACT:
BACKGROUND OF THE INVENTION
The invention relates to a new method for preparing completely soluble microgranules prepared from extracts or solutions of active principles; these microgranules are intended to be used as they are for the reconstitution of solutions or to be incorporated into various galenic forms.
The administration and the use of extracts of active principles, especially of natural origin, in the form of Essential Oils, of solvent extraction solutions pose problems at various levels during use:
incomplete dissolution
difficulty of precise proportioning
masking of taste
inappropriate galenic presentation
The production, in dry form, of these different extracts of active principles involves, for the majority, methods using a substantial supply of heat; nebulization-spray-drying, evaporation under vacuum or otherwise, recovery from grinding or micronization, these various operations being capable of causing substantial adverse modifications. The dry forms of these various extracts which are thus obtained are subjected to adverse modifications of active principles which are linked to high hygroscopicity due to the increases in specific surface area induced by the physical treatments cited.
There has for example been proposed in the document EP-A-0,524,484 a powder for preparing instant drinks which is obtained by aqueous dissolution of tea extracts and of an inulin carrier, the mixture then being dried, and then spray-dried.
Even if a low-calorie composition is obtained by virtue of the degradation of the carrier into fructose units, its preparation requires a large volume of inulin for a given quantity of extract, which contributes towards increasing the cost of the formulation. In addition, the thermal energy released during the phase for spray-drying the powder once the active principle is attached to the inulin leads to the said active principle being thermally degraded, which excludes the use of heat-sensitive active principles. Moreover, the method used excludes the incorporation of any water-insoluble substance, in particular volatile substances, in particular flavourings and essential oils, which will be partially or completely evaporated during the spray-drying process.
SUMMARY OF THE INVENTION
The problem which the invention proposes to solve is therefore to develop a method for the manufacture of an extract of active principle of reduced cost by seeking to optimize the proportions of each of the constituents.
Another objective of the invention is to provide stability over time to the manufactured preparation by using a method free of thermal degradation which makes it possible to incorporate active principles or extracted substances which are heat-sensitive.
The aim of the invention is also to provide a method for the manufacture of an extract of active principle in which the choice of solvent is not limiting, which thus makes it possible to use any type of active principle independently of its physicochemical characteristics.
DESCRIPTION OF THE INVENTION
To solve all of these problems, the invention provides a method for the preparation of an extract of at least one active principle in the form of completely soluble dry granules, which consists:
first, in preparing an extract of an active principle in a solvent medium;
then, in depositing this extract on the internal and external walls of a microporous carrier insoluble in the solvent medium, provided in the form of microgranules, having a specific surface area of at least 0.50 m
2
/g;
and in drying the impregnated granular carrier obtained;
then, in coating the impregnated walls of the microporous carrier with a film-forming polymer; characterized in that the microporous carrier is a soluble dietary fibre based on a polymer selected from the group comprising inulin and oligofructoses and fructo-oligosaccharides, on their own or mixed.
In other words, the invention consists:
in a first instance, in preparing extracts of plant, animal or other origin, or solutions of active principles;
in a second instance, in impregnating the microgranules whose specific surface area of at least 0.50 m
2
/g provides optimum impregnation, these microgranules being insoluble in the extracts or solutions of active principles;
in a third instance, in evaporating the solvent by drying, the substances in the extract or the solution of active principles remaining absorbed in the microscopic structure of the microgranular carrier;
and finally, in coating the microgranule obtained with a film of polymers allowing it to offer stability over time inside the galenic form which will carry it during its administration, and also to be able to offer gradual release of the active principles retained, through the film of polymers.
In the description and in the claims, “extracts or solutions of active principles” should be understood to mean any form of solution containing active principles of plant, animal or other origin, such as solutions of synthetic active principles or active principles of inorganic origin (trace elements and the like), maceration liquids, essential oils, gums, resins. These extracts are prepared in a known manner, in particular in a solvent medium appropriate for the desired active principles, or by a specific physical method, that is to say respectively ethanol for the extract, or steam distillation (essential oils, volatile substances). Depending on the active principles, there is used as solvent a solvent which solubilizes the said active principles and which preserves the structure of the microgranular carrier, and which is not toxic. In practice, ethanol is used. It is possible to add adjuvants to the extract or to the solution of active principles with the aim of facilitating the dissolution or the dispersion of the active principles during the manufacture, or of providing mechanical protection of the final product.
In the description and in the claims, “dietary fibres” designate any compound from plant cells which is resistant to the various enzymatic hydrolyses used during the physiological process of digestion. These fibres are composed of cellulose, hemicellulose, oligosaccharides, pectin, gums, waxes and lignin; these various compounds are those taken into account in the analyses of dietary fibres.
In practice:
the active principle is an extract of plants or of a portion of plants;
the solvent medium consists of a solvent from the group comprising water, ethanol, acetone, dichloromethane;
the microporous carrier is a microgranule obtained by spray-drying or by wet granulation;
the spray-dried microgranule is based on soluble fibres which can be combined with other substances such as polyalcohols (sorbitol, xylitol, mannitol), polyols (maltodextrins and the like), or fatty substances;
the extract is deposited on the walls by wet granulation and the drying is carried out with hot air;
the film-forming polymer is a compound which is soluble in the gastrosoluble (hydroxypropylmethylcellulose) or gastro-resistant (hydroxypropylmethylcellulose phthalate) digestive system;
the film-forming polymer is pulverized in a turbine or in a fluidized bed.
Once this extract or solution of active principles has been prepared in a known manner, the microgranule is prepared by the technique of spray-drying or wet granulation which makes it possible to obtain a microgranular carrier having a porous structure which is quantified by its specific surface area: unit of surface area/unit of mass; generally, there are used as dietary fibres soluble fibres such as inulin and oligofructoses which are natural plant substances allowing the storage of carbohydrates in various plants which are used for human consumption, such as leek, onion, wheat, garlic, chicory, artichoke and the like.
According to a first embodiment of the invention, the microgranular carrier is a powder based on inulin obtained by extraction from chicory roots and from any other multi-rich plant.
Inulin is a mixture of oligomers and of polymers of fructose, whose structure is represented by the formula GFn, in which:
G: glucosyl unit
F: fructosyl unit
n: number of
Di Nola-Baron Liliana
Page Thurman K.
Vegetalys Corporation
Wall Marjama & Bilinski
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