Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1992-03-03
1994-04-26
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424489, 424490, 424493, 424494, 514777, 514778, 514779, 514781, 514782, 514784, A61K 946
Patent
active
053065069
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a pharmaceutical formulation suitable for the administration of drugs and in particular of microcapsules of drugs in a monodose sachet form, the contents of which are poured into water at the moment of use. A process for preparing the formulation is also included.
In the description and the claims which follow we will use mostly the terms microcapsules or microencapsulated drugs, but the present invention can also be applied to solid drug particles (powders, crystals, granules) which are insoluble or slightly soluble in water or drinkable aqueous liquids (milk, fruit juices, etc.) and of which one desires to obtain an extemporary and homogeneous suspension.
In the following description and claims the term: granules, pellets and also liquid drops, coated in a polymeric membrane a membrane drug plus the excipients of the formulation water and which increase in density and viscosity allowing solid particles to be suspended.
Microencapsulation is a process known from some time and consists of coating substances with a continuous film based on natural or synthetic polymers.
The processes of microencapsulation are numerous. Many of these and the relative patents are cited and described in the volumes "Microcapsules and Microencapsulation Techniques" (published in 1976) and "Microcapsules and other Capsules. Advance since 1975" (published in 1979) both by M. H. Guttcho. Among the preferred processes are those described in the U.S. Pat. Nos. 3,196,827 and 3,253,944 by D. E. Wurster which describe methods of mechanical coating consisting of spraying a membrane around particles using suitable apparatus, and those cited in U.S. Pat. Nos. 3,415,758, 3,155,590 and 3,341,416 which described methods of chemicophysical coating based on the coacervation or separation of phases, in which the polymer making up the membrane is dissolved in a suitable solvent or vehicle of microencapsulation and the substance to be dissolved is suspended in this solution and kept in agitation.
The coacervation of the polymer around the substance to be coated is obtained in various manners, such as for example temperature variation, addition of another more soluble polymer in the vehicle, addition of a non solvent of the polymer constituting the membrane, etc. The membrance can be hardened and so the microcapsules are separated from the vehicle for example by filtration or centrifuging and finally drying.
In the pharmaceutical field, microencapsulation is used to mask unpleasant tastes, for slowing down the release of the drug, for preventing irritation arising from contact of the drugs with the gastrointestinal mucosa, for protecting drugs from degradation, for separating drugs which react with each other, for transforming the drug into a more easily used form, such as for example, converting it from a liquid state into a powder composed of microcapsules.
A common form of dosage for the oral administration of drugs, and especially of microencapsulated drugs, is that of monodose sachets. This moreover is the most convenient solution, if not the only one, if one must administer high doses of drugs. Monodose sachets containing microcapsules have been prepared in the past, sometimes also on an industrial scale, as cited in the volume "Microencapsulation" by J. R. Nixon, Chapter 7, page 93.
However they often present various disadvantages due especially to the hydrorepulsion of polymers making up the microcapsule membrane (for example polymers with a base of cellulose or waxy substances) and to the specific weight of the microencapsulated substances and therefore of the said microcapsules.
In fact when the contents of the sachets were poured out, as usual, in a glass of water or in fruit juice or in milk, the microcapsules formed a sediment on the bottom of the glass or floated on the surface, adhering partly to the walls of the said glass. This brought a notable inaccuracy to the quantity of the drug taken as well as poor acceptance by the patient who saw the particles floating or felt an unpleasant scraping sensat
REFERENCES:
patent: 4806358 (1989-02-01), Khan et al.
patent: 4888177 (1989-12-01), Gergely et al.
Mapelli Luigi G.
Marconi Marco G.
Zema Marco
Eurand International S.p.A.
Mandel Adley F.
Page Thurman K.
Spear James M.
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