Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1993-09-10
1996-07-09
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424465, 424489, 5147723, 514778, 514781, 514784, 514960, 514961, A61K 916, A61K 920, A61K 31195
Patent
active
055342620
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This application is a 371 of PCT/RU92/00004, filed Jan. 10, 1992. The present invention relates to the technology of medicaments--to be more exact--to new granulated compositions well tabletted and containing water-soluble, non-pressed and/or difficulty pressed, crystalline pharmaceutical substances, and a method for producing same.
PRIOR ART
Known in the art are granulated compositions intended for tabletting and containing water-soluble, non-pressed and/or difficulty pressed, crystalline pharmaceutical components in which an amount of auxiliary substances reaches 40-90% by weight (EP 342106, EP I08218).
However, a high content of auxiliary ingredients in said compositions reduces bioaccessibility of pharmacological components and considerably changes their pharmacokinetics. Besides, introduction of large amounts of auxiliary substances into pharmaceutical compositions brings about significant power consumption and material expenditures.
Known is a method of producing granulated pharmaceutical compositions (Remington's pharmaceutical sciences, 17-th edition, 1985, Mack publishing company, Eastern Pennsylvania, pp. 16IO-1612).
According to said method, the pharmaceutical compositions are prepared by granulating a powder of pharmaceutical substance with a solution of binding agent in an air-fluidized bed apparatus, by drying the resultant granulate and by sequentially powdering same with a lubricating agent. However, this method does not permit obtaining the granulated compositions containing water-soluble, non-pressed and/or difficulty pressed crystalline pharmaceutical compositions with a minimum of the contained auxiliary substances.
ESSENCE OF THE INVENTION
The claimed granulated composition and method of its production are new and not described in literature.
it is the principal object of the present invention to create a new granulated composition, well tabletted and containing water-soluble, non-pressed and/or difficulty pressed, crystalline pharmaceutical components with a minimal content of auxiliary substances and to elaborate a method of its preparation.
Said object is solved owing to the fact that the claimed granulated composition of the invention comprises following components: by weight, as calculated for the total final composition; to 2.0% by weight; of from 0.5 to 1.0% by weight;
The claimed granulated composition comprises a minimum of auxiliary substances, which secures a maximal bioaccessibility of pharmacologically active components and the most favourable pharmacokinetics thereof. Besides this, the claimed granulated composition is well tabletted (pressed into tablets), the tablets possessing the required strength and the controlled time of dissolution, a factor that enables one to avoid the locally irritating effect of pharmacological active components.
The method of obtaining the claimed granulated composition of the invention includes following stages: or its concentrated solution in water. It is advantageous to use the powder of said pharmaceutical substance with a particle size of main fractions not exceeding about 0.3 mm. Said pre-granulation is preferably conducted in an air-fluidized bed apparatus; a pharmaceutical substance with a solution of binder in water or an organic solvent or a mixture thereof in an air-fluidized bed apparatus; moisture content of between 1 and 3% by weight;
The claimed method of obtaining a granulated composition contributes to improving its plasticity by changing the shape and structure of granules and to reducing the manufacturing cost of the tablets.
PREFERRED EMBODIMENT OF THE INVENTION
The pharmaceutical components (glycine, mannitol and histidine) a binding component--polyvinylpyrrolidone, organic solvents and water meet the quality requirements of the State pharmacopoeia of the USSE; binding components--starch, cellulose esters and also lubricating components, stearic acid and its salts meet the quality requirements of the technical-norm documentation of the USSR.
The powders of pharmaceutical components comprise above
REFERENCES:
patent: 3063900 (1962-11-01), Winsor
patent: 4036948 (1977-07-01), Kitamori et al.
patent: 4465660 (1984-08-01), David et al.
patent: 4486455 (1984-12-01), Wolf et al.
patent: 4702919 (1987-10-01), Kitamori et al.
patent: 4748023 (1988-05-01), Tamas et al.
patent: 4973470 (1990-11-01), Mills
Dobrotvorsky Anatoly E.
Khuchua Galina N.
Komissarova Irina A.
Rozputnyak Yaroslav A.
Page Thurman K.
Spear James M.
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