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EP0255002A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

New pharmaceutical formulations with programmed release containing antiphlogistics

Assignee: Alfa Wasserman SpA
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Filing: 1987-07-17
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Granted: —
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Expires: 2007-07-17
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Abstract

Abstract New galenic formulations with programmed release, to be administered by oral route, containing as the active ingredient a compound endowed with antiphlogistic, analgesic and antipyretic activity like, for instance, an arylacetic or an arylpropionic acid and the pharmaceutical­ly acceptable salts thereof. In these new formulations, a portion of the active ingredient is released in a short time, so that the drug can quickly develop its therapeutic action reaching the necessary hematic levels, while the remaining portion of the active constituent is released in a longer interval of time so as to allow the therapeutic coverage till the subsequent administration. Said therapeutic coverage can even last 24 hours; thus the new galenic formulations object of the present invention are suitable for a once a day administration.

Inventors

  • 👤 Leone Gabriele Rotini
  • 👤 Egidio Marchi

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-07 19:11
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/185; A61K31/19; A61K9/00; A61K9/20; A61K9/2072; A61K9/2077; A61K9/48; A61K9/50; A61K9/5084; A61P; A61P25/00; A61P25/04; A61P29/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 85 words
Process for the production of a galenic formulation for oral use with programmed release containing as the ac­tive principle a compound endowed with antiinflammatory, analgesic and antipyretic activity, characterized by mixing a granulate having immediate release containing from about 30% to about 70% of the whole amount of the active principle in admixture with binding, disintegrating and lubricating agents, and a granulate having controlled release containing from about 30% to about 70% of the whole amount of the ac­tive principle in admixture with retarding agents.
Claim 2
Dependent Claim 85 words
Process for the production of a galenic formulation for oral use with programmed release containing as the ac­tive principle a compound endowed with antiinflammatory, analgesic and antipyretic activity, characterized by mixing a granulate having immediate release containing from about 30% to about 70% of the whole amount of the active principle in admixture with binding, disintegrating and lubricating agents, and a granulate having controlled release containing from about 30% to about 70% of the whole amount of the ac­tive principle in admixture with retarding agents.
Claim 3
Dependent Claim 36 words
Process according to claim 1, characterized in that the active principles having antiinflammatory, analgesic and antipyretic activity are arylacetic and arylpropionic acids both as free acids and as pharmaceutically acceptable salts with organic or inorganic bases.
Claim 4
Dependent Claim 29 words
Process according to claim 2, characterized in that the active principles having antiinflammatory, analgesic and antipyretic activity are selected from naproxen, ibuprofen, flurbiprofen, ketoprofen, fenoprofen, indomethacin, diclofe­nac and fentiazac.
Claim 5
Dependent Claim 23 words
Process according to claim 3 wherein the active prin­ciples having antiinflammatory, analgesic and antipyretic ac­tivity are selected from naproxen, ibuprofen, ketoprofen and diclofenac.
Claim 6
Dependent Claim 52 words
Process according to claim 1 wherein the binding agents are selected from polyvinylpyrrolidone, carboxymethyl­cellulose, microcrystalline cellulose, lactose, saccharose, mannitol, arabic gum, pectin and gelatin, the disintegrating agents are selected from starchs, alginates, sodium starch glycolate and reticulated polyvinylpyrrolidone, the lubricat­ing agents are selected from magnesium stearate, talc, stear­ic acid and silica gel.
Claim 7
Dependent Claim 73 words
Process according to claim 1 wherein in the granulate having controlled release the retarding agents are selected from ethylcellulose, methylcellulose, polyvinylacetate, met­acrylic acid esters, cellulose acetate, fatty alcohols con­taining from 10 to 22 carbon atoms, esters of fatty acids and alcohols having from 21 to 31 carbon atoms, paraffin, beeswax, unbleached wax, candelilla wax, carnauba wax, seal­ing wax, spermaceti, ozokerite, hydrogenated castor oil, hy­drogenated peanut oil, hydrogenated cotton seed oil and mixtures thereof.
Claim 8
Dependent Claim 20 words
Process according to claim 6 wherein the retarding agents are selected from methylcellulose, ethylcellulose, hydrogenated vegetable oils and mixtures thereof.
Claim 9
Dependent Claim 42 words
Process according to claim 1 wherein the granulate having immediate release contains from 60% to 70% of the ac­tive principle, from 20% to 30% of binding agents, from 8% to 12% of disintegrating agents and from 0.2% to 1% of lu­bricating agents.
Claim 10
Dependent Claim 36 words
Process according to claim 1 wherein the granulate having controlled release contains from 60% to 70% of the active principle and from 30% to 40% of a retarding agent or of a mixture of retarding agents.
Claim 11
Dependent Claim 15 words
Process according to claim 9 wherein the retarding agents are defined as in claim 7.

References Cited (Backward Citations)

FR1159165A Cited
BE658905A Cited

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