Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1996-11-27
1999-02-09
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424451, 424456, 424463, 424465, 424494, A61K 920, A61K 928, A61K 948, A61K 956
Patent
active
058691022
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a solid pharmaceutical composition containing (S)-2-(4-isobutylphenyl)propionic acid as active ingredient and, more particularly, it relates to a solid pharmaceutical composition suitable for the preparation of pharmaceutical forms in tablets, sachets and capsules, containing (S)-2-(4-isobutylphenyl)-propionic acid as active ingredient.
2-(4-Isobutylphenyl)propionic acid, which will be referred herein after to as the International Nonproprietary Name Ibuprofen, is a known non-steroidal anti-inflammatory drug (The Merck Index-XI Ed., No. 4812, page 476) used in therapy for its analgesic, antipyretic and anti-inflammatory activity.
Notwithstanding Ibuprofen is used in therapy from years in racemic form, it is known from some time that its active enantiomer is the one having (S) configuration, hereinafter referred to as (S)-Ibuprofen.
To the best of our knowledge, the first solid formulation of (S)-Ibuprofen described in literature is reported in example 1 of the European patent application No. 267321 (Medice Chem.-Pharm. Fabrik Puetter GmbH & Co.).
This formulation in tablets contains (S)-Ibuprofen (300 mg), insoluble polyvinylpyrrolidone (20 mg) as disintegrating agent, microcrystalline cellulose (150 mg) as diluent and magnesium stearate (10 mg) as lubricant.
In the same European patent application it is reported that the formulation of (S)-Ibuprofen in tablets or in other formulations suitable for the oral administration is carried out in a conventional way by using known diluents and carriers (page 3, lines 48-50).
Contrary to what stated in European patent application No. 267321, the formulation of (S)-Ibuprofen in tablets, or in solid pharmaceutical forms in general, is a problem anything but conventional and difficult to solve by using common excipients and carriers.
In fact, as widely reported in literature, the formulation of (S)-Ibuprofen in solid pharmaceutical forms such as tablets, sachets and capsules shows considerable drawbacks mainly due to the low melting point of (S)-Ibuprofen (51.degree.-55.degree. C.) and to the formation of eutectic mixtures with usual excipients (see for example Romero A. J. et al., Drug Development and Industry Pharmacy, 17(5), 777-792 (1991) e Romero A. J. et al., J. Pharm. Belg., 1993, 48, 1, 27-32). In fact, these physical features of the active ingredient make difficult the mixture and the compression of the powders.
Some solid formulation containing (S)-Ibuprofen have been described in literature.
European patent No. 478838 and International patent application No. WO 93/23026, both in the name of Pharmatrans Sanaq AG, disclose (S)-Ibuprofen compositions with improved properties of compression due to the use of the active ingredient in the form of its calcium salt.
Analogously, International patent applications WO 92/20334 and WO 94/10994 (The Boots Company PLC) disclose pharmaceutical compositions containing (S)-Ibuprofen as salt, in particular as sodium salt.
Obviously the use of (S)-Ibuprofen in the form of a salt allows to increase the melting point and to avoid the formulation problems specifically bound to the low melting temperature of the active ingredient.
International patent application WO 93/04676 (The Boots Company PLC) discloses (S)-Ibuprofen formulations prepared by using agglomerates containing (S)-Ibuprofen (70-97% by weight) and starch (3-30% by weight).
European patent application No. 398287 (Medice Chem.-Pharm. Fabrik Puetter GmbH & Co.) discloses solid solutions of (S)-Ibuprofen in low melting polyethyleneglycols or polyethyleneoxides useful for filling hard gelatine capsules.
The use of low melting excipients allows the preparation of a melted mixture which is directly poured into the capsules where at room temperature it solidifies.
This kind of formulation cannot be used for the preparation of tablets or sachets.
International patent application WO 94/10993 (Nycomed Dak A/S) discloses pharmaceutical formulations containing (S)-Ibuprofen (40-70% by weight), a hydrosoluble ligand different from polyvinylpyrrol
REFERENCES:
patent: 4681897 (1987-07-01), Brand
patent: 4713248 (1987-12-01), Kjorn et al.
patent: 4812446 (1989-03-01), Brand
patent: 4831058 (1989-05-01), Pankhania et al.
patent: 4839176 (1989-06-01), Pankania
patent: 5164398 (1992-11-01), Sims et al.
Bonadeo Daniele
Gazzaniga, deceased Annibale
Gazzaniga, legal representative Paola Maria
Pagano Alberto
Stroppolo Federico
Page Thurman K.
Shelborne Kathryn E.
Zambon Group, S.P.A.
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