Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1996-05-30
1998-06-16
Jarvis, William R. A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A61K 3119
Patent
active
057671613
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP94/04066 filed Dec. 7, 1994.
The present invention relates to a pharmaceutical composition for topical use and, more particularly, it relates to a pharmaceutical composition for topical use containing (S)-2-(4-isobutylphenyl)propionic acid.
The compound 2-(4-isobutylphenyl)propionic acid, which will be indicated herein after with its international nonproprietary name Ibuprofen, is a known nonsteroidal anti-inflammatory drug (Merck Index XI Ed., no. 4812, page 476) used in therapy for its analgesic, antipyretic and anti-inflammatory activity.
Very recently, it has been described in literature that Ibuprofen has also a strong antifungal activity (Sanyal et al., Letters in Applied Microbiology, 1993, 17, 109-111). Notwithstanding for years Ibuprofen has been used in therapy in racemic form, for some time it has been known that the active enantiomer is the one having (S) configuration, herein after referred to as (S)-Ibuprofen.
In literature, several topical pharmaceutical compositions containing Ibuprofen are known. As an example we can cite: the analgesic compositions in the form of an oil-in-water emulsion described in the European patent application no. 499399 (American Home Products Corporation) which contain high concentrations of Ibuprofen in solid crystalline form, the compositions described in the British patent application no. 2236250 (The Mentholatum Company Limited) based on solutions of Ibuprofen in benzyl alcohol, the hydroalcoholic gel with pH 3.5-6.0 described in the European patent application no. 439344 (McNeil-PPC Inc.), the gel described in the Japanese patent application no. 60/185712 (Kyushin Pharm. K. K.). Some of these compositions provide for the use of ethanol or propylene glycol or mixtures thereof as solvent systems but always in the presence of one or more further components which are essential for achieving an increase in the cutaneous permeation of Ibuprofen, such as for example triethanolamine above cited British patent application no. 2236250).
It is evident that the formulation of (S)-Ibuprofen in topical dosage forms can be therapeutically very useful for the treatment of diseases such as backache, reumatic and muscular pain, sprains, strains and neuralgia or for the treatment of localized mycoses.
However, the formulation of (S)-Ibuprofen in topical dosage forms shows remarkable problems due to the different characteristics of the enantiomer with respect to the racemic mixture.
The International patent application no. WO 92/20334 (The Boots Company PLC) describes pharmaceutical compositions for oral, rectal or topical administration containing (S)-Ibuprofen sodium salt as active ingredient. In the above patent application it is reported that, the pharmaceutical composition being the same, the substitution of (S)-Ibuprofen sodium salt with the free acid, that is with (S)-Ibuprofen, does not give acceptable results.
We have now surprisingly found that (S)-Ibuprofen can be formulated in a topical pharmaceutical composition containing ethanol and propylene glycol in a ratio from 0.6:1 to 4:1, so obtaining topical compositions which are suitable from a pharmaceutical point of view, and, in addition, allow to achieve an increased cutaneous permeation of the active ingredient with respect to those obtained by known topical pharmaceutical compositions containing an equivalent or higher amount of Ibuprofen.
Therefore, object of the present invention is a pharmaceutical composition for topical use containing 2.5-10% by weight of (S)-2-(4-isobutylphenyl)propionic acid in admixture with a suitable pharmaceutically acceptable carrier characterized by the presence of 20-30% by weight of ethanol and 5-50% by weight of propylene glycol so that the weight ratio ethanol:propylene glycol is between 0.6:1 and 4:1.
In the pharmaceutical composition object of the present invention the remaining up to 100% by weight is represented by excipients such as lipophilic substances, surfactants, gelling substances, solvents, structuring agents, preserving agents, colouri
REFERENCES:
patent: 3749773 (1973-07-01), Ninger
patent: 4282216 (1981-08-01), Rovee et al.
patent: 4954487 (1990-09-01), Cooper et al.
patent: 5093133 (1992-03-01), Wisniewski et al.
Bonadeo Daniele
Gazzaniga, deceased Annibale
Gazzaniga, legal representative Paola Maria
Riccardi Alberto
Stroppolo Federico
Jarvis William R. A.
Zambon Group S.p.A.
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