Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-04-21
1998-08-18
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514629, A61K 3119, A61K 3116
Patent
active
057959161
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to an external preparation composition containing a water-soluble salt of diclofenac, and specifically to an external preparation composition which contains a water-soluble salt of diclofenac dissolved in a base and is useful as a medicinal preparation or the like having a stable composition and high absorption.
Background Art
Diclofenac sodium, which is a water-soluble salt of diclofenac, is one of medicines most widely used these days as non-steroidal anti-inflammatory analgesics and in clinics, is employed in the form of oral preparations or suppositories. Due to its strong drug efficacy, however, its use may be limited, for example, where there is a potential problem of a shock or gastrointestinal ulcer as a side effect by an abrupt rise in its blood concentration.
Numerous attempts have been made to date with a view to maintaining drug efficacies without side effects by percutaneously administering drugs. For example, Japanese Patent Application Laid-Open (Kokai) No. SHO 62-103015 discloses that incorporation of a fatty acid monoalkylolamide as a penetration enhancer in a drug-containing composition permits efficient absorption of the drug through a skin or mucosa.
The above patent application discloses diclofenac sodium as an illustrative drug, but contains only one working example directed to a diclofenac sodium composition which is an oil-base suppository. In this suppository composition, diclofenac sodium is evenly dispersed but is not completely dissolved.
On the other hand, Japanese Patent Application Laid-Open (Kokai) No. SHO 63-91318 discloses a diclofenac-sodium-containing plaster in which a crosslinked water-containing gel with diclofenac sodium and 1,3-butylene glycol dissolved therein is spread on a backing. Further, Japanese Patent Application Laid-Open (Kokai) No. HEI 3-291222 discloses a diclofenac-sodium-containing topical medicinal composition in the form of a clear gel, which does not contain any emulsified fat layer.
It is however still difficult to assure solubility and stability of the water-soluble salt of diclofenac in a preparation even by these techniques. It is the current situation that no one has succeeded yet in developing a stable external preparation having excellent absorption.
Under the above-described circumstances, it has been desired to develop an external preparation composition of diclofenac, which contains a water-soluble salt of diclofenac dissolved in a base, is stable without precipitation of diclofenac or its salt, and has high skin permeability of the active ingredient.
Disclosure of the Invention
With the foregoing circumstances in view, the present inventors have proceeded with an extensive investigation to develop an external preparation composition which maintains the solubility of a water-soluble salt of diclofenac in the preparation and is excellent in stability and skin permeability of the active ingredient. As a result, it has been found that dissolution of a water-soluble salt of diclofenac in an aqueous solution of a fatty acid dialkylolamide or its polyoxyethylene adduct can provide a stable preparation and can achieve the above-described object.
It has also been found that addition of a pharmaceutically-acceptable additive to an aqueous solution of the above preparation can further increase the solubility of the water-soluble salt of diclofenac in the preparation and the skin permeability of diclofenac, leading to the completion of the present invention.
Namely, the present invention provides an external preparation composition comprising a water-soluble salt of diclofenac, water, and a fatty acid dialkylolamide and/or a polyoxyethylene adduct thereof.
Best Modes for Carrying Out the Invention
Examples of the water-soluble salt of diclofenac, which is an active ingredient in the external preparation composition according to the present invention, include the sodium, potassium, pyrrolidine, piperidine, N-hydroxyethylpyrrolidine, N-hydroxyethylpiperidine, triethanolamine, diethanolamine, ethylenediam
REFERENCES:
patent: 5176916 (1993-01-01), Yamanaka et al.
Nakagawa et al., JP 62-228027 (1987) (Abstract).
Ishikawa Kazuyuki
Ogura Eiji
Ota Shin'ichi
Sekine Takashi
Spivack Phyllis G.
Tsumura & Co.
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