Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-07-21
1999-07-27
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514912, A61K 31195
Patent
active
059291150
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an anti-inflammatory eye drop comprising diclofenac sodium (hereinafter referred to as DFNa) as an effective component, to which .gamma.-cyclodextrin (hereinafter referred to as .gamma.-CyD) which is a water-soluble cyclodextrin and a polyvinylpyrrolidone (hereinafter referred to as PVP) are added to impart storage stability over a long period of time to the eye drop and to alleviate ocular irritation thereof.
BACKGROUND ART
An aqueous eye drop comprising DFNa which is a non-steroidal anti-inflammatory agent has been used for protecting a patient from suffering from post-operative inflammatory conditions and complications during and after operations, when the patient is subjected to cataract surgery, because of the strong prostaglandin biosynthesis-inhibitory action of the anti-inflammatory agent. If the non-steroidal anti-inflammatory agents are used in eye drops, most of these anti-inflammatory agents have an irritating action to mucous membranes and eyes and an effect of causing a strong ocular pain.
The inventors of this invention have provided an anti-inflammatory eye drop which comprises at least one non-steroidal anti-inflammatory agents selected from the group consisting of ibuprofen, indometacin, ketoprofen, naproxen and flufenamic acid as a basis and a salt of calcium or magnesium with a physiologically acceptable acid as an ocular irritation-alleviating "J.P. KOKOKU) No. Hei 1-19362! in order to alleviate the ocular irritation and the ocular pain induced by the non-steroidal anti-inflammatory agent. In addition, the inventors have provided an anti-inflammatory eye drop which comprises DFNa and polyoxyethylene sorbitan monooleate or .alpha.- and .beta.-cyclodextrin, as an auxiliary agent for dissolution, in an amount ranging from 5 to 10 times (weight basis) the amount of DFNa (J.P. KOKOKU No. Hei 2-6329). Moreover, the inventors of this invention have developed an eye drop which comprises a chemically modified .beta.-cyclodextrin in combination with DFNa and which does not cause ocular irritation immediately after being dropped in the eyes and is Un-Examined Patent Publication (hereinafter referred to as "J.P. KOKAI") No. Hei 6-16547!.
Furthermore, there has been proposed a therapeutic agent comprising an aqueous solution which contains DFNa as an effective component, a buffering agent, an auxiliary agent for dissolution and a preservative and which further comprises 2-amino-2-hydroxymethyl-1,3-propanediol or a homologue thereof having up to 10 carbon atoms as a stabilizer for the effective component and the preservative (J.P. XOKAI No. Sho 62-242617). On the other hand, there have been proposed, as cyclodextrin-containing eye drops, an anti-inflammatory ophthalmic solution which comprises 2-(2-fluoro-4-biphenylyl)propionic acid or a salt thereof and .beta.-cyclodextrin (hereinafter referred to as ".beta.-CyD") or .gamma.-CyD (J.P. KOKOKU No. Hei 3-30571); an anti-inflammatory ophthalmic solution which comprises 2-(2-fluoro-4-biphenylyl)propionic acid or a salt thereof, .beta.-CyD or .gamma.-CyD and a calcium salt or a magnesium salt (J.P. KOKAI No. Sho 60-136516); or an aqueous ophthalmic solution which comprises 3,4-dihydro-2,8-diisopropyl-3-thioxo-2H-1,4-benzoxadine-4-acetic acid or a salt thereof as a basis and cyclodextrin (J.P. KOKAI No. Hei 5-213757).
The calcium or magnesium salt of a physiologically acceptable acid shows a satisfactory effect of alleviating the ocular irritation of the resulting eye drop, but the eye drop containing the same suffers from a problem such that it is insufficient in the long term storage stability. The .alpha.-cyclodextrin as disclosed in J.P. KOKOKU No. Hei 2-6329 does not have any effect of alleviating the ocular irritation due to DFNa, while .beta.-CyD shows a weak ocular irritation-alleviating effect, but the effect is insufficient. Thereafter the inventors of this invention have found out that the incorporation of a chemically modified water-soluble .beta.-CyD into such an eye drop containing DFNa in
REFERENCES:
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patent: 4960799 (1990-10-01), Nagy et al.
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Database WPI, Derwent Publications, AN 83-823242, JP 58-174309, Oct. 13, 1983.
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Maeda Makoto
Maruyama Hiroki
Oguma Touru
Suzuki Hiroe
Takeuchi Masanobu
Fay Zohreh
Wakamoto Pharmaceutical Co., Ltd.
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