Adhesive preparation
AssigneeOno Pharmaceutical Co., Ltd.
InventorsAkio Nishiura, Hikaru Sugihara, Kazuya Abe
Life of this patent
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Abstract
An adhesive preparation which has a pressure-sensitive adhesive layer comprising two components, i.e., a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-osocyclopentyl)ethyl]sulfanyl}butanoic acid and a silicone-based pressure-sensitive adhesive. This is an effective and safe preparation which is stable, shows little change in skin permability and release a drug not rapidly but continuously.
Claims18
A sustained release adhesive preparation which is stable and has a low skin permeation rate ratio, comprising a sustained release adhesive layer containing two components, a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoic acid and a silicone adhesive.
A sustained release adhesive preparation which is stable and has a low skin permeation rate ratio, comprising a sustained release adhesive layer containing two components, methyl 4-{[2((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoate and a silicone adhesive and satisfying the following conditions (1) to (6):
- (1) a concentration of methyl 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoate is from 0.1% by mass to 2% by mass of the total of the adhesive layer;
- (2) a concentration of methyl 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoate is from 10 μg/cm2 to 200 μg/cm2;
- (3) an area of the adhesive preparation is from 1 cm2 to 25 cm2;
- (4) a thickness of the adhesive layer is from 20 μm to 120 μm;
- (5) a residual ratio of methyl 4-{[2((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoate after storage at 40° C. for 1 month is 90% or more;
- and
- (6) a skin permeation rate ratio for a stratum corneum-removed skin to that for a normal skin is from 1 to 5.
A method of stabilizing a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoic acid contained in a sustained release adhesive preparation, wherein a sustained release adhesive layer in the adhesive preparation contains two components, a C1-4 alcohol ester of 4-{[2-((1R,2R,3R)-3-hydroxy-2-{(1E,3S)-3-hydroxy-4-[3-(methoxymethyl)phenyl]but-1-enyl}-5-oxocyclopentyl)ethyl]sulfanyl}butanoic acid and a silicone adhesive.
Dependencies are inferred from the claim text.