Relationship between Amount of β-Blockers Permeating through the Stratum Corneum and Skin Irritation after Application of β-Blocker Adhesive Patches to Guinea Pig Skin

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タイトル別名
  • Relationship between Amount of .BETA.-Blockers Permeating through the Stratum Corneum and Skin Irritation after Application of .BETA.-Blocker Adhesive Patches to Guinea Pig Skin.
  • Relationship between Amount of ベータ Bloc

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We evaluated the relationship between the cumulative amounts of 5 kinds of β-blockers (alprenolol, oxprenolol, timolol, acebutolol and atenolol) permeating through the stratum corneum and a* values obtained by measuring the formation of erythema, a skin irritation reaction, with a chromameter after transdermal application of adhesive patches containing a β-blocker to the skin of guinea pigs.The cumulative amount of β-blocker released from each adhesive patch to the skin increased with the increase in application time. The contents of alprenolol, oxprenolol and timolol in the stratum corneum and in the stripped skin increased markedly up to 4h after application and thereafter were maintained at high levels up to 24h. The contents of acebutolol and atenolol, on the other hand, increased up to 24h, but these values were low. a* values of all adhesive patches 24h after application were higher than those before application.The correlation coefficients between the cumulative amounts of alprenolol, oxprenolol, timolol, acebutolol or atenolol permeating through the stratum corneum and (Δa*-Δa*Pleacbo) values were 0.739, 0.717, 0.722, 0.551 and 0.633, respectively. The correlation coefficient calculated by averaging the cumulative amounts of 6 kinds of β-blockers permeating through the stratum corneum [including propranolol which was reported previously (Kobayashi I., et al., Biol. Pharm. Bull., 19, 839-844 (1996))] was 0.731, higher than the correlation coefficient between contents of these β-blockers in the stripped skin and (Δa*-Δa*Placebo) values (r=0.552). This suggests that there was a high correlation between the cumulative amounts of β-blockers permeating through the stratum corneum and (Δa*-Δa*Placebo) values.

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