気管支喘息治療薬ツロブテロールの経皮吸収型製剤の開発

概要

論文の詳細を見る
β_2-Adrenergic agonists have been widely used to treat patients with asthma. Usually, oral dosage forms of β_2-agonists have been used, but side effects such as palpitation and tremor have been reported because of excessive serum levels around Tmax. It is said that circadian variations exist in the manifestation of asthma with maximum incidence of asthma attacks in early morning at around 4 a.m., the so-called morning dip. Chronotherapy for asthma based on circadian rhythm should be more efficient and have a lower frequency of side effects. Accordingly we developed a transdermal delivery system or the β_2-agonist tulobuterol adapted to the circadian rhythm. The system is designed to administer the appropriate dose or the drug at an optimal time using the so-called Crystal Reservoir System. The superiority or the transdermal formulation of tulobuterol over the current therapy using oral formulations of β_2-stimulants was indicated by its excellent pharmacokinetic profile, and confirmed by the results of clinical trials. This formulation is the first transdermal chrono-delivery system reported anywhere in the world, and is expected to provide more effective and safe treatment or asthma and related diseases not only in adults, but also especially in children.
社団法人日本薬学会の論文
2002-01-01