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The role of stratum corneum in percutaneous absorption of BN • HCl was investigated (3H-TSN 09 tape; 4 x 4 cm, BN • HCl content is 20μg/sheet) in a model of normal or damaged skin rats. 1. The microautoradiograms of skin at 8 hr after percutaneous administration of 3H-BN • HCl as a tape formulation (3H-TSN-09) in normal skin rats showed that the radioactivity was predominantly distributed in the stratum corneum. 2. After percutaneous administration of 3H-BN.HCl to damaged skin rats, the radioactivity concentra tion in the blood reached the Cmax at 5 hr and then decreased with the t1/2 of 5.5 days. And the AUC0 _ value was about 4 times higher than that in normal skin rats. 3. After percutaneous administration of 3H-BN.HCl to damaged skin rats, the coefficient of variation of the Cmax was about one-third of that in normal skin rats. 4. It was considered that 3H-BN. HC1 was mainly absorbed by transcellular route and the stratum corne um played important role in percutaneous absorption of 3H-BN.HCl as evidenced by; i) decreasing the ab sorption of 3H-BN • HCl and ii) causing inter-individual difference in blood radioactivity.

yakubutsu dōtai

Pharmacokinetics of Buprenorphine Hydrochloride (BN HCl). (2): Role of Stratum Corneum in Percutaneous Absorption of TSN-09 (BN HCl containing tape) in Male Rats.