Drug Discov Ther. 2017;11(5):253-258. (DOI: 10.5582/ddt.2017.01050)

Skin permeability of tulobuterol in two transdermal formulations and their followability.

Takizawa Y, Goto T, Sato S, Ohmori N, Mori K, Shimada Y, Chen K, Miyagi T, Fukai F

Various generic transdermal formulations of tulobuterol containing rubber and acrylate base polymers are commercially available in Japan. However, none of the formulations have been compared directly with respect to the skin permeability of tulobuterol and to their follow ability. Tulobuterol Tape Sawai of rubber base and Tulobuterol Tape NP of acrylate base were used to conduct the in vitro 24-hour skin permeability test of tulobuterol at receiver solution temperatures of 32°C, 37°C, and 40°C. Furthermore, the followability of these tapes were examined by measuring the depth of the pores that were formed in their adhesive layer. Consequently, the maximum flux of tulobuterol was greater for Tulobuterol Tape NP. Arrhenius plot analysis revealed that Tulobuterol Tape Sawai was more sensitive to skin surface temperature compared with Tulobuterol Tape NP. Skin abrasion had a greater effect on the skin permeability of tulobuterol in Tulobuterol Tape Sawai than in Tulobuterol Tape NP. Followability was greater for Tulobuterol Tape NP than for Tulobuterol Tape Sawai. These results suggest that a transdermal formulation of acrylate base is preferable to that with a rubber base when skin surface temperature varies or when the skin is abraded. In clinical settings, therefore, a formulation of acrylate base is preferable to a formulation of rubber base when skin surface temperature varies or when the skin is abraded. The formulation needs to be applied to the skin of less asperity for the achievement of better transdermal absorption of tulobuterol.

Full Text: