A New Theophylline Ointment with Rapid and High Transdermal Delivery.

Accession number;99A0636876
Title;A New Theophylline Ointment with Rapid and High Transdermal Delivery.
Author; KIZU J (Tokyo Univ.) YAZAWA M (Tokyo Univ.) YASUNO N (Tokyo Univ.) TSUCHIYA M (Tokyo Univ.) ARAKAWA Y (Tokyo Univ.)
Journal Title;Japanese Journal of Hospital Pharmacy
Journal Code:Y0888A
ISSN:0389-9098
VOL.25;NO.3;PAGE.239-248(1999)
Figure&Table&Reference;FIG.4, TBL.3, REF.14
Pub. Country;Japan
Language;English
Abstract;A transdermal therapeutic system(TTS) for the delivery of theophylline would be useful for treating bronchial asthma, especially in the case of asthma attacks in outpatients. We prepared several new types of theophylline and aminophylline ointments using transdermal absorption enhancers and measured the in vivo transdermal absorption efficiency of theophylline in rats. Among the ointments tested, a washable ointment of theophylline with N-methyl-2-pyrrolidone as a solvent and isopropyl myristate as an absorption enhancer showed the best results. The highest absorption was obtained with a concentration of 2% theophylline and 57% isopropyl myristate. The ointment was quite stable for at least 56 days at room temperature. An aminophylline ointment prepared in the same way showed less absorption and the change in appearance started after 1 week at room temperature. The serum levels of theophylline in the rats applied with the new theophylline ointment reached 10.MU.g/mL after 2h and a maximum level of 20.MU.g/mL after 6h. There was no apparent time lag in the absorption. These results suggest that a transdermal therapeutic system for the delivery of theophylline can be useful, even in the case of asthma attack. (author abst.)