The development of a transdermal therapeutic system offers the advantages of constant plasma levels i.e. avoiding of plasma peaks and providing of therapeutic plasma level during the early morning hours

Tulobuterol is a beta 2 adrenergic receptor agonist, related structurally to terbutaline, used as bronchodilator. The substance is mainly used in the long-term therapy of asthma, especially in Germany and in Japan. The typical oral daily dose is 2-4 mg.

The development of a transdermal therapeutic system offers the advantages of constant plasma levels i.e. avoiding of plasma peaks and providing of therapeutic plasma level during the early morning hours.

Project status: LTS has developed a prototype monolithic matrix system which showed suitable flux rates in vitro permeation studies. Based on accelerated stability studies at 40oC, we assume excellent stability of the current formulation.

Furthermore, a small clinical study (n=6) comparing the TTS and an oral formulation (Atenos) was conducted. It was found that the patch formulation shows less inter-individual variation as the oral delivery. The measured plasma levels of tulobuterol indicated that a constant delivery with therapeutically effective amounts is feasible.

From the in vitro/in vivo correlation it is anticipated that the delivery rate will remain essentially constant for 2-3 days.

Having developed a suitable TTS formulation the future steps in the development are the technical scale up to pilot plant and a pharmacokinetic study in humans

Phase II

Licensees sought

N/A