Effect of the Transfer Activator on Functional Properties of the Bromocain Matrix Transdermal Therapeutic Systems

摘要

The construction and composition of the bromocain matrix transdermal therapeutic system (TTS) based on microemulsion preparation are presented. Comparative study of the bromocain TTS functional properties in vitro and in vivo with and without the presence of the transfer activator docusate sodium salt (DSS) in the preparation was conducted using the high-performance liquid chromatography method. It was shown that the introduction of the transfer activator in the TTS increased both the release of the active ingredient from the drug and the rate of diffusion and, consequently, the amount of the diffused active pharmaceutical ingredient (API). The diffusion rate of 120.09 ± 21.6 and 332.34 ± 70.7 μg/(h cm~2) was reached on addition of the DSS to the TTS with active surface area of 10 cm~2 and bromocain dose of 50 and 100 mg, respectively. The diffusion rates were only 23.09 + 3.7 and 31.34 ±8.1 μg/(h cm~2) in the absence of the activator. It was established that the initial bromocain content in the TTS did not affect the diffusion rate of the drug through the skin in the absence of the activator.