Preformulation Studies Of Formoterol Transdermal Patch

Formoterol is a long-acting β2-adrenergic receptor completely selective agonists, mainly for the treatment of bronchial asthma, bronchitis, chronic bronchitis, emphysema and other obstructive airway disease. Especially for patients with the need for long-term using β2 adrenergic receptor agonists, and it has significant anti-inflammatory and bronchodilator effects.Compared with similar drugs, the application of a small amount of formoterol can achieve the same therapeutic effect.Based on the persistent, extensive, early morning attack and medication inconvenient features of asthma, the administration of patch which has many advantageous a long time to maintain a stable blood concentration, easy to be self administered, compliance, and no first-pass effect is more suitable for the treatment of asthma. The main purpose of this study is to select suitable matrix, master the effect of a variety of penetration enhancers on penetration effect of formoterol.Pressure sensitive adhesive select test by checking the compatibility of pressure-sensitive adhesive DT(?) A, B, C, D and E glue with formoterol, the effects of different pressure sensitive adhesive on transdermal behavior of formoterol, drug loading capabilities of different pressure-sensitive adhesive. Select the potency matrix with the advantages of comprehensive stable, good compatibility with formoterol, high drugs loading amount is quite important. The results showed that different types of pressure-sensitive adhesive drug loading capacity of DT(?) D> E glue> A> B> C, the impact of pressure-sensitive adhesive on drug transdermal acts as E glue> DT(?) B> C> A> D. The compatibility of pressure-sensitive adhesive with formoterol order to be DT(?) A> E glue> B> C> D.Finally, we have chosen DT(?) A with the features of better drug loading capabilities, good compatibility with drug, general to release drug for further research.Penetration enhancers are an important part of a patch, which works by disrupting the lipid layer structure, increasing the distribution of the drug in the lipid layers of the stratum corneum barrier and facilitate drug into the body through the loop.Our studied the impact of higher fatty acids, higher fatty acid esters, long chain alcohols and other TD penetration enhancers on the transdermal behavior of drug when use a single penetration enhancers.The results show that for DT(?) A, when using a single penetration enhancers, penetration effect as follows:penetration enhancers TD> higher fatty acid esters> long-chain alcohols> higher fatty acids> no penetration enhancers.