Preparation of orally fast-dissolving tablets of etilefrine hydrochloride to achieve efficient absorption

Abstract

Etilefrine hydrochloride (ET) is commonly used in the treatment of hypotension in dosage forms of oral tablets and parenteral injections. However, oral tablets only temporarily achieve high plasma levels and have low bioavailability (BA), while intravenous injections may cause pain and necrosis around administration sites. In an attempt to overcome these limitations, the buccal delivery of ET using oral droplets has been investigated. In this study, a buccal tablet as an alternative dosage form was developed for practical use. Buccal tablets were prepared by the direct compression method with sodium alginate (AL) and mannitol (MA) as excipients. Their disintegration and in vitro drug release were rapid (more than 50% being released after 3 min). Furthermore, effective plasma levels (> 5–7 ng/mL) were reached within 0.5 h of buccal administration in rats. The systemic absorption of these tablets was similar to that of buccal droplets. Therefore, the ET buccal tablets developed herein have potential as an alternative dosage form for hypotension therapy.