Drug Res (Stuttg) 2017; 67(11): 653-660
DOI: 10.1055/s-0043-114012
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

In vitro Controlled Release of two new Tuberculocidal Adamantane Aminoethers from Solid Pharmaceutical Formulations (II)

Marilena Vlachou1, Angeliki Siamidi1, Dimitrios Spaneas1, Dimitrios Lentzos1, Polixeni Ladia1, Konstantina Anastasiou1, Ioannis Papanastasiou2, Angeliki-Sofia Foscolos2, Markos-Orestis Georgiadis2, Vangelis Karalis1, Tahsin Kellici3, Thomas Mavromoustakos3
  • 1School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Technology, National and Kapodistrian University of Athens, University Campus, Athens, Greece
  • 2School of Health Sciences, Department of Pharmacy, Section of Pharmaceutical Chemistry, National and Kapodistrian University of Athens, University Campus, Athens, Greece
  • 3Department of Chemistry, Laboratory of Organic Chemistry, National and Kapodistrian University of Athens, University Campus, Athens, Greece
Further Information

Publication History

received 10 April 2017

accepted 18 June 2017

Publication Date:
19 July 2017 (eFirst)

Abstract

The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids. The results suggest that both analogues, albeit more lipophilic than SQ109, and aminoethers (I) and (II), have the requisite in vitro release characteristics for oral administration. In conclusion, these formulations merit further assessment by conducting in vivo studies, at a later stage.