caa a22 4500 477126529 CHVBK 20180405111651.0 cr unu---uuuuu 170330e19971201xx s 000 0 eng 10.1023/A:1012127829032 doi (NATIONALLICENCE)springer-10.1023/A:1012127829032 In Vivo and In Vitro Diclofenac Sodium Evaluation After Rectal Application of Soft Gelatine Capsules Enabling Application Induced Transformation (AIT) into a Semisolid System of Liquid Crystals (SSLC) for Controlled Release [Elektronische Daten] [Axel Schneeweis, Christel Müller-Goymann] Purpose. Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitro and in vivo drug release from these systems after rectal application. Methods. In vitro drug release was determined in a self-constructed dissolution apparatus to simulate rectal application. For in vivo bioavailability studies rabbits were used as animal models. In vitro release and in vivobioavailability of the capsules was compared to Voltaren® suppositories. Results. The release profiles of the in vitro experiments show zero-order kinetics. The in vivo bioavailability studies show bioequivalence in terms of AUC for both formulations (capsules and Voltaren® suppositories). The mean residence time (parameter of sustained release) of the capsules is three time longer in comparison to Voltaren® suppositories. Conclusions. Rectal administration of capsules provides an appropiate route for controlled release via AIT-SSLC which could be clearly verified in rabbits. Plenum Publishing Corporation, 1997 diclofenac sodium nationallicence lecithin nationallicence liquid crystals nationallicence reverse micellar solution nationallicence controlled release nationallicence rectal application nationallicence Schneeweis Axel Institut für Pharmazeutische Technologic, TU Braunschweig, Mendelssohnstr. 1 D-, 38106, Braunschweig aut Müller-Goymann Christel Institut für Pharmazeutische Technologic, TU Braunschweig, Mendelssohnstr. 1 D-, 38106, Braunschweig aut Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/12(1997-12-01), 1726-1729 0724-8741 14:12<1726 1997 14 11095 https://doi.org/10.1023/A:1012127829032 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1023/A:1012127829032 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Schneeweis Axel Institut für Pharmazeutische Technologic, TU Braunschweig, Mendelssohnstr. 1 D-, 38106, Braunschweig aut NATIONALLICENCE 700 1- Müller-Goymann Christel Institut für Pharmazeutische Technologic, TU Braunschweig, Mendelssohnstr. 1 D-, 38106, Braunschweig aut NATIONALLICENCE 773 0- Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/12(1997-12-01), 1726-1729 0724-8741 14:12<1726 1997 14 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer