caa a22 4500 477125689 CHVBK 20180405111648.0 cr unu---uuuuu 170330e19970101xx s 000 0 eng 10.1023/A:1012019820603 doi (NATIONALLICENCE)springer-10.1023/A:1012019820603 The Use of Scintigraphy to Provide 'Proof of Concept' for Novel Polysaccharide Preparations Designed for Colonic Drug Delivery [Elektronische Daten] [Dawn Adkin, Carole Kenyon, E. Lerner, Isaac Landau, Eric Strauss, David Caron, Adel Penhasi, Abraham Rubinstein, Ian Wilding] Purpose. The aim of the present study was to provide 'proof of concept' data in man for novel polysaccharide preparations designed for colonic drug delivery using gamma scintigraphy. Methods. Two placebo calcium pectinate matrix tablet formulations were studied: one contained calcium pectinate and pectin (CaP/P) and was designed to rapidly disintegrate in the ascending colon, the other contained calcium pectinate and guar gum (CaP/GG) and was designed to disintegrate more slowly, releasing its contents throughout the ascending and transverse colon. Both formulations were enteric coated in order to protect them from the stomach. Ten healthy volunteers received either a CaP/P or CaP/GG tablet, in a randomised cross-over study. Transit and disintegration of the radiolabelled formulations was followed by gamma scintigraphy. Rat studies were conducted in order to verify that the expected colonic degradation of the polysaccharide formulations was as a consequence of bacterial enzyme attack. Results. Thein vivo clinical study confirmed the results obtained in the rat and bench in vitro fermentation models; complete tablet disintegration for Formulation CaP/GG appeared to be slower than that of Formulation CaP/P and the time and the location of complete tablet disintegration was more reproducible with Formulation CaP/P compared to Formulation CaP/GG. Conclusions. These results provide 'proof of concept' data for the use of calcium pectinate preparations for drug delivery to the colon and highlight the value of scintigraphy in focusing the development strategy for colonic targeting preparations. Plenum Publishing Corporation, 1997 calcium pectinate nationallicence colon targeting nationallicence gamma scintigraphy nationallicence 'proof of concept.' nationallicence Adkin Dawn Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut Kenyon Carole Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut Lerner E. Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut Landau Isaac Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut Strauss Eric Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut Caron David Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut Penhasi Adel Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut Rubinstein Abraham School of Pharmacy, The Hebrew University of Jerusalem, P.O. Box 12065, 91120, Jerusalem, Israel aut Wilding Ian Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/1(1997-01-01), 103-107 0724-8741 14:1<103 1997 14 11095 https://doi.org/10.1023/A:1012019820603 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1023/A:1012019820603 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Adkin Dawn Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut NATIONALLICENCE 700 1- Kenyon Carole Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut NATIONALLICENCE 700 1- Lerner E. Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut NATIONALLICENCE 700 1- Landau Isaac Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut NATIONALLICENCE 700 1- Strauss Eric Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut NATIONALLICENCE 700 1- Caron David Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut NATIONALLICENCE 700 1- Penhasi Adel Perio Products Limited, P.O. Box 23950, 91237, Jerusalem, Israel aut NATIONALLICENCE 700 1- Rubinstein Abraham School of Pharmacy, The Hebrew University of Jerusalem, P.O. Box 12065, 91120, Jerusalem, Israel aut NATIONALLICENCE 700 1- Wilding Ian Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, UK aut NATIONALLICENCE 773 0- Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/1(1997-01-01), 103-107 0724-8741 14:1<103 1997 14 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer