caa a22 4500 477127789 CHVBK 20180405111655.0 cr unu---uuuuu 170330e19970801xx s 000 0 eng 10.1023/A:1012113714552 doi (NATIONALLICENCE)springer-10.1023/A:1012113714552 Spreading and Retention of Vaginal Formulations in Post-Menopausal Women as Assessed by Gamma Scintigraphy [Elektronische Daten] [J. Brown, G. Hooper, C. Kenyon, S. Haines, J. Burt, J. Humphries, S. Newman, S. Davis, R. Sparrow, I. Wilding] Purpose. In this paper we report on the first scintigraphic evaluation of vaginal dosage forms in post-menopausal women. To date, almost nothing is known about the in vivo performance of pharmaceutical formulations in the human vagina, which is a major deficiency in the rational design of drug delivery systems for both existing and new indications. Methods. The vaginal spreading and clearance of a radiolabelled pessary formulation and Replens® (polycarbophil) gel, was assessed in six healthy, post-menopausal female volunteers over a six hour period using the technique of gamma scintigraphy. Results. In five out of the six subjects studied, clearance of the two formulations exhibited very little intra-subject variation. However, there was considerable inter-subject variability in clearance; in Subject 5 circa 80% of the products were retained whilst in Subject 2 less than 2% was present at the end of the six hour imaging period. Importantly, there was no evidence to suggest that either of the formulations dispersed material beyond the cervix, into the uterus, in any of the subjects studied. Conclusions. The lack of significant retention of these products in most of the volunteers has obvious implications for the delivery of therapeutic agents. This study shows that gamma scintigraphy is an invaluable technique with which to assess novel formulations aimed at optimising retention in the vagina for topical or systemic drug delivery. Plenum Publishing Corporation, 1997 vaginal delivery nationallicence gamma scintigraphy nationallicence bioadhesion nationallicence pessary nationallicence post-menopausal women nationallicence Brown J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Hooper G. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Kenyon C. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Haines S. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Burt J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Humphries J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Newman S. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Davis S. Department of Pharmaceutical Sciences, Nottingham University, University Park, Nottingham, NG7 2RD, U.K aut Sparrow R. Department of Human Morphology, Queen's Medical Centre, Clifton Boulevard, NG7 2UH, Nottingham, U.K aut Wilding I. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/8(1997-08-01), 1073-1078 0724-8741 14:8<1073 1997 14 11095 https://doi.org/10.1023/A:1012113714552 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1023/A:1012113714552 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Brown J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Hooper G. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Kenyon C. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Haines S. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Burt J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Humphries J. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Newman S. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 700 1- Davis S. Department of Pharmaceutical Sciences, Nottingham University, University Park, Nottingham, NG7 2RD, U.K aut NATIONALLICENCE 700 1- Sparrow R. Department of Human Morphology, Queen's Medical Centre, Clifton Boulevard, NG7 2UH, Nottingham, U.K aut NATIONALLICENCE 700 1- Wilding I. Pharmaceutical Profiles Limited, 2 Faraday Building, Highfields Science Park, NG7 2QP, Nottingham, U.K aut NATIONALLICENCE 773 0- Pharmaceutical Research Kluwer Academic Publishers-Plenum Publishers 14/8(1997-08-01), 1073-1078 0724-8741 14:8<1073 1997 14 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer