title: In vivo disintegration profiles of encapsulated and nonencapsulated sumatriptan: gamma scintigraphy in healthy volunteers.
abstract: The goal of this exploratory pilot study was to use gamma scintigraphy to evaluate, under physiological conditions, disintegration profiles of encapsulated and nonencapsulated formulations of 100 mg sumatriptan. Using a crossover design, healthy volunteers (n = 10) ingested 100-mg doses of sumatriptan tablets radiolabeled with 111Indium, as well as encapsulated sumatriptan tablets that were prepared similarly, then placed within a gelatin capsule and backfilled with an excipient blend radiolabeled with 99mTechnetium. A gamma camera recorded scintigraphic images until 5 hours postdose. Initial disintegration of the gelatin capsule was observed at a mean (range) of 5 minutes (1-11 minutes); disintegration was complete within 14 minutes (5-24 minutes). For nonencapsulated versus encapsulated tablets, the mean (+/- standard deviation) time to initial disintegration (6 +/- 5 minutes vs 8 +/- 5 minutes) and time to complete disintegration (18 +/- 14 minutes vs 16 +/- 7 minutes) were comparable. Results of this study demonstrate that encapsulated and nonencapsulated sumatriptan have equivalent in vivo dissolution rates.
authors.affiliation: Pharmaceutical Profiles, Ltd, Nottingham, United Kingdom.
authors.forename: Ian R
authors.initials: IR
authors.lastname: Wilding
authors.forename: Darren
authors.initials: D
authors.lastname: Clark
authors.forename: Heather
authors.initials: H
authors.lastname: Wray
authors.forename: Jeff
authors.initials: J
authors.lastname: Alderman
authors.forename: Nancy
authors.initials: N
authors.lastname: Muirhead
authors.forename: Carolyn R
authors.initials: CR
authors.lastname: Sikes
mesh_terms: D000328:Adult; D001682:Biological Availability; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D005260:Female; D015902:Gamma Cameras; D005772:Gastrointestinal Transit / Q000502:physiology; D006801:Humans; D008297:Male; D008875:Middle Aged; D010865:Pilot Projects; D011877:Radionuclide Imaging / Q000379:methods; D012995:Solubility; D018170:Sumatriptan / Q000378:metabolism*
chemical_list: D002214:Capsules; D018170:Sumatriptan