Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy.
In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC>MG>DS tablets. The mean in vivo onset time for all tablets (DC: 6.7±3.8 min, MG: 18.3±8.1 min, DS: 67±18.9 min) did not differ significantly from in vitro onset time (DC: 5.3±1 min, MG: 16.8±3.9 min, DS: 61.8±4.7 min). The mean in vivo completion times were found to be 36.6±9.7 (DC tablets), 70±18.3 min (MG tablets) and 192.5±39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.
Ghimire
Manish
M
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK. mghimire@colorcon.co.uk
Hodges
Lee Ann
LA
Band
Janet
J
Lindsay
Blythe
B
O'Mahony
Bridget
B
McInnes
Fiona J
FJ
Mullen
Alexander B
AB
Stevens
Howard N E
HN
D000328:Adult; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D005227:Fatty Acids / Q000737:chemistry; D005772:Gastrointestinal Transit; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011877:Radionuclide Imaging; D012995:Solubility; D013607:Tablets; D016284:Technetium Tc 99m Pentetate / Q000493:pharmacokinetics; D055815:Young Adult
D003692:Delayed-Action Preparations; D005079:Excipients; D005227:Fatty Acids; D013607:Tablets; C086409:glyceryl behenate; D002482:Cellulose; C008079:hydroxypropylcellulose; D016284:Technetium Tc 99m Pentetate