Controlled release of paracetamol from amylodextrin tablets: in vitro and in vivo results.
Amylodextrin is a suitable excipient for the design of solid controlled-release systems. The release of paracetamol from tablets containing 30% drug and 70% amylodextrin was studied in vitro and in vivo. In vitro dissolution profiles showed almost-constant drug release rates during 8 hr, when measured in 0.05 M buffer, pH 6.8. Peroral administration of the tablets to man showed almost-constant paracetamol plasma levels up to 14 hr, as compared to fast absorption and fast elimination of a reference paracetamol solution. The plasma profiles of eight volunteers demonstrated a small intersubject variability during the first day after tablet administration. Increasing variability and decreasing plasma levels during the second day were caused by excretion of tablets from the bodies. Cumulative input as a function of time showed near-zero-order drug release during the first day. The in vivo results indicate that amylodextrin tablets are not hydrolyzed by alpha-amylase, present in the gastrointestinal tract.
van der Veen
J
J
Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, The Netherlands.
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D000082:Acetaminophen / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000328:Adult; D003692:Delayed-Action Preparations; D003912:Dextrins; D005079:Excipients; D006207:Half-Life; D006801:Humans; D008297:Male; D012995:Solubility; D013607:Tablets
D003692:Delayed-Action Preparations; D003912:Dextrins; D005079:Excipients; D013607:Tablets; D000082:Acetaminophen; C010026:amylodextrins