Biopharmaceutical evaluation of time-controlled press-coated tablets containing polymers to adjust drug release.
This paper deals with press-coated modified release tablets in which the drug dose is situated in the core or is divided between the core and the coat. The coat contains polymer (sodium alginate or hydroxypropylmethyl cellulose, HPMC) to control drug release. The main objective was to investigate how the pharmacokinetic profile of the model drug could be modified by altering the proportion of the drug between the core and the coat. The effect of the amount of the polymer in the coat was also studied. Bioavailability tests were carried out on healthy volunteers. In the absorption curves of the tablets containing 50%, 67% and 80% of the drug in the core and 180 mg HPMC in the coat a bimodal profile was observed. No bimodal release pattern in the in vitro dissolution studies was found. If the whole dose was incorporated in the core the absorption curve has only one clear t(max) value at about 10 h. Doubling the amount of HPMC in the coat dramatically decreased drug absorption. It was concluded that, if a slightly reduced t(max)-value was required, the viscosity grade of HPMC used should be lowered.
Halsas
M
M
Department of Pharmacy, University of Helsinki, Finland.
Ervasti
P
P
Veski
P
P
Jürjenson
H
H
Marvola
M
M
D000328:Adult; D000464:Alginates / Q000737:chemistry; D001682:Biological Availability; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004337:Drug Carriers; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D006801:Humans; D007052:Ibuprofen / Q000737:chemistry / Q000493:pharmacokinetics*; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility; D013607:Tablets / Q000737:chemistry / Q000493:pharmacokinetics*
D000464:Alginates; D004337:Drug Carriers; D006603:Hexuronic Acids; D011108:Polymers; D013607:Tablets; D020723:Glucuronic Acid; D007052:Ibuprofen