In vitro and in vivo evaluation of medicinal carbon granules and tablet on the adsorption of acetaminophen.
Medicinal carbon (MC) granules were prepared by wet granulation using maltitol (MT), and the MC tablet was produced by compression of the granules. The physical properties and the in vitro adsorption capacity for AA of the formulations were examined. Further, the effects of MC alone and the granules on gastrointestinal absorption of AA were examined in rats when they were administered intragastrically at 15 or 45 min after the intragastrical administration of AA. AA was rapidly adsorbed by MC, and the maximum adsorption capacity of MC was 0.329g AA per gram MC. The granules and tablet exhibited adequate strength, and the tablet disintegrated rapidly. The granules and tablet showed similar adsorption profiles, but somewhat lower adsorption capacity than MC alone. MC alone and granules administered at 15 min reduced the AUC(0-infinity) significantly against the control (no treatment); however, the suppression effect on the plasma concentration was lower with the granules than with MC alone. Thus, granules and tablet are useful as a compact dosage form of MC; though the reduced adsorption capacity must be taken into account in order to expect efficacy equivalent to that of MC alone.
Yamamoto
Kenta
K
Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan.
Onishi
Hiraku
H
Ito
Akihiko
A
Machida
Yoshiharu
Y
D000082:Acetaminophen / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D000327:Adsorption; D018712:Analgesics, Non-Narcotic / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D000931:Antidotes / Q000737:chemistry / Q000494:pharmacology*; D002606:Charcoal / Q000737:chemistry / Q000494:pharmacology*; D005079:Excipients / Q000737:chemistry; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D008320:Maltose / Q000031:analogs & derivatives / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013402:Sugar Alcohols / Q000737:chemistry; D013607:Tablets
D018712:Analgesics, Non-Narcotic; D000931:Antidotes; D005079:Excipients; D013402:Sugar Alcohols; D013607:Tablets; D002606:Charcoal; D000082:Acetaminophen; D008320:Maltose; C010745:maltitol