Influence of route of administration on the absorption and disposition of alpha-, gamma- and delta-tocotrienols in rats.
A study was conducted to evaluate the bioavailability of alpha-, gamma- and delta-tocotrienols administered via oral, intravenous, intramuscular and intraperitoneal routes in rats. Three separate experiments, each conducted according to a two-way crossover design, were carried out to compare intravenous and oral, intramuscular and oral, and intraperitoneal and oral administration. Oral absorption of all three tocotrienols was found to be incomplete. Of the three tocotrienols, alpha-tocotrienol had the highest oral bioavailability, at about 27.7+/-9.2%, compared with gamma- and delta-tocotrienols, which had values of 9.1+/-2.4% and 8.5+/-3.5%, respectively. Such biodiscrimination was also observed in their total clearance rates (estimated from the intravenous data). alpha-Tocotrienol showed the lowest clearance rate at about 0.16 L kg(-1) h(-1), whereas that of delta- and gamma-tocotrienols was quite similar, with values of 0.24 and 0.23 L kg(-1) h(-1), respectively. Interestingly, all three tocotrienols were found to be negligibly absorbed when administered intraperitoneally and intramuscularly. Thus, these two routes of administration should be avoided when evaluating the biological activities of the tocotrienols in whole animal experiments.
Yap
Siew Ping
SP
School of Pharmaceutical Sciences, University of Science Malaysia, 11800 Minden, Penang, Malaysia.
Yuen
Kah Hay
KH
Lim
Ai Beoy
AB
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002839:Chromans / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D007262:Infusions, Intravenous; D007263:Infusions, Parenteral; D007273:Injections, Intramuscular; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution; D024508:Tocotrienols; D014810:Vitamin E / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*
D002839:Chromans; D024508:Tocotrienols; D014810:Vitamin E; C082097:tocotrienol, delta; C013649:plastochromanol 8; C082032:tocotrienol, alpha