Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax

Int J Pharm. 2000 Nov 4;208(1-2):81-6. doi: 10.1016/s0378-5173(00)00549-4.

Abstract

The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant). t50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVDt50%Cmax value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow formulations, respectively. A significantly higher value of Cmax was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116 +/- 22.6% compared to the Ibu-slow matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anti-Inflammatory Agents, Non-Steroidal / blood
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Biological Availability
  • Cross-Over Studies
  • Humans
  • Ibuprofen / blood
  • Ibuprofen / pharmacokinetics*
  • Male
  • Middle Aged
  • Starch / pharmacokinetics*
  • Statistics, Nonparametric
  • Tablets
  • Waxes / pharmacokinetics*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Tablets
  • Waxes
  • Starch
  • Ibuprofen