Bioavailability of starch based hot stage extrusion formulations

Int J Pharm. 1999 Oct 5;187(2):185-91. doi: 10.1016/s0378-5173(99)00186-6.

Abstract

The aim of the study was to develop a starch based hot stage extrusion formulation for controlled drug delivery and to evaluate its in vivo behavior. The extrusion mixture consisted of 53% corn starch as the matrix forming agent, 15% sorbitol as a plasticizer, 30% theophylline monohydrate as the model drug and 2% glyceryl monostearate as a lubricant. The extrudates were produced by means of a corotating twin screw extruder of APV Baker equipped with a twin screw powder feeder and a 3-mm cylindrical die. During extrusion 20% water (based on the wet mass) was added to the powder mixture. The extrudates were dried in an oven at 60 degrees C during 48 h, cut and filled out in hard gelatine capsules, in a way that the content of two capsules corresponded with a dose of 300 mg anhydrous theophylline. The dissolution profile of the experimental dosage form was retarded with a drug release of around 80% in 8 h. The in vivo behavior of the experimental formulation was evaluated in a randomized crossover design study (n=8) with a commercially available multiple unit sustained release product as the reference formulation. The plasma samples were analyzed by a validated HPLC-UV method with solid phase extraction for the sample preparation. It was clear that the experimental formulation exhibited sustained release behavior, but that it performed less well than the multiple unit dosage form.

Publication types

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

MeSH terms

  • Adult
  • Biological Availability
  • Chemistry, Pharmaceutical
  • Cross-Over Studies
  • Delayed-Action Preparations
  • Drug Delivery Systems*
  • Humans
  • Male
  • Starch / administration & dosage*
  • Theophylline / administration & dosage*
  • Theophylline / pharmacokinetics

Substances

  • Delayed-Action Preparations
  • Starch
  • Theophylline