Phytostanol tablets reduce human LDL-cholesterol

J Pharm Pharmacol. 2005 Jul;57(7):889-96. doi: 10.1211/0022357056343.

Abstract

The feasibility of using solid dosage forms containing stanol lecithin to lower human LDL-cholesterol was investigated. The particle size distribution of a coarse aqueous dispersion of a stanol lecithin mixture was determined at various weight ratios of the components. At a stanol-to-lecithin weight ratio of 1.00-1.50, dispersions could be spray dried and the solid reconstituted with water to produce a particle size distribution that was similar to that of the aqueous dispersion from which it was derived. Two solid dosage forms containing this spray-dried stanol lecithin preparation had different disintegration times--tablets less than 10 min and capsules greater than 45 min. Each delivery system was then tested for LDL-cholesterol reduction activity in a placebo-controlled, double-blind clinical trial containing a total of 52 subjects. After a six-week treatment period, the group that received rapidly disintegrating stanol lecithin tablets (1.26 g stanols daily) experienced a decrease in both LDL-cholesterol and the ratio of LDL-cholesterol to HDL-cholesterol by 10.4% (P = 0.01) and 11.5% (P = 0.03), respectively, relative to placebo. On the other hand, with slowly disintegrating capsules (1.01 g daily) there was no statistically significant difference in any lipid parameter between the active group and placebo group. Taken together, these studies demonstrate that for maximum LDL-cholesterol reduction activity the stanol lecithin formulation must be delivered in a rapidly dispersible form to reach the site of cholesterol absorption.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Oral
  • Adult
  • Chemistry, Pharmaceutical
  • Cholesterol, LDL / drug effects*
  • Double-Blind Method
  • Female
  • Humans
  • Hypercholesterolemia / drug therapy*
  • Male
  • Middle Aged
  • Particle Size
  • Placebos
  • Sitosterols / chemistry
  • Sitosterols / pharmacokinetics*
  • Sitosterols / pharmacology*
  • Solubility
  • Tablets

Substances

  • Cholesterol, LDL
  • Placebos
  • Sitosterols
  • Tablets
  • plant stanol ester