Effect of plant stanol tablets on low-density lipoprotein cholesterol lowering in patients on statin drugs.

The objective of this study was to show that plant sterols in tablet form provide additional low-density lipoprotein (LDL) cholesterol lowering for patients on statin therapy. Dispersible phytosterol tablets were tested in a double-blind, placebo-controlled, parallel clinical trial. Twenty-six patients who were following the American Heart Association Heart Healthy Diet and on long-term statin therapy were studied for 9 weeks. After 3 weeks of placebo treatment, the subjects were randomized to receive either 1.8 g of soy stanols or placebo for 6 weeks in addition to their usual statin regimen. Stanol tablets reduced LDL cholesterol 9.1% (p = 0.007) or 12.2 mg/dl. Total cholesterol was reduced by 12.9 mg/dl (p = 0.03). A strong inverse correlation (r(s) = -0.82, p = 0.0007) was found between the baseline LDL cholesterol and the percent change in LDL cholesterol observed after stanol treatment. The additional LDL cholesterol lowering with stanol/lecithin tablets provided a potential adjunctive therapy for patients who have not reached their target LDL cholesterol goal during statin therapy.

Phytostanol tablets reduce human LDL-cholesterol.

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.