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.
McPherson
Timothy B
TB
St. Louis College of Pharmacy, 4588 Parkview Place, St. Louis, MO 63110, USA.
Ostlund
Richard E
RE
Goldberg
Anne C
AC
Bateman
Joyce H
JH
Schimmoeller
Linda
L
Spilburg
Curtis A
CA
D000284:Administration, Oral; D000328:Adult; D002626:Chemistry, Pharmaceutical; D008078:Cholesterol, LDL / Q000187:drug effects*; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D006937:Hypercholesterolemia / Q000188:drug therapy*; D008297:Male; D008875:Middle Aged; D010316:Particle Size; D010919:Placebos; D012855:Sitosterols / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D012995:Solubility; D013607:Tablets
D008078:Cholesterol, LDL; D010919:Placebos; D012855:Sitosterols; D013607:Tablets; C407042:plant stanol ester