Y. Akiyama, M. Yoshioka, H. Horibe
Aug 1, 1994
Citations
0
Influential Citations
13
Citations
Quality indicators
Journal
Journal of Pharmacy and Pharmacology
Abstract
Abstract— An oral controlled‐release drug delivery system based on microspheres of polyglycerol esters of fatty acids (PGEFs), was applied to an anti‐hypertensive, delapril hydrochloride. The in‐vitro release profile was controlled by selecting a PGEF with an appropriate hydrophilic‐lipophilic balance value for the matrix. The microspheres from which 80% of the drug was released in 6 h were orally administered to rats. The plasma concentration of the active metabolite was sustained after administration of the microspheres in comparison with administration of a solution. The in‐vivo release profile was in good agreement with the in‐vitro release profile. When the microspheres were administered, the pharmacological effect of delapril hydrochloride on the angiotensin I‐induced pressor response was also sustained showing consistency with the plasma concentration‐time curve.