Y. Akiyama et al., ANTIHYPERTENSIVE EFFECT OF ORAL CONTROLLED-RELEASE MICROSPHERES CONTAINING AN ACE-INHIBITOR (DELAPRIL HYDROCHLORIDE) IN RATS, Journal of Pharmacy and Pharmacology, 46(8), 1994, pp. 661-665
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-lipoph
ilic balance value for the matrix. The microspheres from which 80% of
the drug was released in 6 h were orally administered to rats. The pla
sma concentration of the active metabolite was sustained after adminis
tration of the microspheres in comparison with administration of a sol
ution. The in-vivo release profile was in good agreement with the invi
tro release profile. When the microspheres were administered, the phar
macological effect of delapril hydrochloride on the angiotensin I-indu
ced presser response was also sustained showing consistency with the p
lasma concentration-time curve.