Akiyama Y, Yoshioka M, Horibe H, Inada Y, Hirai S, Kitamori N, Toguchi H
DDS Research Laboratories, Takeda Chemical Industries Ltd, Osaka, Japan.
J Pharm Pharmacol. 1994 Aug;46(8):661-5. doi: 10.1111/j.2042-7158.1994.tb03878.x.
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.
一种基于脂肪酸聚甘油酯（PGEFs）微球的口服控释给药系统被应用于抗高血压药物盐酸地拉普利。通过为基质选择具有合适亲水亲油平衡值的PGEF来控制体外释放曲线。将在6小时内释放80%药物的微球口服给予大鼠。与溶液给药相比，微球给药后活性代谢物的血浆浓度得以维持。体内释放曲线与体外释放曲线高度吻合。当给予微球时，盐酸地拉普利对血管紧张素I诱导的升压反应的药理作用也得以维持，与血浆浓度-时间曲线一致。
