CONTROLLED DRUG RELEASE FROM POLYMERIC DELIVERY DEVICES .5. HYDROXY GROUP EFFECTS ON DRUG RELEASE KINETICS AND THERMODYNAMICS

被引：25

作者：

CHIEN, YW ^{[1
]}

JEFFERSON, DM ^{[1
]}

COONEY, JG ^{[1
]}

LAMBERT, HJ ^{[1
]}

机构：

[1] SEARLE LABS,DEPT NEW PROD DEV,SKOKIE,IL 60077

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 06期

关键词：

Dosage forms—controlled release; progesterone from silicone matrix; effect of hydroxylation; kinetics; thermodynamics; Hydroxylation—progesterone; effect on release from silicone matrix; Progesterone—controlled‐release dosage forms; effect of hydroxylation on release from silicone matrix; Steroids—controlled‐release dosage forms; progesterone;

D O I：

10.1002/jps.2600680608

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The effects of progesterone hydroxylation on silicone matrix drug release kinetics and thermodynamics were investigated. Hydroxylation at positions 11, 17, and/or 21 substantially reduced progesterone release. The magnitude of this reduction depended on the number and position of the hydroxy groups and could be attributed to decreased polymer matrix diffusivity (Dm) and polymer solubility (Cp). Thermodynamically, hydroxy group addition to positions 11 and/or 21 reduced the activation energy for matrix diffusion (Ed,m) but increased the solvation energy for dissolution in silicone polymer (ΔHT,m) Adding an hydroxy group to position 17 increased the Ed,m but decreased the ΔHT,m. The overall (Ed,m + ΔHT,m) values were relatively constant and independent of hydroxylation. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：689 / 693

页数：5

共 25 条

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