ACID-CATALYZED POLY(ORTHO ESTER) MATRICES FOR INTERMEDIATE TERM DRUG DELIVERY

被引:7
作者
SHIH, C
LUCAS, S
ZENTNER, GM
机构
[1] INTERx Research Corporation/Merck Sharp and Dohme Research Laboratories, Lawrence, KS 66047
[2] Department of Pharmaceutical Chemistry, University of Kansas, Lawrence
关键词
BIOERODIBLE POLYMER; POLY(ORTHO ESTER) MATRICES; ACID CATALYZED EROSION; DRUG RELEASE MECHANISM; CONTROLLED RELEASE OF TIMOLOL MALEATE;
D O I
10.1016/0168-3659(91)90103-K
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The in vitro release of timolol maleate from poly(ortho ester) matrices was studied. Release profiles ranged from simple zero-order to complex multiphasic release patterns. The observed profile was dependent on both the polymer and the catalyst selected. Polymers that contained greater-than-or-equal-to 50 mol% of cyclohexane-trans-1,4-dimethanol (CDM) in the backbone consistently gave linear drug release profiles. Multiphasic drug release profiles were associated with polymers of < 50 mol% of CDM and lipophilic acid catalysts. The nature of the drug release profile was related to the T(g) of the polymer-drug-catalyst composite. A purely surface or bulk erosion-controlled drug release mechanism could not account for the observed drug release profiles. Linear release from devices of varied geometries suggested that diffusion through a rate controlling surface skin layer may be a limiting step in the overall drug release mechanism.
引用
收藏
页码:55 / 63
页数:9
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