Sustained release of isoniazid in vivo from a single implant of a biodegradable polymer

P.R.J. Gangadharam , D.R. Ashtekar , D.C. Farhi , D.L. Wise
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引用次数: 32

Abstract

In order to solve the problem of poor patient compliance, attempts were made to prolong the bioavailability of anti mycobacterial drugs after a single administration. A single implant of polylactic-co-glycolic acid (PLGA) co-polymer containing isoniazid ensured its sustained release up to 6 weeks. The levels are comparable with those obtained from daily doses. Homogenates of liver and lungs from animals killed at 6 weeks after a single implant showed high antimycobacterial activity against Mycobacterium tuberculosis. Sera from the implant and daily dose group animals showed no significant difference in renal, hepatic and haematological parameters. The implant caused no local or systemic toxicity.

生物可降解聚合物单次植入体内异烟肼的持续释放
为了解决患者依从性差的问题,尝试延长单次给药后抗分枝杆菌药物的生物利用度。单次植入含有异烟肼的聚乳酸-羟基乙酸共聚物(PLGA)确保其缓释长达6周。这一水平与每日剂量所获得的水平相当。单次植入后6周死亡动物的肝脏和肺部匀浆显示出对结核分枝杆菌的高抑菌活性。植入物组和日给药组动物血清的肾脏、肝脏和血液学参数均无显著差异。植入物未引起局部或全身毒性。
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