Nakamura K, Natsugoe S, Kumanohoso T, Aikou T, Shinkawa T, Yamada K, Fukuzaki H
Department of Pharmacy, Kagoshima University School of Medicine, Japan.
Anticancer Drugs. 1995 Jun;6(3):483-7. doi: 10.1097/00001813-199506000-00020.
By use of four types of in vivo degradable polylactic acid (PLA), i.e. PLA with an average molecular weight of 1500 (1500DL), 2200 (2200DL), 2800 (2800DL) and 3500 (3500DL), preparations of bleomycin (BLM)-containing solid forms (polymers) were tested. The in vitro release of BLM from the polymers was also examined in an immersion system. By the melt-pressing technique, five types of BLM (2.5 mg) containing solid forms, i.e. 1500DL polymer, 2200DL polymer, 2800DL polymer, 3500DL polymer and 1500DL + 3500DL (a mixture of 1500DL and 3500DL) polymer were prepared. In all five types of polymers, cumulative BLM release was controlled to less than 5% by the third day and no initial burst of the release was observed. BLM release from the polymer continued for 3 weeks at the shortest and 6 weeks at the longest. Various polymers containing BLM could be useful for the site of drug administration or anti-cancer release pattern.
通过使用四种体内可降解聚乳酸（PLA），即平均分子量为1500的PLA（1500DL）、2200的PLA（2200DL）、2800的PLA（2800DL）和3500的PLA（3500DL），对含博来霉素（BLM）的固体形式（聚合物）制剂进行了测试。还在浸没系统中研究了BLM从聚合物中的体外释放情况。通过熔融压制技术，制备了五种含BLM（2.5毫克）的固体形式，即1500DL聚合物、2200DL聚合物、2800DL聚合物、3500DL聚合物和1500DL + 3500DL（1500DL和3500DL的混合物）聚合物。在所有五种聚合物中，到第三天时BLM的累积释放量控制在5%以下，且未观察到释放的初始突发现象。BLM从聚合物中的释放最短持续3周，最长持续6周。各种含BLM的聚合物可能对药物给药部位或抗癌释放模式有用。
