Fukuzaki H, Yoshida M, Asano M, Kumakura M, Mashimo T, Yuasa H, Imai K, Yamanaka H
Department of Development, Takasaki Radiation Chemistry Research Establishment, Japan Atomic Energy Research Institute.
Biomaterials. 1991 May;12(4):433-7. doi: 10.1016/0142-9612(91)90014-2.
Amorphous copoly(L-lactide)/glycolide, 70/30 mol%) with weight average molecular weights of 16,900-41,300 were synthesized by ring-opening polymerization in the presence of catalysts using a molecular weight moderator lauryl alcohol. The in vivo degradation profiles of the copolyesters, which were evaluated by implanting them subcutaneously in the back of rats, showed a typical S-type degradation pattern. A luteinizing hormone-releasing hormone agonist (LH-RH agonist), des-Gly10-[Leu6]-LH-RH ethylamide monoacetate, was incorporated into the small cylinders of copoly (L-lactide/glycolide) with a weight average molecular weight of 24,000. The cumulative amount of drug released in vivo from the cylinders showed an S-type profile in analogy with the in vivo degradation pattern. This was demonstrated from data such as serum drug level and pharmacological influence on rat prostates.
采用分子量调节剂月桂醇，在催化剂存在下通过开环聚合反应合成了无定形聚（L-丙交酯）/乙交酯共聚物（摩尔比70/30），其重均分子量为16,900 - 41,300。通过将共聚酯皮下植入大鼠背部来评估其体内降解情况，结果显示出典型的S型降解模式。将促黄体生成素释放激素激动剂（LH-RH激动剂），即去甘氨酸10-[亮氨酸6]-LH-RH乙酰胺单乙酸盐，掺入重均分子量为24,000的聚（L-丙交酯/乙交酯）小圆柱体中。圆柱体在体内释放药物的累积量呈现出与体内降解模式类似的S型曲线。这从血清药物水平以及对大鼠前列腺的药理影响等数据中得到了证实。
