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生物降解型长效避孕埋植剂是一种可以免除在药物释放完后须经手术将埋植剂取出的、新型的、能恒速释放避孕药的皮下埋植剂。本文报道了以嵌段型聚已内酯丙交酯(CL-b-LA)为载体材料,制备生物降解左旋-18甲长效避孕埋植剂的方法,以及测定其药物含量的方法。同时,详细探讨这种皮下埋植剂体外释放的规律,研究了影响药物释放的各种因素,包括埋植剂载体材料的共聚组成、添加不同固体分散剂、固体分散剂用量和分子量、埋植剂包衣等对LNC药物释放的影响。在上述研究的基础上,选择(?)-已内酯/DL-丙交酯为85/15的嵌段共聚物作为载体材料,研制了三种不同的埋植剂:①载药量为30％;②载药量为50％;③载药量为30％+20％PEG6000。并进行了其体外药物释放的研究。结果表明,这是一种有临床应用前景、能恒速释放左旋-18甲基炔诺酮的长效避孕埋植剂。
Biodegradable long-term contraceptive implants is a new type of subcutaneous implants that can release contraceptives at a constant rate, which can remove the implants to be surgically removed after the drug is released. In this paper, a method for preparing biodegradable L-18 methotrexate implants using block polylactide-lactide (CL-b-LA) as carrier material and a method for determining its drug content were reported. In the meantime, the rules of in vitro release of such implants were discussed in detail. Various factors influencing the release of drugs were investigated, including the composition of the implants, the composition of the implants, the addition of different solid dispersants, the dosage of solid dispersants and the molecular weight of implants Effect of agent coating on LNC release. Based on the above studies, we chose three different implants as the carrier materials: (1) the block copolymer of (?) - caprolactone / DL-lactide was 85/15; %; ② drug loading was 50%; ③ drug loading was 30% + 20% PEG6000. And conducted its in vitro drug release studies. The results show that this is a long-term contraceptive implants with a promising clinical application for the sustained release of L-18 norethindrone.