左旋18-甲基炔诺酮长效避孕埋植剂的研究

The Research of the Long-Term Effective Contraceptive Implant Device-"Sino-lmplant"

本研究旨在制得一种相当于Norplant-2(Ⅱ型)的长效避孕埋植剂,每组2根,每根含LNG75mg,使用时埋于妇女上臂皮下,有效期5年,所用硅橡胶材料立足国内,埋植剂及所用材料均达到体内长期植入安全性要求,体内外释药速度达到零级稳态释放,为临床提供一种长期、有效、安全、可复的新药具。通过硅橡胶的合成及释药硅橡胶管的配方筛选及药芯配伍、模具设计、工艺流程研究,所制成的埋植剂经药理、毒理和质量标准以及体外762天释药量的检测,证明呈零级稳态释放,一年内的平均释放量为90μg/天,符合临床抗生育的要求。研究了合成和配合中诸因素对体外释放量的影响,得到了最佳的结果。药代动力学动物体内一年平均释药量为23.0μg/天,临床效果佳。

Norplant-2 was invented by the Population Council. It consists of 2 rods with 70mg levonorgestrel (LNG) each. In 1984, Shanghai Institute of Rubber Products (SIRP) began to research on subdermal implanted system. The effect of this contraceptive implant comprizine 2 silicone capsule rods with 75mg LNG each can last about 5 years long. SIRP is in charge of the material synthesis and the implant manufacturing. All used silicone material are required to reach the biological safety standard of long term implant material in vivo. Sino-Implant has passed the national drug regulatory criterions which includes: pharmacological, toxicological test, LNG pharmacokinetic drug, release rate and clinical trials etc. The release rate of LNG from the implant has been approved at zero order in vitro by the continuing 762 days records (average 90μg/vday) After a lot of work on the development of synthesis conditions the formula of silicone rubber which release the pharmacentical and the study of technological process, the long-term effective contraceptive Sino-Implant was successfully produced. It provide a simplier, safer and more effective fertility regulating methods for Chinese women, expecially for those in rural areas.