摘要
用非药理活性的、人体内所含有的小分子物质作为药物控释载体,可避免合成高分子载体可能带来的毒性问题,并具有工艺简单、成本低、药效可靠的优点.方法:用胆固醇为载体,采用自制药丸成型装置用半熔融共混挤压法制成十八甲基炔诺孕酮的长效理植药丸(直径2.5mm,长4～6mm).在体外研究了该药丸的药物释放行为.结果:用自制药丸成型装置制成的共混药丸大小、重量均匀,重现性好;药丸体外释放实验表明十八甲基炔诺孕酮的释放速率恒定,同时使用4个6mm长的药丸平均每天可释放十八甲基炔诺孕酮82±15μg,预计体内植入4个上述药丸即可达到有效避孕剂量.
To formulate an implantable long-acting levonorgestrel ( LNG)-releasing pellet using cholestrol as control-release carrier. The new system featured many advantages, including simplicity in manufacturing, low cost and ensured effectiveness. Methods: Naturally occurring cholestrol was mixed with drug and melted at the temperature below the drug' s melting point to form small cylindrical pellet. Results: The technique was reproducible. The pellets showed well controlled drug release rate. Four pieces of 6.0cm length pellets release 82 ± 15/μg LNG per day, which is very close to the recommanded contraceptive dosage. Conclusion: A new method for long-term delivery of LNG has been established. It can achieve constant low-dosage LNG supply by a single implantation . It could be a more reliable and acceptable LNG delivery system.
出处
《生物医学工程与临床》
CAS
1999年第1期32-35,共4页
Biomedical Engineering and Clinical Medicine
关键词
皮下埋植
药物释放
避孕
Subcutaneous implant Controlled-release Contraception pellet Levonorgestrel
