摘要
用包封了伊维菌素的玉米醇溶蛋白微球制备新型伊维菌素微球片剂。通过片剂崩解试验和硬度测试,优化了其配比和干燥时间;将制得的片剂在温度为(40±2)℃、相对湿度为(75±5)%的条件下进行为期6个月的加速稳定性试验,评估环境因素对片剂质量的影响;通过对猪蛔虫病的疗效试验,确定了该伊维菌素微球片剂的推荐剂量及药效持续时间。按照优化配方制备的药片崩解时间小于15 min,对温度和湿度不敏感,稳定性佳;剂量在0.3 mg/kg以上的各伊维菌素微球片剂处理组给药7、14、21 d后,蛔虫卵转阴率均超过90%,与未经药物处理的空白对照组有极显著差异(P<0.01)。结果证实,该新型片剂符合《中华人民共和国兽药典(二2 2五年版)》的要求,对猪蛔虫病的治疗效果较好,推荐剂量为0.3 mg/kg,药效能持续3周以上,具有很好的临床应用前景。
Ivermectin tablet based on compressed zein microspheres was fabricated as a novel ivermectin formulation.The proportion and drying time were optimized according to the tests of disintegration and hardness.In order to evaluate the effects of environmental factors on the quality of the tablet,an accelerated stability test in 6 months at（40±2）℃ and（75±5）%relative humidity was performed on the prepared tablets.Additionally,the therapeutic effect of the prepared tablets on ascariasis in pigs was evaluated to determine the recommended dosage and effective duration.The tablet formulation disintegrated less than 15min,and was insensitive to temperature and humidity,indicating that the tablet formulation had good stability.Besides,the ivermectin tabletted microsphere-treated groups with above 0.3mg/kg in dosage reached negative conversion ratio up to 90% on day 7,14 and 21 post-beginning of administration,which was very significantly different from the positive control group.In conclusion,the novel ivermectin formulation meet the requirements of The Veterinary Pharmacopoeia of the People＇s Republic of China,which had the advantages of good efficacy on the treatment of ascariasis with the recommended dosage of 0.3mg/kg,longer effective duration（≥3 weeks）,high safety and d possessed brilliant prospects for clinical application.
出处
《中国兽医科学》
CAS
CSCD
北大核心
2010年第12期1307-1311,共5页
Chinese Veterinary Science
基金
国家高技术研究发展计划(863)项目(2002AA327100)
国家重点基础研究发展计划(973)项目(2005CB724306)
国家自然科学基金资助项目(30870635
31070868)
