摘要
应用薄膜分散法研制出卡氨芥脂质体注射液，其中以多层大脂质体（ｍｕｔｉｌａｍｅｌｌｏｒｌａｒｇｅｖｅｓｉ－ｃｌｅｓ，ＭＬＶ）为主，小单层脂质体（ｓｍａｌｌｕｎｉｌａｍｅｌｌｏｒｖｅｓｉｃｌｅｓ，ＳＵＶ）为少数；粒径：５μｍ以内为９６．３２％，１０μｍ以内为９９．９５％；包封率：９０．７％±０．７％，ξ电位：９０．８５ｍＶ，相变温度：１１５℃。ＬＤ＿（５０）：１８８．２４±２５．６ｍｇ／ｋｇ。动物试验表明，本品对血管壁无刺激性，对脑胶质瘤有明显的抑制作用。
Carmustin is a chemotherapy drug which belongs to nitrosourea. Its spectrum of an-titumour is wider and it can pass through blood-cerebral barrier. It is effective in combating cere-broma and its metastatic carcinoma, Hodgkin’s disease,leukemia lymphoma,lung cancer,breastcancer,melanoma and carcinoma of colon. It kills normal cells and cancerous cells. It also restrainsmarrow. Liposome can improve the therapy by reducing side effect.We studied the intraveous in-jection of carmustin liposome(Inj BL)by film dispersion method and its physical and chemical na-ture. There were a great number of multilamellor vesicles(MUV) and a little of small unilamellorvesicles(SUV)in this solution. The percentage of the particle size smaller than 5 μm was 96.32%,smaller than 10 μm 99. 95%. Entrapment rate was 90.7%±0.7%. The particle loaded nega-tive charge. The potential of ξwas 90.85 mV. The phase inversion temperature of Inj BL was115℃,LD_(50)188.24±25.6 mg/kg.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1995年第6期345-348,共4页
Chinese Pharmaceutical Journal
基金
国家卫生部资助课题
关键词
卡氮芥脂质体
包封
相变温度
Ζ电位
抗癌药
carmustin liposome,entrapment rate,phase inversion temperature,potential of ξ
