壳聚糖修饰的L-天门冬酰胺酶脂质体血浆稳定性及药动学的初步研究

发布时间：2018-01-14 04:22

本文关键词：壳聚糖修饰的L-天门冬酰胺酶脂质体血浆稳定性及药动学的初步研究　出处：《中国药学杂志》2017年19期 　论文类型：期刊论文

【摘要】：目的考察壳聚糖修饰的L-天门冬酰胺酶脂质体的血浆稳定性及药动学特性。方法血浆稳定性:于不同时间点,分别测定L-天门冬酰胺酶和壳聚糖修饰的L-天门冬酰胺酶脂质体在大鼠空白血浆中的活性。大鼠静脉注射L-天门冬酰胺酶和壳聚糖修饰的L-天门冬酰胺酶脂质体后,分别考察其药动学特性。采用DAS药动学软件计算药动学参数。结果在空白血浆中,壳聚糖修饰的L-天门冬酰胺酶脂质体的活性高于L-天门冬酰胺酶;壳聚糖修饰的L-天门冬酰胺酶脂质体的活性-时间曲线下面积(AUC_(0-48 h))约为L-天门冬酰胺酶的3.3倍,壳聚糖修饰的L-天门冬酰胺酶脂质体的平均滞留时间(MRT_(0-48 h))约为ASP的2.3倍。结论壳聚糖修饰的L-天门冬酰胺酶脂质体能提高L-天门冬酰胺酶的血浆稳定性及生物利用度。
[Abstract]:Objective to investigate the plasma stability and pharmacokinetics of chitosan modified L- asparaginase liposomes. Methods Plasma stability: at different time points. The activity of L- asparaginase liposomes and chitosan modified L- asparaginase liposomes in blank plasma of rats were determined respectively. Intravenous injection of L- asparaginase and chitosan modified L- asparagine in Rats. After the enzyme liposome. The pharmacokinetic properties were investigated. The pharmacokinetic parameters were calculated by DAS software. Results in blank plasma, the activity of chitosan modified L- asparaginase liposome was higher than that of L- asparaginase. The acid-time curve of chitosan modified L- asparaginase liposomes was about 3.3 times of that of L- asparaginase. The average residence time of chitosan modified L- asparaginase liposomes and MRT: 0-48 hth). Conclusion chitosan modified L- asparaginase lipids can improve the plasma stability and bioavailability of L- asparaginase.
【作者单位】：重庆医科大学重庆高校药物工程研究中心;
【分类号】：R965
【正文快照】： 白血病是常见的造血组织异常恶性疾病,会导致患者中性粒细胞减少,血小板减少,造血功能减弱,其主要临床表现为发热、出血、贫血及感染等[1]。目前,治疗白血病主要靠造血干细胞移植及化疗,但很难找到合适的配型[2-3],化疗药物在杀伤肿瘤细胞的同时,也会杀伤正常细胞,部分患者因

【相似文献】