摘要
目的评价大鼠外用脂质体鬼臼毒素混悬液后经时血药浓度变化规律。方法观察组大鼠涂抹脂质体鬼臼毒素混悬液（载药量0.5％）,对照组大鼠涂抹0.5％鬼臼毒素酊剂。涂药后1、2、4、6、8.10、12和24h心脏采血,用荧光光度法测定不同时间血中鬼臼毒素浓度。结果对照组浓度曲线下面积是观察组的2.3倍。观察组用药8h后鬼臼毒素血药浓度达峰值[（166.395±14.634）ng/ml],而对照组用药后2h即达峰值[（378.603±26.105）ng/ml]。观察组鬼臼毒素的峰值浓度较低,与对照组相比有显著性差异（P<0.001）。结论 脂质体鬼臼毒素混悬液外用后,全身吸收明显低于外用鬼臼毒素酊剂,表明脂质体鬼臼毒素外用后能降低全身毒副作用。
Objective To investigate the changes of serum concentration of podophyllotoxin after topical application of lipo-some podophyllotoxin suspension on rat skin. Methods SD rats were used in this study, which were divided into test group (ra=48) to receive application of liposome podophyllotoxin (0.5%) suspension and control group (n=48) treated with 0.5% podophyllotoxin alcohol solution. Blood samples were obtained from the heart at 1, 2, 4, 6, 8, 10, 12 and 24 h respectively after drug application, and the serum concentration of podophyllotoxin was determined by spectrofluorometry. Results The area under the curve of plasma drug concentration of the control group was 2.3-fold greater than that of the test group. Eight hours after drug application, the serum concentration of podophyllotoxin reached the peak in the test group, while in the control group, only two hours was needed to reach the peak. The peak serum level of podophyllotoxin in the test group were significantly lower than that of the control group (166.395?4.634 ng/ml vs 378.603 + 26.105 ng/ml, P<0.001). Conclusion The systemic absorption of podophyllotoxin in rats after its topical application in liposome suspension is significantly lower than that after application of 0.5% podophyllotoxin alcohol solution, therefore the systemic toxicity may be reduced.
出处
《第一军医大学学报》
CSCD
北大核心
2002年第9期782-783,787,共3页
Journal of First Military Medical University
基金
国家自然科学基金(39970680)
关键词
脂质体
鬼臼毒素
荧光光度法
药物动力学
liposome
podophyllotoxin
spectrofluorometry
pharmacokinetics
