不同剂型普罗布考对大鼠肠系膜淋巴转运及药代动力学的影响
Q95-33%R-332; 目的 通过一种新型的肠系膜淋巴管-颈静脉辅助回流模型,比较普罗布考橄榄油制剂与普罗布考混悬液制剂对大鼠肠系膜淋巴转运及药代动力学的影响.方法 12只SD大鼠随机分为4组,即混悬液制剂-颈静脉单插管组(H-JD组)、混悬液制剂-颈静脉和肠淋巴管双插管组(H-JCS组)、橄榄油制剂-颈静脉单插管组(G-JD组)、橄榄油制剂-颈静脉和肠淋巴管双插管组(G-JCS组).用液相色谱和串联质谱联用(LC-MS/MS)法测定各组大鼠在不同时间全血和淋巴液中普罗布考的浓度,绘制药-时曲线,计算药代动力学参数、相对生物利用度(Frel)和淋巴液剂量百分比.结果 各组的药-时曲线符合非...
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| Published in | 实验动物与比较医学 Vol. 42; no. 4; pp. 275 - 283 |
|---|---|
| Main Authors | , , , , , |
| Format | Journal Article |
| Language | Chinese |
| Published |
中国科学院分子细胞科学卓越创新中心动物实验技术平台,上海200031%上海中医药大学实验动物中心,上海200031
25.08.2022
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| Subjects | |
| Online Access | Get full text |
| ISSN | 1674-5817 |
| DOI | 10.12300/j.issn.1674-5817.2022.026 |
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| Abstract | Q95-33%R-332; 目的 通过一种新型的肠系膜淋巴管-颈静脉辅助回流模型,比较普罗布考橄榄油制剂与普罗布考混悬液制剂对大鼠肠系膜淋巴转运及药代动力学的影响.方法 12只SD大鼠随机分为4组,即混悬液制剂-颈静脉单插管组(H-JD组)、混悬液制剂-颈静脉和肠淋巴管双插管组(H-JCS组)、橄榄油制剂-颈静脉单插管组(G-JD组)、橄榄油制剂-颈静脉和肠淋巴管双插管组(G-JCS组).用液相色谱和串联质谱联用(LC-MS/MS)法测定各组大鼠在不同时间全血和淋巴液中普罗布考的浓度,绘制药-时曲线,计算药代动力学参数、相对生物利用度(Frel)和淋巴液剂量百分比.结果 各组的药-时曲线符合非房室模型.前述各组到达峰值时间(Tmax)分别为(11±12)h、(5±2)h、(13±9)h和(19±9)h;到达峰值浓度(Cmax)分别为(148±60)ng/mL、(207±137)ng/mL、(453±204)ng/mL和(309±177)ng/mL;药-时曲线下面积(AUClast)分别为(3210±885)h·ng·mL-1、(3677±2014)h·ng·mL-1、(12360±6629)h·ng·mL-1和(8080±3064)h·ng·mL-1.H-JCS组和G-JCS组的淋巴液剂量百分比分别为(1.29±0.50)％和(2.59±0.43)％.与H-JD组相比,G-JD组中普罗布考的Frel为(409±269)％;与H-JCS组相比,G-JCS组中普罗布考的Frel为(309±256)％.与H-JD组和H-JCS组相比,G-JD组和G-JCS组大鼠全血的Cmax、Tmax、AUClast和淋巴液剂量百分比显著升高(P<0.05);其中G-JD组全血的AUClast显著高于G-JCS组(P<0.05),而H-JD组和H-JCS组差异无统计学意义(P>0.05).结论 使用橄榄油制剂可以提高普罗布考通过肠系膜淋巴液的转运吸收率和生物利用度. |
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| AbstractList | Q95-33%R-332; 目的 通过一种新型的肠系膜淋巴管-颈静脉辅助回流模型,比较普罗布考橄榄油制剂与普罗布考混悬液制剂对大鼠肠系膜淋巴转运及药代动力学的影响.方法 12只SD大鼠随机分为4组,即混悬液制剂-颈静脉单插管组(H-JD组)、混悬液制剂-颈静脉和肠淋巴管双插管组(H-JCS组)、橄榄油制剂-颈静脉单插管组(G-JD组)、橄榄油制剂-颈静脉和肠淋巴管双插管组(G-JCS组).用液相色谱和串联质谱联用(LC-MS/MS)法测定各组大鼠在不同时间全血和淋巴液中普罗布考的浓度,绘制药-时曲线,计算药代动力学参数、相对生物利用度(Frel)和淋巴液剂量百分比.结果 各组的药-时曲线符合非房室模型.前述各组到达峰值时间(Tmax)分别为(11±12)h、(5±2)h、(13±9)h和(19±9)h;到达峰值浓度(Cmax)分别为(148±60)ng/mL、(207±137)ng/mL、(453±204)ng/mL和(309±177)ng/mL;药-时曲线下面积(AUClast)分别为(3210±885)h·ng·mL-1、(3677±2014)h·ng·mL-1、(12360±6629)h·ng·mL-1和(8080±3064)h·ng·mL-1.H-JCS组和G-JCS组的淋巴液剂量百分比分别为(1.29±0.50)％和(2.59±0.43)％.与H-JD组相比,G-JD组中普罗布考的Frel为(409±269)％;与H-JCS组相比,G-JCS组中普罗布考的Frel为(309±256)％.与H-JD组和H-JCS组相比,G-JD组和G-JCS组大鼠全血的Cmax、Tmax、AUClast和淋巴液剂量百分比显著升高(P<0.05);其中G-JD组全血的AUClast显著高于G-JCS组(P<0.05),而H-JD组和H-JCS组差异无统计学意义(P>0.05).结论 使用橄榄油制剂可以提高普罗布考通过肠系膜淋巴液的转运吸收率和生物利用度. |
| Author | 刘季俊 陈国元 张笑瑞 吴倩倩 曹静 吴宝金 |
| AuthorAffiliation | 中国科学院分子细胞科学卓越创新中心动物实验技术平台,上海200031%上海中医药大学实验动物中心,上海200031 |
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| Author_FL | CHEN Guoyuan WU Qianqian LIU Jijun ZHANG Xiaorui WU Baojin CAO Jing |
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| Keywords | 普罗布考 药代动力学 SD大鼠 肠系膜淋巴液 转运 |
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| Title | 不同剂型普罗布考对大鼠肠系膜淋巴转运及药代动力学的影响 |
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