用在体皮肤微透析法研究黄芩苷凝胶经大鼠皮肤吸收的局部药动学

娄月芬; 朱全刚; 尤本明; 李洁; 顾小燕; 张若曦

doi:10.3969/j.issn.1006-0111.2014.06.011

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用在体皮肤微透析法研究黄芩苷凝胶经大鼠皮肤吸收的局部药动学

娄月芬, 朱全刚, 尤本明, 李洁, 顾小燕, 张若曦

文章导航 > 药学实践与服务 > 2014 > 32(6): 444-447

娄月芬, 朱全刚, 尤本明, 李洁, 顾小燕, 张若曦. 用在体皮肤微透析法研究黄芩苷凝胶经大鼠皮肤吸收的局部药动学[J]. 药学实践与服务, 2014, 32(6): 444-447. doi: 10.3969/j.issn.1006-0111.2014.06.011

引用本文:

LOU Yuefen, ZHU Quangang, YOU Benming, LI Jie, GU Xiaoyan, ZHANG Ruoxi. Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo[J]. Journal of Pharmaceutical Practice and Service, 2014, 32(6): 444-447. doi: 10.3969/j.issn.1006-0111.2014.06.011

Citation:

LOU Yuefen, ZHU Quangang, YOU Benming, LI Jie, GU Xiaoyan, ZHANG Ruoxi. Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo[J]. Journal of Pharmaceutical Practice and Service, 2014, 32(6): 444-447. doi: 10.3969/j.issn.1006-0111.2014.06.011

用在体皮肤微透析法研究黄芩苷凝胶经大鼠皮肤吸收的局部药动学

doi: 10.3969/j.issn.1006-0111.2014.06.011

1.
上海市第一人民医院分院药剂科, 上海 200081
2.
上海中医药大学附属岳阳中西医结合医院药学部, 上海 200437;第二军医大学附属长海医院药学部, 上海 200433
3.
第二军医大学附属长海医院药学部, 上海 200433
4.
上海中医药大学附属岳阳中西医结合医院药学部, 上海 200437

基金项目: 上海市卫生局课题(20114061);上海市教委预算内项目(2013JW51);上海市药理学会皮肤药理学专业委员会基金(No.201302).

Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo

1.
Department of Pharmacy, Branch of Shanghai First People's Hospital, Shanghai 200081, China
2.
Department of Pharmacy, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 200437, China;Department of Pharmacy, Changhai Hospital Affiliated to Second Military Medical University, Shanghai 200433, China
3.
Department of Pharmacy, Changhai Hospital Affiliated to Second Military Medical University, Shanghai 200433, China
4.
Department of Pharmacy, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 200437, China

摘要: 目的建立大鼠在体皮肤微透析技术,研究黄芩苷凝胶经皮吸收局部药动学。方法采用HPLC-MS/MS联用技术测定大鼠皮肤微透析液中黄芩苷的浓度。SD大鼠在麻醉状态下做皮肤微透析预处理,然后将黄芩苷凝胶涂于探针所在皮肤表面,收集皮肤微透析液样品进行黄芩苷浓度测定,绘制黄芩苷浓度-时间曲线,计算经皮吸收局部药动学参数。结果用于定量分析的离子对为m/z 447.3→271.2,黄芩苷在检测浓度范围内线性关系良好,色谱的专属性、精密度等测定结果均符合生物样品测定要求。体内皮下探针对黄芩苷的回收率为(24.40±0.91)%,240 min内各取样点回收率保持稳定;黄芩苷经皮给药后8 h内微透析液中均可检测到黄芩苷的存在,且药物在皮肤组织内浓度持续升高,AUC_0-t为(50.04±34.17) (mg·min)/L。结论在体皮肤微透析法可用于黄芩苷经皮吸收局部药动学研究。
- 黄芩苷凝胶 /
- 微透析 /
- 经皮吸收局部药动学 /
- 大鼠
Abstract: Objective To develop a novel skin microdialysis technology in vivo,and to determine the pharmacokinetic of baicalin after transdermal administration in rats. Methods An HPLC-MS/MS method used for the determination of baicalin in skin microdialysis samples was established,SD rats were pretreated with skin microdialysis operation under anesthesia, and then the baicalin gel was applied to the skin surface of probe in vivo. The baicalin concentration of skin microdialysates was determined, the time curve of baicalin concentration was drawn and the topical pharmacokinetics parameters of percutaneous absorption was calculated. Results Baicalin was optimized at the transitions m/z 447.3→271.2. The linearity correlation was good and the assay exhibited good precision and accuracy. The subcutaneous probe recovery of baicalin in vivo was(24.40±0.91)% and was stable over the 240 min study period. Baicalin could be detected in the microdialysis samples after transdermal administration, and its concentration continued to rise in 8 h. AUC_0-t in skin tissue was(50.04±34.17) mg·min·L^-1. Conclusion The method of skin microdialysis in vivo could be used in the local pharmacokinetic research of baicalin.
- baicalin gel /
- microdialysis /
- dermatopharmacokinetics /
- rat

[1]	王雷,王学艳,周雪琴,等. 黄芩苷凝胶设计与体外透皮性能的研究[J]. 中草药,2008,39(10):1502-1504.
[2]	陈芳,胡晋红,朱全刚. 用微透析法测定氢溴酸东茛菪碱凝胶经皮给药大鼠体内药动学研究[J]. 药学服务与研究,2012,12(4):270-273.
[3]	李洁,朱全刚,尤本明,等. 采用微透析联用HPLC法测定透析液中黄芩苷的浓度[J]. 药学服务与研究,2012,12(1):73-74.
[4]	Xing J, Chen X, Zhong D. Stability of baicalin in biological fluids in vitro[J]. J Pharm Biomed Anal, 2005,39(3-4):593-600.
[5]	Huang H, Zhang Y, Yang R,et al. Determination of baicalin in rat cerebrospinal fluid and blood using microdialysis coupled with ultra-performance liquid chromatography-tandem mass spectrometry[J]. J Chromatogr B Analyt Technol Biomed Life Sci, 2008,874(1-2):77-83.

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用在体皮肤微透析法研究黄芩苷凝胶经大鼠皮肤吸收的局部药动学

doi: 10.3969/j.issn.1006-0111.2014.06.011

1. 上海市第一人民医院分院药剂科, 上海 200081

2. 上海中医药大学附属岳阳中西医结合医院药学部, 上海 200437;第二军医大学附属长海医院药学部, 上海 200433

3. 第二军医大学附属长海医院药学部, 上海 200433

4. 上海中医药大学附属岳阳中西医结合医院药学部, 上海 200437

基金项目: 上海市卫生局课题(20114061);上海市教委预算内项目(2013JW51);上海市药理学会皮肤药理学专业委员会基金(No.201302).

收稿日期: 2014-01-02
修回日期: 2014-09-03

关键词:

黄芩苷凝胶 /

微透析 /

经皮吸收局部药动学 /

大鼠

摘要: 目的建立大鼠在体皮肤微透析技术,研究黄芩苷凝胶经皮吸收局部药动学。方法采用HPLC-MS/MS联用技术测定大鼠皮肤微透析液中黄芩苷的浓度。SD大鼠在麻醉状态下做皮肤微透析预处理,然后将黄芩苷凝胶涂于探针所在皮肤表面,收集皮肤微透析液样品进行黄芩苷浓度测定,绘制黄芩苷浓度-时间曲线,计算经皮吸收局部药动学参数。结果用于定量分析的离子对为m/z 447.3→271.2,黄芩苷在检测浓度范围内线性关系良好,色谱的专属性、精密度等测定结果均符合生物样品测定要求。体内皮下探针对黄芩苷的回收率为(24.40±0.91)%,240 min内各取样点回收率保持稳定;黄芩苷经皮给药后8 h内微透析液中均可检测到黄芩苷的存在,且药物在皮肤组织内浓度持续升高,AUC_0-t为(50.04±34.17) (mg·min)/L。结论在体皮肤微透析法可用于黄芩苷经皮吸收局部药动学研究。

English Abstract

Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo

1. Department of Pharmacy, Branch of Shanghai First People's Hospital, Shanghai 200081, China

2. Department of Pharmacy, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 200437, China;Department of Pharmacy, Changhai Hospital Affiliated to Second Military Medical University, Shanghai 200433, China

3. Department of Pharmacy, Changhai Hospital Affiliated to Second Military Medical University, Shanghai 200433, China

4. Department of Pharmacy, Yueyang Hospital of Integrated Traditional Chinese and Western Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 200437, China

Received Date: 2014-01-02
Rev Recd Date: 2014-09-03

Keywords:

Abstract: Objective To develop a novel skin microdialysis technology in vivo,and to determine the pharmacokinetic of baicalin after transdermal administration in rats. Methods An HPLC-MS/MS method used for the determination of baicalin in skin microdialysis samples was established,SD rats were pretreated with skin microdialysis operation under anesthesia, and then the baicalin gel was applied to the skin surface of probe in vivo. The baicalin concentration of skin microdialysates was determined, the time curve of baicalin concentration was drawn and the topical pharmacokinetics parameters of percutaneous absorption was calculated. Results Baicalin was optimized at the transitions m/z 447.3→271.2. The linearity correlation was good and the assay exhibited good precision and accuracy. The subcutaneous probe recovery of baicalin in vivo was(24.40±0.91)% and was stable over the 240 min study period. Baicalin could be detected in the microdialysis samples after transdermal administration, and its concentration continued to rise in 8 h. AUC_0-t in skin tissue was(50.04±34.17) mg·min·L^-1. Conclusion The method of skin microdialysis in vivo could be used in the local pharmacokinetic research of baicalin.

引用本文:

Citation:

LOU Yuefen, ZHU Quangang, YOU Benming, LI Jie, GU Xiaoyan, ZHANG Ruoxi. Study on local pharmacokinetics of baicalin gel after transdermal administration in rats by skin microdialysis in vivo[J]. Journal of Pharmaceutical Practice and Service, 2014, 32(6): 444-447. doi: 10.3969/j.issn.1006-0111.2014.06.011