| 引用本文: | 赵玉姣,姚瑶,张海龙,吴翠芳,邓珍珍,王胜峰.吲哚美辛亚微乳胶药动学及体内外相关性研究[J].中国现代应用药学,2019,36(1):31-35. |
| ZHAO Yujiao,YAO Yao,ZHANG Hailong,WU Cuifang,DENG Zhenzhen,WANG Shengfeng.Pharmacokinetics and Correlation Between in Vivo and in Vitro Transdermal Penetration of Indomethacin Submicron Emulsion Gel[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(1):31-35. |
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| 吲哚美辛亚微乳胶药动学及体内外相关性研究 |
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赵玉姣1,2, 姚瑶3, 张海龙3, 吴翠芳1, 邓珍珍1, 王胜峰1,3
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1.中南大学湘雅三医院药学部, 长沙 410013;2.广州朗圣药业有限公司, 广州 510670;3.中南大学湘雅药学院, 长沙 410013
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| 摘要: |
| 目的 研究吲哚美辛（indomethacin，IMC）亚微乳胶在兔体内的药动学，评价其生物利用度和经皮渗透性行为的体内外相关性。方法 采用改良Franz扩散池法，以SD大鼠腹部皮肤进行体外经皮渗透性实验。以家兔为实验动物，两侧腹部去毛涂抹亚微乳胶或市售普通乳膏10 g（相当于IMC 100 mg），不同时间点心脏取血，用高效液相色谱法测定IMC的血药浓度。采用反卷积分法对体外经皮渗透数据和体内药动学数据进行体内外相关性研究。结果 IMC亚微乳胶体外24 h累积经皮渗透量是市售IMC普通乳膏的2倍；经皮给药后，与市售IMC普通乳膏相比，IMC亚微乳胶的Tmax、Cmax、T1/2均无显著性差异；AUC0-24和AUC0-∞均为市售IMC普通乳膏的2倍。IMC亚微乳胶体内外相关性系数r=0.930。结论 与市售IMC普通乳膏相比，IMC亚微乳胶能够增加IMC渗透入血量，提高IMC的相对生物利用度，且其体内外经皮渗透行为具有良好的体内外相关性。 |
| 关键词: 吲哚美辛 亚微乳胶 药动学 生物利用度 体内外相关性 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.01.007 |
| 分类号:R969.1 |
| 基金项目:湖南省卫生计生委科研计划项目（B20180636） |
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| Pharmacokinetics and Correlation Between in Vivo and in Vitro Transdermal Penetration of Indomethacin Submicron Emulsion Gel |
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ZHAO Yujiao1,2, YAO Yao3, ZHANG Hailong3, WU Cuifang1, DENG Zhenzhen1, WANG Shengfeng1,3
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1.Department of Pharmacy, The Third Xiangya Hospital of Central South University, Changsha 410013, China;2.Regenex Pharmaceuticals Ltd., Guangzhou 510670, China;3.Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China
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| Abstract: |
| OBJECTIVE To study the pharmacokinetics of indomethacin(IMC) submicron emulsion gel in rabbits and evaluate its bioavailability and correlation between in vivo and in vitro transdermal penetration. METHODS A modified Franz diffusion cell method was used to test the transdermal penetration of IMC submicron emulsion gel on SD rat abdominal skin. A single dose of 10 g (equivalent to IMC 100 mg) submicron emulsion gel or commercial IMC cream was laid on abdominal skin of rabbit on both sides for an area of 40 cm2. Blood samples were collected from heart at predetermined time points and plasma concentration was determined by HPLC-UV. Deconvolution method was used to study the correlation between in vitro transdermal penetration data and in vivo pharmacokinetic data. RESULTS The cumulative transdermal permeation amount of IMC submicron emulsion gel in vitro for 24 h was twice that of the commercial IMC cream. Compared with the commercial IMC cream, the Tmax, Cmax, T1/2 had no significant differences, the AUC0-24 and AUC0-∞ of IMC submicron emulsion gel was about twice that of the commercial indomethacin cream. The in vitro and in vivo correlation coefficient of IMC submicron emulsion gel was 0.930. CONCLUSION Compared with the commercial IMC cream, IMC submicron emulsion gel can increase the amount of IMC penetrated into blood, improve the bioavailability of IMC, and the correlation between in vivo and in vitro transdermal penetration is good. |
| Key words: indomethacin submicron emulsion gel pharmacokinetics bioavailability correlation between in vivo and in vitro |
