镰形棘豆总黄酮理化性质及体外经皮渗透性的研究

蔡小辉; 曾棋平; 杨丽娜; 曹毅祥; 陈锦珊

doi:10.3969/j.issn.1006-0111.2019.05.010

留言板

尊敬的读者、作者、审稿人, 关于本刊的投稿、审稿、编辑和出版的任何问题, 您可以本页添加留言。我们将尽快给您答复。谢谢您的支持!

姓名
邮箱
手机号码
标题
留言内容
验证码

x 关闭永久关闭

应中央军委要求，2022年9月起，《药学实践杂志》将更名为《药学实践与服务》，双月刊，正文96页；2023年1月起，拟出版月刊，正文64页，数据库收录情况与原《药学实践杂志》相同。欢迎作者踊跃投稿！

镰形棘豆总黄酮理化性质及体外经皮渗透性的研究

蔡小辉, 曾棋平, 杨丽娜, 曹毅祥, 陈锦珊

文章导航 > 药学实践与服务 > 2019 > 37(5): 440-443,449

蔡小辉, 曾棋平, 杨丽娜, 曹毅祥, 陈锦珊. 镰形棘豆总黄酮理化性质及体外经皮渗透性的研究[J]. 药学实践与服务, 2019, 37(5): 440-443,449. doi: 10.3969/j.issn.1006-0111.2019.05.010

引用本文:

CAI Xiaohui, ZENG Qiping, YANG Lina, CAO Yixiang, CHEN Jinshan. Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge[J]. Journal of Pharmaceutical Practice and Service, 2019, 37(5): 440-443,449. doi: 10.3969/j.issn.1006-0111.2019.05.010

Citation:

CAI Xiaohui, ZENG Qiping, YANG Lina, CAO Yixiang, CHEN Jinshan. Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge[J]. Journal of Pharmaceutical Practice and Service, 2019, 37(5): 440-443,449. doi: 10.3969/j.issn.1006-0111.2019.05.010

镰形棘豆总黄酮理化性质及体外经皮渗透性的研究

doi: 10.3969/j.issn.1006-0111.2019.05.010

中国人民解放军联勤保障部队第九○九医院/厦门大学附属东南医院制剂科, 福建漳州 363000

基金项目: 原南京军区科技创新项目（14MS085）；漳州市自然科学基金（ZZ2018J15）

Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge

Department of Pharmacy, No. 909 Hospital of Joint Service Support Force/Southeast Hospital Affiliated to Xiamen University, Zhangzhou 363000, China

摘要: 目的考察镰形棘豆总黄酮的溶解度、表观油水分配系数等理化常数，研究其体外经皮渗透性能，为指导其经皮给药剂型设计和制备提供参考。方法采用紫外分光光度法测定镰形棘豆总黄酮在水及不同溶剂中的溶解度，同时测定其在正辛醇/水缓冲溶液中的P值，以大鼠离体皮肤为模型，采用双室渗透扩散装置考察其经皮渗透情况。结果镰形棘豆总黄酮在甲醇、乙醇及pH 5.0~7.4的磷酸盐缓冲液中溶解度较好。镰形棘豆总黄酮的P值与溶液pH有一定关系，当pH值在2.5~7.4时，随着pH值的增加，总黄酮的logP值逐渐减小且基本控制在0.38~1.34之间。24 h药物累积透过量为155.44 μg/cm²，时滞为（11.52±0.95）h。结论镰形棘豆总黄酮水溶性差，较易溶于甲醇、乙醇及pH 5.0~7.4的磷酸盐缓冲液，其皮肤透过性不高，累积透过率较低，且有一定的时滞，经皮给药剂型设计时需综合考虑以上特点。
- 镰形棘豆总黄酮 /
- 理化性质 /
- 溶解度 /
- 表观油水分配系数 /
- 经皮渗透性
Abstract: Objective To investigate the physicochemical constants such as the solubility and the apparent oil-water partition coefficient of total flavonoids from Oxytropis falcata Bunge and study the in vitro percutaneous permeability for providing the reference for the design and preparation of transdermal drug formulations. Methods The solubility of total flavonoids from Oxytropis falcata Bunge in water and different solvents were determined by ultraviolet spectrophotometry. The apparent oil-water partition coefficient of n-octanol/water buffer solution was also determined. Percutaneous penetration of total flavonoids from Oxytropis falcata Bunge was investigated by a double-chamber osmotic diffusion device with rat isolated skin as a model. Results The total flavonoids from Oxytropis falcata Bunge had good solubility in methanol, ethanol and phosphate buffer at pH 5.0-7.4. The apparent oil-water partition coefficient(P) of total flavonoids from Oxytropis falcata Bunge had a certain relationship with the pH of the solution. At 2.5-7.4, the lgP value of total flavonoids decreased with increasing pH value and the lgP value is between 0.38 and 1.34. The cumulative amount of drug in 24 hours is 155.44 μg/cm² and the time lag was (11.52±0.95) h. Conclusion The total flavonoids from Oxytropis falcata Bunge had poor water solubility, but were more soluble in ethanol, methanol and phosphate buffer at pH 5.0-7.4. The skin permeability was not high, and the cumulative transmittances was low with a time lag. The above characteristics should be considered comprehensively in the design of transdermal drug dosage forms.
- total flavonoids from Oxytropis falcata Bunge /
- physicochemical properties /
- solubility /
- the apparent oil-water partition coefficient /
- percutaneous permeability

[1]	魏学红,金莉.藏药镰形棘豆的研究进展[J].中国药理学通报,2010,26(11):1535-1538.
[2]	陈锦珊,杨钦磊,刘晓玲,等.藏药镰形棘豆的化学成分、药理作用及毒理学研究进展[J].中国药房,2016,27(28):3945-3948.
[3]	钱江,陈锦珊,胡永狮,等.镰形棘豆防晒霜对海训官兵日晒伤防护研究[J].东南国防医药,2012,14(2):105-107.
[4]	LOU C H,YANG G M,CAI H,et al.2',4'-Dihydroxychalcone-induced apoptosis of human gastric cancer MGC-803 cells via down-regulation of survivin mRNA[J].Toxicol In Vitro,2010,24(5):1333-1337.
[5]	LIN X F,CHEN K J,SHI H K,et al.Therapeutic effect and mechanism of Oxytropis falcata gel on deep second-degree burn in rats[J].Evid Based Complement Alternat Med,2017,2017:3729547.
[6]	王艺红,蔡小辉,曾棋平,等.藏药镰形棘豆抗深Ⅱ度烧伤活性部位筛选[J].解放军药学学报,2018,34(1):11-14.
[7]	曾棋平,王艺红,蔡小辉,等.星点设计-效应面法优化镰形棘豆总黄酮的提取工艺[J].中国药师,2017,20(5):801-804.
[8]	蔡小辉,曾棋平,杨丽娜,等.正交法优化大孔树脂纯化镰形棘豆中总黄酮的工艺[J].解放军药学学报,2018,34(5):387-389.
[9]	李俊生,吕佳佳,王兴慧,等.黄芩总黄酮及其单体的溶解性及体外经皮渗透性能研究[J].中草药,2014,45(2):200-207.
[10]	乔建卫,裴广庆,刘向东,等.黄芩总黄酮溶解度和表观油水分配系数的测定[J].中国医院药学杂志,2013,33(24):2026-2028.

[1]	徐己人, 郑紫云, 李园, 鲁莹, 储智勇. 河豚毒素处方前初步研究 . 药学实践与服务, 2023, 41(9): 544-546, 551. doi: 10.12206/j.issn.2097-2024.202304024
[2]	王宇, 邓意辉, 宋艳志, 刘广宣. 辅酶Q₁₀乳剂的处方工艺改进与质量评价 . 药学实践与服务, 2022, 40(6): 526-531. doi: 10.12206/j.issn.2097-2024.202106117
[3]	刘晓玲, 杨育儒, 蔡小辉, 陈锦珊. 镰形棘豆总黄酮的含量测定方法研究 . 药学实践与服务, 2021, 39(5): 422-425, 459. doi: 10.12206/j.issn.1006-0111.202012018
[4]	李佩瑶, 黄月英, 李传灵, 卞俊. 微凝胶的制备及其在药物缓控释系统中的应用 . 药学实践与服务, 2019, 37(3): 212-215,221. doi: 10.3969/j.issn.1006-0111.2019.03.004
[5]	毕亚静, 王艳萍, 刘福强, 赵楠, 刘丹, 韩丹, 刘天娇. 胆甾醇琥珀酰基白芨多糖的制备及其理化性质研究 . 药学实践与服务, 2013, 31(3): 220-223. doi: 10.3969/j.issn.1006-0111.2013.03.018
[6]	韩丹, 王艳萍, 毕亚静, 刘福强. 白芨多糖提取方法的优选及其理化性质研究 . 药学实践与服务, 2013, 31(1): 35-37. doi: 10.3969/j.issn.1006-0111.2013.01.010
[7]	仝永涛, 高勇, 高保安, 岳力群, 陈建明. 姜黄素在PEG-400中的溶解度及稳定性研究 . 药学实践与服务, 2013, 31(1): 53-56. doi: 10.3969/j.issn.1006-0111.2013.01.016
[8]	夏爱晓, 宋倩倩, 孙渊. 固体脂质纳米粒制备及应用研究进展 . 药学实践与服务, 2012, 30(5): 331-333,368. doi: 10.3969/j.issn.1006-0111.2012.05.003
[9]	杜青云, 洪佳妮, 李茂星, 陈锦珊. 正交试验优选镰形棘豆总黄酮活性炭脱色工艺 . 药学实践与服务, 2011, 29(2): 105-108.
[10]	吴诚, 许惠琴. 镰形棘豆中2′,4′-二羟基查尔酮抗炎止血作用的实验研究 . 药学实践与服务, 2010, 28(6): 431-432,436.
[11]	陈建达, 洪佳妮, 杜青云. 镰形棘豆霜制备工艺的优化研究 . 药学实践与服务, 2010, 28(3): 170-172.
[12]	兰芝荟, 刘延彤, 何毅刚, 李茂星, 杜青云, 贾正平. 镰形棘豆总黄酮霜剂的处方筛选及稳定性考察 . 药学实践与服务, 2010, 28(6): 422-425.
[13]	傅秋生, 衣淑珍. 山萘酚-3-O-芸香糖苷磷脂复合物的制备与理化性质研究 . 药学实践与服务, 2009, 27(3): 186-188.
[14]	刘延彤, 李茂星, 杜青云, 张汝学, 贾正平. 大孔吸附树脂富集藏药镰形棘豆总黄酮的工艺研究 . 药学实践与服务, 2008, (6): 428-440.
[15]	殷萌, 杨峰, 张欣荣. 药物多晶型的研究现状 . 药学实践与服务, 2008, (3): 163-165.
[16]	管清香, 林天慕, 王恩思. 甲磺酸地拉韦啶解离常数及分配系数的测定 . 药学实践与服务, 2007, (5): 290-291.
[17]	刘倩, 高玮, 尚北城. 传递体作为酮康唑经皮渗透载体的体外研究 . 药学实践与服务, 2005, (4): @-210,223.
[18]	徐伟, 肖宣, 柳雪枚. 中药露蜂房水溶性蛋白NV-PP-4的分离纯化及部分理化性质鉴定 . 药学实践与服务, 2000, (5): 284-285.
[19]	胡晋红, 张万国, 郑晓梅. 酮基布洛芬贴片的制备及体外渗透性研究 . 药学实践与服务, 1999, (1): 27-28.
[20]	卢绍炎, 刘能德, 陈华辉. 药用塑料容器渗透性能的考察 . 药学实践与服务, 1995, (3): 171-172.

点击查看大图

计量

文章访问数: 2978
HTML全文浏览量: 355
PDF下载量: 320
被引次数: 0

镰形棘豆总黄酮理化性质及体外经皮渗透性的研究

doi: 10.3969/j.issn.1006-0111.2019.05.010

中国人民解放军联勤保障部队第九○九医院/厦门大学附属东南医院制剂科, 福建漳州 363000

基金项目: 原南京军区科技创新项目（14MS085）；漳州市自然科学基金（ZZ2018J15）

收稿日期: 2018-12-27
修回日期: 2019-06-12

关键词:

溶解度 /

摘要: 目的考察镰形棘豆总黄酮的溶解度、表观油水分配系数等理化常数，研究其体外经皮渗透性能，为指导其经皮给药剂型设计和制备提供参考。方法采用紫外分光光度法测定镰形棘豆总黄酮在水及不同溶剂中的溶解度，同时测定其在正辛醇/水缓冲溶液中的P值，以大鼠离体皮肤为模型，采用双室渗透扩散装置考察其经皮渗透情况。结果镰形棘豆总黄酮在甲醇、乙醇及pH 5.0~7.4的磷酸盐缓冲液中溶解度较好。镰形棘豆总黄酮的P值与溶液pH有一定关系，当pH值在2.5~7.4时，随着pH值的增加，总黄酮的logP值逐渐减小且基本控制在0.38~1.34之间。24 h药物累积透过量为155.44 μg/cm²，时滞为（11.52±0.95）h。结论镰形棘豆总黄酮水溶性差，较易溶于甲醇、乙醇及pH 5.0~7.4的磷酸盐缓冲液，其皮肤透过性不高，累积透过率较低，且有一定的时滞，经皮给药剂型设计时需综合考虑以上特点。

English Abstract

Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge

Department of Pharmacy, No. 909 Hospital of Joint Service Support Force/Southeast Hospital Affiliated to Xiamen University, Zhangzhou 363000, China

Received Date: 2018-12-27
Rev Recd Date: 2019-06-12

Keywords:

Abstract: Objective To investigate the physicochemical constants such as the solubility and the apparent oil-water partition coefficient of total flavonoids from Oxytropis falcata Bunge and study the in vitro percutaneous permeability for providing the reference for the design and preparation of transdermal drug formulations. Methods The solubility of total flavonoids from Oxytropis falcata Bunge in water and different solvents were determined by ultraviolet spectrophotometry. The apparent oil-water partition coefficient of n-octanol/water buffer solution was also determined. Percutaneous penetration of total flavonoids from Oxytropis falcata Bunge was investigated by a double-chamber osmotic diffusion device with rat isolated skin as a model. Results The total flavonoids from Oxytropis falcata Bunge had good solubility in methanol, ethanol and phosphate buffer at pH 5.0-7.4. The apparent oil-water partition coefficient(P) of total flavonoids from Oxytropis falcata Bunge had a certain relationship with the pH of the solution. At 2.5-7.4, the lgP value of total flavonoids decreased with increasing pH value and the lgP value is between 0.38 and 1.34. The cumulative amount of drug in 24 hours is 155.44 μg/cm² and the time lag was (11.52±0.95) h. Conclusion The total flavonoids from Oxytropis falcata Bunge had poor water solubility, but were more soluble in ethanol, methanol and phosphate buffer at pH 5.0-7.4. The skin permeability was not high, and the cumulative transmittances was low with a time lag. The above characteristics should be considered comprehensively in the design of transdermal drug dosage forms.

引用本文:

Citation:

CAI Xiaohui, ZENG Qiping, YANG Lina, CAO Yixiang, CHEN Jinshan. Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge[J]. Journal of Pharmaceutical Practice and Service, 2019, 37(5): 440-443,449. doi: 10.3969/j.issn.1006-0111.2019.05.010