| 镰形棘豆总黄酮理化性质及体外经皮渗透性的研究 |
| 投稿时间：2018-12-27 修订日期：2019-06-12 点此下载全文 |
| 引用本文：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].药学实践杂志,2019,37(5):440~443,449 |
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| 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） |
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| 中文摘要: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。 |
| 中文关键词: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 |
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| Physicochemical properties and percutaneous penetration of total flavonoids from Oxytropis falcata Bunge |
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| 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. |
| keywords:total flavonoids from Oxytropis falcata Bunge physicochemical properties solubility the apparent oil-water partition coefficient percutaneous permeability |
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