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雷公藤甲素-甘草次酸复方微乳的制备及其理化性质和体外释药特性研究
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| 篇名： | 雷公藤甲素-甘草次酸复方微乳的制备及其理化性质和体外释药特性研究 |
| TITLE： | |
| 摘要： | 目的：建立雷公藤甲素-甘草次酸复方微乳的含量测定方法，优化其处方，并考察其理化性质及体外释药特性。方法：采用超高效液相色谱法测定雷公藤甲素-甘草次酸复方微乳的含量，色谱柱为ACQUITY UPLC BEH C18，流动相为0.1％甲酸水溶液-乙腈（梯度洗脱），流速为0.4 mL/min，柱温为40 ℃，检测波长为218 nm，进样量为5 μL。采用水滴定法绘制伪三元相图，以油相、表面活性剂、助表面活性剂为指标优化处方；采用体外释放试验考察所制微乳的体外释放特性。结果：雷公藤甲素、甘草次酸的检测质量浓度线性范围分别为1～40 μg/mL（r＝0.999 7）、10～400 μg/mL（r＝0.999 8）；定量限分别为0.5、0.8 μg/mL，检测限分别为0.1、0.2 μg/mL；精密度、稳定性、重复性试验的RSD均小于2％；加样回收率分别为100.32％～101.15％（RSD＝0.36％，n＝6）、99.78％～101.42％（RSD＝0.59％，n＝6）。最优处方为以中链甘油三酯为油相，聚乙二醇羟基硬脂酸酯为表面活性剂，无水乙醇为助表面活性剂，水为水相，四者质量比为8 ∶ 28 ∶ 14 ∶ 50。所制微乳为水包油型，外观透明澄清，其平均粒径为（62.38±3.44）nm，平均多分散指数为0.096±0.001，平均黏度为（26.84±1.10）mPa·S。所制微乳在24 h内的雷公藤甲素、甘草次酸累积释放度分别为99.8％、99.7％（pH 2.0的磷酸缓冲盐溶液中），99.3％、99.4％（pH 7.4的磷酸缓冲盐溶液中），98.9％、98.4％（pH 9.0的磷酸缓冲盐溶液中）；单方微乳中的雷公藤甲素和甘草次酸释放均快于复方微乳。结论：所建含量测定方法操作简便、准确；所得优化处方稳定、可行；所制雷公藤甲素-甘草次酸复方微乳较单方微乳具有更好的缓释作用。 |
| ABSTRACT： | OBJECTIVE： To establish content determination method of Triptolide-glycyrrhetic acid compound microemulsion， optimize the formula and investigate its physicochemical properties and release rate in vitro. METHODS： The content of Triptolide- glycyrrhetic acid compound microemulsion was determined by UPLC. The determination was performed on ACQUITY UPLC BEH C18 column with mobile phase consisted of 0.1％ formic acid aqueous solution-acetonitrile （gradient elution） at the flow rate of 0.4 mL/min. The column temperature was 40 ℃. The detection wavelength was set at 218 nm， and sample size was 5 μL. Pseudo-ternary phase diagrams were drawn by water titration method. Using oil phase， surfactants and co-surfactants as index， the formula was optimized， and in intro release characteristics was investigated by in vitro release test. RESULTS： The linear range of triptolide and glycyrrhetinic acid were 1-40 μg/mL（r＝0.999 7） and 10-400 μg/mL（r＝0.999 8）， respectively. The limits of quantitation were 0.5 and 0.8 μg/mL； the limits of detection were 0.1 and 0.2 μg/mL. RSDs of precision， stability and reproducibility tests were all less than 2％. Average recoveries were 100.32％-101.15％ （RSD＝0.36％， n＝6）， 99.78％-101.42％ （RSD＝0.59％，n＝6）. The optimal formula included that medium chain triglyceride as oil phase， polyethylene glycol hydroxy stearate as surfactants， ethanol as co-surfactants， water as water phase， the proportion of them was 8 ∶ 28 ∶ 14 ∶ 50. The obtained microemulsion was O/W type， being transparent and clear， with average diameter， average polydispersity index and average viscosity of （62.38±3.44） nm， 0.096±0.001 and （26.84±1.10） mPa·S. Within 24 h， cumulative release rates of triptolide and glycyrrhetinic acid in obtained microemulsion were 99.8％ and 99.7％ （in PBS pH 2.0）， 99.3％ and 99.4％ （in PBS pH 7.4）， 98.9％ and 98.4％ （in PBS pH 9.0）， respectively. Triptolide and glycyrrhetinic acid released faster in the single microemulsion than in the compound microemulsion. CONCLUSIONS： Established content determination method is simple and stable. The optimized formula is stable and feasible. Obtained iriptolide-glycyrrhetinic acid compound microemulsion show better sustained-release effect than sigle microemulsion. |
| 期刊： | 2019年第30卷第12期 |
| 作者： | 郑恒，李晓东，翟晓莹，董淑英，张铎，杨瑞 |
| AUTHORS： | ZHENG Heng，LI Xiaodong，ZHAI Xiaoying，DONG Shuying，ZHANG Duo，YANG Rui |
| 关键字： | 雷公藤甲素；甘草次酸；复方微乳；超高效液相色谱法；伪三元相图；处方优化；体外释放度 |
| KEYWORDS： | Triptolide；Glycyrrhetic acid；Compound microemulsion；UPLC； Pseudo-ternary phase diagrams； Formula optimization； in vitro release rate |
| 阅读数： | 454 次 |
| 本月下载数： | 4 次 |
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