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盐酸丁卡因醇质体的制备工艺优化
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| 篇名： | 盐酸丁卡因醇质体的制备工艺优化 |
| TITLE： | |
| 摘要： | 目的：建立盐酸丁卡因（TCH）醇质体的含量测定方法，并对其制备工艺进行优化。方法：采用高效液相色谱法测定TCH的含量；采用注入-超声法制备TCH醇质体。以TCH对照品加入量、蛋黄卵磷脂质量浓度、乙醇体积分数为因素，以包封率为指标，在单因素试验基础上采用星点设计-响应面法对工艺进行优化，并对所制醇质体进行表征以及初步稳定性考察。结果：TCH的质量浓度线性范围为10～100 μg/mL（r＝0.999 5）；定量限为0.045 μg/mL，检测限为0.021 μg/mL；精密度、稳定性、重复性试验的RSD均小于2％；加样回收率为97.80％～103.20％（RSD＝0.36％，n＝9）。最优制备工艺为TCH对照品加入量1 mg，蛋黄卵磷脂质量浓度7 mg/mL，乙醇体积分数33％；在此工艺条件下，平均包封率为64.50％（n＝3），与预测值（64.92％）的相对误差为0.64％。TCH醇质体为微有蓝色乳光的澄清液体，其外观为球形，形态圆整、光滑，大小均一，平均粒径为（80.33±2.24）nm，平均电位为（－22.6±1.33）mV。初步稳定性试验结果显示，TCH醇质体在4 ℃避光且密封的环境中放置10 d稳定性良好。结论：优化所得TCH醇质体的制备工艺稳定、可行；所建含量测定方法操作简便、快捷。 |
| ABSTRACT： | OBJECTIVE： To establish a method for determining the content of tetracaine hydrochloride （TCH） ethosomes， and to optimize the preparation technology. METHODS： The content of TCH was determined by HPLC. TCH ethosomes were prepared with injection-ultrasonic method. Using drug-loading amount， egg lecithin concentration and ethanol volume fraction as factor， encapsulation efficiency as index， central composite design-response surface methodology was used to optimize the prescription based on the single factor test. The prepared ethosomes were characterized and the stability was evaluated. RESULTS： The linear range of TCH was 10-100 μg/mL （r＝0.999 5）； the limit of quantification was 0.045 μg/mL， and detection limit was 0.021 μg/mL. RSD of precision， stability and repeatability tests were less than 2％. The recoveries ranged 97.80％-103.20％ （RSD＝0.36％， n＝9）. The optimal preparation technology included that the adding amount of TCH control was 1 mg； the concentration of egg lecithin was 7 mg/mL， and ethanol volume fraction was 33％. Under this technology， the average encapsulation efficiency was 64.50％ （n＝3）， the relative error of which from the predicted value （64.92％） was 0.64％. TCH ethosome was a clear blue liquid with a blue opalescence. Its appearance was spherical， its shape was round， smooth， uniform in size； the average particle size was （80.33±2.24） nm， and the average Zeta potential was （－22.6±1.33） mV. TCH ethosome was stable during 10 days under 4 ℃， sealed and protected from light. CONCLUSIONS： The optimal preparation process is stable and feasible. Established method is simple and rapid. |
| 期刊： | 2019年第30卷第24期 |
| 作者： | 张楠，张丹参，景永帅，苏晓梅，张健美 |
| AUTHORS： | ZHANG Nan，ZHANG Danshen，JING Yongshuai，SU Xiaomei，ZHANG Jianmei |
| 关键字： | 盐酸丁卡因；醇质体；高效液相色谱法；注入-超声法；星点设计-响应面法；包封率；工艺优化 |
| KEYWORDS： | Tetracaine hydrochloride； Ethosomes； HPLC； Injection-ultrasonic method； Central composite design-response surface methodology； Encapsulation efficiency； Technology optimization |
| 阅读数： | 377 次 |
| 本月下载数： | 6 次 |
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