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
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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
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