佐米曲普坦-双氯芬酸微乳的制备及体外透皮研究 点击下载
论文标题: 佐米曲普坦-双氯芬酸微乳的制备及体外透皮研究
英文标题:
中文摘要: 目的:制备佐米曲普坦-双氯芬酸微乳,并进行质量评价和体外透皮研究。方法:以溶解度和伪三元相图中的微乳面积为指标,筛选佐米曲普坦-双氯芬酸微乳的油相种类和混合乳化剂比例;以粒径、Zeta电位、外观形态和稳定性考察微乳的质量,采用高效液相色谱法测定微乳中佐米曲普坦和双氯芬酸的含量,使用透皮扩散试验仪,将2 g微乳涂抹于离体鼠皮角质层,检测24 h内的累积透皮率。结果:微乳处方为油相(辛酸/癸酸甘油三酯)10%、混合乳化剂[聚山梨酯80-苄泽97(1 ∶ 1)]25%、1,2-丙二醇8.3%,佐米曲普坦25 mg、双氯芬酸1.25 g,水加至100 mL。所制微乳的平均粒径为(28.2±2.5) nm,Zeta电位为(-3.25±0.33) mV,外观圆整,室温下放置1个月未见分层或絮凝;佐米曲普坦和双氯芬酸的含量分别为0.248、12.46 mg/mL(n=3);24 h累积透皮率分别为80%、75%。结论:制得佐米曲普坦-双氯芬酸微乳,其体外透皮性较好。
英文摘要: OBJECTIVE: To prepare zolmitriptan-diclofenac microemulsion, and conduct quality evaluation and in vitro transdermal study. METHODS: Using solubility and microemulsion area in pseudo-ternary phase diagram as indexes, the types of oil phase and mixed emulsifier ratio of zolmitriptan-diclofenac microemulsion were screened; the microemulsion quality was inspected using particle size, Zeta potential, appearance and stability. HPLC was used to measure the contents of zolmitriptan and diclofenac. Transdermal diffusion test instrument was used, 2 g microemulsion was smeared in cuticle of extracouporeal rats’ skin, and cumulative transdermal rate in 24 h was determined. RESULTS: The microemulsion formulation was as follow as 10% oil phase (octanoic acid triglyceride), 25% mixture emulgator [polysorbate 80-brij 97 (1 ∶ 1)], 8.3% propylene glycol and 25 mg zolmitriptan, 1.25 mg diclofenac, and water adding to 100 mL. The average particle size of prepared microemulsion was (28.2±2.5) nm, Zeta potential was (-3.25±0.33) mV, the appearance was rounding; the microemulsion showed no stratification or flocculation at room temperature after placed for 1 month. Contents of zolmitriptan and diclofenac were 0.248 mg/mL, 12.46 mg/mL (n=3); 24 h cumulative transdermal rates were 80%, 75%. CONCLUSIONS: Zolmitriptan-diclofenac microemulsion is prepared, and its in vitro transdermal ability is good.
期刊: 2017年第28卷第13期
作者: 杨晓艳,易蕾
英文作者: YANG Xiaoyan,YI Lei
关键字: 佐米曲普坦;双氯芬酸;微乳;伪三元相图;制备;透皮吸收
KEYWORDS: Zolmitriptan; Diclofenac; Microemulsion; Pseudo-ternary phase diagram; Preparation; Transdermal absorption
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