佐米曲普坦-双氯芬酸微乳的制备及体外透皮研究

发布时间：2019-05-24 09:08

【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)m V,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。
[Abstract]:Objective: to prepare zomitriptan diclofenac microemulsion and evaluate its quality and transdermal study in vitro. Methods: according to the solubility and the area of microemulsion in pseudo-ternary phase diagram, the types of oil phase and the proportion of mixed emulsifier in zomitriptan-diclofenac microemulsion were selected. The quality of microemulsion was investigated by particle size, Zeta potential, appearance morphology and stability. The contents of zomitriptan and diclofenac in microemulsion were determined by high performance liquid chromatography (HPLC). The transdermal diffusion tester was used. 2 g microemulsion was smeared on the keratin layer of isolated rat skin, and the cumulative transdermal rate within 24 hours was detected. Results: the formulation of microemulsion was oil phase (caprylic acid / decanoic acid glycerol) 10%, mixed emulsifier [polysorbate 80-benzazer 97 (1:1)] 25%, 2-propanediol 8.3%, zomitriptan 25 mg, diclofenac 1.25g, Add water to 100 mL. The average particle size of the microemulsion was (28.2 卤2.5) nm,Zeta potential (- 3.25 卤0.33) m V,), and no stratification or flocculation was found at room temperature for 1 month. The contents of zomitriptan and diclofenac were 0.248, 12.46 mg/mL (n 鈮，

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