【摘要】：目的:制備佐米曲普坦-雙氯芬酸微乳,并進(jìn)行質(zhì)量評(píng)價(jià)和體外透皮研究。方法:以溶解度和偽三元相圖中的微乳面積為指標(biāo),篩選佐米曲普坦-雙氯芬酸微乳的油相種類和混合乳化劑比例;以粒徑、Zeta電位、外觀形態(tài)和穩(wěn)定性考察微乳的質(zhì)量,采用高效液相色譜法測(cè)定微乳中佐米曲普坦和雙氯芬酸的含量,使用透皮擴(kuò)散試驗(yàn)儀,將2 g微乳涂抹于離體鼠皮角質(zhì)層,檢測(cè)24 h內(nèi)的累積透皮率。結(jié)果:微乳處方為油相(辛酸/癸酸甘油三酯)10%、混合乳化劑[聚山梨酯80-芐澤97(1∶1)]25%、1,2-丙二醇8.3%,佐米曲普坦25 mg、雙氯芬酸1.25 g,水加至100 mL。所制微乳的平均粒徑為(28.2±2.5)nm,Zeta電位為(-3.25±0.33)m V,外觀圓整,室溫下放置1個(gè)月未見分層或絮凝;佐米曲普坦和雙氯芬酸的含量分別為0.248、12.46 mg/mL(n=3);24 h累積透皮率分別為80%、75%。結(jié)論:制得佐米曲普坦-雙氯芬酸微乳,其體外透皮性較好。
[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 鹵2.5) nm,Zeta potential (- 3.25 鹵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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