佐米曲普坦-双氯芬酸微乳的制备及体外透皮研究  

Preparation and in vitro Transdermal Study of Zolmitriptan-Diclofenac Microemulsion

作　　者：杨晓艳[1] 易蕾[1] 

机构地区：[1]武汉科技大学附属天佑医院药剂科,武汉430064

出　　处：《中国药房》2017年第13期1841-1844,共4页China Pharmacy

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。OBJECTIVE：To prepare zolmitriptan-diclofenac microemulsion,and conduct quality evaluation and in vitro trans-dermal 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＆#39;skin,and cumula-tive 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 poten-tial was（-3.25±0.33）mV,the appearance was rounding;the microemulsion showed no stratification or flocculation at room tem-perature after placed for 1 month. Contents of zolmitriptan and diclofenac were 0.248 mg/mL,12.46 mg/mL（n=3）;24 h cumula-tive transdermal rates were 80%,75%. CONCLUSIONS：Zolmitriptan-diclofenac microemulsion is prepared,and its in vitro trans-dermal ability is good.

关 键 词：佐米曲普坦 双氯芬酸 微乳 伪三元相图 制备 透皮吸收 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]