Preparation and in vitro Transdermal Study of Zolmitriptan-Diclofenac Microemulsion / 中国药房

ABSTRACT

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'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 (11)],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.