[关键词]
[摘要]
目的 以具有抗老年痴呆作用的石菖蒲挥发油为模型药物,制备石菖蒲挥发油鼻喷微乳。方法 根据石菖蒲挥发油在各溶媒中的溶解度初步确定微乳处方组成,并通过绘制伪三元相图,通过比较微乳区域大小、稳定性、载药量等优选最优处方。结果 优选最优处方为石菖蒲挥发油-Cremophor EL-丙三醇-水(6.25∶20.83∶10.42∶62.5),平均粒径为(30.5±0.2)nm,多分散系数(PDI)为0.150±0.002,黏度(2.80±0.21)mPa·s;以β-细辛醚计,体外透皮速率为(1 288.76±16.20)μg/(cm2·h),比石菖蒲挥发油普通乳透皮速率提高了14倍;蟾蜍纤毛毒性实验显示该制剂无显著毒性。结论 所制得的石菖蒲挥发油鼻喷微乳理化性质稳定,透皮性能好,对鼻黏膜纤毛毒性低。
[Key word]
[Abstract]
Objective Taking the volatile oil of Acori Tatarinowii Rhizoma with the effect of anti-senile dementia as model drug to prepare Acori Tatarinowii Rhizoma-volatile oil microemulsion (AO-ME). Methods The composition of microemulsion was preliminarily determined according to the solubility of volatile oil from Acori Tatarinowii Rhizoma in various solvents. By drawing pseudo-ternary phase diagram, the optimal microemulsion formulation was selected according to the size of particles and microemulsion region, stability of preparations and drug loading. Results The optimal microemulsion formulation was that volatile oil of Acori Tatarinowii Rhizoma-Cremophor EL-glycerol-water was 6.25∶20.83∶10.42∶62.5. The average particle size of AO-ME was (30.5 ±0.2) nm with a polydispersity index of 0.150 ±0.002. The viscosity value of AO-ME was (2.80 ±0.21) mPa∙s. In vitro transdermal rate of AO-ME was (1 288.76 ±16.20) μg/(cm2∙h), measured in β-asarone. Compared with ordinary emulsion, the transdermal rate of AO-ME was increased 14 times. The ciliary toxicity test of toad showed that the preparation had no significant toxicity. Conclusion The preparation of AO-ME was prepared with stable physicochemical properties, good transdermal properties, and low toxicity to nasal mucosa cilia.
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[基金项目]
广东省科技计划项目(2013B021800173);广东省医学基金项目(A2016587);广东省教育厅青年创新人才项目(2017GKQNCX037)