目的 制备青藤碱液晶凝胶,并对其进行表征;研究其流变学性能与体外透皮特性,并与青藤碱软膏与青藤碱亲水凝胶进行比较。方法 采用植烷三醇-水体系制备青藤碱液晶凝胶,并利用偏光显微镜(PLM)及小角X射线衍射(SAXS)对青藤碱液晶凝胶进行表征;利用DHR-2流变仪考察青藤碱液晶凝胶的流变特性,并与青藤碱软膏和青藤碱亲水凝胶进行比较;采用改良Franz扩散池进行体外透皮实验,并比较青藤碱液晶凝胶、亲水凝胶与软膏的体外透皮特性。结果 青藤碱液晶凝胶外观无色、澄清、透明,PLM下为暗视野,SAXS显示为立方相;流变学参数良好;青藤碱液晶凝胶、软膏、亲水凝胶的体外稳态透皮速率分别为153.93、119.99和106.89 μg·cm-2·h-1,累积释放量Qn(%)分别为93.76%、91.55%和87.60%。结论 PLM和SAXS可用于表征液晶凝胶,外观良好,流变性适宜,青藤碱液晶凝胶的体外累积释放量和体外透皮速率均优于青藤碱软膏和亲水凝胶,可为青藤碱经皮给药剂型提供理论参考。
Abstract
OBJECTIVE To prepare and characterize sinomenine liquid crystal gel, study the rheological properties and in vitro transdermal properties and compare with sinomenine ointment and sinomenine hydrophilic gel. METHODS Sinomenine liquid crystal gel was prepared by using phytanetriol-water system and then characterized by polarized light microscope(PLM)and small angle X-ray diffraction(SAXS). Using DHR-2 rheometer,the rheological properties of sinomenine liquid crystal gel were investigated and compared with those of sinomenine ointment and sinomenine hydrophilic gel. Modified Franz diffusion cell was used for in vitro transdermal experiment and the in vitro transdermal properties were compared with sinomenine hydrogels and ointments. RESULTS The appearance of sinomenine liquid crystal gel was colorless, clear and transparent, and showed dark field under PLM. SAXS showed cubic phase. The rheological parameters were good. The steady-state infiltration rates of sinomenine liquid crystal gel, ointment and hydrophilic gel were 153.93, 119.99, and 106.89 μg·cm-2·h-1,and their 48 h cumulative permeation amounts(%)were 93.76%,91.55%, and 87.60%, respectively. CONCLUSION PLM and SAXS can be used to characterize the liquid crystal gel.The prepared sinomenine liquid crystal gel has good appearance and suitable rheology, and its infiltration rate and 48 h cumulative permeation amount are superior to those of ointment and hydrophilic gel, which provides theoretical reference for sinomenine percutaneous administration.
关键词
青藤碱 /
液晶 /
凝胶 /
流变学 /
体外透皮
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Key words
sinomenine /
liquid crystal /
gel /
rheology /
in vitro transdermal penetration
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中图分类号：
R944
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脚注
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基金
国家自然科学基金资助项目(81274099);校级探索性科研项目资助(2016ts066)
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