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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106.89μg·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。
Objective To prepare sinomenine liquid crystal gel and characterize it. The rheological properties and transdermal properties in vitro were studied and compared with sinomenine ointment and sinomenine gel. Methods The sinomenine liquid crystal gel was prepared by phytantriol-water system. The sinomenine liquid crystal gel was characterized by polarized light microscopy (PLM) and small-angle X-ray diffraction (SAXS). The gel was characterized by DHR-2 rheometer Compared with sinomenine ointment and sinomenine hydrogel, the modified Franz diffusion cell was used to compare the rheological properties of sinomenine gel and the sinomenine gel, In vitro transdermal properties of gels and ointments. Results The appearance of sinomenine liquid crystal gel was colorless, clear and transparent. The dark field was observed under PLM. The SAXS showed cubic phase. The rheological parameters were good. The steady state of sinomenine gel, ointment and hydrophilic gel in vitro The transdermal rates were 153.93, 119.99 and 106.89 μg · cm -2 · h -1, respectively, and the cumulative release Qn (%) were 93.76%, 91.55% and 87.60%, respectively. Conclusions PLM and SAXS can be used to characterize liquid crystal gels with good appearance and suitable rheological properties. Both in vitro cumulative release and in vitro transdermal rate of sinomenine liquid crystal gel are better than sinomenine ointment and hydrophilic gel, Nicotine percutaneous administration of dosage forms provide a theoretical reference.