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目的:研究考察川芪眼用微乳原位凝胶的流变学及释放动力学行为,为该制剂的后续研究与开发提供参考。方法:使用MCR 102型流变仪考察川芪眼用微乳原位凝胶的流体性质及线性粘弹区域。体外释放度采用改良Franz扩散池法,以半透膜为释放膜,川芎嗪、藁本内酯为指标成分,取样时间点分别为0.5,1,2,4,6,8 h。结果:川芪眼用微乳原位凝胶是一种假塑性流体并存在线性粘弹区域。以剪切力为指标,确定的线性粘弹区域为0~302.74 Pa,以形变为指标得到的线性粘弹区域范围为0~7.45%。在临界点时,其储能模量(G’)等于损耗模量(G″),均为2 976.60 Pa;临界剪切力为302.74 Pa;临界形变7.45%。8 h内6份样品中川芎嗪的平均累积释放量33.71μg,平均累积释放率90.08%,释放动力学遵循Higuchi方程。8 h内6份样品中藁本内酯平均累积释放量为68.46μg,平均累积释放率为84.32%,其释放动力学遵循零级动力学方程。结论:川芪眼用微乳原位凝胶具有较好的粘弹性,并在一定范围内可以发生可逆形变。川芎嗪释放动力学是川芎嗪的理化性质与基质骨架共同作用的结果,藁本内酯的释放动力学主要受其理化性质的影响。
Objective: To study the rheology and release kinetics of microemulsion in-situ gels for eyelid of Chuanxiong, and provide reference for the follow-up research and development of this preparation. METHODS: The fluid properties and linear viscoelastic regions of the microemulsion in situ gel for eye drops of Chuanxiong were investigated using a MCR 102 rheometer. The in vitro release rate was modified by Franz diffusion cell method, semipermeable membrane was the release membrane, ligustrazine and ligustilide were used as index components, and the sampling time points were 0.5, 1, 2, 4, 6, and 8 h, respectively. RESULTS: The microemulsion in-situ gelation of Chuanxiong eye is a pseudoplastic fluid with a linear viscoelastic region. Using the shear force as the index, the linear viscoelastic region was determined to be 0-302.74 Pa. The range of the linear viscoelastic region obtained from the deformation index was 0-7.45%. At the critical point, its storage modulus (G′) is equal to the loss modulus (G′′), which is 2 976.60 Pa; the critical shear force is 302.74 Pa; the critical deformation is 7.45%. The average cumulative release of triazine was 33.71 μg, and the average cumulative release rate was 90.08%. The release kinetics followed the Higuchi equation. The average cumulative release of ligustilide from 6 samples within 8 h was 68.46 μg, and the average cumulative release rate was 84.32%. The release kinetics follow the zero-order kinetic equation.Conclusion: The microemulsion in-situ gel of eye of Chuanxiong has good viscoelasticity and reversible deformation can occur within a certain range.The ligustrazine release kinetics is the physicochemical properties of ligustrazine As a result of the combination of nature and the matrix skeleton, the release kinetics of ligustilide are mainly affected by its physicochemical properties.