摘要
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： In this paper, the rheology and release kinetics of Chuanqi ophthalmic microemulsion in situ gel were investigated. Method： The fluid properties and linear viscoelastic regions of this preparation were investigated by MCR 102 rheometer. The release kinetics of Chuanqi ophthalmic microemulsion in situ gel was evaluated by modified Franz diffusion cell method,the ligustrazine and ligustilide were selected as the indictors,and semi-permeable membrane was used as a barrier. Result： Chuanqi ophthalmic microemulsion in situ gel was a pseudoplastic fluid and it had a linear viscoelastic region. The range of the linear viscoelastic region was 0-302. 74 Pa while shear stress as an indicator. The range of the linear viscoelastic region was 0-7. 45% while strain as an indicator. At the critical point, the storage modulus（ G＇） = the loss modulus（ G″） =2 976. 60 Pa,critical shear force was 302. 74 Pa and critical strain was 7. 45%. The release amount of ligustrazine was 33. 71 μg within 8 h and its average cumulative release rate was 90. 08%, the release kinetics followed Higuchi equation. The release amount of ligustilide was 68. 46 μg within 8 h,its release rate was 84. 32%,and its release kinetics followed zero-order kinetics equation. Conclusion： Chuanqi ophthalmic microemulsion in situ gel has excellent viscoelasticity, and the deformation is reversible in a certain range. The release kinetics of ligustrazine is result from synergistic effect of its physicochemical properties and matrix skeleton,but the release kinetics of ligustilide is mainly affected by its physicochemical properties.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2017年第24期23-27,共5页
Chinese Journal of Experimental Traditional Medical Formulae
基金
国家自然科学基金项目(81373977)
关键词
流变学
线性粘弹区域
眼用原位凝胶
微乳
川芪方
川芎嗪
藁本内酯
rheology
linear viscoelastic region
ophthalmic in situ gel
microemulsion
Chuanqiprescription
ligustrazine
ligustilide
