[关键词]
[摘要]
目的 研究超微粉碎对虎杖膏透皮吸收和流变性的影响。方法 采用普通粉碎和超微粉碎工艺制备虎杖普通粉和虎杖超微粉,再分别制成虎杖膏和超微虎杖膏;以离体小鼠皮肤为屏障,采用改良Franz扩散池法进行透皮吸收实验,以虎杖苷、白藜芦醇、大黄素为考察指标比较虎杖膏和超微虎杖膏体外经皮渗透性的差异;以表观黏度、屈服应力为指标,采用旋转流变仪测定,比较虎杖膏和超微虎杖膏流变性的差异。结果 虎杖普通粉和超微粉的d0.9分别为(210.011±3.468)、 (63.496±2.570)μm,径距分别为5.412±0.055、2.913±0.117。虎杖膏中虎杖苷、白藜芦醇和大黄素的累积透过量分别为 (2.100 3±0.154 5)、(2.114 5±0.341 6)、(6.210 4±0.750 0)μg/cm2,透皮速率分别为(0.175 3±0.022 6)、(0.234 0±0.020 2)、(0.337 4±0.051 6)μg/(cm2·h);超微虎杖膏中虎杖苷、白藜芦醇和大黄素的累积透过量分别为(14.247 9±4.875 0)、 (4.399 3±0.628 7)、(6.768 6±0.728 6)μg/cm2,分别比虎杖膏提高6.8、2.1、1.1倍,透皮速率分别为(0.815 9±0.277 1)、(0.313 2±0.043 0)、(0.393 7±0.042 6)μg/(cm2·h),分别比虎杖膏提高4.7、1.3、1.2倍。虎杖膏和超微虎杖膏的表观黏度分别为34.940、8.865 Pa·s,屈服应力分别为41.211、7.381 Pa。结论 超微虎杖膏与虎杖膏相比透皮吸收效果更优,且膏体细腻,黏稠度和屈服应力更小,涂展性更好。
[Key word]
[Abstract]
Objective To study the effect of ultrafine comminution on transdermal absorption and rheology of P. cuspidatum ointment (PCO). Methods Common and ultrafine common powder of P. cuspidatum was got by common and ultrafine comminution technology respectively, and then prepared into common and ultrafine PCO. The skin permeation of common and ultrafine PCO was investigated through in vitro excised mice skin using improved Franz diffusion cell, with polydatin, resveratrol, and emodind as the indexes to compare the effect on the cumulative permeation amount and permeation rate of ointments. Then the effect on the rheology of ointments with apparent viscosity and yield stress as the indexes was compared. Results The d0.9 of common and ultrafine powder of P. cuspidatum were (210.011 ±3.468) and (63.496 ±2.570) μm; And the spans were (5.412 ±0.055) and (2.913 ±0.117), respectively. The cumulative permeation amount of polydatin, resveratrol, and emodind of PCO were (2.100 3 ±0.154 5), (2.114 5 ±0.341 6), and (6.210 4 ±0.750 0) μg/cm2, and the permeation rate were (0.175 3 ±0.022 6), (0.234 0 ±0.020 2), and (0.337 4 ±0.051 6) μg/(cm2·h), respectively. The ultrafine cumulative permeation amounts of polydatin, resveratrol, and emodind of PCO were (14.247 9 ±4.875 0), (4.399 3 ±0.628 7), and (6.768 6 ±0.728 6) μg/cm2, which were 6.8, 2.1, and 1.1 times compared to common PCO; The permeation rates were (0.815 9 ±0.277 1), (0.313 2 ±0.043 0), and (0.393 7 ±0.042 6) μg/(cm2·h), which were 4.7, 1.3, and 1.2 times compared to common PCO respectively. The cumulative permeation amounts and permeation rates of ultrafine PCO were 6.8, 2.1, 1.1 and 4.7, 1.3, 1.2 times compared to common PCO. The apparent viscosity and yield stress of common and ultrafine PCO were 34.940, 8.865 Pa·s and 41.211, 7.381 Pa. Conclusion Compared with common PCO, the transdermal permeability and fineness of ultrafine PCO were improved, and the apparent viscosity and yield stress decreased, which facilitates of spreadability.
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[基金项目]
贵州省科技厅联合基金项目(黔科合LH字[2015]7548号,黔科合LH字[2015]7481号);贵州省大学生创新创业训练计划项目(201410661030);遵义医学院自然科学招标项目(遵医院办发[2014]10号)