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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d_(0.9)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/cm~2,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/(cm~2·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/cm~2,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/(cm~2·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。
Objective To study the effects of ultrafine pulverization on transdermal absorption and rheological properties of Polygonum cuspidatum. Methods The common powder of Polygonum cuspidatum and Polygonum cuspidatum were prepared by ordinary pulverization and ultrafine pulverization, and then were respectively made into Polygonum cuspidatum and Polygonum cuspidatum. The skin of ex vivo mouse was used as barrier, and the modified Franz diffusion cell method was used for transdermal absorption . The differences of percutaneous permeability between Polygonum cuspidatum and Polygonum cuspidatum in vitro were investigated by using polydatin, resveratrol and emodin. The apparent viscosity and yield stress were measured by rotary rheometer. Differences in rheology between creams and superfine Polygonum. Results The d_ (0.9) of common powder and ultrafine powder of Polygonum cuspidatum were (210.011 ± 3.468) and (63.496 ± 2.570) μm, respectively. The radial distances were 5.412 ± 0.055 and 2.913 ± 0.117, respectively. The cumulative permeation rates of polydatin, resveratrol and emodin in P. hupensis were (2.100 3 ± 0.154 5), (2.114 5 ± 0.341 6) and (6.210 4 ± 0.750 0) μg / cm 2, respectively. The transdermal rate (0.175 3 ± 0.022 6), (0.234 ± 0.020 2) and (0.337 4 ± 0.051 6) μg / (cm 2 · h), respectively. The contents of polydatin, resveratrol and emodin The cumulative permeabilities were (14.247 9 ± 4.875 0), (4.399 3 ± 0.628 7) and (6.768 6 ± 0.728 6) μg / cm 2, respectively, which were increased by 6.8, 2.1 and 1.1 times (0.815 9 ± 0.277 1), (0.313 2 ± 0.043 0) and (0.393 7 ± 0.042 6) μg / (cm ~ 2 · h) respectively, which were respectively 4.7, 1.3 and 1.2 times higher than that of Humacun. The apparent viscosity of Polygonum cuspidatum and Polygonum cuspidatum were 34.940 and 8.865 Pa · s respectively, and the yield stresses were 41.211 and 7.381 Pa respectively. Conclusion Superfine Polygonum cuspidatum has better transdermal absorption compared with Polygonum cuspidatum, and the paste is exquisite, the viscosity and yield stress are smaller, and the spreadability is better.