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[摘要]
目的 研究芍药苷、羟基芍药苷、苯甲酰芍药苷、四乙酰芍药苷、五乙酰芍药苷和五乙酰芍药内酯苷在人源结肠腺癌细胞系Caco-2细胞单层模型中的吸收特性。方法 利用Caco-2细胞单层模型检测上述6个化合物从孔板顶端(AP)→底端(BL)、BL→AP的双向转运过程。应用偶联紫外检测器的HPLC法测定上述6个化合物,计算转运参数和表观渗透系数(Papp),并与阳性对照药普萘洛尔和阿替洛尔进行比较。结果 芍药苷双向转运的Papp值与阿替洛尔的Papp值皆在10?7 cm/s数量级;其他5个化合物的Papp值介于在Caco-2细胞单层模型中吸收良好的普萘洛尔与难以吸收的阿替洛尔的Papp值之间。芍药苷、羟基芍药苷、苯甲酰芍药苷浓度为10~200 μmol/L,四乙酰芍药苷和五乙酰芍药内酯苷浓度为10~150 μmol/L,五乙酰芍药苷浓度为10~100 μmol/L时,其转运效率与浓度呈正相关。结论 6个受试化合物可以通过小肠上皮细胞被动吸收进入体内,芍药苷属于难吸收的化合物,羟基芍药苷、苯甲酰芍药苷、四乙酰芍药苷、五乙酰芍药苷和五乙酰芍药内酯苷属于中等吸收的化合物;苯甲酰芍药苷具有促进阿替洛尔在Caco-2细胞单层模型吸收转运的作用。
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[Abstract]
Objective Through orthogonal test to find out the scientific conditions for dry-heat sterilization process of Scutellaria Baicalensis Radix powder. Methods The microbial (bacterium and molds) quantity and the content of baicalin as the indexes, the temperature, time, thickness of powder as factors, the sterilization process for Scutellaria Baicalensis Radix powder was determined by L9(34) orthogonal test. Results The optimal technological conditions for sterilization were 100 ℃, 10 h, and the powder thickness of 2 cm. Conclusion This condition is proved by the amplified test and the large scale production, after the sterilization, the hygiene indexes of Scutellaria Baicalensis Radix powder can reach the requirements of Chinese Pharmacopoeia 2010. There is a good reproducibility but no significant difference for the content of baicalin before and after the sterilization.
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