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目的:从药效和药物吸收两方面比较两种剂型的青黛,为将青黛开发成分散片形式的新型配方颗粒提供试验依据。方法:采用相同剂量青黛饮片和配方分散片药液进行预防给药,以腹腔注射四氯化碳建立小鼠急性肝损伤模型,检测各组动物血清中ALT和AST;建立大鼠原位灌注模型,灌注相同剂量药液,2h后检测大鼠胃和十二指肠中灌注液靛蓝、靛玉红浓度。结果:同等剂量下,两种剂型的青黛均能显著降低四氯化碳所致小鼠急性肝脏损伤模型动物ALT、AST,减轻病理性损伤,其中分散片剂型效果更佳。同时,青黛配方分散片在胃和十二指肠中的吸收率均高于原饮片。结论:青黛配方分散片使药物有效成分在水中溶出度大幅度增加,有利于其在体内的吸收,从而增强药物疗效。
OBJECTIVE: To compare the two types of indigo from the pharmacodynamics and drug absorption, to provide the experimental basis for the development of the new formula granule in the form of dispersible tablets. Methods: The same dosage of Indigo decoction and dispersible tablets were used for prophylaxis. Acute liver injury model was established by intraperitoneal injection of carbon tetrachloride. ALT and AST were measured in serum of rats in each group. In situ perfusion model was established , Perfusion of the same dose of drug solution, 2h after the test rat stomach and duodenum perfusion solution indigo, indirubin concentrations. Results: At the same dosage, indigo in both formulations significantly reduced ALT and AST in mice induced by carbon tetrachloride-induced acute liver injury and alleviated the pathological damage. At the same time, the absorption rate of indigo formula dispersible tablets in the stomach and duodenum were higher than the original. Conclusion: Indigo dietary dispersible tablets make the dissolution of active ingredients in water significantly increase, which is beneficial to its absorption in the body, thereby enhancing the efficacy of the drug.