ABSTRACT
This study primarily concentrated on scientific problems of poor taste caused by unclear critical quality attributes of oral preparations manufactured by Chinese materia medica, successfully established an identification method for taste critical quality attribute and a taste improvement method combining electronic tongue with human senses, and determined the optimal taste formula, to improve patients' oral medication compliance. The study received ethical approval from the Review Committee of the Beijing University of Chinese Medicine. The results showed that the proportion of bitterness of Xiaoer Qingrening Granule was 61.8%, and its bitterness grade was 3.70, it was determined that bitterness is the critical quality attribute that caused the poor taste of Xiaoer Qingrening Granule. Additionally, the optimal taste formula per milliliter of Xiaoer Qingrening sugar-free intermediate was determined with allowable daily intake, solubility, and sweetness as the limiting conditions, which was 40 mg hydroxypropyl β-cyclodextrin, 180 mg trehalose, and 1.5 mg acesulfame potassium. Compared with the Xiaoer Qingrening Granule, the sensory evaluation score of the optimal taste formula was increased by 37.5 points. In conclusion, this study achieved the taste improvement of Xiaoer Qingrening Granule and formed a set of taste improvement strategies including the identification of taste critical quality attribute, the selection of the type and dosage of corrigent, and the optimization of taste formula, which provided a thought reference for the taste improvement of other oral preparations and a new perspective for quality control of intelligent manufacturing of traditional Chinese medicines.
ABSTRACT
Coptidis Rhizoma-Evodia Fructus is a classic herb pair in traditional Chinese medicine prescriptions, the famous prescription is called Zuojinwan, which comes from Danxi Xinfa, is composed of Coptidis Rhizoma-Evodia Fructus (6∶1). In this formula, Coptidis Rhizoma has the effect of clearing heat and drying diuresis, purging fire to remove toxin and clearing heart. Evodia Fructus has the effects of expelling cold and alleviating pain, checking upward adverse flow of Qi tostop vomiting, and assisting yang to stop diarrhea. Coptidis Rhizoma has the properties of bitter and cold, and Evodia Fructus has the properties of pungent and calidus. Pungent drugs have divergent effects, and bitter drugs have sedimentation effect, when used in combination, they can clear the liver and purge fire, calm the adverse-rising energy and stop vomiting. On the basis of Zuojinwan, Coptidis Rhizoma-Evodia Fructus medicine has derived different compatibility ratios. Different ratios are different in terms of efficacy, usage, clinical application. Although with the application of modern analytical instruments and the development of molecular pharmacology theory, the chemical constituents and Pharmacological effects of Coptidis Rhizoma and Evodia Fructus have been fully studied, as to the principle of compatibility, and the study of pharmacological effects and chemical constituents after the compatibility of the two drugs in different proportions, there is still no comprehensive system summary. This article makes a systematic and comprehensive explanation of Coptidis Rhizoma-Evodia Fructus from the aspects of famous literature, chemical composition, pharmacological effects and clinical applicationthrough querying literature and ancient books. In order to make this herb pair more standardized, and provide reference materials for further research and development for this herb pair.
ABSTRACT
Objective: A network model of ulcerative colitis-associated colon cancer (UCRCC) and NF-κB signaling pathway was established, in order to predict the key inflammatory targets of UCRCC and identify the effect of GQD and composition of index components on these targets. Methods: HPLC method was used, the mobile phase was acetonitrile-0.2% phosphoric acid aqueous solution, and the gradient elution was carried out. The 10 indicators were determined. The literature of databases such as Pubmed and ScienceDirect were searched, the terms of the upstream and downstream proteins of UCRCC disease and NF-κB pathway were examined. The Cytoscape software was used to predict the key inflammatory targets of UCRCC. The UCRCC model was established by AOM/DSS method, and the effect of GQD and composition of index components on key inflammatory targets were identified by immunohistochemistry and ELISA. Results: The contents of puerarin, daidzin, glycyrrhizin, jatrorrhizine, baicalin, palmatine, berberine, baicalein, glycyrrhizic acid and wogonin in GQD were 1.677, 0.154, 0.159, 0.045, 0.448, 0.035, 0.095, 0.013, 0.111 and 0.006 μg/g, respectively. The top eight inflammatory factors of the key protein in the interaction network were NF-κBp65, iNOS, COX-2, Bcl-2, TNF-α, IL-1β, ICAM-1 and VCAM-1. Compared with the model group, the high-, medium- and low-dose groups of GQD, the composition of index components group and the 5-ASA group were able to down-regulate the relative expression levels of NF-κBp65, iNOS, Bcl-2, COX-2 in colonic tissues of UCRCC mice (P < 0.01), and down-regulate the expression levels of TNF-α, IL-1β, ICAM-1, VCAM-1 in serum of UCRCC mice (P < 0.05, 0.01). Conclusion: GQD and composition of index components can improve the pathological condition of colon tissue in UCRCC mice, down-regulate the expression of inflammatory factors in colon tissue of UCRCC mice, and have a certain intervention effect on UCRCC, which laid the foundation for determining the quality marker (Q-marker) of GQD.