ABSTRACT
OBJECTIVE@#Traditional Chinese medicine (TCM) has been widely used throughout China to prevent and cure diseases for thousands of years, and now it is a part of the integrative medicine field that is available in Western societies. To ensure the safety and quality of the herbal medicines that are a major part of the TCM tradition, they must be held to modern pharmaceutical standards. Erzhi pill (EZP) is a Chinese Pharmacopeia-listed herbal preparation that is used in the long-term clinical management of post-menopausal symptoms, osteoporosis and menstrual disorders. Until now, whether the drug release mechanism of EZP is in line with its intended TCM usage has not been studied.@*METHODS@#The release of specnuezhenide from three EZPs (self-made, Leiyunshang and Renhe) in simulated gastric fluid (SGF), acetate buffer (pH 4.5 buffer) and simulated intestinal fluid (SIF) was investigated in a dissolution test. The water uptake capacity and erosion extent of the three EZPs were investigated using swelling and erosion studies. The drug release mechanism was further assessed through statistical model fitting, using DDSolver software.@*RESULTS@#The release of specnuezhenide from all three EZPs in SGF was less than 50% within a 4 h period. However, over 70% of the specnuezhenide was released from each EZP in both pH 4.5 buffer and SIF in the same time. Analysis of the swelling and erosion behaviors and the drug release mechanism of the three EZPs confirmed that the release rate from EZP followed a sustained release profile, which was an interactive combination of swelling and erosion.@*CONCLUSION@#This study showed that the release pattern from the pills was in line with the intended TCM use of EZP. TCM had not only theoretically considered sustained release from the pills, but also formulated them to achieve this release pattern. When establishing quality control standards for pills, the theoretical TCM usage and the actual release patterns need to be considered.
ABSTRACT
Based on the concept of network pharmacology, the main nephroprotective components in Erzhi Pill reported in previous studies, were used to predict the targets through the PharmMapper method. Molecular docking was applied to screen for potential targets and biological information annotation databases (DAVID) was used to analyze the molecular function and biological process of the action targets. The Cytoscape software was used to construct the “ingredient-target-pathway” network of Erzhi Pill for renal injury treatment. TTD and GAD database were then applied to screen for the targets of renal disease for building “ingredient-core target” network. We found that 17 major active ingredients of Erzhi Pill regulated 32 targets (including ESR1, ESR2, GCK, MMP3) and affected 6 pathways, such as PI3K-Akt signaling pathway, estrogen signaling pathway and purine metabolism. This study reflected the nature of traditional Chinese medicine as multi-ingredients, multi-targets and multi-pathways, providing new clues for basic science research on the nephroprotective pharmacological mechanism of Erzhi Pill.
ABSTRACT
This study was designed to construct a "drug-core target-pathway" network of Erzhi Pill for hepatic injury treatment in an effort to explore the "multi-components, multi-targets, multi-pathways" mechanism. ADME/T calculation method was used to screen the active components of Erzhi Pill, and then predict the potential targets according to the reverse pharmacophore matching method. Biological information annotation databases (DAVID) was used to analyze the molecular function and biological process of the action targets. The Cytoscape software was used to construct the "ingredient-core target-pathway" network of Erzhi Pill for hepatic injury treatment. It was found that 39 major active ingredients of Erzhi Pill regulated 321 targets (HRAS, DCK, HSD17B1, UCK2, et al) and affected 51 pathways, such as insulin signaling pathway, FoxO signaling pathway, metabolic pathways and glycolysis/gluconeogenesis. The method revealed the action features of traditional Chinese medicine as multi-ingredients, multi-targets, multi-pathways, providing new clues for further basic study on the hepatic injury pharmacological mechanism of Erzhi Pill.
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OBJECTIVE To investigate the material basis and action mechanism for preventing osteoporosis of Erzhi Pill through network pharmacology. METHODS Autodock 4.0 was used to establish the interactions of compounds from Erzhi Pill with 36 target proteins related to OP, and the “ingredient-target-pathway” network of Erzhi Pill for OP treatment was constructed and analyzed by Cytoscape3.6.0. RESULTS 21 ingredients of Erzhi Pill were found to dock with 35 target proteins(POR,CYP17A1,PTH, et al) and 15 pathways, such as HIF-1 signaling pathway, Rheumatoid arthritis and Thyroid hormone signaling pathway, were affected. CONCLUSION The mechanism of Erzhi Pill for OP treatment may be linked with regulating metabolism pathways, intervening related diseases,adjusting the level of estrogen, and so on, reflecting the action features of multi-ingredients, multi-targets and multi-pathways of traditional Chinese medicine.This study provides new clues for further basic study on the pharmacological mechanism of Erzhi Pill.
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Objective To determine the dissolution rate of Erzhi pill which was prepared by using different crushing technologies with specnuezhenide as index - and study the influence of superfine pulverization technology on the dissolution of Erzhi pill. Methods Crude drugs were crushed into the fine powder by employing general crusher and ultra-micro pulverizer-respectively. The water-honeyed pills were prepared by using these fine powders. The method of rotating basket and HPLC were used for the determination of dissolution of specnuezhenide in vitro. The data were analyzed by applying the law of Weibull. Results Compared with Erzhi pill B- the dissolution parameters of specnuezhenide in Erzhi pill A - including T50, T60, T70, T80, T90, F1h and F2h- showed significant differentce(P<0.05). Conclusion Applying the superfine pulverization technology can improve the dissolution of Erzhi pills in vitro.
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Objective To optimize the molding process of Erzhi pill. Methods Using the external properties of pill the pill weight, disintegration time as the comprehensive evaluation index, the L9(34) orthogonal test was used to test the effects of three factors: the relative density of thick paste(A), the powder fineness(B), and the proportion of powder and honey (C). Results The best molding process was as follows: the relative density of thick paste was 1.25, the powder fineness was 100 meshes, and the proportion of powder and honey was 1: 0.6. Conclusion This optimized molding process proved to be repeatable simple and feasible. The Erzhi pill made by this preparation technology are round, the color and luster are uniform and the dissolving time is short. It provides the basis for studying the molding process of Erzhi pill.
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Objective To optimize the molding process of Erzhi pill. Methods Using the external properties of pill, the pill weight, disintegration time as the comprehensive evaluation index, the L9(34) orthogonal test was used to test the effects of three factors:the relative density of thick paste(A), the powder fineness(B), and the proportion of powder and honey(C). Results The best molding process was as follows: the relative density of thick paste was 1.25, the powder fineness was 100 meshes, and the proportion of powder and honey was 1: 0.6. Conclusion This optimized molding process proved to be repeatable, simple and feasible. The Erzhi pill made by this preparation technology are round, the color and luster are uniform and the dissolving time is short. It provides the basis for studying the molding process of Erzhi pill .
ABSTRACT
Objective To determine the dissolution rate of Erzhi pill which was prepared by using different crushing technologies with specnuezhenide as index , and study the influence of superfine pulverization technology on the dissolution of Erzhi pill. Methods Crude drugs were crushed into the fine powder by employing general crusher and ultra-micro pulverizer,respectively. The water-honeyed pills were prepared by using these fine powders. The method of rotating basket and HPLC were used for the determination of dissolution of specnuezhenide in vitro. The data were analyzed by applying the law of Weibull. Results Compared with Erzhi pill B,the dissolution parameters of specnuezhenide in Erzhi pill A ,including T50、T60、T70、T80、T90、F1h and F2h, showed significant differentce(P<0.05). Conclusion Applying the superfine pulverization technology can improve the dissolution of Erzhi pills in vitro.