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Zhou W.,Nanjing University | Zhou W.,Jiangsu Engineering Research Center for Efficient Delivery System of | Zhou W.,Nanjing Engineering Research Center for Industrialization of Chinese Medicine Pellets | Cai B.,Nanjing University | And 6 more authors.
International Journal of Molecular Sciences | Year: 2015

Traditional Chinese medicines (TCMs) have attracted extensive interest throughout the [world due to their long history of health protection and disease control, and the internalization [of TCM preparations or patented drugs has been considered a wind vane in the process of TCM [modernization. However, multi-target effects, caused by multiple components in TCMs, hinder [not only the construction of the quality evaluation system (bioavailability), but also the application [of pharmaceutical technologies, which results in the poor efficacy in clinical practice. This review [describes the methods in the literature as well as in our thoughts about how to identify the marker [components, establish the evaluation system of bioavailability, and improve the bioavailability in [TCM preparations. We expect that the current study will be positive and informative. © 2015 by the authors; licensee MDPI, Basel, Switzerland.

Cai B.,Nanjing University | Cai B.,Nanjing Haichang Chinese Medicine Group Co. | Cai B.,Key Laboratory of State Administration of TCM for Standardization of Chinese Medicine Processing | Qin K.,Nanjing University | And 9 more authors.
Progress in Chemistry | Year: 2012

Chinese medicine processing is a traditional Chinese pharmaceutical technology, and it is also the main characteristic property that distinguish traditional Chinese medicine and natural medicine. There are complex chemical changes during the process of Chinese medicine processing, and these chemical constituents which changed during processing maybe the basis of clinical efficacy changes. To clarify the changes of the chemical constituents and the chemical reactions in Chinese medicine during the processing process is the main purpose of the chemical mechanism research of Chinese medicine processing. In recent years, many research institutions at home and abroad have done deeply research in chemical mechanism during the process of Chinese medicine processing. The chemaical reactions and chemical mechanisms ocurred in some traditional Chinese medicines during the process of Chinese medicine processing were initially clarified. The main chemical reactions occurred in the Chinese medicine processing are hydrolysis reaction, oxidation reaction, replacement reaction, isomerization reaction, decomposition reaction, etc. The main achievements in the chemical mechanism research during the process of Chinese medicine processing are reviewed. The research directions and future in the chemical mechanism research of Chinese medicine processing are prospected.

Zhou W.,Nanjing University | Qin K.M.,Nanjing Haichang Chinese Medicine Group Co. | Shan J.J.,Nanjing University | Ju W.Z.,Nanjing University | And 4 more authors.
Phytomedicine | Year: 2012

Forsythoside A (FTA), one of the main active ingredients in weeping forsythia extract, possesses strong antibacterial, antioxidant and antiviral effects, and its content was about 8% of totally, higher largely than that of other ingredients, but the absolute bioavailability orally was approximately 0.5%, which is significant low influencing clinical efficacies of its oral preparations. In the present study, in vitro Caco-2 cell, in situ single-pass intestinal perfusion and in vivo pharmacokinetics study were performed to investigate the effects of absorption enhancers based on tight junctions: sodium caprate and water-soluble chitosan on the intestinal absorption of FTA, and the eventual mucosal epithelial damage resulted from absorption enhancers was evaluated by MTT test, measurement of total amount of protein and the activity of LDH and morphology observation, respectively. The pharmacological effects such as antioxidant activity improvement by absorption enhancers were verified by PC12 cell damage inhibition rate after H2O2 insults. The observations from in vitro Caco-2 cell showed that the absorption of FTA in weeping forsythia extract could be improved by absorption enhancers. Meanwhile, the absorption enhancing effect of water-soluble chitosan may be almost saturable up to 0.0032% (w/v), and sodium caprate at concentrations up to 0.64 mg/ml was safe for the Caco-2 cells, but water-soluble chitosan at different concentrations was all safe for these cells. The observations from single-pass intestinal perfusion in situ model showed that duodenum, jejunum, ileum and colon showed significantly concentration-dependent increase in P eff-value, and that Peff-value in the ileum and colon groups, where sodium caprate was added, was higher than that of duodenum and jejunum groups, but Peff-value in the jejunum group was higher than that of duodenum, ileum and colon groups where water-soluble chitosan was added. Intestinal mucosal toxicity studies showed no significant toxicity below 800 μg/ml sodium caprate and water-soluble chitosan at different concentrations. In pharmacokinetics study, water-soluble chitosan at dosage of 50 mg/kg improved the bioavailability of FTA in weeping forsythia extract to the greatest extent, and was safe for gastrointestine from morphological observation. Besides, treatment with weeping forsythia extract with water-soluble chitosan at dosage of 50 mg/kg prevented PC12 cell damage upon H2O2 stimulation better than that of control. All findings above suggested that water-soluble chitosan at dosage of 50 mg/kg might be safe and effective absorption enhancer for improving the bioavailability of FTA and the antioxidant activity in vivo in weeping forsythia extract. © 2012 Elsevier GmbH.

Qin K.-M.,Nanjing University | Qin K.-M.,Nanjing Haichang Chinese Medicine Group Co. | Qin K.-M.,Key Laboratory of State Administration of TCM for Standardization of Chinese Medicine Processing | Shu Y.-C.,Nanjing University | And 13 more authors.
Chinese Traditional and Herbal Drugs | Year: 2013

Chinese materia medica (CMM) processing is one of the characteristics and advantages of traditional Chinese medicine (TCM), which is also an important discipline with our independent intellectual property rights. The mechanism of CMM processing is the key point of CMM research, which is also the key node of CMM modernization. Most mechanisms of CMM processing are unclear until now, which request the systematical and deep research. Raw and processed Rehmanniae Radix have the different pharmacological effects in clinical application, because there are lots of chemical reactions occurred during the steaming process. In the recent years, scientists all over the world have done lots of research on the changes and mechanisms of Rehmanniae Radix by steaming process under high temperature, and series of research achievements were obtained with the application of many new methods and technologies. These achievements provide not only many new ideas and methods for the mechanism exploration of CMM processing, but also the demonstration for researching and clarifying the mechanisms of CMM processing.

Guo H.,Nanjing University | Liu X.,Nanjing University | Liu X.,Nanjing Haichang Chinese Medicine Group Co. | Cai H.,Nanjing University | And 4 more authors.
Chinese Traditional and Herbal Drugs | Year: 2013

Objective: To carry out a preliminary study on serum parmacochemistry of Dahuang Fuzi Decoction (DFD) and to research the pharmacodynamic material basis through analyzing the constituents absorbed into blood. Methods: HPLC fingerprints of DFD and serum of rats after DFD treatment were established with serum pharmacochemistry method. The serum samples collected after DFD and single crude drug treatments were compared, the constituents absorbed into the serum after DFD ig administration was determined. Results: After the rats were ig administered with DFD, 18 transitional constituents to blood were detected, among which 14 were metabolites and 4 were prototype constituents. Conclusion: After DFD treatment, the constituents absorbed into blood are mainly from Rhei Radix et Rhizoma and Aconiti Lateralis Radix Praeparata, and the serum pharmacochemistry signs could provide the evidence for the further research of the material basis of the decoction.

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