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The enterohepatic circulation is an important form of drug absorption and excretion.Drugs with enterothepatic circulation can induce toxic side effects,and elucidate the mechanism of induced side effects is a necessary understanding of the phenomenon of adverse drug reaction.Enterohepatic circulation of drugs involves in two ways:one is based on the drug prototype for enterohepatic circulation;the other is phase Ⅱ metabolic pathway for enterohepatic circulation.In this paper,two kinds of enterohepatic circulation were reviewed.The toxic side effects of six kinds of drugs with enterohepatic circulation were introduced,and the possible mechanism were described and discussed,so as to have contributed to more rational use of drugs in clinical practice.Furthermore,it can promote the research and development of new drugs.
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OBJECTIVE:To investigate the prevention and treatment effect of Xiaochaihu decoction on irinotecan(CPT-11)-in-duced bloodystool in model mice with delayed diarrhea. METHODS:40 mice were randomly divided into normal control group (equal volume of normal saline),model control group(equal volume of normal saline),Xiaochaihu decoction group(1500 mg/kg, calculated by crude drug)and loperamide group(positive control,0.5333 mg/kg),ig,once a day,for 17 days. Except for normal control group,other groups were intraperitoneally injected CPT-11 to induce delayed diarrhea in 4th-10th day. Body mass changes, bloodystool rate of mice were determined,and pathological changes in large intestine and small intestine were observed. RE-SULTS:After 17 days of administration,compared with normal control group,the body mass in modeling groups was obviously declined (P<0.05),while body mass in Xiaochaihu decoction group was higher than model control group (P<0.05). In the 11th-17th day,bloodystool rate in Xiaochaihu decoction group and loperamide group were significantly lower than model control group(P<0.01),and bloodystool rate in Xiaochaihu decoction group was lower than loperamide group(P<0.05). Pathological re-sults showed,obvious diffuse necrosis and inflammatory cell infiltration were observed in mucosal epithelial cells of large intestine and small intestine in model control group,and the intestinal mucosal tissue in administration groups tended to be normal. CON-CLUSIONS:Xiaochaihu decoction can effectively reduce bloodystool rate,improve intestinal mucosa injury,and has prevention and treatment effect on CPT-11-induced bloodystool in mice,with superior effect to loperamide.
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AIM To establish an ultra-performance liquid-chromatography tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous content determination of five constituents in Jiangzhi Huoxue Tablets (Polygoni multiflori Radix,Astragali Radix,Chuanxiong Rhizoma,etc.).METHODS The 50% methanol extract of this drug was performed on a 40 ℃ thermostatic Restek UItra BiPh column (100 mm × 2.1 mm,5 μm),with the mobile phase comprising of acetonitrile (containing 0.1% formic acid)-0.1% formic acid flowing at 0.4 mL/min in a gradient elution manner.RESULTS Stilbene glycoside,tanshinone Ⅱ A,emodin,ferulic acid and puerarin showed good linear relationships within the ranges of 4.01-1 027,0.7-187,1.48-380,3.98-1 020 and4.285-1 097 ng/mL (r >0.994 0),whose average recoveries were 98.57%-101.0% with the RSDs (n =6) of less than 4.79%.CONCLUSION This specific and sensitive method can be used for the quality control of Jiangzhi Huoxue Tablets.
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Paris polyphylla, the dried rhizome of Paris polyphylla Smith Var.yunnanensis (Franch.) Hand-Mazz.or Paris polyphylla Smith Var.chinensis (Franch.) Hara, has been commonly used as a traditional Chinese folk medicine for thousands of years.The extensive pharmacological studies indicated that steroidal saponins had multiple pharmacological activities, such as potential anticancer activity, antibacterial, antivirus, hemostasis, sedative activity, protecting cardiovascular and liver tissues.Obviously, the studies on steroidal saponins activity are very important in the development and clinical application of the potential new drug.The recent research advances in the pharmacological activities of Paris polyphylla reported in the paper could provide reference for the further utilization of Paris polyphylla.
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Dioscin chemical compositions are the main effective components in clinical commonly used Chinese medicines such as Diaoxinxuekang capsules and Xinnaoshutong capsules etc , which show distinct curative effect on cardiovascular and cerebrovascular diseases.Meanwhile, they are the important raw materials for the synthesis of steroid hormone drugs .The studies on the extraction technology exhibit important significance in the exploration of pharmacological activities of the components , which also are the external requirements for the growing demand of steroid hormone drugs market .In this paper , the relatively mature extraction methods re-searched in recent years were summarized ,and the advantages and disadvantages of the different processes were discussed in order to provide reference for the further studies and application .
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Diphylleia sinensis is the dried rhizome of Diphylleia sinensis H.L.Li., which belongs to the subfamily of podophyl-lum ( berberidaceae ) , which is always recorded in monograph on materia medica in all ages as one of traditional Chinese medicine“Guijiu” herbal resources .Based on the previous researches in our laboratory and the literatures , the research progress in pharmacog-nosy, chemical constituent, endogeny fungus, quality control, pharmacology and the other aspects of Diphylleia sinensis were systemati-cally reviewed for the comprehensive utilization of its resources , and the development prospects of Diphylleia sinensis was also discussed in the paper , which can provide complete references and ideas for the rational utilization and development of Diphylleia sinensis.
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Objective To explore a clean and efficient new method for extraction of Diosgenin. Methods Yield of the total saponins was evaluated to determine the optimal enzymolysis temperature,pH,solid to liquid ratio,dosage of enzyme and enzymolysis time.Using diosgenin yield as an index,solid to liquid ratio,concentration of sulfuric acid and hydrolysis time were optimized in the saponins hydrolysis process via orthogonal experiment. Results The best conditions for the enzyme pretreatment were as follows:the temperature for enzymolysis was 70℃,pH 5.5,solid to liquid ratio was 1:4,dosage of enzyme was 8 mL?kg-1,and extraction time was 24 h.The best conditions of total saponins hydrolysis were as follows:the solid to liquid ratio was 1:4,concentration of sulfuric acid was 2.0 mol?L-1 ,and hydrolysis time was 5 h. Conclusion The new method is environmental friendly and highly efficient,and expected to be applied in industrial production.
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Objective To establish the fingerprint of Forsythia suspensa dispensing granule by HPLC. Methods The total of 10 samples of Forsythia suspensa were analyzed by HPLC on a Waters SunFire C18 column(4. 6 mm×250 mm,5 μm) with mobile phase of A:acetonitrile and mobile phase B:0. 4% acetic acid solution as gradient elution, with flow rate at 1. 0 mL·min-1 , wavelength at 277 nm and column temperature at 30 ℃. Results There were 13 characteristic common peaks in the Forsythia suspensa dispensing granule, in which two peaks identified as forsythoside A and forsythin, the similarities were more than 0. 999. Conclusion The HPLC fingerprint of Forsythia suspensa dispensing granule is stable, and is easy to manipulate, which can provide more information for the quality control of Forsythia suspensa dispensing granule.
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Dioscin is the main raw material for the synthesis of steroid hormone drugs. Currently, the direct acid hydrolysis is the mainly industrial production method for dioscin. However, the use of strong acid can not only destroy the structure of dioscin resulting in very low yield, but also produce a large amount of waste water and residues, which seriously pollute the environment. So the clean production of dioscin is the urgent demand of water conservation and environmental protection. In the paper, the recent research pro-gresses in the clean production technology and process of dioscin were summarized, and the advantages and problems were discussed in order to provide reference for the improvement and application of the new technology and process.
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Objective:To optimize the conditions of semi-bionic extraction for Jinyin Qingre oral liquids. Methods:The best con-ditions of the semi-bionic extraction for Jinyin Qingre oral liquids was optimized by uniform design with the yield of chlorogenic acid, geniposide and total phenolic acid, and the dried extract weight as the indices in a comprehensive evaluation. Results:The optimal pH of water for the three-time decoction was 2. 89, 6. 50 and 8. 43, respectively, and the total extraction time was 2. 0 h. Conclusion:Combined with the actual production, the pH value of water is 3. 0, 6. 5 and 8. 5 with the decoction time of 1. 0, 0. 5 and 0. 5h, re-spectively.
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Objective: To optimize the alcohol concentration for Jinyin Qingre oral liquids extracted by semi-bionic extraction (SBE). Methods:Using proportional division method to set up 5 alcohol concentration 30%,55%,61. 25%,67. 5%,80% for the ex-periment . The dried extract yield and the contents of chlorogenic acid ,geniposide,salviandic acid B and total phenolic acid were set up as indexes which were standardized as the comprehensive evaluation value ( Y) ,using the weighting coefficient had been set. Choosing the appropriate concentration by comparing the value of Y. Results:The order of comprehensive evaluation value was as follows:30%>61. 25% >55% >80% >67. 5%. Conclusion:Combining the clarity of the oral liquids, the best alcohol concentration in SBE for Jinyin Qingre oral liquids is 61. 25%.
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Radix bupleuri is mainly used to treat cold fever and liver disease, and the curative effect is remarkable. The prepara-tions previously explored including bupleurum injection, tablets and capsules all show their own characters and different applicable peo-ple. Recently, many researchers carried out extensive research on its dosage forms. The early formulations have been improved as well, and successively developed dropping pill, nasal sprays, transdermal patches and the other new dosage forms. In the paper, the recent research progress in bupieurum preparations were summarized in order to provide reference for the improvement and application.
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Objective:To compare the taxol content in different parts of Taxus madia and Taxus chinensis var. mairei to provide reference for the future researches. Methods:The active ingredients were extracted by a mixed solvent (50% acetone and 50% ethyl acetate) , the target compound taxol was separated by a neutral Al2 O3 solid phase column, and then the taxol content was analyzed and compared among the different parts of Taxus madia and Taxus chinensis var. mairei by HPLC. Results:Taxol in velamen of Taxus ma-dia had the highest content among all the samples, which was 0. 0439% and 88 times as high as that in the bark of Taxus chinensis var. mairei. Conclusion:Among all the samples of Taxus madia and Taxus chinensis var. mairei, velamen of Taxus madia has the highest taxol content.
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Phillyrin is an important lignans compound from Forsythia. It is not only found in the raw medicinal material with high content, but also shows a variety of pharmacological activities. In the paper, the recent advances in extraction methods, pharmacology-toxicology, pharmacokinetics and the other studies of phillyrin were reviewed in order to provide reference and suggestions for the fur-ther research.
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Objective: To optimize the conditions of semi-bionic extraction for Kanggan Liyan syrups. Methods: The samples were extracted by water with different pH values under the same conditions of formula composition and dosage, extraction temperature, filtration method, water voulme, centrifugal time and concentration multiple. The best conditions of the semi-bionic extraction for Kang-gan Liyan syrups were screened by uniform design with the content of forsythoside A, polydatin, baicalin and emodin and the dried ex-tract weight as the indices. Results:The best technical conditions were as follows:the pH value of water for the 1st, 2nd and 3rd de-coction was 4. 9, 7. 5 and 9. 0, respectively, and the total extraction time was 2h. Conclusion:According to the industrial production conditions, the pH value of water for the 1st, 2nd and 3rd decoction is 5. 0, 7. 5 and 9. 0 with the extraction time of 1h,0. 5h and 0. 5h, respectively.
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Objective: To optimize the extraction conditions of semi-bionic extraction for Gardenia jasminoides Ellis. Methods:The best extraction conditions of the semi-bionic extraction for Gardenia jasminoides Ellis was screened by uniform design with yield of geniposide, total iridoid glycosides and dry extract as the indices. Results:The optimal conditions were as follows:the pH value of wa-ter for the lst, 2nd and 3rd decoction was 2. 0, 6. 5 and 9. 0, respectively, and the extraction time was 2. 0, 1. 0 and 1. 0h according-ly. Conclusion:The optimized extraction conditions by uniform design is scientific and reasonable.
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Objective:To establish a method for the determination of tanshinoneⅡA and salvianolic acid B in Zhiyou capsules by HPLC. Methods:The chromatographic column was Waters Atlantis@T3(150 mm × 4. 6 mm,3 μm)using acetonitrile and aqueous ammonium acetate solution(adjusting pH to 2. 4 with formic acid)as the mobile phase with gradient elution,the flow rate was 1. 0 ml ·min-1 and the detection wavelength was 260 nm. Results:The contents of salvianolic acid B and tanshinoneⅡA showed good linear relationship within the range of 1. 20-60. 00μg·ml-1(r=0. 999 7)and 0. 40-20. 00 μg·ml-1(r=0. 999 8),respectively. The av-erage recovery was 101. 53%(RSD=1. 14%)and 95. 17%(RSD=4. 33%),respectively. Conclusion:The method is efficient,con-venient and accurate,which can be used in the quality control of Zhiyou capsules.
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Objective:To compare the content of total saponins in Paridis Rhizome from Wudang mountain area to explore the cor-relation between the quality of medicinal materials and the production areas and species. Methods: The content of total saponins in Paridis Rhizome was determined by an ultraviolet-visible spectrophotometer at 406nm with perchloric acid as the chromogenic reagent. Results:The saponins content in Paridis Rhizome from Wudang mountain area had obvious differences:the minimum was 1. 29%, and the maximum was up to 10. 22%. The content of total saponins had no obvious correlation with species, production area and altitude. Conclusion:The quality of Paridis Rhizome is unstable in Wudang mountain area, and that will affect the effectiveness and safety of the clinical medication. Only by promoting the standardized planting of Chinese medicine materials, the stable quality of Paridis Rhizo-me can be ensured.
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Objective:To investigate the distribution of four polyphyllins in different parts of paris polyphylla by means of compa-ring the contents of relative constituents in paridis rhizome and fibril to provide reference for comprehensive exploitation and utilization of paris polyphylla. Methods:Paris polyphylla samples were collected from Wudang mountain area and Shennongjia forest area. The contents of main secondary metabolites including polyphillinⅠ,Ⅱ,Ⅵ andⅦin paridis rhizome and fibril were evaluated by HPLC. Results:The four polyphyllins contents had obvious differences in different parts of polyphylla. The total content of four polyphillins in fibril was significantly higher than that in rhizome. Diosgenin compositions had no significant difference in the two parts, and the con-tents of pennogenin compositions in fibril showed significantly higher than those in rhizome. Conclusion:As for the main chemical com-positions contained in polyphylla, there is chemistry equality between fibril and rhizome, thus both of them can be used for medicine. However, as for the contents of four steroidal saponins, the distribution of secondary metabolites has obvious difference between fibril and rhizome, and the result may be caused by steroidal saponins transferred to rhizome for storage after the synthesis in fibril.
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Objective:To optimize semi-bionic extraction(SBE)of Forsythia suspensa. Methods: The best conditions of semi-bionic extraction of Forsythia suspense were screened by uniform design with the total content of forsythoside A,and forsythin and dried extract weight as the indices. Results:The results of the uniform design were analyzed by DPS data, and combined with the industrial production conditions, the optimal extraction technology was as follows:the pH value of water in the three-time extraction was 2. 0,7. 0 and 10. 0 with the extraction time of 1. 0h,0. 5h and 0. 5h, respectively. Conclusion: The technology provides a theoretical basis for the extraction optimization of Forsythia suspensa.