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2008 Vol. 26, No. 3

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2008, (3): 161-162,205.
Abstract(1893) PDF (431KB)(1813)
Abstract:
2008, (3): 163-165.
Abstract(2158) PDF (424KB)(1939)
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Studies on chemical constituents of Incarvillea mairei var.granditlora(Wehrhahn) Grierson
SU Yong-qing, SHEN Yun-heng, ZHANG Wei-dong
2008, (3): 166-168,171.
Abstract(2343) PDF (551KB)(542)
Abstract:
Objective: To study the chemical constituents of Incarvillea mairei var.granditlora(Wehrhahn) Grierson. Methods: Isolation and purification were carried out by macroporous absorption resin and silica gel column chromatography,and twelve compounds were identified by spectral and chemical methods. Results: Twelve compounds were obtained from alcohol extract and were determined as o-hydroxy benzoic acid,palmitic acid,hexacosanoic acid,β-sitosterol,daucosterol,oleanolic acid,ursolic acid,quercetin,vincetoxicoside B,p-hdroxy benzoic acid、3-mthoxy 4-hydroxy-benzoic acid,sgmasterol. Conclusion: All of 12 compounds were obtained from the plant for the first time.
2008, (3): 169-171.
Abstract(2533) PDF (555KB)(1266)
Abstract:
2008, (3): 172-174,207.
Abstract(1646) PDF (219KB)(584)
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Synthesis and the antiplatelet aggregative activity of 4,5-dihydro-3(2 H)-pyridazinones
XU Yong, HUANG Xiao-jin, XU Jian-ming, CAI Ling-zhi, SONG Yan, ZHAO Qing-jie, Wu Qiu-ye
2008, (3): 175-177,190.
Abstract:
Objective: To study the antiplatelet aggregative activity of 6-(4-substituted acetamido-phenyl)-4,5-dihydro-3(2H)-pyridazinones inletting different piperazine groups. Methods: Ten target compounds were designed and synthesized.All of them were confirmed by 1H-NMR spectra.Born method was applied for preliminary pharmacological test in vitro. Results: All of the target compounds were reported.The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent.Compound(1)/(4)and performed better than MCI-154 in vitro. Conclusion: The carbochain’s length of piperazine’s 4-substituted groups impacted the antiplatelet aggregative activity promintly.
3 D-QSAR Study of a Series of 6-[4-Substituted-piperazinyl) phenyl]-4,5-Dihydro-3(2H)-Pyridazinones
ZHANG Jun, SUN Qing-yan, XU Jian-ming, XUE Yun-yun, ZENG Juan, HUANG Xiao-jin, WU Qiu-ye
2008, (3): 178-181.
Abstract(2094) PDF (432KB)(606)
Abstract:
Three dimensional structure-activity relationship(3D-QSAR) has been studied on a series of 6-[4-Substituted-piperazinyl) phenyl]-4,5-Dihydro-3(2H)-Pyridazinones by using.Using comparative molecular field analysis(CoMFA).The resulting CoMFA model had a cross validated coeffiecient q2 of 0.663 respectively,which showed a strong predictive ability.The 3D contour maps of CoMFA provided a smooth and interpretable explanation of the structure-antiplatelet aggregation activity relationship for the compounds.The analysis of the 3D contour plots permitted interesting conclusions about the effects of different substituent groups at the position of the N atom on the terminal of piperazidine group on the antiplatelet aggregation activity,which will guide the design of novel antiplatelet aggregation compounds with relatively high activity.
Preparation technology and in-vitro release characteristics of metronidazole-loaded carboxymethyl chitosan sustained-release microspheres
KANG Xian-wu, WANG Qiang, WANG Yi, GU Qi-sheng, JIANG Li-xia
2008, (3): 182-184.
Abstract(2356) PDF (604KB)(739)
Abstract:
Objective: To study the optimum technology for preparing metronidazole-loaded carboxymethyl chitosan(MZ-CMC) microspheres by emulsification and cross-linking process and to investigate the in-vitro release characteristics of MZ-CMC microspheres. Methods: An orthogonal test,based on 4 factors including CMC concentration,MZ/CMC(W/W),glutaradehyde/CMC(W/W) and agitation speed,was employed to determine the optimum preparetion technology of microspheres.The in vitro release behavior was recorded and evaluated. Results: For this 4 factors,the degree of influence on the quality of microspheres were gradually lower in the sequence of "agitation speed","MZ/CMC(W/W)","glutaradehyde/CMC(W/W)",and "CMC concentration".Prepared with optimized method in this test,the proportion of microspheres with diameter from 50-200 μm was 48.86%.The drug content was 48.19%,and the enveloping rate was 37.46%.The in virto release time was from 6-8 h in 3 types of buffer solution of pH1.2,6.8 and 7.6. Conclusion: The preparing technology for MZ-CMC microspheres used in this test is dependable,and the in vitro release of MZ from the microspheres is sustained.
Antidepressant activity of Centalla Asiatic Triterpenic acid and its main constituents
CAO Wei-wei, LU bo
2008, (3): 185-187.
Abstract(2634) PDF (451KB)(579)
Abstract:
Objective: To investigate the antidepressant activity of Centalla asiatic triterpenic acid(CATA),and its main comstituerts asiatic acid(AA) and madecassic acid(MA). Methods: The forced swimming test(FST),tail suspension test(TST),open field activity(OFA) test and reserpine-induced ptosis test were carried out to examine the antidepressant activity in mice.Mice immobility duration in FST and TST,spontaneous activity frequency in OFA,and ptosis in reserpine antagonistic test were observed. Results: CATA,AA and MA could significantly shorten mice immobility time in FST at the dosages of 60 and 120 mg/kg and could markedly shorten mice immobility time in TST at the dosages of 30,60 and 120 mg/kg.They could not reduce mice spontaneous activity in OFA.CATA,AA and MA could reduce ptosis mice in reserpine antagonistic test. Conclusion: CATA,AA and MA exert an antidepressant activity in animal models.
Protective effect of total glycosides of Xihuang for injection on chronic hepatic injury induced by carbon tetrachlorid in rats
QIU Yan, CHEN Min, MAO Yu-guo, LIU Jing
2008, (3): 188-190.
Abstract(1772) PDF (195KB)(530)
Abstract:
Objective: To investigate the preventive effect of total glycosides of Xihuang for injection on carbon tetrachlorid-induced chronic hepatic injury in rats. Methods: Chronic carbon tetrachlorid-induced hepatic injury model was prepared in rats by hypodermic injection of 25% carbon tetrachlorid in peanut oil twice a week for 3 weeks.The total glycosides of Xihuang was given intravenously at the doses of 3、6、12 mg/kg compared with the model of Yinzhihuang injection 3 days before-making,once a day,3 weeks in total.One hour after the last dose,blood serum was separated to be determined the activities of ALT,AST,TP and ALB.Then the rats were killed to observe the pathologic changes of their liver tissue. Results: Compared with the model group,total glycosides of Xihuang could decrease the activities of serum AST and ALT and increase serum TP and ALB(P<0.01 or P<0.001). Conclusion: Total glycosides of Xihuang for injection could protect liver and decrease the effects of enzyme and has a preventive effect on chronic hepatic injury.
Quality control for compound cordycepic polysaccharide buccal tablets
Su Ying, Song Yan, Huang Lei, Zou Hao, Zhou Xuan-wei
2008, (3): 191-193,221.
Abstract(2243) PDF (297KB)(793)
Abstract:
Objective: To establish a quality control method for compound cordycepic polysaccharide buccal tablets(cordycepic polysaccharide,extract of Grosvenor momordica fruit,Panax quinquefolium extract,and tea polyphenols). Methods: The extract of Grosvenor momordica and Panax quinquefolium L.were identified by TLC.Tea polyphenols was identified according to the principle of display reaction between tea catechins and vanillin.Cordycepic polysaccharide was determined by spectrophotometry method. Results: The methodological study showed that the calibration curve of polysaccharide was linear in the concentration range(r=0.996 4).The average recovery was 97.13% with the RSD of 1.41%(n=5). Conclusion: The method is simplea,ccurate,repeatilde with and high precision.This method can be used for quality control for compound cordycepic polysaccharide buccal tablets.
Determination of dichlorovos residue in rice by microwave-assisted extraction/HPLC
WANG Tao, CHAI Yi-feng, FAN Guo-rong, MI He-ming
2008, (3): 194-196.
Abstract(1862) PDF (495KB)(477)
Abstract:
Objective: To develop a method of microwave-assisted extraction(MAE)followed by HPLC for the determination of the residue of dichlorovos in rice. Methods: Pesticide residues were extracted from rice samples with a solvent mixture.Extracts were cleaned up with a column filled with Florisil and neutral aluminum oxide.Nova-Pak C18 column(4 μm,3.9×150 mm)was used with acetonitrile:water(3070,V/V)solution as mobile phase,and the flow speed was 1.0mL/min.The ultraviolet detection wavelength was 200nm. Results: Good linear correlation for dichlorovos was found in the concentration range of 2.00-25.00 μg/mL.The detection limit was 0.5 μg/mL for dichlorovos(S/N=3).The average recovery rate of rice hull and brown rice were 81.1%(RSD3.9%) and 78.9%(RSD4.0%),respectively. Conclusion: This method is simple and rapid.It can be used for the determination of dichlorovos residue in rice with satisfactory results.
Effects and mechanism of Acanthopanax senticosus saponins on myocardial ischemia and reperfusion in rats
YU Da-hai
2008, (3): 197-199,232.
Abstract(2261) PDF (218KB)(288)
Abstract:
Objective: To observe the protective effect of acanthopanax senticosus saponins(ASS) on myocardial ischemia-reperfusion in rats and to find a possible mechanism. Methods: An in vitro myocardial injury model was made by 30 min of ischemia followed by 30 min of reperfusion in the isolated rat heart from anesthetized rat.The change of heart function and coronary flow in normal and reperfusion conditions were observed. Results: ASS can improve the heart function at the dose of 20 mg/L;and at the dose of 10 mg/L and 20 mg/L ASS it can increase the coronary flow in normal and reperfusion conditions at dose-dependent ways;The effects can be cancelled by nitric oxide syntheses inhibitor. Conclusion: ASS has a weak influence on the normal heart function in vitro rats heart,but significantly improve the heart function after myocardial ischemia and reperfusion in rats.This mechanism may be related to the improvement in the myocardial ischemia and the coronary artery through increasing the nitric oxide.
Preparation of Puerarin by microemulsion drug delivery system
Chen Han, Zhong Yan-qiang, Lu Ying
2008, (3): 200-203.
Abstract(2407) PDF (622KB)(602)
Abstract:
Objective: To develop a microemulsion drug delivery system of Puerarin(PUE-ME). Methods: Formulation of PUE-ME was screened by solubility experiments,compatibility tests and pseudo-ternary phase diagrams,with the consequence of visual examination as parameter. Results: The maximum drug corporation was 77.11 mg/mL.The formulation was composed of IPM(10%),brij-96V(37.5%),ethanol(37.5%),and water(25%). Conclusion: The formulation of PUE-ME preparation could meet the general requirements of the design.
Preparation and quality control of compound ornidazole liniment
XING Qing-de, ZHANG Zhi-wu, LI Hong-bing, LI Guo-zhu
2008, (3): 203-205.
Abstract(2403) PDF (202KB)(337)
Abstract:
Objective: To study the preparotion and quality control of compound ornidazole liniment. Methods: Prepared compound liniments with ornidazole and boric acid as principle agents.The contents of these two qroups were measured respectively.by UV spectrophotometry adn neutralization method.Then the stability of it was examined. Results: The average recoveries of ornidazole and boric were 99.98% and 100.29% with the RSD of 0.49%,0.97%. Conclusion: The compound ornidazole liniment formula was reasonable;the quality control method was viable;the outcoming liniment was stable,and in line with the 2005 version of Chinese Pharmacopoeia.It could meet the clinical requirment.
Extracting and inclusion process of essential oil in Orange peels and Radix auckladiae
Jin Lie
2008, (3): 206-207.
Abstract(2267) PDF (133KB)(388)
Abstract:
Objective: To Search for best extracting and inclusion process in Orange peels and Radix auckladiae. Methods: The contents of essential oil extracted by steam distillation in orange peels and radix auckladiae were observed.The optimal conditions of the saturated aqueous solution method to bundle the essential oil were selected by orthogonal experiment design. Results: The best extracting process was by using 10 times water to immersion for 30 min,then extracted for 5 h.The best inclusion process was essential oil:β-CDas110,and the temperature was 60 ℃ for 3 h. Conclusion: The extracting process can extract essential oil sufficiently.The inclusion process has high inclusion rate,and it was stable and easy to operate.
Effect on dissolution of baicalin and chlorogenic acid in Compound Herba Houttuyniae in different combinations
LIU Bin-guo, YANG Ben-ming, LU Li-jun, MI He-ming
2008, (3): 208-210.
Abstract(2298) PDF (608KB)(674)
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Objective: To investigate the dissolution of baicalin and chlorogenic acid in decoctions of Composition Herba Houttuyniae and simple recipe. Methods: The contents of baicalin and chlorogenic acid were determined in decoctions of Composition Herba Houttuyniae and simple recipe by HPLC. Results: The decoctions of composition Herba Houttuyniae were compared with simple recipe: the content of baicalin in the former decreased 100%,and the chlorogenic acid decreased 25.4%. Conclusion: Different combinations of complex prescription of Chinese herbal medicine in the form have great influence on the dissolution of chemical component content.
Dissolution of naproxen sodium tablets and evaluation of in vitro-in vivo correlation about this drug
LE Jian, LIU Qian, SHI Jin-min, CHEN Gui-liang
2008, (3): 211-213.
Abstract(2133) PDF (605KB)(943)
Abstract:
Objective: To study the dissolution of naproxen sodium tablets and evaluate in vitro / in vivo correlation. Methods: Dissolution test method in naproxen sodium tablets adopted by USP was used for determination of dissolution in vitro.The concentrations of naproxen sodium tablets in human plasma were determined by HPLC. Results: The linear equation based on the dissolution rate(X) and absorption percentage(F) was F=0.330 3X+0.699 8 and the correlation coefficient was 0.991 5. Conclusion: To a certain extent,the in vitro dissolution test in USP could reflect the in vivo absorption.
Chiral separation of five triazole antifungals by capillary zone electrophoresis
HOU Ying, JI Song-gang, ZHAO Liang, SUN Qing-yan, CHAI Yi-feng
2008, (3): 214-217.
Abstract(1837) PDF (492KB)(474)
Abstract:
Objective: To investigate the factors that influence the chiral separation of triazole antifungals by capillary zone electrophoresis using β-cyclodextrin derivatives as chiral selector. Methods: Analyse were carried out on a P/ACE 5000 capillary electrophoresis system(Beckman,USA) with a UV detector,using an uncoated fused-silica capillary 50 μm × 47 cm with an effective length of 40 cm.Samples were injected into the capillary by 50 mbar pressure for 3 s.The detective wavelength was set at 200 nm.Three β-cyclodextrin derivatives were used as chiral selectors. Results: Satisfactory separation of the five triazole antifungals were achieved when using carboxymethylated-β-cyclodextrin(CM-β-CD) while the sulfobutyl-ether-β-cyclodextrin(SBE-β-CD) and difluoro-carboxymethylated-β-cyclodextrin showed no chiral separation ability to the five triazole antifungals.When using CM-β-CD,the enantiomeric separation of the five compounds and the best results were obtained in 30 mmol/L NaH2PO4 buffer(adjust to pH 2.2 with H3PO4)containing 5 mmol/L CM-β-CD.The voltage was 20 KV and the temperature was 20 ℃.The five triazole compounds were well separated on this condition. Conclusion: The type of β-CD and the pH of buffer is the major factor influencing the separation of the five triazole antifungals.
Determination of salicylic acid and tetracation hydrochloride in Compound onychomycosis cream by HPLC
GU Wei-feng, PIAO Shu-juan, ZHANG Chun
2008, (3): 217-219.
Abstract(1985) PDF (208KB)(1038)
Abstract:
Objective: To establish a HPLC method for the determination of salicylic acid and tetracation hydrochloride in compound onychomycosis cream. Methods: Agilent-C18(4.6 mm×150 mm,5 μm) column was used with a mobile phase of methanol-water-phosphoric(50500.04) and a flow rate of l.0 mL/min,at the detection wavelength of 313 nm. Results: This method showed good linear relation(r= 0.999 9) in the range of 82.00~410.00 μg/mL for salicylic acid,and 5.00~25.00 μg/mL for tetracation hydrochloride.The average recoveries were 99.80% and 99.75%,with the relative standard deviation of 1.68% and 1.36%,respectively. Conclusion: The method is simple,quick,accurate and suitable for the quality control of compound onychomycosis cream.
2008, (3): 220-221.
Abstract(1905) PDF (114KB)(403)
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The inspirations of American and Japanese pharmaceutical chemistry major postgraduates’ basic education
ZHANG Da-zhi
2008, (3): 222-223,225.
Abstract(1968) PDF (643KB)(457)
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A series of ways and means in graduate education in American and Japan are introduced.The graduate training program in these two countries is a strict and professional training process which is full of modern education theory and rich in academic atmosphere.Their ways are worth learning and practicing in China.
2008, (3): 224-225.
Abstract(1669) PDF (399KB)(276)
Abstract:
2008, (3): 226-227.
Abstract(1993) PDF (306KB)(407)
Abstract:
2008, (3): 228-230.
Abstract(1865) PDF (109KB)(358)
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A Study on the Work Values of Pharmaceutical Students
LEI Ting, LI Fang-Fei
2008, (3): 230-232.
Abstract(2364) PDF (355KB)(609)
Abstract:
Objective: Understanding the work values Orientation and characteristics of pharmaceutical students. Methods: Investigating on the 4th grade pharmaceutical students of Fudan University using the revised Super’s work values inventory and analyzing the data. Results: Influenced by the social culture,pharmaceutical students’ work value has no obvious characteristics. Conclusion: Conclusions: To serve the development of pharmaceutical industry and the whole society,good work values should be promoted in pharmacy education.
2008, (3): 233-235,240.
Abstract(1633) PDF (853KB)(332)
Abstract:
2008, (3): 236-239.
Abstract(1654) PDF (393KB)(499)
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