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2010 Vol. 28, No. 5

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2010, 28(5): 321-324.
Abstract(2309) PDF (530KB)(645)
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2010, 28(5): 325-327,338.
Abstract(2260) PDF (230KB)(1472)
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2010, 28(5): 328-330.
Abstract(2560) PDF (173KB)(1577)
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Study on pharmacokinetics of compound Danshen dropping pills of new matrix
Wang Wei, Wang Xiao-hua, Zhang Xiao-jie, Chen Jian-ming
2010, 28(5): 331-333.
Abstract(2431) PDF (204KB)(618)
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Objective To study the pharmacokinetics of compound Danshen dropping pills of new matrix. Methods HPLC was used as a detection method.New Zealand rabbits were taken as experimental animals.The compound Danshen dropping pills sold in market were taken as comparison products. Results There was a significant difference of Cmax and Ka between two kinds of pills(P<0.05).There was no significant different of tpeak、AUC、t1/2β,MRT and VRT.The relative bioavailability of compound Danshen dropping pills of new matrix was 114.5%. Conclusion The absorption rate constant and Cpeak of compound Danshen dropping pills of new matrix were much higher than the pills sold on the market.New matrix could improve the performance of quick Results and high efficiency of the dropping pills.The peak-time,the time of maintaining effective concentration and the elimination of drugs were same as old ones on the whole.
Determination and structural elucidation of sesquiterpene lactones from Inula racemosa
HUO Yan, SHI Hai-ming, LI Wei-wei, GUO Cheng, LI Xiao-bo
2010, 28(5): 334-338.
Abstract(2256) PDF (390KB)(669)
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Objective To establish a method of HPLC for the simultaneous quantification of three sesquiterpene lactones in Inula racemosa. Methods Agilent Zorbax XDB-C18 column(250 mm×4.6 mm,5 μm) was uesed with a mobile phase consists of 55% acetonitrile and 45% water,at a flow rate of 1.0 ml/min,and detection wavelength of 210 nm. Results Three sesquiterpene lactones in Inula racemosa Hook.f.,namely igalane(1),isoalantolactone(2) and alantolactone(3) has good linear relation in 17.40~1 740.00,21.20~2 120.00,20.40~2 040.00 μg/ml with the lowest detection limit of 0.087,0.042,0.041 μg/ml respectively.The RSD of repeatability and stability were all less than 2.85%.The average recovery rate of there constituents were all less than 104.43% with RSD less than<1.20%. Conclusion The method was rapid,accurate,reliable and could be suitable as a quality control method for I.racemosa.Two minor isomers from I.racemosa were isolated by semi-preparative HPLC which structures were elucidated on the basis of NMR analysis.
Development of nimodipine solid dispersion
YANG Ling, ZHONG Yan-qiang
2010, 28(5): 339-341,344.
Abstract(2585) PDF (328KB)(1060)
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Objective To prepare Nimodipine solid dispersion and increase its dissolution rate.Methonds Using polyvinylpyrrolidone(PVP) as a carrier,nimodipine solid dispersion was prepared by spray-drying method.differential scanning calorimetry and X-Ray powder Diffractometer were used to investigate the status of nimodipine in carriers,and dissolution characteristics were studied in vitro. Results Nimodipine was in the form of molecular in its carrier.The solubility of solid dispersion was significantly increased comparing with that of the pure drug or physical mixtures.Dissolution Results showed that higher carrier-Nimodipine ratio led to faster drug dissolution,t50 of solid dispersions(NimodipinePVP=1:3) is only 0.972 6 min. Conclusion Polyvinylpyrrolidone(PVP) as a carrier of Nimodipine solid dispersion has a high load ability;spray-drying method has good reproducibility;dispersoid particles need not to be smashed and can satisfy request for each kind of solid dosage form.Spray drying technique is a ideal method for the preparation of nimodipine solid dispersion.
Determination of seven baleful trace elements in nine Chinese patent medicine treating diabetes mellitus
BAO Li-li, YU Kun, XUE Da-fang, LI Hong, TENG Wen-feng
2010, 28(5): 342-344.
Abstract(2021) PDF (176KB)(453)
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Objective To determine Pb,Cd,Hg,As,U,Th,Tl in nine clinical commonly used Chinese traditional medicine treating diabetes mellitus,which provide reference data for modern medication.Methonds The samples were treated by microwave digestion,and determined by ICP-MS. Results The Results showed that the contents of seven elements Pb,Cd,Hg,As,U,Th,Tl in these samples were detected,in which Pb,Cd,Hg,As were all accord with the Import Standards Draft of Green Plants for medical use and Southeast Asia Import Standards for Chinese Patent Medicine,but still had gap with Recommending Standard Graft of Traditional Medicine Quality Standards and Import Chinese Traditional Medicine Standards of France.Compared three radioactive elements such as U,Th,Tl,which showed that Th had the largest scope of content,and mean comparative Results is Th>U>Tl. Conclusion Some problems still exist when making contrast between content of harmful elements with that in food and medical standards.The contents of U,Th,Tl in samples were low,and hadn't poison effect on human.Much importance should be attached on the quality control of baleful trace elements in the production of Chinese Patent Medicines.
Synthesis of N-tert-butoxycarbonyl-DL-(±)-homo-tyrosine
LIU Hong-ming, QIN Ye, YAO Jian-zhong, SHENG Chun-quan, MIAO Zhen-yuan, ZHANG Wan-nian
2010, 28(5): 345-347,384.
Abstract(2151) PDF (288KB)(917)
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Objective To prepare N-tert-butoxycarbonyl-DL-(±)-homo-tyrosine(1),a key unusual amino acid and pharmaceutical intermediate for the total synthesis of novel peptides drug including cyclic or straight chain peptide. Methods Starting from L-aspartic acid(2),the target compound 1 was synthesized via 6 steps including N-methoxycarbonylation,intramolecular dehydration and anhydridation,Friedel-Crafts reaction with 2-chloroanisole,catalytic hydrogenation with 10% Pd-C,N-demethoxycarbonylation and demethylation with 48% HBr-HOAc followed by N-Butoxycarbonylation. Results Target compound 1 had been successfully synthesized in an overall yield of 49.7%.The structure of the target compound was confirmed by ESI-MS,1H NMR and 1C NMR. Conclusion The process developed has several advantages such as cheap materials,convenient workup and high yield.
Effects of Protoveratrine A on cardiovascular and respiratory system in rats
ZHAO Yu, JIANG Hua, XI Gui-lin, LI Hui-linag, YUAN Bo-jun, LU Guo-cai, ZHANG Wei-dong
2010, 28(5): 348-351.
Abstract(2548) PDF (215KB)(506)
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Objective To observe the effects of Protoveratrine A(PA) on cardiovascular and respiratory system in rats. Methods The experimental rats(n=40,mf=1:1) were equally randomized into 4 groups: blank control group and groups of low dose(ig,0.25 mg/kg,single dose of PA),medium dose(ig,0.50 mg/kg,single dose of PA) and high dose(ig,1.00 mg/kg,single dose of PA).Carotid artery cannulation was established following anaesthesia in the rats and the effects of PA on the blood pressure,ECG,respiratory rate and width of rats were measured. Results The systolic blood pressure,diastolic blood pressure,mean arterial pressure,heart rate and respiratory rate of rats were decreased,the corrected QT(QTc) interval was prolonged and the respiratory width was increased in rats.The dose-effect relationships were observed for all the changes.However,these parameters returned to normal within 150 min. Conclusion PA has some effects on cardiovascular and respiratory systems in rats in reducing the blood pressure and heart rate,prolonging the QTc interval,decreasing the respiratory rate and increasing the respiratory width.
2010, 28(5): 351-351.
Abstract(2212) PDF (108KB)(292)
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Hepatoprotective effect of Shugananlening extract against acute hepatic injury in mice
XIA Ai-jun, ZHANG Qi, LIANG Yuan
2010, 28(5): 352-353,380.
Abstract(2552) PDF (177KB)(890)
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Objective To study the hepatoprotective effect of shugananlening extract against mice liver damage which induced by carbon tetrachloride(CCl4). Methods Acute chemical liver jnjury model was induced by CCl4 in mice.The activities of ALT,AST in serum and the content of MDA,GSH,GSH-Px in liver were measured. Results Different dose of shugananlening extract significantly increased the content of GSH,GSH-Px in liver(P<0.01),decreased the activities of ALT,AST in serum and content of MDA in liver(P<0.05). Conclusion Shugananlening extract has a good protective effect on acute chemical liver injury in mice,which possibly due to the antioxidative capability of strengthening GSH system.
Comparative study on promoting blood circulation to remove blood stasis function of different processed rhubarb products
ZHU Shi-ta, LI Xin-zhong, WEN Xiao-li, LEI Peng
2010, 28(5): 354-355,358.
Abstract(2931) PDF (181KB)(575)
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Objective To select four processed rhubarb products(i.e.,crude rhubarb,prepared rhubarb,rhubarb charcoal and rhubard stir-fried with wine) and to compare their function on promoting blood circulation to remove blood stasis. Methods The different function on promoting blood circulation to remove blood stasis was observed using rat mode of blood stasis due to stagnation. Results Greatest function on promoting blood circulation to remove blood stasis in rats was found in rhubard stir-fried with wine,followed by prepared rhubarb,and crude rhubarb has a little function.However,rhubarb charcoal did not show the function. Conclusion Rhubard stir-fried with wine can be used for promoting blood circulation to remove blood stasis.
The clinical observation of the analgesia effect and safety of Fentanyl Transdermal System for day surgery patients with anus surgeries
LU Xiao-fang, LI Qiong-zhen, ZHU Tao
2010, 28(5): 356-358.
Abstract(2302) PDF (182KB)(605)
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Objective To observe the analgesia effect and safety of Fentanyl Transdermal System and tramadol for day surgery patients with anus surgeries. Methods 120 cases of anus surgeries undergo spinal anesthesia were randomly divided into three groups.Patients of group A had Fentanyl Transdermal System affixed on for analgesia.Patients of group B were received an oral dose of 100 mg tramadol in 3 h after operation.Patients of group C had no analgesia.The analgesia effects of three groups were estimated with VAS score after operation in different time points.The sedation effects of three groups were estimated with Ramsay score after operation in different time points,while observing the occurrence of adverse reactions. Results The analgesia effect of group A and group B were superior to group C at 4,24,48 h after operation.But the analgesia effect of group A was superior to group B and group C at 24,48 h after operation.The sedation effect of group A was superior to group B and group C at 24,48 h after operation.And the sedation effect of group B was superior to group C at 24 h after operation.Only dizziness and drowsiness was higher significantly between group A and group C in the the incidence of adverse reactions.Methods The Fentanyl Transdermal System was a safe,simple and better effect medicament for ease the pain undergo the anus surgeries of day-case.
2010, 28(5): 359-360.
Abstract(1950) PDF (128KB)(385)
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Chemical stability of cyclophosphamide in glass bottle and PVC infusion bags
WANG Yan-qiong, ZHANG Shun-guo, Xu Tiao, CHEN Ming-lin, GUO Xiao-wen
2010, 28(5): 361-362.
Abstract(2348) PDF (134KB)(401)
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Objective To investigate chemical stability of cyclophosphamid in glass bottles and PVC infusion bags. Methods Cyclophosphamide was dissolved with 0.9% sodium chloride respectively in glass bottles and PVC bags.The storage condition for the solutions was room temperature.Solutions were sampled at 0,1,2,4,6,8,12 and 24 h,and the appearance and traits were observed.Cyclophosphamide concentrations were determined by HPLC. Results No obvious changes were founded in cyclophosphamide under different conditions.Two solutions were stable before 12h.The statistic Results had no significant difference(P>0.05). Conclusion Cyclophosphamide is stable in glass bottles and PVC bags in 0.9% sodium chloride injection.
The pharmacokinetics study of tinidazole pectin matrics colon-specific sustained-release tablets in dogs
LIU Fu-qiang, WANG Yan-ping, ZHAO Nan, WANG Xiang-yang, CUI Hai-zhen
2010, 28(5): 363-365,368.
Abstract(2493) PDF (328KB)(344)
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Objective To develop a method to study the pharmacokinetics of tinidazole pectin matrics colon-specific sustained-release tablets in dogs. Methods The plasma concentrations were determined by HPLC.Two-period cross over self-control trail was conducted to 6 Beagle dogs which were administrated a single dose of the oral test tablets and reference tablets. Results The pharmacokinetics of two preparations fitted to two-compartment model.The main pharmacokinetic parameters:Tmax were(7.0±0.92)and(2.0±0.31) h;Cmax were(66.97±5.9)and(112.2±7.4) μg/L;AUC0-t were(1 243.88±25.67)and(1 523.84±27.89) mg·h/L;AUC0-∞ were(1 277.18±30.58)and(1 548.67±20.89) mg·h/L and test tablets showed a relative bioavailability of 82.47%. Conclusion The method was accurate and sensitive which was suitable for Tinidazole pectin matrics pharmacokinetics study.
Improvement of preparation and the stability of furacillin solution
LI Zhi-yuan, WANG Xin-hong, LIU Gui-gang, YAN Qiong
2010, 28(5): 366-368.
Abstract(2278) PDF (165KB)(531)
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Objective To improve the preparation method for furacillin solution and observe the stability of the solution. Methods The original preparation technics was modified.The furacillin solution was qualitatively analyzed by observation and quantitatively determined by UV spectrophotometry. Results The furacillin solution prepared in new method was proved to be stable in quality,without separating sediments in 4 months.However,sediment of furacillin solution prepared in old method was observed,color of the solution became deeper and content was out of quality 2 months later. Conclusion Improved method is convenient and feasible,which could increase the stability and ensure the safety and efficacy of furacillin solution in clinical use.
Study on in vitro release and correlation between in vivo and in vivo of thienorphine hydrochloride microspheres
YANG Yang, GAO Yong-liang
2010, 28(5): 369-371,382.
Abstract(2229) PDF (368KB)(350)
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Objective To establish a method for the determination of in vitro release of thienorphine hydrochloride micro-spheres with a good correlation between in vivo and in vitro. Methods Immediate release and dialysis release Methods were used to determine the in vitro release rate of thienorphine hydrochloride microspheres.The residue thienorphine hydrochloride microspheres in the injection site was determined by HPLC,and in vivo release rate of thienorphine hydrochloride microspheres was caculated.The optimal release solution was chosen based on the correlation evaluation between the in vivo and in vitro Results . Results Immediate release and dialysis release Methods had a good in vitro and in vivo correlation. Conclusion Immediate release and dialysis release method could be used to determine the in vitro release of thienorphine hydrochloride microspheres.
Content determination of carbamazepine tablet by liquid chromatographic tandem mass spectrometry
XIE Hua, WANG Rong, JIA Zheng-ping, ZHANG Juan-hong
2010, 28(5): 372-373,395.
Abstract(2048) PDF (300KB)(793)
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Objective To develop liquid chromatography with tandem mass spectrometry(LC-MS/MS) detection for the content determination of carbamazepine tablet. Methods The method was used.The sample was analyzed on Zorbax Extend-C18(150 mm×4.6 mm,5 μm),with mobile phase consisting of methanol-0.01 mmol/l amine acetic acid(80:20,v/v) at a flow rate of 0.3 ml/min. Results It was proved to be linear in the range of 0.05~40 μg/ml with a regression coefficient of 0.999 4.The average recovery rate was 100.2%(n=5) and RSD was 1.02%.The RSD of average contents of intra-day and inter-day was 1.72% and 1.91% respectively.The concentrations of four lot samples were 96.3%,98.6%,96.5% and 99.0%,respectively. Conclusion This method is accurate,precise,sensitive and specific to be used in the content determination of carbamazepine tablet.
Analysis on utilization of anti-infection drugs in our hospital between 2007 and 2009
YANG A-jing, YANG Ning, ZHANG Juan
2010, 28(5): 374-377.
Abstract(2284) PDF (233KB)(198)
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Objective To provide evidences for clinical rational use and scientific management of the anti-infection drugs through investigating the application status of the anti-infection drugs in our hospital. Methods Utilization of anti-infection drugs was analyzed by the index of DDD,DDDs and DDC. Results Cephalosporins,quinolones,macrolides ranked the top three on the consumption sum list of the anti-infection drugs between 2007 and 2009.Cefaclor,cefuroxime,cefalexin,cefoperazone/sulbactam,levofloxacin,roxithromycin,azithromycin and clarithromycin ranked the front rows on the consumption sum list.The most anti-infection drugs used in our hospital were the fist line drugs with certain effect,convenience for application,fewer adverse effect and cheaper price,moreover,mainly for oral administration.Resistance rates of common pathogenic bacteria were relatively high,especially to levofloxacin which had the highest rate of 77.8%. Conclusion The utilization of anti-infection drugs in our hospital was unreasonable in some respects.The application administration of anti-infection drugs still should be strengthened.
2010, 28(5): 378-380.
Abstract(1625) PDF (167KB)(201)
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2010, 28(5): 381-382.
Abstract(1656) PDF (176KB)(518)
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2010, 28(5): 383-384.
Abstract(2175) PDF (124KB)(338)
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2010, 28(5): 385-386,400.
Abstract(2127) PDF (168KB)(245)
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2010, 28(5): 387-389.
Abstract(1808) PDF (187KB)(643)
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2010, 28(5): 390-392.
Abstract(1562) PDF (175KB)(589)
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2010, 28(5): 393-395.
Abstract(2074) PDF (173KB)(308)
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2010, 28(5): 396-400.
Abstract(1887) PDF (327KB)(1083)
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