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2013 Vol. 31, No. 1

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Application of ten independent component analysis methods in pharmaceutical analysis
SONG Qing, LU Feng
2013, 31(1): 1-4,74. doi: 10.3969/j.issn.1006-0111.2013.01.001
Abstract(2932) PDF (565KB)(205)
Abstract:
The principles and applications of ICA methods were reviewed. Firstly, a summary of the background and development prospects of the ICA were described, the definition, basic principles, and ten algorithms of ICA were briefly introduced,and then the practical application of the ICA in pharmaceutical analysis was discussed.
Recent progress on biological activity and synthesis of 2-substituted Benzofuran derivatives
CHEN Huan, LI Ke
2013, 31(1): 5-10,71. doi: 10.3969/j.issn.1006-0111.2013.01.002
Abstract:
Benzofuran derivatives were a series of attracting heterocyclic compounds with a variety of biological activity. Based on the recently published literatures, these derivatives had shown antitumor, antioxidant, calcium influx blockade, angiotensin II receptor antagonistic, adenosine A1 receptor antagonistic, antifungal, antibacterial and platelet aggregation antagonistic activities. As Benzofuran derivatives had broad activity, which had attracted many research interests. In order to better study of these compounds both in synthesis and biological activity, the review focused on the biological activity and synthetic methods of 2-substituted Benzofuran derivatives in recent years, which would provide valuable information for the development of 2-substituted benzofuran compounds.
Progress on the mechanisms of protective effects on endothelial progenitor cells from natural medicines and their active compounds
DONG Ya-fen, SHU Jing-jing, MA Jing, LI Fei, PENG Cheng, JIN Lei, XIE He-hui, ZHANG Chuan
2013, 31(1): 11-13,31. doi: 10.3969/j.issn.1006-0111.2013.01.003
Abstract(2744) PDF (374KB)(124)
Abstract:
The integrity and function of the endothelium played a key role in the prevention of cardiovascular diseases (CVDs). The maintenance of normal endothelial function not only depended on pre-existing endothelial cells, but also included the recruitment of endothelial progenitor cells (EPC), and EPC might serve as a therapeutic target of CVDs. Application of natural medicines and their active compounds in the treatment of CVDs, and their effects on EPC had been reported previously. The mechanisms underlying the protection of natural medicines and their active compounds on endothelial progenitor cells were summarized in this paper.
Advance in drug therapy of gout
XU Na, CHEN Hai-sheng
2013, 31(1): 14-18. doi: 10.3969/j.issn.1006-0111.2013.01.004
Abstract(4149) PDF (281KB)(729)
Abstract:
With the development of the living standard, the incidence of gout was rising and the trend of patient age with gout getting younger. Developing high-effective and low-adverse anti-gout drugs was a priority of the research agenda. At present, conventional therapies of gout lean on western medicines. These drugs relieved or treated gout with different mechanisms, but all of them had different side-effects. Recently, more and more researchers started to develop traditional Chinese medicine to treat gout and their effectiveness and the side-effects need further clinical verification. The commonly used anti-gout drugs or new drugs under research including their treatment characteristics, potential hazards and their therapeutic principles at different clinical stages were summarized in this article, especially in some anti-hyperuricemia or anti-gout Chinese Medicine, which gave an effective way to develop new anti-gout drugs.
Progress on the multiple pharmacological activity and mechanism of statins
ZHAO Xin-bin, NI Min, TAO Xia
2013, 31(1): 19-21. doi: 10.3969/j.issn.1006-0111.2013.01.005
Abstract(3702) PDF (268KB)(410)
Abstract:
Statins were a mainstay in the treatment of hyperlipidemia and used in the primary and secondary prevention of coronary artery disease. Recent studies indicated that there were some cholesterol-independent or pleiotropic effects of statins, including improving endothelial function, decreasing oxidative stress, inhibiting inflammation, enhancing the stability of atherosclerotic plaques and used for anticancer therapy. The effects and mechanisms of statins on vascular disease and cancer were reviewed in this paper.
The clinical features of drug-induced liver injury in elderly
TANG Xian-feng, SUN Jie, LU Ming-zhu
2013, 31(1): 22-23,66. doi: 10.3969/j.issn.1006-0111.2013.01.006
Abstract(2754) PDF (444KB)(171)
Abstract:
Drug-induced hepato-toxicity was an important reason for the liver disease in elderly,which was four times more common than in adults and might include all known liver disorders. Reports related to drug side effects were rare in people >60 years of age group since most clinical trials exclude patients >75~80 years of age. Further clinical studies should be need to investigate hepatic side effects of drugs in elderly patients. The main clinical manifestations and diagnosis of drug-induced liver injury in elderly as well as common drugs (cardiovascular drugs and anti-microbial agents) cause liver injury in clinical conditions were reviewed in this paper.
Elucidation of 10-hydroxy-7-methyl-homocamptothecin by electrospray ion trap mass spectrometry
CUI Xiao-ru, GUAN Xiao-duo, MIAO Zhen-yuan, ZHANG Wan-nian, FAN Guo-rong
2013, 31(1): 24-26,60. doi: 10.3969/j.issn.1006-0111.2013.01.007
Abstract(3349) PDF (824KB)(436)
Abstract:
Objective To analyze the fragments of 10-hydroxy-7-methyl- homocamptothecin (TOP-01) by electrospray ion trap mass spectrometry and deduce the MS/MS fragment pathway of it. Methods Samples were directly injected into the instrument and the fragments of the samples were yielded by using multi-stage ion trap mass spectrometry. Results Fragment ions m/z 333, 305, 277, 290 were generated at the positive ion mode and m/z 347, 319, 317, 289, 301 at the negative mode for TOP-01. Conclusion Differences existed in fragmentation pathway between positive and negative ESI-MS,and the main fragmentation characteristics of TOP-01 were m/z 333 and 347 in positive and negative mode respectively. These results provided very important information for the structural modification and the drug metabolic research of homocamptothecin.
Design, synthesis and antifungal activity of novel triazole derivatives
LI Yang-yang, LIU Hua, LIU Hong, ZHANG Yong-qiang, ZHANG Wan-nian, SHENG Chun-quan
2013, 31(1): 27-31. doi: 10.3969/j.issn.1006-0111.2013.01.008
Abstract:
Objective To design the novel triazole derivatives and test their in vitro antifungal activities on the basis of the molecular design model for rational optimization of azole drugs. Methods Ring-open reaction of the oxiranes was used to synthesize the target compounds, whose chemical structures were confirmed by 1H NMR and MS. Serial dilution method was used to determine the in vitro antifungal activities. Results Two novel azole compounds containing trizaolone side chains were synthesized which showed excellent and broad-spectrum antifungal activity. Conclusion The targeted compounds showed better antifungal activity against Candida albicans than the positive drugs fluconazole and ketoconazole, which was worth to further investigate the structure-activity relationship.
Study on clarification process of Bairui oral liquid
YAN Jun, XUAN Wei-dong, BIAN Jun
2013, 31(1): 32-34. doi: 10.3969/j.issn.1006-0111.2013.01.009
Abstract:
Objective To establish a optimum clarification process of Bairui oral liquid with new ZTCI+1-Ⅱ natural clarifying agents. Methods The effects on clarification of Bairui oral liquid were evaluated based on the factors such as adding sequence, added amount and clarification time of ZTCl+1-Ⅱ clarifiers A and B. The contents of astragalin and total flavones were determinate by the HPLC and UV methods respectively to evaluate the removing activities of ZTCl+1-Ⅱon active components. Results The selected clarification process conditions were: adding 20% percentage of each components of ZTCl+1-Ⅱto the condensed herb extract solution, the adding sequence was clarifiers B before clarifiers A, and the clarification time was 12 h, respectively. Conclusion The contents of astragalin and total flavones were not decreased by clarification process, ZTCl+1-Ⅱ could be used as the removing impurity of Bairui oral liquid.
Extracting method optimization and physical and chemical properties of polysaccharide in Bletilla striata
HAN Dan, WANG Yang-ping, BI Ya-jing, LIU Fu-qiang
2013, 31(1): 35-37. doi: 10.3969/j.issn.1006-0111.2013.01.010
Abstract(3719) PDF (341KB)(446)
Abstract:
Objective To establishing the best extraction technology of polysaccharide in Bletilla striata and researching its physical and chemical properties. Methods Water extraction and buck formulation, cellulose enzyme hydrolysis and ultrasonic extraction were used, and the spectrophotometry was used to determine the content of polysaccharide, the receiving rate of polysaccharide in the highest method as the foundation, the contents of polysaccharide as the target to process optimization. The physical and chemical characteristics of polysaccharide were studied according to the Ch.P (2010). Results The ultrasonic extraction method was the best extraction technologywith the condition that: the ratio of material and liquid was 1:20, temperature was 80℃, in 10 min.The extraction rate was 49.90%. Five physical and chemical properties were calculated. Conclusion The extraction rate of ultrasonic method for polysaccharide in Bletilla striata was high than other methods, and suitable for mass productionwhich could provide the references for modern application of polysaccharide in Bletilla striata.
Proliferation inhibition of total alkaloids from Pinellia Ternata in human lung cancer cells
ZHOU Xi, TANG Ying, SUN Huan, WANG Qing-min, LEI Cheng-xiang
2013, 31(1): 38-41. doi: 10.3969/j.issn.1006-0111.2013.01.011
Abstract(3117) PDF (509KB)(327)
Abstract:
Objective To investigate the proliferation inhibition of total alkaloids from Pinellia ternate (TATP) in human lung cancer line A549. Methods The proliferation inhibition of human lung cancer cell line A549 treated with TATP was measured with methyl thiazolil tetracolium colorimetic method and plate clone formation assay. The DNA damage of A549 cell induced by TATP was detected with the single cell gel electrophoresis (SCGE). Results The proliferation in A549 cell treated with TATP was decreased significantly compared with control group and the proliferation inhibition was positively correlated to the TATP concentration and the reaction time. The difference between the control group and the TATP experimental groups was significant in statistic. Compared with the control group, the tail DNA content, the tail length and the tail movement of the TATP experimental groups were different significantly and presented a dose-effect relationship. Conclusion TATP could inhibit the proliferation of A549 cells in vitro, which might be correlated to the DNA damage induced by TAPT.
Protective effect of total flavonoids in Herba Siegesbeckiae on cerebral ischemia in rats
LOU Yue-fen, LI Ying, HU Bin
2013, 31(1): 42-44. doi: 10.3969/j.issn.1006-0111.2013.01.012
Abstract:
Objective To study the protective effect and possible mechanism of total flavonoids in Herba Siegesbeckiae on focal cerebral ischemia in rats. Methods Sprague Dawley (SD) rats were randomly divided into 6 groups: sham operation group, model group, total flavonoids of Herba Siegesbeckiae groups with low, moderate and high dose (5, 10, 20 mg/kg)and ginkgo leaf tablet group (50 mg/kg). Focal cerebral ischemia model was established by middle cerebral artery occlusion. The effects of Herba Siegesbeckiae total flavonoids on nervous behavior, cerebral infarct volume and the content of brain water were observed in rats. The activities of malondialdehyde (MDA), glutathione peroxidase (GSH-Px), superoxide dismutase (SOD) in cerebral tissues were measured. Results total flavonoids of Herba Siegesbeckiae could improve the neurological function, reduce the cerebral infarct volume, the content of brain water and the activity of MDA, increase the activity of SOD and GSH-Px. Conclusion Total flavonoids of Herba Siegesbeckiae could alleviate focal cerebral ischemia injury, and the mechanism might be related to anti-oxidant effect.
Analysis of serum bile acid changes in patient of oral administration of UDCA after hepatocellular carcinoma resection
JIN Rou-nan, LI Le-le, GONG Chun-gui
2013, 31(1): 45-48. doi: 10.3969/j.issn.1006-0111.2013.01.013
Abstract(2705) PDF (419KB)(109)
Abstract:
Objective To analyze the serum bile acid changes in patient of oral administration of UDCA after hepatocellular carcinoma resection and provide reasonable recommendations for clinical staffs. Methods 89 cases with hepatocellular carcinoma after taking UDCA had been analyzed during 2009.01 to 2010.01. Results Serum bile acid concentration changes before medication of UDCA had been showed that the maximum value was 131.10 μmol/L, the minimum value was -69.00 μmol/L, quartile spacing was 15.30 μmol/L,and after medication, the maximum value was 275.20 μmol/L, the minimum value was -49.00 μmol/L, quartile spacing 30.50 μmol/L. The serum bile acid concentrations after medication of UDCA had increased significantly compared with the status before medication, P<0.01. The Child-Pugh scores before the medication of UDCA was correlated to the changes of serum bile acid after the medication of UDCA,P<0.01.The other variables, UDCA dosage, the amount of bleeding during operation, blocking time of portal vein, the different surgeon, cirrhosis were not correlated to the changes of serum bile acid after the medication of UDCA. Conclusion The Child-Pugh scores before the medication of UDCA should be the prime considerable factor as concerned.
Effect of combined therapy with piperazine ferulate and benazepdl on urinary albumin excretion rate in patients with early diabetic nephropathy
TU Chuan-fa, WANG Li-jun, JIN Du, YANG Hong-wei, ZHANG You-you, MOU Xiao-yue
2013, 31(1): 49-50,56. doi: 10.3969/j.issn.1006-0111.2013.01.014
Abstract(2734) PDF (450KB)(115)
Abstract:
To explore the effect of combined therapy with piperazine ferulate and benazepdl on urinary albumin excretion rate (UAER) in patients with early diabetic nephropathy (DN). Methods A total of 164 children were included in the study, 82 of whom accepted piperazine ferulate and benazepdl were put into the observed group, 82 of whom accepted only benazepdl were put into the control group. The difference of the UAER, 24 h urinary protein, Serum creatinine, blood glucose, glycosylated hemoglobin and CRP were compared by T test. Results ①After treatment, the UAER, 24 h urinary protein, CRP and blood pressure were significantly lower than that before treatment in both observed group and control group;②The UAER, 24 h urinary protein and CRP were significantly lower in the observed group than that of the control group after treatment. Conclusion Combined use of piperazine ferulate and benazepdl could significantly lower the levels of UAER in patients with early DN.
The clinical effect of Jiangzhi tablets on hyperlipidemia
WANG Li-jun, LIU Dong, SHEN Lei
2013, 31(1): 51-52,63. doi: 10.3969/j.issn.1006-0111.2013.01.015
Abstract:
Objective To observe the clinical efficacy and safety of Jiangzhi tablet in the treatment of hyperlipoidemia. Methods 117 patients of hyperlipoidemia were randomly divided into 3 groups. Treatment group (39 patients) were treated with Jiangzhi tablet and control group A (41 patients) were treated with Zhibituo tablet, and control group B (37 patients) were treated with lovastatin tablet. The course of treatment was 4 weeks. Results There was no significant difference between treatment group and two control groups in the total effective rate (P>0.05). The level of the total cholesterol and triglycerides in blood were decreased obviously in three groups after treatment (P<0.05). There was significant difference between treatment group and two control groups in decreasing range (P<0.05). Conclusion Jiangzhi tablet had significant effect on hyperlipoidemia with low side effect of toxicity and high safety.
Study on the solubility and stability of curcumin in PEG-400
TONG Yong-tao, GAO Yong, GAO Bao-an, YUE Li-qun, CHEN Jian-ming
2013, 31(1): 53-56. doi: 10.3969/j.issn.1006-0111.2013.01.016
Abstract(4034) PDF (511KB)(542)
Abstract:
Objective To study the solubility and stability of curcumin in PEG-400 and screen the best suitable stabilizer to improve the autoclave stability. Methods Solubility determination was used to determine the solubility of curcumin in PEG-400.The stability under different pH conditions was studied by accelerated testing. The best suitable stabilizer was screened to improve the autoclave stability and the validity of the curcumin solution in PEG-400 with stabilizer was speculated by accelerated testing. Results The solubility of curcumin in PEG-400 was 42 mg/mL;the most stable pH was 3.70. The 0.1% propyl gallate could improve the sterilization stability of curcumin in PEG-400. At room temperature (25℃), the validity duration of curcumin PEG-400 solution with 0.1% propyl gallate was 296.1 days and if at low temperature (6℃), it coulb be up to 5.5 years. Conclusion The study showed that the solubility of curcumin was greatly improved and 0.1% propyl gallate could greatly improve the sterilization stability of curcumin in PEG-400.
Study on quality standard of Xiangping chaqing paiqian granules
DENG Zhao-hui, LIANG Tu-jin, HU Wen-jun
2013, 31(1): 57-60. doi: 10.3969/j.issn.1006-0111.2013.01.017
Abstract(2708) PDF (574KB)(263)
Abstract:
Objective To establish a quality standard for Xiangping chaqing paiqian granules. Methods Chemical methods were used to identify vitamin C in the granules. TLC methods were used to identify green tea extracts and chrysanthemum extracts. Chlorogenic acid and catechin were assayed by HPLC. Results Vitamin C could be identified by chemical method, and green tea extracts and chrysanthemum extracts could be identified by TLC. The content of chlorogenic acid and catechin could be assayed by HPLC. Conclusion The methods were proved to be reliable, good sensitivity and high specificity, which could be used in quality control of Xiangping chaqing paiqian granules.
Determination of Esomeprazole in dog plasma by LC-MS-MS
YANG Xiao-ying, MA Qi-zhen
2013, 31(1): 61-63. doi: 10.3969/j.issn.1006-0111.2013.01.018
Abstract(2755) PDF (537KB)(533)
Abstract:
Objective To establish a method for determining Esomeprazole in dog plasma by LC-MS-MS. Methods Diazepam was used as the internal standard,the samples were precipitated with acetonitril. Analytical column was Shim-pack XR-ODS (2 mm×100 mm, 5 μm). The mobile phase was acetonitrile:2 mmol/L ammonium acetate (containing 0.1% formic acid) at a flow rate of 0.3 ml/min. Mass spectrum conditions was ESI performing in positive ion MRM mode using target ions 346.2→198.2 m/z (esomeprazole)and 285.2→193.2 m/z (diazepam). Results The calibration curve was linear over the range of 0.5~1 200 μg/L. The LLOQ of Esomeprazole in plasma was 0.5 μg/L. The average extracted recovery was (101.0±6.5)%. The RSDs of intra- and inter-day were less than 15%. Conclusion The method was sensitive, simple and accurate to determinate Esomeprazole plasma concentration and suitable to the pharmacokinetics study.
Determination of doxapram hydrochloride glucose injection by HPLC
XUE Zhi-hong, WANG Sheng-hao, PAN Shi-ru
2013, 31(1): 64-66. doi: 10.3969/j.issn.1006-0111.2013.01.019
Abstract(2966) PDF (552KB)(386)
Abstract:
Objective To establish an HPLC method for determination of doxapram hydrochloride glucose injection. Methods COSMOSIL C18 (150 mm×4.6 mm,5 μm) column was adopted. The mobile phase consisted of 0.82 μg/L CH3COONa (using Glacial acetic acid adjust to pH 4.5)-acetonitrile (70:30). The detection wavelength was 214 nm. Results The linearity of doxapram hydrochloride concentration was in the range of 13~91 μg/ml (r=0.999 8). The average recovery was 99.3%,RSD=0.81% (n=9). Conclusion The method was simpleaccurate and sensitive with high specificity.
Analysis and countermeasure of outpatient drug return in our hospital
WANG Xiao-jun
2013, 31(1): 67-68,77. doi: 10.3969/j.issn.1006-0111.2013.01.020
Abstract(2604) PDF (485KB)(257)
Abstract:
Objective To analyze the outpatient drug return in 2011 and promote rational drug use. Methods 1 905 prescriptions of drug return in our hospital between January and December in 2011 were collected. Based on The medical organization drug management stipulation, the return causes and drug kinds were analyzed. Results In 1 095 outpatient drug return prescriptions, the return reason of adverse drug reaction was in the first place, accounted for 36.71%, followed by input error in physicians prescription, accounted for 19.82%,24.48% of drug return were antimicrobial drugs, 20.27% of drug return were circulating system drugs. Conclusion The quality of diagnosis and treatment should be improved, the doctor-patient communication should be strengthened,pharmaceutical care should be improved, medication consultation service should be carried out.Retreat drug management system should be optimized in order to reduce drug return.
The fault analysis and processing method of automatic oral drug dispensing system
WU Pei-zhi, HU Li-hui, LIU Li-juan, WENG Shao-min
2013, 31(1): 69-71. doi: 10.3969/j.issn.1006-0111.2013.01.021
Abstract:
Objective To provide references for the troubleshooting of automatic oral drug dispensing system in hospital pharmacy. Methods The specific reasons of the fault when using automatic oral drug dispensing system were analyzed, and the processing methods were summarized. Results and Conclusion In order to make the automatic oral drug dispensing system run stable and play maximum advantage, the dedicated staff should be responsible for the daily operation and maintenance,who should be required to accurately regulate the use of automatic oral drug dispensing system, and eliminate the fault by careful inspection when encounter problems.
Investigation of antiepileptic drugs in 526 children with epilepsy
XU Jin, LI Jiong, HAN Lin
2013, 31(1): 72-74. doi: 10.3969/j.issn.1006-0111.2013.01.022
Abstract:
Objective To understand the use of antiepileptic drugs for children with epilepsy in our hospital and provide reference for clinical medication individualization. Methods The varieties of antiepileptic drugs, the blood drug levels and the situations of symptom control were analyzed from 526 outpatients with epilepsy in our hospital. Results Sodium Valproate and Carbamazepine were used mostly in our hospital. The blood drug levels and the epileptic symptoms were under control in 86% children with them. Conclusion The use of antiepileptic drugs was reasonable basically in our hospital. Pharmaceutical Services and clinical medication individualization should be strengthened during the processes of antiepileptic treatment.
Cognizance of the subject after the occurrence of the adverse drug reaction
XU Qing-song
2013, 31(1): 75-77. doi: 10.3969/j.issn.1006-0111.2013.01.023
Abstract(2751) PDF (485KB)(103)
Abstract:
In the adverse drug reactions, who should be the one to be responsible for patient suffers, which had been controversial for long time. In the judicial practice, law court often judged hospital to take the responsibility based on the fairness doctrine in civil law. A case was analyzed to point out that the trial of cases of the adverse drug reaction should still be identified according to fault principle. The legal advice to safeguard the legitimate rights in the condition of no-mistake subject was puts forward.