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2012 Vol. 30, No. 4

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Progress on structures and binding structures with small molecules of G-quadruplex
JIANG Zhi-hui, ZHANG Da-zhi
2012, 30(4): 241-247.
Abstract(7454) PDF (1366KB)(2910)
Abstract:
There was a research focus for the prevention of diseases by way of binding to DNA using small molecules.The discovery of structures of G-quadruplex and its fimction related to cancer thtough modern molecular biology techniques provided a big chance for thedesignof anti-cancer drug.This article aimed to present recent advances for the struclures of G-quadruplex and these small binding molecules,which would contribute to understand these binding modes and thus provide a steady support in the rational designof anti-cancer drug.
Progress on synthesis and biological activity of 2-pyridyl ketone derivatives
ZHANG Ming-feng, LV Zhi-liang, LI Ke
2012, 30(4): 248-253,295.
Abstract(2406) PDF (437KB)(477)
Abstract:
Objective To introduce the progress on synthesis and biological activity of 2-pyridyl ketone derivatives.Methods The information described in literature both at home and abroad was reviewed.Results and Conclusion Basedon the results of existedresearch,deep studyon the mechanism of action and the targets would further promote the development processof these conpounds.
Progress on nanostructured lipid carriers as oral poorly soluble drugs delivery systems
WEN Xu, HU Xiong-wei, WU Hao, SONG Hong-tao
2012, 30(4): 254-257,301.
Abstract(2661) PDF (882KB)(1010)
Abstract:
Nanostructured lipid carrier,which could enhance the bioavailability of poorly soluble drugs,was a kind of promisingoral delivery systems for insoluble drugs.The preparation,characterization, drug release in vitro and the mechanism of NLC for enhancing the bioavailability of poorly soluble were reviewed in this paper.
Progress on tissue culture of Catharanthus roseus
ZENG Zhi-fa, LIU Run-hui
2012, 30(4): 258-261,312.
Abstract(2488) PDF (485KB)(764)
Abstract:
Catharanthus roseus (L.) G. Don contained more than 100 known indole alkaloids, some of which had anti-cancer, lowering blood pressure and other biological activity. Catharanthus roseus had a high medicinal value, but the content of alkaloids was very low. In order to improve the content of alkaloid, the technology of tissue culture had been applied in Catharanthus roseas,such as improving the propagation coefficient and controlling the accumulation of secondary metabolites. To provide reference in further development and utilization of Catharanthus roseus drug resources, the main research progress of tissue culture of Catharanthas roseus includingy the impact factors of medicinal components accumulation, suspension cell culture applications, the impact factors of hairy roots and application of genetic engineering technology were reviewed in this paper.
Application of mesoporous molecular sieves in medicine
MENG Hui, MAO Jun-qin, LIU Chang-sheng, WEI Jie
2012, 30(4): 262-265.
Abstract(2579) PDF (368KB)(549)
Abstract:
Mesoporous molecular sieves was a new material in the aperture between the microporous and macroporous, which had significant hemostatic,anti-microbial effect. Mesoporous materials had been widely employed as carriers for controlled drug release and achieved targeted drug delivery. The application of messoporous molecular sieves in recent literatues was reviewed which could provide the scientific basis for the research, development and applicaiion of mesoporous molecular sieves in future.
Progress on the pharmacological actions and mechanism of Danshensu
SHU Jing-jing, LI Fei, DONG Ya-feng, JIN Lei, ZOU Hao, ZHANG Chuan
2012, 30(4): 266-268,298.
Abstract(2628) PDF (391KB)(768)
Abstract:
Salvia was a traditional Chinese medicine, which was widely used for cardiovascular treatment. The water-soluble components of Salvia was Danshensu, which had become one of the research hotspots. In recent years,the pharmacological research of danshensu focused on the characteristics of the activity and its roles in cardiovascular mechanisms. The literatures of past five years were reviewed and new pharmacological actions and mechanism studies of danshensu were summarized.
Preparation and promoting blood circulation effect of Yantongping transdermal ointments
HE Ai-ming, XU Jie, WANG Yi-hui, LIN Shi-ming
2012, 30(4): 269-274,278.
Abstract(2481) PDF (573KB)(795)
Abstract:
Objective To find out the best prescription method for Yantongping transdermal ointments through orthogonal design and research on the effect of promoting blood circulation. Methods With 60 minutes in vitro cumulative penetration rate, using L9(34) orthogonal experiment,the best formula and technology were found out through grinding method,and quality thereafter was evaluated. Mice was picked up as blank groups and model groups, each respectively was divided into six smaller groups as Vaseline, Vaseline and Fatty Alcohol.Yantongping transdermal ointments (low dosage),Yantongping transdermal ointments (medium dosage),Yantongping transdermal ointments (high dosage) and Voltaren Emulsions.△A and △V were measured before and after modeling by microcirculation method and microscopic micro-distance measuring method,while the blood circulation function of each medicine by the scoring of the blood of veinule was compared.Results The bestprescription was confirmed by A2B2C3D2.that was with the weight of the traditional Chinese drugs (TCD) Vaseline ratioes (A) to 50%,with the weight of TCD and Fatty Alcohol ratios (B) to 25%,the order of reagent was as follow:Fatty Alcohol,TCD,Vaseline.The grinding temperature was 80℃,and it passed five quality evaluation asphysical appearance,melting point,water value,stability,irritation.Before modeling,in the △A level measured,antongping group (low dosage) had statistical significance over Vaseline and Fatty Alcohol group in 30 min (P<0.05),while Yantongping group (medium dosage and high dosage) had obviously statistical significance over Vaseline and Fatty Alcohol group in different time periodsin the △A and△V level (P<0.01).In the blood flow quality evaluation measured,Yantongping group (low dosage) had statistical significance over Vaseline and Fatty Alcohol group in 20 min,30 min (P<0. 05); while Yantongping group (medium and high dosage) had obviously significant statistical significance over Vaseline and Fatty Alcohol group (P <0.01).After modeling, in the△A level, Yantongping group (low dosage) had statistical significance over Vaselineand and Fatty Alcohol group in 20 min ( P<0. 05);Yantongping group (low dosage) in 30 min, Yantongping group (medium and high dosage) had obviously significent statistical significance over Vaseline and Fatty Alcohol group in the△A and△V level. In the blood flow quality evaluation measured,Yantongping group (low,medium and high dosage) had obviously significant statistical significance over Vaseline and Fatty Alcohol group (P<0. 01).Conclusions Yantongping transdermal ointments prepared by the best prescription had a good function of promoting blood circulation.
Studies on the chemical constituents in leaves of Rosa Laevigata Michx
WU Jian-lin, WANG Ping, GAO Peng, ZENG Na, LIU Xiang-fang, WANG Sui-yi, SHEN Yang, XU Chao-dou
2012, 30(4): 275-278.
Abstract(2999) PDF (333KB)(521)
Abstract:
Objective To investigate the chemical constituents from leaves of Rosa Laevigata Michx.Methods The chemical constituents were isolated and purifieated by silica gel column chromatography,Sephadex LH-20 and semi-preparative RP-HPLC. Their structures were identified by spectral data together with physicochemical analysis,Results Twelve known compounds were isolated and identified as catechin(1),quercetin(2),naringenin(3),kaempferol(4),ethyl gallate(5),p-hydroxyl ethyl cinnamate(6),ω-hydroxypropioquaiacone(7),hydroxytyrosol(8),o-hydraxybeuzoic acid(9),scopoletin(10),ethyl α-D-arabillofuranoside(11),methyl β-D-glucopyranoside(12).Conclusion Compound 11 was isolated from genus Rosa for the first time,compounds 3,5-9 were isolated from leaves of Rosa Laevigata Michx for the first time.
Analysis of volatile oil from Artemisia argyi Levi.et Vant extracted by three different methods by GC-MS
LI Ling, LV Lei, DONG Xin, LV Di-ya, LOU Zi-yang
2012, 30(4): 279-282,286.
Abstract(2611) PDF (387KB)(768)
Abstract:
Objective To analyze the the compositions of volatile oil from Artemisia argyi Levi.et Vant extracted by three different methods by GC-MS.Methods The volatile oil from Artemisia argyi Levi.et Vant were extracted by Steam distillation,Hexane reflux extraction and Static headspace. GC-MS was used for the separation and identification. Results By the three methods, 80 compounds were identified.59 components were extracted by static headspace, 37 by steam distillation and 31 by hexane reflux extraction.Conclusion Combination of steam distillation and static headspace, sampling was feasible to establish GC-MS representation system for Artemisia argyi Levi.et Vant;there were certain advanlages of static headspace in determination of volatile oil contant.
Establishment of the population pharmacokinetics model of sibutramine in Chinese healthy volunteers
CHEN Xiao-jin, LI Zhong-dong, DING Jun-jie, SHI Xiao-jin, XU Yi-xin
2012, 30(4): 283-286.
Abstract(2814) PDF (793KB)(1007)
Abstract:
objective To develop the population pharmacokinetics model of sibutramine (SIB) in Chinese healthy volunteers.Methods Twenty male healthy volunteers were enrolled into the study.13 blood sampling were drawn after administration of 10 mg SIB within 24h.Theplasma samplesfor SIB concentration were analyzed using validated HPLC/MS method.The population pharmacokinetics was characterized by non-linear mixed effects model (NONMEM).Visual predictive check (VPC) and normalized predictive distribution error (NPDE) were used to evaluate the predictive ability of the model.The reliability and stability of the population pharmacokinetic model developed was further assessed by a nonparametric bootstrap procedure,Results A two-compartment pharmacokinetic model with first-order absorption and elimination was used to describe the concentration-time data.The weight and age had no significant impact on the model parameters.The population typical values (inter-individual variability) of Vl,V2,CL,Q,Ka and Tlag were 7.85 (42.8%) L,2.03 (48.2%)L,1.08 (38.5%)L/h,0.289 (27.1%)L/h,1.95 (56.8%)h~and 0.187 (17.8%)h respectively.Most of parameter estimates from non-parametric bootstrap procedure were comparable and within 10% of the estimates from NONMEM.The stability and the predictive performance were accepted by Bootstrapping,the goodness-of-fit,VPC and NPDE.Conclusion The final population pharmacokinetics model of SIB in Chinese healthy was established by NONMEM,The modcl was steady and reliable.
Process improvement of tamibarotene preparation
ZHAO Ming-zhu, ZANG Cheng-xu, CAI Zhan, JIANG Zhi-hui, HUANG Jing-hua, ZHANG Da-zhi
2012, 30(4): 287-288,304.
Abstract(3077) PDF (254KB)(553)
Abstract:
Objective To improve the preparation process of tamibarotene.Methods 1,2,3,4-tetrahydro-1,1,4,4-tetram-ethyl-6-acelylaminonaphthalimide was prepared from 2,5-dimethyl-2,5-hexanediol by chloridized and Friedel-Craft reaction with acetauilide,which was subjected to deacylation, acylation and hydrolyzation to give tamibarotene.Results The process was successfully improved due to low cost,easier post-processing and good yield. The purity of the product was high (>99.7%) and no impurity more than 0.1%. Conclusion The total yield of the improved process was 26.6%. which was more suitable for industrial manufacturing.the structure of temibarotene was confirmed by 1H-NMR,ESl-MS and elementary analysis.
Research on the transfer rate of baicalin in preparation of Bianyan oral solution
LI Xiang, LIU Gui-yang, AM Jian-li, WANG Xiao-qing, GAO Lei, ZHANG Qin-zhe
2012, 30(4): 289-290,309.
Abstract(2804) PDF (268KB)(881)
Abstract:
Objective To establish the HPLC method for determination of baicalin in Bianyan oral solution,and evaluate the transfer rate in process of production.Methods The Agilent Zorbax Eclipse XDB-C18 (4.6 mm×150 mm,5μm) was used,the mobile phase consisted of methanol-0,5% acetic acid (45:55),the flow rate was 1.0 ml/min,the detection wavelength was at 277nm,the column temperature was at 30 ℃,the inject volume was 10μl.Results A good linear correlation of baicalin was observed within the range of 1.064~106.4 μg/ml (r=0.999 9).The average recovery was 101.26% with RSD 1.92% (n=6).The transfer rates from Radix Scutellariae to intermediate sample and Io Bianyan oral solution were 17.2%~19.0% and 78.7%-79.4%.Conclusions The method was rapid.simple and accurate,which could be used for the quality control and processing technique evaluation of Bianyan oral solution.
Clinical observation of interval usage of furosemide and torasemide in treatment of chronic heart failure
REN Shi-jia, ZHENG Ji-ping, XU En-guo, YANG Jian-guang
2012, 30(4): 291-292,319.
Abstract(2783) PDF (250KB)(901)
Abstract:
Objective To confirm the effect of interval usage of furosemide and torasemide in treatment of chronic heart failure (CHF).Methods By simple randomization,the patients were divided into the observe group (interval usage of furosemide and torasemide) and the control group (continuous usage of furosemide).The difference of the efficiency,urine volume, electrolytes and pro-BNP were compared between the two groups.Results The efficiency,urine volume and serum potassium were signifieanlly higher in the observed group than that of the control group (P<0.05).The pro-BNP and the incidence of adverse reactions were significantly lower in the observed group than that of the control group (P<0.05). Conclusion The interval usage of furosemide and torasemide could get better curative effect in treatment of CHF.
Effect of recombinant human growth hormone therapy on late puberty children with idiopathic short stature
JIN Wei, CHEN Ji-nan, WEN Ge-sheng, GAO Yi
2012, 30(4): 293-295.
Abstract(2383) PDF (277KB)(929)
Abstract:
Objective To assess the efficacy of recombinant human growth hormone (rhGH) therapy in late puberty children with idiopathic short stature. Methods 11 children in late puberty with idiopathic short stature (ISS) were divided into 2 groups according to sex.A group consisted of 5 boys, B group was composed of 6 girls. Bone age (BA) of A group was (14~15) years, and BA of B group was (12.5~13.5) years.The enrolled children were treated with subcutaneous injection of rhGH (0.15 IU/kg·d) daily before sleep for six months,and the growth velocities (GV) and the predicted adult height (PAH) before and after treatment were compared. Results The mean height of A group and B group increased from (148.6±2.6) cm and (139.6±2.9) cm to (153.6±2.1) cm and (143.8±2.5) cm respectively. The growth velocity of A group and B group increased from (3.8±0.5) cm and (3.3±0.6) cm per year to (9.8±1.7) cm and (8.4±1.8) cm per year.PAH of A group and B group increased from (158.9±3.0) cm and (147.6±1.2) cm to (160.3±3.0) cm and (149.2±1.6) cm. There was a significant increase in rhGH therapy (all P<0.05), but no change in BA during the whole course of rhGH therapy. Conclusion rhGH was an effective and safe drug in promoring the growth in late puberty children with ISS.
The curative effect of exenatide combined pioglitazone on type 2 diabetes
JIANG Ping, WANG Xiao-mei, ZHU Bin
2012, 30(4): 296-298.
Abstract(2822) PDF (282KB)(768)
Abstract:
Objective To observe the effect and safety of exenatide combined pioglitazone on type 2 diabetes.Methods 68 patients with type 2 diabetes who took pioglitazone for some time and still could not control the blood glucose effectively.In that case,every patient in treatment group was given exenalide for three months.The variation of the fasting blood-glucose (FPG)、blood glucose after the meal for 2 hours (2hPG)、HbAlC、cholesterol (TC)、triglyeeride (TG)、high-density lipoprotein cholesterol (HDL-C)、lowdensity lipoprotein cholesterol (LDL-C)、cpeptides (C-P) and body mass index (BMI) were observed before and after treatment.Insulin resistance (HOMA-IR) and islet β-cell function (HOMA-β) Were calculate.Results After the treatment,BMI、FPG、2hPG、HbAlC、HOMA-IR、TC and TG were decreased,but C-P、HOMA-β were improved as compared with pre-treatment (P<0.05).Conclusion Exenatide combined pioglitazonc could change thc blood glucose of the patients with type 2 diabetes,which didn't increase the risk of law blood glucose. It also could reduce the patient's weight and improve the patient's quality of life.
The effect of valsartan on patients with hypertension and non-alcoholic fatty liver disease
ZHANG Su-jiang, LIN Lu
2012, 30(4): 299-301.
Abstract(2849) PDF (261KB)(601)
Abstract:
Objective To explore the effect of valsartan on patients with hypertension and non-alcoholic fatty liver disease (NAFLD),Methods A total of 148 patients suffered hypertension and NAFLD were included in the study. Patients were divided into the observed group the compared group.which were given valsartan and analodipine respectively. The difference of the blood pressure,liver ultrasound,liver function,serum lipids,insulin resistance index (RI) and clinical curative effect were compared between the two groups. Results The curative effect in the observed group (93.24%) was significantly higher than that in the compared group (81.08%);After treatment,the alanine aminolransferase,cholesterol,triglyceride,low density lipoprotein and RI in the observed group were significantly lower than that in the compared group (P<0.05). Conclusion The valsartan had a good effect on patients suffered hypertension and NAFLD.
Study on effects of Fe3+ on the stability of ornidazole and sodium chloride injection
LIU Qian-ying, YIN An-fan, NIU Zhi-ying
2012, 30(4): 302-304.
Abstract(2672) PDF (267KB)(939)
Abstract:
Objective To investigate the effects of Fe“on the stability of ornidazole and sodium chloride injection,and ensure the safety in elinical utility. Methods Two kinds of ornidazole and sodium chloride injection which contain no Fe3+ and trace Fe3+ were prepared respectively, The content of ornidazole was determined by HPLC at different temperatures and times,which was used to study chemical dynamics of ornidazole, According to Arrhenitls equation,stability of two kinds of ornidazole and sodium ehloride injection at room temperature were forecasted. Results The degradation of ornidazole followed the first-order reaction kinetics model. At 25℃,t0.9 of ornidazole and sodium chloride injection which not containing Fe3+ and containing trace Fe3+ were 1.71 years and 1.11 years separately. Conclusions Trace Fe3+ could accderate the degradation of ornidazole.which shortened storage period of ornidazole and sodium chloride injection.
Determination of glutathione and oxidized glutathione by HPLC
SUN Wei-zhang, YU Bo-tao, JIANG Yan, ZHOU Mao-zai
2012, 30(4): 305-306,315.
Abstract(3291) PDF (256KB)(360)
Abstract:
Objective To establish a method to determine GSH and GSSG by HPLC. Method The analytical column was Hypersil C18. The mobile phase consisted of 25m mol/L KH2PO4 (pH2.5):tetrahydrofuran (100:1). The flow rate was 1.0 ml/min. Column temperature was 30 ℃ and the detective wavelength was 230 nm. Result The calibration curve of GSH was linear within the range of 3.12 μg/ml~2490.0 μg/ml (r=0.9999) and the average recovery was 101.84%. The calibration curve of GSSG was linear within the range of 3.25 μg/ml~975.0 μg/ml (r=0.9999) and the average recovery was 97,84%. Conclusion The method was proved to be reliable and accurate,which could be used to determinate GSH and GSSG simultaneously.
Determination of buddleoside in Zhikuoyangyin granules by HPLC
WU Wen-fei, ZHANG Li-bin, LI Yu-pin
2012, 30(4): 307-309.
Abstract(2896) PDF (259KB)(646)
Abstract:
Objective To establish a high performance liquid chromatography method for the determination of buddleoside in Zhikuoyangyin granules. Methods The HPLC method was performed on a DIKMA Platisil ODS column (250 mm×4.6 mm,5 μm) with the mobile phase consisting of methanol-water-acetic acid (55:44:2). The flow rate was 1.0 ml/min. The sample injection volume was 20 μl. The detective wavelength was 326 nm. Results The calibration curve of buddleoside showed good linear response ranged from 2.95 to 98.3μg/ml with r=0.9999 (n=5). The average recovery of spiked samples for buddleoside was 100.2% while the relative standard deviation for repetitions was 0.96%(n=15). Conclusion The method was sirepie, sensitive,reliable and repeatable,and could be used for the quantitative determination of buddleoside in Zhikuoyangyin granules.
Reform and practice of pharmacy experiment teaching materials
LIAO Chang-jun, ZANG Zhi-he
2012, 30(4): 310-312.
Abstract(2594) PDF (293KB)(514)
Abstract:
The characteristics of experiment in pharmaceutical specialties and the current situation that sonic experimental teaching courses were fragmented in pharmaceutical specialties were analyzed in this article.According to the general rules of the drug research and development, namely the raw materials-preparation-quality evaluation,the experiment content was made up by two pans:pharmaceutical foundational experiment and pharmacy comprehensive and designing experiment. By studying the whole process of the API to the finished product medicine. students could learn to use the modern detection means and method.take scientific evaluation for quality of API and preparation medicine,drug safety and effectiveness and learn how to get safe and effective drugs.
Exploration and practice of teaching tactics of research in experiment course for pharmaceutical specialties
DAI Wei-quan, ZHANG Ling, ZHOU Chang-jiang, GAO Yue, LU Ying, WANG Xiao-yan
2012, 30(4): 313-315.
Abstract(2564) PDF (307KB)(405)
Abstract:
Objective To build up the teaching tacties of research in experiment course for pharmaceutical specialties,which could promote the ability of practicing and innovation,and cultivate the talents combined with fundamental research,new drug development and production management. Methods Experimentation, investigation, operation and literature research methods were used.Results Teaching contents, organization forms and teaching platform of research teaching in experiment course for pharmaceutical speciaties were built up. Conclusion A marked teaching effects were achieved.
Exploration and optimization of content system of projected teaching material of Pharmaceutical Botany
HUANG Bao-kang, QIN Lu-ping, ZHENG Han-chen
2012, 30(4): 316-319.
Abstract(2579) PDF (388KB)(625)
Abstract:
Pharmaceutical Botany was a professional basic course of pharmacy major. Teaching material was the important part of teaching affair. The edit task of the projected teaching material in four editions had been taken up by us. The 5 th projected teaching material had been graded as national excellent teaching material,and had been widely used by many colleges. In the 6 th teaching material,some important contents were arranged and renewed to strengthen professional ethics education and practical teaching. The related teaching material of pharmaceutical botany had also been written to make the teaching material more close to the practice and satisfy the teaching course better.
2012, 30(4): 320-320.
Abstract(3155) PDF (127KB)(1171)
Abstract: