Archive

• 01 November 2011 Volume 30 Issue 11

    

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  药物研究
  代谢性疾病用药专栏
  药物制剂与药品质量控制
  

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药物研究
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  药物研究

  Cardioprotective Effects and Mechanisms of Pentoxifylline

  HUANG Wei;LI Gui-xia;XIE Yan;QI Hanping;XING Yan

  2011, 30(11): 1401-1406.

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  ObjectiveTo investigate the protective effect of pentoxifylline against myocardial ischemia and detect its possible mechanisms.MethodsThe effects of pentoxifylline on myocardial ischemia were observed on a model of acute myocardial infarction by a permanent ligation of left anterior descending coronary artery in rats.MDA content and SOD activity were measured by ELISA method.Myocardium apoptosis was tested by TUNEL.Bcl2 and Bax protein expression were assayed by immunohistochemical and western blot.Laser scanning confocal microscopy was utilized to assay the effect of pentoxifylline on intracellular calcium concentration (［Ca2＋］i).ResultsPentoxifylline at 100 mg•kg1 shrunk infarct size of myocardium，decreased MDA content，increased SOD activity，improved heart function of rats with myocardial ischemia，upregulated Bcl2 expression as well (P＜0.01)，downregulated Bax expression (P＜0.01) ，and markedly inhibitted ［Ca2＋］i induced by 60 mmol•L1 KCl (P＜0.01).ConclusionPentoxifylline possesses protective effect on myocardial infarction in rats, the possible mechanisms of which are due to drop of ［Ca2＋］i and cardiomyocyte apoptosis inhibition.
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  药物研究

  Antioxidant Activity of Total Flavonoids from Alpinia katsumadai Hayata in Vitro and in Vivo

  WU Zhen;CHEN Yongshun;WANG Qibin

  2011, 30(11): 1406-1409.

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  药物研究

  Antiinflammation，Analgesia and Skin Irritancy of Nimesulide Ethosomes

  YAN Qinyuan;LI Lingyun

  2011, 30(11): 1410-1413.

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  药物研究

  Effect of Calcium Dobesilate on the Expression of Tubulointerstitial Fibronectin in Rats with Unilateral Ureteral Obstruction

  WANG Liping;SHEN Jianming;YE Tingting;TIAN Lin;TIAN Shaojiang;LI Junfeng

  2011, 30(11): 1414-1417.

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  ObjectiveTo assess the effects and mechanism of calcium dobesilate on the expression of fibronectin(FN) in the rat model of renal interstitial fibrosis(RIF) induced by unilateral ureteral obstruction(UUO).MethodsFortytwo SD rats were randomly divided into the shamoperated group，UUO model group， calcium dobesilate treated group (CDT).The RIF model was established by ligating left ureters of the animals.The renal fibrosis and FN expression were checked after 7 and 14 d, respectively.and immunohistochemistry staining was employed to study FN expression.ResultsFibrosis was developed in the renal interstitium of rats with obstructive nephropathy 7 d after operation(P＜0.01).FN expression was upregulated and enhanced 14 d after operation.Compared with those in the model group, the area of fibrosis was lessened and FN expression was attenuated in CDT group (P＜0.01).There were a positive correlation between the area of RIF and FN in left kidneys (P＜0.01).ConclusionCalcium dobesilate attenuates renal interstitial fibrosis due to downregulating FN expression of in UUO rats.
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  药物研究

  Hepatic Protection by Early Fluid Resuscitation with Hydroxyethyl Starch on Septic Shock in Newborn Rabbits

  YU Jinfen;YE Xiaofeng;YU Ling;CAO Wei

  2011, 30(11): 1418-1421.

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  ObjectiveTo study the hepatic protective effect of early fluid resuscitation with hydroxyethyl starch(HES) on septic shock in newborn rabbits.Methods60 New Zealand longear newborn rabbits received cecal ligation and puncture (CLP)were randomly divided into three groups(20 rabbits/group):group I(CLP without liquid)，group II(CLP， HES 10 mL•kg1 plus lactate Ringer’s injection 20 mL•kg1)，group III(CLP，HES 30 mL•kg1).The right carotid artery of rabbits were annulated with a microtip transducer for continuous recording of MAP during the experiment process.The left carotid vein was catheterized to infuse the fixed fluid for 1 hour.Arterial blood samples were taken for blood gas analysis, liver was stained with HE and observed under microscope, and NFκB protein levels in hepatic tissue were measured at 8 h after CLP.ResultsCompared with MAP at 0 h, which gradually decreased in group I.No obvious change of blood pressure appeared in both group Ⅱ and Ⅲ.In comparison to group I, blood pressure was elevated after 2 h in group II and Ⅲ(P＜0.05).The artery PaO2 was higher in groupⅡ and Ⅲ than that in group I(P＜0.05).No significant difference in pH and PaCO2 were found among three groups.The expression of NFκB protein in hepatocyte was stronger in group I than that in group Ⅱ and Ⅲ, and which was more in group Ⅲ than in group Ⅱ(P＜0.05).ConclusionEarly fluid resuscitation with HES, especially at 10 mL•kg1 prosessed protective effect on septic shock in newborn rabbits.
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  药物研究

  Effect of Flos Lonicerae Extracts on Herpes Simplex Keratitis

  LIU Ying;WANG Guoli

  2011, 30(11): 1421-1424.

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  ObjectiveTo study therapeutic efficacy of Flos Lonicerae extracts on herpes simplex keratitis.MethodsA model of Vero cells infected with herpes simplex virusⅠ(HSVⅠ) was established.The in vitro antivirus effect of different doses of Flos Lonicerae extracts was evaluated by using cytopathic effect (CPE) and therapeutic index (TI) .In vivo model of rabbit corner keratitis induced with herpes simplex (HSK) were established.Rabbits were treated with Flos Lonicerae extracts，Acyclovir(ACV) and normal saline for 15 days, respectively.The rabbit cornea was checked after dyeing with flouresceinnatrium under slitlamp.ResultsIt was showed that the Flos Lonicerae extracts possessed distinct antiHSVⅠ effect on Vero cells，TC0 of which was 384 mg•L1and TI was 26.56.Compared with the model group in vivo，both Flos Lonicerae extracts and ACV significantly reduced severity of HSVⅠdendritic keratitis，shortened healing time of HSK.There was no statistical significance between Flos Lonicerae extracts and ACV (P＞0.05).ConclusionFlos Lonicerae extracts are effective against HSK.
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  药物研究

  Security and Pharmacodynamic Test of Yam Shenqi Pill in Treating Type 2 Diabetic Rats

  XU Yanbo;GAO Yongxi;YAO ping;LIU Chaohua;WANG Peng;LI Meng;MA Kuan

  2011, 30(11): 1425-1429.

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  ObjectiveIn order to provide a theoretical basis for the clinical application of yam shenqi pill，we evaluated the therapeutic effect and safety of yam shenqi pill.MethodsThe experimental acute and longterm toxicology testing of different doses of yam shenqi pill in normal rats, and the establishment of rat model of type 2 diabetes observed yam shenqi pill on blood glucose and blood lipids.ResultsIn the acute toxicology experiment, various mice’s outward appearance, the behavior, the breath, four extremity activities, the feed, the excretion have not seen obviously exceptionally; In the longterm toxicology experiment, the yam shenqi pill treatment groups compared with the control group, in the blood, blood biochemistry and histology were no significant differences (P＞0.05), the treatment of blood glucose (Glu) were significantly reduced (P＜0.01 or P＜0.05); large, medium dose group and the metformin group can lower total cholesterol (CHO), triglyceride (TG), low density lipoprotein (LDL) levels, a significant difference between results (P＜0.05) each treatment group compared with the model of highdensity lipoprotein (HDL) levels tended to increase, but the result was no significant difference.ConclusionAcute and chronic toxicity test found no toxicity yam shenqi pill type 2 diabetic rats significantly reduced the Glu, TG and CHO content, prompted by the proposed use of yam shenqi pill, dosage, treatment efficacy in clinical applications precise and safe.
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  药物研究

  Material Foundation of Ixeris Chinesis (Thunb) Nakai for Treating Diabetic Complications in Rats

  DI Zizhen;WANG Guanghan;JIANG Hong;ZOU Guixin

  2011, 30(11): 1429-1431.

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  ObjectiveTo study the material foundation of ixeris chinesis (Thunb) Nakai for treating diabetic complications in rats.MethodsThe diabetic rats were treated with different extracts of ixeris chinesis (Thunb) Nakai.The glycolated hemoglobin and fructosamine were tested and which were referred as dependent variable,the relative area for 36 common peaks of extracts as independent variable for the correlation determination by SPSS software.ResultsAfter treatment, the glycolated hemoglobin in rats treated with nbutanol extracts, ethyl acetate extracts and water extracts were (13.71±1.57)%,(13.44±1.18)% and (12.81±0.87)%,respectively;the fructosamine were(0.23±0.01) and （0.23±0.02） mmol•L1 by nbutanol extracts and ethyl acetate extracts, respectively, which were lower than that in the model and positive groups.The glycolated hemoglobin of positive control (metformin and shenqi sugar declining granule) were（10.77±1.60）% and（12.40±1.36）%, respectively,which was significantly fewer compared with the model group(P＜0.05).The related coefficience of the active substances and extracts of ixeris chinesis (Thunb) Nakai was determined by statistics software.ConclusionIt’s primarily demonstrated that the chromatographic peaks significantly related to the reduction of glycolated hemoglobin and fructosamine are the material foundation of ieris chinesis (Thunb) Nakai，and the molecules corresponding to the peaks may share the same or similar functional groups that are medium polar molecules.
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  药物研究

  Study on Bioequivalence of Nicotinic Acid SustainedRelease Tablets

  SHU Chengren;DENG Bin;ZHOU Xueping;LI Weiyong

  2011, 30(11): 1432-1434.

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  ObjectiveTo establish a method for determination of nicotinic acid in human plasma and study its bioequivalence in Chinese healthy volunteers.MethodsThirty healthy volunteers were orally administered with 1 500 mg nicotinic acid (test) tablets in a randomized crossover design.The drug levels in plasma samples were determined by a HPLCMS/MS method.ResultsThe main pharmacokinetic parameters of the test and reference preparations were as follows：AUC0→15 was (20 046.1±16 286.8)，(21 605.0±18 058.5) ng•h•mL1, AUC0→∞ was (20 806.0±16 300.7) and (22 811.2±18 468.3) ng•h•mL1；Cmax was (8 716.3±6 811.2) and (9 570.2±8 217.1) ng•mL1；tmax was (4.414±1.337) and (4.310±1.285) h；t1/2 was (4.000±4.898) and (2.906±3.393) h.The relative bioavailability of the test tablet was (96.6±30.9) %.ConclusionThe domestically made nicotinic acid tablets and those imported are bioequivalent.
代谢性疾病用药专栏
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  代谢性疾病用药专栏

  Effect of Gout Decoction on 100 Cases of Primary Gout

  MEI Shasha;SONG Enfeng

  2011, 30(11): 1437-1439.

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  ObjectiveTo investigate the clinical curative effect of selfmade traditional Chinese medicine on patients with gout.Methods200 patients were divided into 2 groups with random number and 100 patients in each.The treatment group was treated with the selfmade traditional Chinese medicine and the control one with western medicine, continuously for 4 weeks.Then the efficacy and laboratory data were investigated.ResultsThe total effective rate of the treatment group was 89.0% and significantly higher than that in the control group(68.0%,P＜0.05).The blood uric acid, β2M, hemoglobin (Hb), pH of urine, and 24hour urinary protein were obviously improved in comparison to those in the control group（P＜0.05）.ConclusionThe selfmade traditional Chinese medicine is effective for gout.
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  代谢性疾病用药专栏

  A Preliminary Study on Treating Subacute Thyroiditis with Prednisolone under the Guidance of Ultrasound Elastography

  XU Chenke;WANGGang;FANG Jianhua;BAO Lingyun;ZHU Luoxi;ZHAN Yuhong

  2011, 30(11): 1439-1442.

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  ObjectiveTo explore the clinical effect of treating subacute thyroiditis with prednisone under the guidance of ultrasound elastography.MethodsFortysix patients suspected of subacute thyroiditis (SAT) received fine needle aspiration biopsy(FNAB) under the guidance of ultrasound elastography，and thirtynine patients diagnosed with SAT were randomly divided into two groups: the control group received prednisone according to clinical symptoms，and the tested group received prednisone under the guidance of ultrasound elastography.Patients of both groups were followup for twelve months after drug discontinuation.ResultsPatients with SAT had mild to moderate thyroid enlargement in affected side，some patients had bilateral thyroid enlargement.Patients in both groups showed no side effect in the process of treatment.The curative rate of tested group and control groups were 96.77% and 71.43%，respectively, which showed significant difference between two groups(P＜0.05).There were no significant differences on dosage and course of prednisolone between two groups (P＞0.05).ConclusionThe sonographic image of patient with SAT has a characterized manifestation.Using ultrasound elastography to observe the efficacy of prednisone for patients with SAT has an important clinical implication on guidance for drug usage.
药物制剂与药品质量控制
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  药物制剂与药品质量控制

  Determination of Paeoniflorin and Albiflorin in Different Germplasms and Parts of Peony Root

  ZHOU Xuegang;CHEN Shuxin;WEI Donghua;SUN Shiqin;ZONG Ming

  2011, 30(11): 1477-1480.

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  ObjectiveTo compare the content and distribution of paeoniflorin and albiflorin in different germplasms and parts of peony root under the same analysis.MethodsThe HPLC method was taken by using Lichro CART RPC18（4 mm×250 mm，5 μm）column with HCN 0.1% phosphoric acid(V：V=14：86) as mobile phase，flowing at 1.0 mL•min-1，with the detection wavelength as 230 nm, column temperature at 30 ℃ and loading volume as 10 μL. ResultsPaeoniflorin and albiflorin in different germplasms were quite different.It was showed that rhizoma＞fibrous root＞axial root in terms of peoniflorin contained in peony root; fibrous root＞rhizoma＞axial root in terms of albiflorin in different parts of radix paeonia alba.ConclusionThe main reason for content difference of paeoniflorin and albiflorin was germplasms.There is small variation for paeoniflorin and albiflorin in geoauthentic product area of germplasm.
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  药物制剂与药品质量控制

  Quality Evaluation of Polysorbate 80 by a Differential Scanning Calorimetry

  HAN Rong;LI Meng;ZHANG Haiyan;QI Yun;YANG Ming;LIAO Yonghong

  2011, 30(11): 1481-1484.

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  ObjectiveTo investigate the applicability of differential scanning calorimetry (DSC) to evaluate the quality of polysorbate 80.MethodsEight different brands of polysorbate 80 were characterized by DSC, and the melting points and peak shape of polysorbate 80 were analyzed.The hemolysis of rabbit in vitro induced by polysorbate 80 was determined with ELISA at 540 nm，whilst the muscle irritation was tested by using creatine kinase (CK) kit following exposure of L6 cells with polysorbate 80.ResultsDSC thermograms showed an excellent reproducibility for the same brand and same batch of polysorbate 80 with the RSD of melting points within 5%.In addition，they were sensitive and distinguished difference between batches or brands of polysorbate 80.DSC thermograms was directly related to the quality.Different batches of polysorbate 80 presented different DSC thermograms, demonstrating differences within constituents of samples, which was confirmed by the results of hemolysis and muscle irritation.ConclusionDSC has the potential to be utilized as a semiquantitative means for the quality evaluation of polysorbate 80.
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  药物制剂与药品质量控制

  Determination of Berberine Hydrochloride in Jieze Lotion by HPLC

  MA Yonggui;XIE Wei;FANG Jianguo;CHEN Zhuo

  2011, 30(11): 1484-1486.

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  ObjectiveTo establish a HPLC method for determination of berberine hydrochloride in jieze lotion.MethodsChromatography was carried out on a column of the Phenomsil ODS (4.6 mm×150 mm，5 μm), with a mobile phase as Mentol0.1%Phosphoric Acid(40：60).The flow rate was set at 1.0 mL•min1, and the detection wavelength was at 265 nm; The sample was loaded for 10 μL and column temperature was 40 ℃.ResultsA good linearity of berberine hydrochloride was obtained within 2.53－101.20 μg•mL1; The average recoveries of berberine hydrochloride was 102.88%(RSD=2.13%)，98.01%(RSD=0.17%)，100.15%（RSD=2.57%）（n=3），respectively.ConclusionThe method is simple，rapid，sensitive and accurate, which can be used for quality control of berberine hydrochloride in jieze lotion.
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  药物制剂与药品质量控制

  A Study on Ultrasonic Extraction Techniques for Total Flavonoids from Nymphaea candida Presl

  JIN Xiaohong;GENG Wei;GUI Hongwu

  2011, 30(11): 1487-1489.

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  ObjectiveTo optimize the ultrasonic extraction for total flavonoids from Nymphaea candida Presl.MethodsThe optimum process was determined with the single factor experiment and orthogonal test by evaluating effect of ethanol concentration，ratio of materia/extraction solution，extraction course, times and amount of total flavonoids extracted.ResultsThe remarkable factors affecting total flavonoids extraction from Nymphaea candida Presl.included ethanol concentration，ratio of materia/extraction solution，extraction times and extraction duration.The optimum extraction for total flavonoids from Nymphaea candida Presl.was using 80% ethanol，keeping the ratio of materia/extraction solution as 1：16，making extraction for 5 times and 30 minutes in each time.ConclusionThe optimum process is stable and reproducible.
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  药物制剂与药品质量控制

  Isolation and Purification of Total Triterpenoidic Acid from Longtube Ground Ivy Herb with Macroporous Resin

  TAO Feng;ZHOU Renyi;WU Mingxi;XIA Jie;ZHANG Yi;HUANG Junjun;ZHANG Rusong

  2011, 30(11): 1490-1493.

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  ObjectiveTo explore the optimal condition for purification of total triterpenoidic acid from Longtube Ground Ivy Herb with macroporous resin.MethodsGradient solution of alcohol was used to elute total triterpenoidic acid absorbed on macroporous resin guided by the purification degree and recovery rate with UVspectrophotometric method.ResultsThe best way for purification of total triterpenoidic acid was obtained by using AB8 type macroporous resin as absorption agent and 80 mL 70% ethanol pH 6 as an eluent.ConclusionThe method is the basis for industrial purificaiton of total triterpenoidic acid from Longtube Ground Ivy Herb.
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  药物制剂与药品质量控制

  Measurement of Formaldehyde in Formaldehyde and Cresol Solution by Spectrophotometry

  GONG Xuepeng;HUANG Lihua;SHI Chunyang

  2011, 30(11): 1493-1495.

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  ObjectiveTo set up a method for detecting formaldehyde in formaldehyde and cresol solution.MethodsBased on a yellowpurple complex with a specific absorption wavelength at 413 nm yielded by reacting with NH+4 and acetylacetone, the formaldehyde in formaldehyde and cresol solution was measured by spectrophotometry.ResultsThere was a good linearization between the absorbency from UV and formaldehyde within 4.39～30.73 μg , R2=0.999 9.The average recovery was 99.4% and RSD 1.4%.ConclusionThe method is accurate, simple, rapid, specific and can be used to measure formaldehyde in formaldehyde and cresol solution.
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  药物制剂与药品质量控制

  Preparation and Quality Control of Ionsensitive in Situ Gel of Indometacin for Eye Use

  GUO Fengguang;HAO Jifu;XIAO Jianhua;WANG Jianzhu;LI Fei;YAO Xin

  2011, 30(11): 1495-1498.

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  ObjectiveTo study the preparation of ionsensitive in situ gel of indomethacin for eye use by using sodium alginate as matrix and hydroxypropyl methyl cellulose（HPMC）as thickener, and investigate the quality standard and in vitro release of indomethacin gel.MethodsTo prepare ionsensitive in situ gel of indomethacin for eye use and screen the best matrix of gel by comparing ratios of sodium alginate to HPMC.To determine content of indomethacin with UV spectrophotometic method and study on characteristics and mechanism of drug release by a dialysis technique.ResultsCompared with indomethacin solution， the release time of indomethacin in situ gel was prolonged to 8 h and the amount reached to 93%.ConclusionThe in situ gel of indomethacin produced by sodium alginate and HPMC with a suitable ratio is stable, unirritated and has a slowrelease and long term effect.

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  药物制剂与药品质量控制

  Quality Control of Qinyu Shaoshang Solution

  CAI Xiaocui;HE Jinhua;LI Weiqiang;MAO Yan;

  2011, 30(11): 1499-1501.

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  ObjectiveTo establish methods for identification of Cortex Phellodendri amurensis and Borneolum syntheticum，and for content determination of baicalin in qinyu shaoshang solution.MethodsCortex Phellodendri amurensis and Borneolum syntheticum were identified by TLC.The content of baicalin in Radix Scutellariae was determined by HPLC.ResultsThe TLC spots of Cortex Phellodendri amurensis and borneolum syntheticum were clear，reproducible and specific.The linear range of baicalin was 8.046－80.46 μg•mL1(r=0.999 5) with an average recovery of 101.0% (RSD=1.69%，n=6). ConclusionThe established standard can be used for quality control of qinyu shaoshang solution.