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2010 Vol. 28, No. 3

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2010, 28(3): 161-163,188.
Abstract(2269) PDF (709KB)(2066)
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2010, 28(3): 164-166,180.
Abstract(1995) PDF (210KB)(1321)
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2010, 28(3): 167-169,195.
Abstract(2223) PDF (214KB)(1289)
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Optimization study on preparation technology of falcate crazyweed herb cream
CHEN Jian-da, HONG Jia-ni, DU Qing-yun
2010, 28(3): 170-172.
Abstract(2378) PDF (191KB)(690)
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Objective To optimize the formulation and preparation process of falcate crazyweed herb cream of O/W type. Methods The orthogonal experimental design is applied.By investigating the emulsification conditions impacting the quality and stability of the cream as well as the adding amount of active ingredient impacting the UV absorption property,the optimum preparation process and the best prescription are determined. Results When the ratio of emulsifier span-60Tween-80 was 20:35,the oil phase and water phase are added respectively.When the emulsifying temperature was 80 ℃,the emulsion can gain stable quality and uniformity texture.When the adding amount of the total flavones reaches 2.5%(w),the obtained cream has a good stability and good UV absorption. Conclusion Both stability and UV absorption property of the product are satisfactory,which is expected to be developed further into a new kind of natural sunscreen articles.
Influence of danshensu on hemodynamics of anesthetic dog
CHEN Wei-zhong, CHEN Da-gui, JIAO Yong, ZHANG Chuan
2010, 28(3): 173-176.
Abstract(2106) PDF (276KB)(370)
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Objective To observe the influence of danshensu-sodium injection on the hemodynamics of anesthetic dog including heart rate,blood pressure,cardiac systolic/diastolic function. Methods The hemodynamics of dog after injected danshensu-sodium injection(2,4,8 mg/kg)were measured by cardiac catheter method respectively.Hemodynamics index such as heart rate(HR)、systolic arterial pressure(SAP)、diastolic arterial pressure(DAP)、mean arterial pressure(MAP)、left ventricular systolic pressure(LVSP)、mean left ventricular pressure(MLVP)、the maximal change rate of left intraventricular pressure(±dp/dtmax)、and left ventricular end diastolic pressure(LVEDP)was analysed. Results Danshensu-sodium injection can increase LVSP、±dp/dtmax remarkably,has no significant influence on SAP、DAP、MDP.And heart rate slows down obiviously in the high dosage group. Conclusion Danshensu-sodium injection can improve the cardiac function significantly through decreasing cardiac load and myocardial consumption of oxygen.
Pharmacokinetics of levofloxacin in beagle dogs with open abdominal wound by different seawater immersion process
WANG Qianga, ZHANG Yia, SHANG Li-qun, YU Ji-yaoc, YU Cun-linga, WANG Da-pengb
2010, 28(3): 177-180.
Abstract(2254) PDF (270KB)(456)
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Objective To compare the pharmacokinetics of levofloxacin(LVFX) between beagle dogs with open abdominal wound by seawater immersion for different time and normal dogs. Methods Twelve healthy beagle dogs were randomly divided into control group(A group,n=4),open abdominal wound and immersion for 45 min group(B group,n=4) and open abdominal wound and immersion for 90 min group(C group,n=4).The beagle dogs in B group and C group were immersed into artificial seawater for 45 or 90 min before administered,respectively.All the animal were administered a single dose of LVFX(25 mg/kg) by infusion into saphenous vein for 90 min.LVFX in plasma at different sampling time was determined by HPLC,at the same time,the temperature of animal was monitored.The pharmacokinetic parameters were calculated by 3P97 software and examined by SPSS 12.1 program. Results The temperature of animal in B and C group dropped significantly compared with A group in immersion process and after immersion,and these drops temperature were increased along with the extension of immersion process.The plasma concentration-time curve of three groups were fit to a two-compartment model with the main pharmacokinetic parameters as follows: Cmax were(30.05±1.75),(36.10±4.74)and(42.34±4.19) mg/ L,t1/2β were(8.23±0.65),(11.02±0.54) and(13.19±3.87) h,AUC were(247.00±14.10),(345.22±56.68) and(417.79± 83.32) mgoh/ L,Vc(6.97±2.02),(6.68±1.67) and(7.82±1.62) L,ClS(1.20±0.15),(1.06±0.12) and(0.92±0.15) L/ h,respectively.In comparison to A group,t1/2β and AUC of B group was increased remarkably(P<0.05,respectively),and t1/2β,Cmax and AUC of C group was also increased remarkably,respectively.(t1/2β,P<0.01;Cmax,AUC,P<0.05).At the same time,there was sinificantly difference in t1/2β between B group and C group(P<0.05). Conclusion Metabolism and elimination of LVFX in open abdominal wound by seawater immersion was obviously decreased when the immersion process was increased,and hypothermia in beagle that immersion led to might be invovled in these events.
Study on the protection mechanism of UTP against cerebral ischemia reperfusion injury in rats
TIAN Mou-lia, LI Tie-junb, LIU Hua, ZOU Zuia, SHI Xue-yina
2010, 28(3): 181-183,234.
Abstract(1876) PDF (272KB)(463)
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Objective To observe the protective effect of uridine 5'-triphosphate(UTP) on cerebral ischemia reperfusion(IR) injury in rats. Methods The injury model of middle cerebral artery occlusion(MCAO) was established by suture method.UTP were delivered through tail venousr via microinfusion pump 30 min after the occlusion of MCA at a rate of 5 ml/(kg·min).Neurological deficit score(NDS) and brain water content were determined 24 h after reperfusion.The effect of UTP on the contraction of rat arteria carotis in vitro was examined. Results The protective effect of UTP on cerebral ischemia reperfusion showed a dose-dependent relationship.The 90 μg/kg group of UTP had the best protective effect among the 3 groups.The effect of UTP on the contraction of rat arteria carotis in vitro showed that UTP can significantly reduce the blood vessel tension induced by PE. Conclusion UTP has a dose-dependent protective effect on cerebral IR,which may be related to the expansion of the blood vessels of the infarct area.
Study on preparation and dissolution of andrographolide self-emulsifying drug delivery soft capsules
MENG Hui, XU Yong
2010, 28(3): 184-185,208.
Abstract(2379) PDF (189KB)(1021)
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Objective To prepare the andrographolide self-emulsifying drug delivery soft capsules(ASESC) and evaluate its quality. Methods The andrographolide self-emulsifying soft capsules were prepared.To screen the dissolution of andrographolide,the dissolution media and dissolution method of Ch.P were analysied.The dissolution of SMESC was measured,taking the commercial capsule as reference. Results The self-emulsifying drug delivery system was composed of ethyl oleate(10%),Tween 80(54%),n-Butanol(36%).The percent of accumulated dissolution of andrographolide in self-emulsifying drug delivery soft capsules in 0.2% SDS fluid was up to 70% at 45 min,which was far more than the commercial capsule. Conclusion The andrographolide self-emulsifying drug delivery capsules has been successfully prepared,and the dissolution of andrographolide was remarkably improved.
Determination of trehalose in Candida albicans by HPLC-MS
DONG Ling-ling, CAO Ying-ying, CHAI Yi-feng
2010, 28(3): 186-188.
Abstract(2223) PDF (215KB)(585)
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Objective To establish a high performance liquid chromatography-mass spectrum(HPLC-MS) method to determine trehalose in the biofilm of Candida albicans. Methods Shisheido CAPCELL NH2(150 mm×4.6 mm,5 μm) was used in this method and the mobile phase is 75% acetonitrile and 25% pure water.MS detector with an ESI ion source in negative mode was used. Results It has a good separation of trehalose and internal standard,and there is no interference of endogenous impurity.Linear was from 0.05~50 μg/ml(r=0.999 3),recovery was in the range of 81.50% to 96.29% and the RSD of precision is less than 2.1 %. Conclusion This method is a simple method for quantification of trehalose in fungus.
The protective effect of wikstromol on cultured cortical neurons induced by H2O2 and excitatory neurotransmitter
YE Li, ZHU De-qiu, YE Xian-cheng
2010, 28(3): 189-192.
Abstract(2455) PDF (283KB)(472)
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Objective To identify the material basis of the novel neuroprotective compounds from traditional chinese medicine Daphne giraldii in the treatment of neurodegenerative disorders.

Methonds Activity-guided fractionation of several chromatographic techniques were used for the isolation of the neuroprotective compounds.The cultured cortical neurons of rats were used as screening system. Results The methanolic extract from dried roots of Daphne giraldii significantly mitigated the neurotoxicity induced by L-glutamate,kainic acid and 2O2 in this screening system.The neuroprotective compound was identified as wikstromol.At a concentration of 50 μM,wikstromol significantly reduced neurotoxicity induced by 2O2.Wikstromol significantly reduced the decrease of glutathione,superoxide dismutase,and other enzymes that participate in the cellular defense against oxidative stress.Furthermore,wikstromol alleviated neurotoxicity induced by the excitotoxic neurotransmitter,L-glutamate and kainic acid,but not that mediated by N-methyl-D-aspartate. Conclusion Wikstromol was demonstrated to be efficacious in protecting neurons from oxidative stress.The neuroprotective mechanism of wikstromol may due to its antioxidant effect.
Experimental studies on anti-inflammatory and analgesic action of the Tongmaiyushang capsule
WU Xue-bin, YU Hui-hua, Tang Liang, YOU Ben-ming
2010, 28(3): 193-195.
Abstract(2376) PDF (264KB)(369)
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Objective To study the anti-inflammatory and analgesic effects of Tongmaiyushang capsule. Methods Tumidness of small rat ears was induced by dimethylbenzene.Acute and chronic inflammation of rats were induced by carrageenin and tampon embedding respectively.The pain model was made by hot plate and writhing tests.Animals were divided into five groups: the blank control group;the positive control group;the low,middle and high dose of Tongmaiyushang capsule groups to investigate the anti-inflammatory and analgesic effect of the Tongmaiyushang capsule. Results The capillary permeability was decreased and the effusion of inflammatory mediator was reduced in small rat.Tumidness of small rat ears caused by dimethylbenzene and inflammation reaction induced by carrageenin were significantly inhibited with the reduction of leukocytes.The hyperplasia of granulation tissue in rats was also be inhibited.The capsule could improve the threshold of pain,prolong the incubation period of pain,decrease the quantity of body wrest of small rats.The analgesia rate of three groups was 49.6%,43.5%,33.3%,respectively. Conclusion Tongmaiyushang capsule has good anti-inflammatory and analgesic effects.
Simultanous determination of curculigoside and curculigoside B in the rhizome of Curculigo orchioides from different regions by HPLC-DAD
Zeng Qian, Ji Hui
2010, 28(3): 196-198.
Abstract(2513) PDF (211KB)(324)
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Objective To determine the content of curculigoside and curculigoside B in the rhizome of Curculigo orchioides from different regions,and provide scientific basis for production and clinical application of these medicinal materials. Methods According to the characteristic of geographical distribution of Curculigo orchioides,12 medicinal materials from different locations as well as 6 commercial medicinal materials were collected.The method of HPLC-DAD was used to determine the content of curculigoside and curculigoside B. Results There have significant varieties in the content of curculigoside and curculigoside B among 12 collected Curculigo orchioides samples and 6 commercial medicinal materials.For collecting samples,the content of curculigoside and curculigoside B were 0.028%0.538% and 0.103%0.330% respectively.For commercial samples,the content of curculigoside and curculigoside B were 0.161%0.733% and 0.033%0.123%,respectively.The contents of curculigoside were higher in commercial samples than in collecting samples. Conclusion There have significant varieties in the content of curculigoside and curculigoside B in 12 collected Curculigo orchioides samples which indicated that the quality of Curculigo orchioides may be related with geographic location where it grows,climates,growing and collecting times,and the method of process and storage.
Determination of ephedrine and pseudoephedrine in Xuanfei Qingre mixture by HPLC
LIU Hui-jun, CHEN Rui, WANG Juan
2010, 28(3): 199-200,205.
Abstract(2833) PDF (213KB)(811)
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Objective To set up a method of simultaneously determining the contents of ephedrine and pseudoephedrine in Xuanfei Qingre mixture(Herba Ephedrae,Semen Armeniacae amarum,Bulbus Fritillaria thunbergii,Radix scutellaria,etc). Methods The HPLC-quantitative analysis was carried out on a column of Agilent ZORBA× SB-CC18 by using a mobile phase of acetonitrile-0.02 mol/L potassium dihydrogen phosphate(adjusted with phosphoric acid pH=2.7),(4100,with 0.1% triethylamine)under a flow rate of 1.2 ml/min.207 nm was selected as the wavelength of detector. Results The linear range of ephedrine was 11.04~222.8 μg/ml(r=0.999 9)and pseudoephedrine's was 8.27~165.4 μg/ml(r=0.999 9).The recoveries of them were all between 95% and 105%(RSD<3%). Conclusion This method is simple,reproducible and specific.
Determination of residual organic solvents in orlistat by headspace gas chromatography
WEN Yan, WEN Jun, TAO Xia
2010, 28(3): 201-202.
Abstract(2117) PDF (147KB)(539)
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Objective To establish a method for determination of four residual organic solvents in orlistat. Methods The residual organic solvents in orlistat are hexane、heptane、methanol and acetonitril.They were quantitatively determined by headspace gas chromatography(GC) on HP-INNOWAX column with FID detector,nitrogen as the carries. Results Four residual solvents were completely separated.There was a good linearity in the experimental concentration(r=0.999 0~0.999 3).The RSD of precision was less than 10%.The average recovery rate ranged from 97.1% to 101.9%.The detection limits was between 0.009~1.833 μg/ml. Conclusion The method proves to be rapid,sensitive and accurate.It can be used for quality control for the determination of four residual organic solvents in orlistat.
Orthogonal design of formula optimization for Huanggui enema
DENG Li-qin, ZHANG Yan
2010, 28(3): 203-205.
Abstract(2219) PDF (166KB)(492)
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Objective To choose the best formula for Huanggui enema. Methods The orthogonal test was used to optimize formula,and the clearance index in mice and antibacterial action in vitro were observation index.The best formula was designed according to the result of this study. Results The formula is: Rhizoma Coptids 60 g,Cortex phellodendn 180 g,Ramulus Cinnamoni 120 g,Radixet Rhizoma Rhei 48 g per 1 000 ml.The clearance index in mice is greater 20%,diameter of inhibition zone is greater 35 mm. Conclusion The optimized formula is reasonable and provided an experimental basis for clinical application.
Effect on gel microcolumn assay of ceftazidime IgM and IgG in human serum with red cells packed by drug under different pH
LIN Guan-yang, GUO Hong, YU Lei
2010, 28(3): 206-208.
Abstract(2139) PDF (223KB)(834)
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Objective To observe the effect on gel microcolumn assay of ceftazidime IgM and/or IgG in human serum with red cells packed by drug under different pH. Methods Drug-coated red blood cells were prepared by incubating 10 volumes of ceftazidime in the barbital buffer solution(pH=7.0,8.0,9.6) for 2 hour at room temperature.600 human serum samples were prepared for the drug-coated red cells test which the incubation pH was 9.6,and 10 samples were selected according to the Results .Among 10 samples three were positive,four were negative,the others were week positive All were tested by the drug-coated red cells which the incubation pH was 7.0 or 8.0. Results In the three week positive samples,one of them becomes negative when the incubation was pH8.0;all of them become negative when the incubation was pH7.0.The other seven were no different between the incubation pH was 9.6 or 8.0 or 7.0. Conclusion The Results of gel microcolumn assay of ceftazidime IgM and /or IgG in Human Serum may be false negative when the incubation pH is lower than 9.6.
Optimization of extraction process of compound Shuiniujiao granule by orthogonal test
CAO Wen, XU Dao-long, LI Tie-jun
2010, 28(3): 209-210,222.
Abstract(1933) PDF (164KB)(495)
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Objective To select the best extraction process in preparation of compound Shuiniujiao granule. Methods The extraction solvent,add water,extraction times and extraction time as the study factors,each factor orthogonal design method developed three horizontal,and use the Results of the corresponding pharmacodynamic evaluation of the efficacy of each role in a process,combined with the yield and the actual production process to select the best. Results 50% ethanol,plus 8 times the amount of extracted three times,each time a small process when the compound derived from buffalo horn grain yield of preparation and pharmacodynamics of the most satisfactory Results. Conclusion Orthogonal design and the corresponding pharmacodynamic Results of the experiment to select the extraction process is a reasonable approach should be advocated.
2010, 28(3): 211-212,214.
Abstract(1662) PDF (172KB)(1364)
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Compatible stability of glucose and sodium potassium chloride injection mixing with cefepime Hydrochloride for injection
WEI Jing-hai
2010, 28(3): 213-214.
Abstract(2360) PDF (390KB)(551)
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Objective To study the stability of glucose and sodium potassium chloride injection(GNK) mixing with cefepime hydrochloride in room temperature. Methods RP-HPLC was applied to determine the content change of cefepime hydrochloride in different time.The pH,quantity of non-soluble particulate and appearance of mixtures were also observed. Results In room temperature the mixtures produced neither gas nor sediment.The pH,quantity of non-soluble particulate and content did not change within 8 hours. Conclusion The mixtures of GNK mixing with cefepime hydrochloride are stable in 8 hours.
The complex forming ability of medium substituted degree hydroxypropyl-β-cyclodextrins on dexamethasone
ZHANG Yue
2010, 28(3): 215-216,240.
Abstract(2524) PDF (295KB)(831)
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Objective To investigate synthesis of medium substituted degree hydroxypropyl-β-cyclodextrins and the complex forming capability of dexamethasone. Methods Medium substituted degree hydroxypropyl-β-cyclodextrins were prepared and tested by pharmacopoeia.Dexamethasone were included with the product and performed by the phase-solubility diagram. Results The substituted degree of hydroxypropyl-β-cyclodextrins were 7.875.Dexamethasone was formed a 11 molar ratio inclusion complex with the product and improved solubility about 33 times. Conclusion The product accord with the request of pharmacopoeia.The dissolution capability of dexamethasone was increased by hydroxypropyl-β-cyclodextrins.
Synthesis of hairpin-polyamides containing β-alanine
LI Peng
2010, 28(3): 217-219,231.
Abstract(2576) PDF (363KB)(390)
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Objective To develop a new method and strategy for the synthesis of hairpin-polyamides containingβ-alanine. Methods The hairpin-polyamides were synthesized by the HOBT/DCC coupling reaction in good yields through the optimization of hydrogenation of nitro group and the 2+2 fragment coupling strategy. Results A hairpin-polyamide NO2ImPyβImPyγImPyβPyPyβCOOC2H2 was synthesized successfully with good yield. Conclusion The hairpin-polyamides containing β-alanine in the molecular can be easily and efficiently synthesized through the optimization of reaction temperature,solvent and fragment coupling strategy.
Synthesis and anoxia endurance activity of thiadiazole derivatives
ZHU Zhan-zhou
2010, 28(3): 220-222.
Abstract(2613) PDF (519KB)(280)
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Objective To design and synthesize novel thiadiazole derivatives and evaluate their anoxia endurance activity. Methods Beginning with thiosemicarbazide,title compounds were synthesized in three steps,then the anoxia endurance activity was evaluated. Results and Conclusion Seven novel thiadiazole derivatives were synthesized and their anoxia endurance activity was evaluated.One of the title compounds exhibited the same anoxia endurance activity as that of acetazolamide,which can be used as the lead for further study.
Comparison of total alkaloids content of Fructus Broussonetia from different habitats
PANG Su-qiu
2010, 28(3): 223-224.
Abstract(2198) PDF (130KB)(238)
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Objective To compare the total alkaloids content of Fructus Broussonetiae from different habitats. Methods Total alkaloids were isolated by acid-ethanol and determined by acid dye colorimetry method under 410nm. Results The calibration cure of alkaloids was linear(r=0.999 5),the recovery rate was 98.52% and RSD was 0.91%.The total alkaloids content of Fructus Broussonetia from different habitats was 7.98~23.53 mg/g. Conclusion The total alkaloids content of Fructus Broussonetiae from different habitats was significantly different.
Study on the chemical constituents of Crinum latifalium
WEN Qian
2010, 28(3): 225-227.
Abstract(1989) PDF (172KB)(351)
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Objective To investigate the chemical constituents of Crinum latifalium. Methods The chemical constituents of methanol extract of C.latifalium were seperated by various chromatography Methods.The structures of these chemical constituents were identified by spectral data and physicochemical property. Results 15 compounds were respectively identified as:-sitosterol(1),daucosterol(2),5-Methyl-2,4(1H,3H)-pyrimidinedione(3),-purine(4),p-hydroxybenzonic acid(5),ethyl 4-hydroxybenzoate(6),cinnamyl D-glucopyranoside(7),benzyl-D-glucopyranoside(8),adenosine(9),uridine(10),Z-cinnamic acid(11),5-O-nitrosouridine(12),3-methyl-1H-pyrimidine-2,4-dione(13),N-methyl-benzamide(14),E-cinnamic acid(15). Conclusion Compounds 3-4,7-10,12-14 were isolated from C.latifalium for the first time.
2010, 28(3): 228-231.
Abstract(1705) PDF (194KB)(321)
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2010, 28(3): 232-234.
Abstract(1809) PDF (177KB)(255)
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2010, 28(3): 235-240.
Abstract(1778) PDF (419KB)(1293)
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