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    药物研究
  • 药物研究
    HU Chunling;TANG Yinping;SHI Jingni;LIU Yanwen
    2011, 30(5): 561-562.
    ObjectiveTo study the solidphase synthesis of the active antihepatic fibrosis peptides of Carapax Trionycis, and provide the theoretical basis for developing the medicines against hepatic fibrosis. MethodsSolidphase synthesis was carried out with resin Wang as a carrier, Fmoc as an amino acids protector. After condensed with the mix reagents of TBTV/NMM, deprotected with 20% priperdine, the crude produts of synthetic peptide were cut down from the wang resin by the cleared reagents TFA/TLS/H2O.ResultsThe purity of the target peptides was over 98% by RPHPLC analysis, the molecular weight of which was identical with the theoretical value by massspectrum identification. ConclusionThis synthesis method is mild, safety, efficient and easy to operate, which can be applied to the large scale synthesis of objective peptides.
  • 药物研究
    YANG Li;TANG Ying;CHEN Fang;ZHU Yiliang
    2011, 30(5): 563-565.
    ObjectiveTo investigate the long term effect of qiliandecoction granula on diabetic complications of rats.MethodsThe type 2 diabetes mellitus(T2DM)model was set up on rats by i.p. injection of streptozotocin(STZ)and feeding with high calorie food. Rats were treated with qiliandecoction granula for six months. The cognition and memory capability, renal function, urine protein,incidence of cataractous were tested. Pathological changes in kidney, brain and eyeguound were observed. ResultsLongterm administration of qiliandecoction granula attenuated the injury on cognition and memory capability, renal function, and decreased the excretion of urine protein and cataractous incidence. ConclusionQiliandecoction granula has a good therapeutic efficacy for T2DM, which can delay the development of diabetic complications and ameliorate the injury on organs and function of DM rats caused by long term dyslipidemia and hyperglycemia.
  • 药物研究
    SHAO Zhiling;HE Xuexin;XIANG Jinyi
    2011, 30(5): 566-570.
    ObjectiveTo observe the effects of urotensin II(UⅡ)on the cardiomyocytes hypertrophy and ERK/NFκB signaling pathway. MethodsThe neonatal rat cardiomyocytes were cultured, and the cell size was assessed by immunofluorescence; total protein was determined by coomassie brilliant blue and protein synthesis rate was measured by [3H]Leucine incorporation. ERK activity was measured by immunoprecipitation. The electrophoretic mobility shift assay(EMSA)was performed to detect the activity of NFκB. The expression of NFκB(p65)and pIκBα(NFκB inhibitor)phosphorylation were assessed by using Western blot. ResultsCompared with the control, UⅡ enlarged the cell size, raised total protein and protein synthesis rate; increased the phosphorylation of IκBα; upregulated activities of NFκB and ERK, elicited p65 expression. ConclusionThe hypertentrophic effect of UⅡ on cardiomyocyte hypertrophy was associated with enchancing the activity of ERK/NFκB signaling pathway.
  • 药物研究
    WANG Yaping;ZHAO Guangfeng;LIU Liu;LI Pengfei;HOU Yayi
    2011, 30(5): 570-573.
    ObjectiveTo investigate the effects of glossy gnoderma sore oil on the proliferation, apoptosis, miR16 expression of human lung adenocarcinoma LTEPa2 cell line, and explore its anticancer mechanism. MethodsThe LTEPa2 cells were treated with glossy ganoderma spore oil for 24 and 48 hours. The inhibition on cell growth was determined by using cell count kit(CCK8), cell morphological changes were observed by light microscopy, cell apoptosis was analyzed by flow cytometry, and the expression of miR16, Bcl2 and PDCD4 were determined by realtime PCR. ResultsGlossy ganoderma spore oil timeand dosedependently inhibited the LTEPa2 cells proliferation; changed the cell morphology obviously after the glossy ganoderma spore oil reached to 2 μL•mL1. Glossy ganoderma spore oil induced the LTEPa2 cells apoptosis even at a low concentration by AnnexinV/PI double stained detection; and it upregulated the expression of miR16 and downregulated the bcl2 and VEGF expression significantly. ConclusionGlossy ganoderma spore oil could inhibit the cell proliferation obviously and change the cell morphology, the mechanisms of which should be associated with upregulating the miR16 expression and downregulating the bcl2 and VEGF expression.
  • 药物研究
    XI Na;DUAN Tonghua;XI Chuanpo;YU Fa;HE Bin
    2011, 30(5): 573-577.
    ObjectiveTo study effects of penetration enhancers on the transdermal permeation of dexamethasone acetate chitosan gel. MethodsThe permeation enhancerfree group and enhancer added group were set up. There were 0.75% dexamethasone acetate and 5% chitosan gel in the permeation enhancerfree group. The permeation enhancer group was composed of 0.75% dexamethasone acetate and 5% chitosan gel, which subdivided into azone plus propylene glycol,azone,propylene glycol plus dimethyl sulfoxide,and dimethyl sulfoxide plus azone groups. Skin samples as permeability barriers were obtained from hairless rats for in vitro tests of the drug permeability. The permeation parameters,named as steady srate flux(Js)and Js enhancement ratio were evaluated. ResultsJs in the permeation enhancerfree group①was(3.75±0.56) μg•(cm2)1•h-1,and that in the permeation enhancer group were(8.12±0.58) μg•(cm2)•h-1(dimethyl sulfoxide plus azone group②)(5.41±0.74) μg•(cm2)1•h-1(Azone plus propylene glycol group③),(4.31±0.42) μg•(cm2)1•h-1(propylene glycol plus dimethyl sulfoxide group④),(4.35±0.36) μg•(cm2)1•h-1(azone group⑤,)respectively. Compared with ①,the Js enhancement ratio of ② was 2.17%(P<0.01),and the Js enhancement ratio were 1.51,1.89,1.87(P<0.05 or P<0.01), respectively, compared with③,④,⑤,which all showed significant differences. ConclusionThe mixed permeation enhancer has better permeation properties than the single enhancer.
  • 药物研究
    HONG Yi
    2011, 30(5): 577-581.

    ObjectiveTo prepare crosslinked microspheres of chitin/alginate particles and characterize the microstructure and morphology. MethodsThe crosslinked microspheres of chitosan and sodium alginate mixture were prepared. The microstructure and morphology were detected by using infrared spectroscopy(FTIR)and scanning electron microscopy(SEM). The drug slowly delivery property was studied with bovine serum albumin(BSA)as a drug model. Results It was showed that the chitin/alginate was well mixed and the crosslinked microspheres were formed under Ca2+ solvent. The encapsulation efficiency and release properties of the crosslinked microspheres were improved in comparison to the alginate microspheres, which being from 42% to 74% and drug release delayed from 4 h to 24 h. ConclusionThe chitin/alginate microspheres show pH responsive drug delivery properties, which release slowly under pH 1.2, and quickly under pH 7.0~7.4, and can be used in the colontargeted, drug delayed delivery system.

  • 药物研究
    SHI Shaojun;LIU Yani;WU Jianhong;ZENG Fandian
    2011, 30(5): 581-584.
    ObjectiveTo establish a HPLC method for determination of 6thioguanine nucleotides(6TGNs)in red blood cells(RBC). MethodsThe RBC samples were deproteinated by 70% perchloric acid. 6TGNs were hydrolyzed to 6thioguanine(6TG)by heating for 45 min at 100 ℃. Separation was carried out on Hypersil GOLD C18 column(4.6 mm×250 mm, 5 μm)with UV detection at 342 nm. The mobile phase consisted of 20 mmol•L1 KH2PO4(pH 3.3)acetonitrile(95:5, V/V)with flow rate of 1.0 mL•min1.ResultsThe linear relationship was occurred over the range of 8.09-809.89 pmol•(8×108)1RBC for 6TG (r= 0.997 8)and the limit of quantitation was 8.09 pmol•(8×108)1 RBC. The intra and interassay coefficients of variation were less than 7.71% and 6.64%, respectively. The mean analytical recoveries were 98.07%~108.08%, and the mean extraction recoveries were all more than 60%. ConclusionThis method is simple, rapid, sensitive and specific, which could be used for quantitation of 6TGNs in RBC from patients under AZA therapy.
  • 药物研究
    LIU Hongmei;WANG Zhiyong;ZHAO Hongguang;DU Xia;DONG Di;SONG Xiaodan;WU Linhua
    2011, 30(5): 584-586.
    ObjectiveTo set up a method of content determination for omeprazole in human plasma by HPLC and study the pharmacokinetics and relative bioavailability of omeprazole entericcoated capsules. MethodsA single dose of reference and test omeprazole entericcoated capsules was given to 20 healthy volunteers, respectively, in a randomized 2way crossover study. The plasma concentration of omeprazole was determined by HPLC and their pharmacokinetics as well as relative bioavailability was measured. ResultsThe main pharmacokinetic parameters of two formulations, reference and test ones were as follows: Cmax were(906.01±589.55 )and(875.87±662.95) ng•mL1, tmax were(2.21±0.88)and(2.07±0.87)h, AUC012 were(1 778.70±1 164.11)and(1 834.25±1 342.25)ng•h•mL1; t1/2 Ke were(0.96±0.25)and(0.85±0.18)h. The relative bioavailability of F0→12 was(104.02 ±13.60)%. ConclusionThe two kinds of omeprazole entericcoated capsules are bioequivalent.
  • 药物与临床
  • 药物与临床
    LIU Yong;XI Qingsong;ZHAO Jing;YU Shiying
    2011, 30(5): 598-601.
    ObjectiveTo compare the efficacy and toxicity between standard dose regimen and weekly dose regimen in the secondline treatment of refractory/resistant small cell lung cancer(SCLC). MethodsFiftytwo cases of refractory/resistant SCLC were enrolled, 28 cases were randomized to receive standard dose regimen of topotecan(TPT): TPT 1.5 mg•(m2)-1 iv gtt d15, in a cycle of 21 days; 24 cases were treated with weekly dose regimen: TPT 3.5 mg•(m2)-1 iv gtt d1,8,15, every 4 weeks(3 weeks on and 1 weeks off). The efficacy and toxicities were evaluated after two cycles. ResultsThe median survival time was 4.4 months in the standard dose group and 4.3 months in the weekly dose group, respectively( P>0.05). For the cases with standard dose regimen, the overall response was 2 cases. For the cases with weekly dose regimen, the overall response was 2 cases, too.There was no significant difference between two groups( P>0.05). Grade 3/4 neutropenia, thrombocytopenia and anemia occurred more frequently in the standard dose group; there was no statistical difference of grade 3/4 nonhaematological toxicities between two groups. ConclusionWeekly dose regimen of TPT for SCLC has a similar efficacy to the standard dose regimen, besides reducing haematological toxicities significantly.
  • 药物与临床
    LI Xuebin;LIANG Hui;HAN Ruquan
    2011, 30(5): 602-604.
    ObjectiveTo investigate the infusion of mannitol on plasma colloid osmotic pressure(COP) and electrolyte in patients undergoing craniotomy. Methods250 mL 20% mannitol was infused in forty eight ASA Ⅰ~Ⅱ patients undergoing elective craniotomy. The plasma COP and electrolyte were measured before infusion, just right after infusion, and 30 min after infusion. ResultsBy the end of the infusion, COP decreased significantly and increased again 30 min after infusion. K+ was increased and Na+ was decreased 30 min after infusion. Conclusion Infusion of mannitol during craniotomy may lead to a transient drop of COP, Na+ decline, and K+ elevation.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    CAI Hua;YANG Guangyi;DU Shiming;YE Fang;WANG Gang
    2011, 30(5): 629-632.
    ObjectiveTo optimize the best extraction condition for liposoluble and watersoluble ingredients in Salvia miltiorrhiza Bge. of fangling.MethodsThe semibioniccellulase zymolysis,alcohol and water dual extraction and integration extraction were compared by regarding the contents of TanshinoneⅡA,salvianolic acidB, total phenolic acid and extracta sicca in Salvia miltiorrhiza Bge. of fangling as indicators and referring to the reflux extraction(Chinese Pharmacopoeia 2010 ). ResultsThe semibioniccellulase zymolysis extraction was the most efficient technique. ConclusionSemibioniccellulase zymolysis for extraction of Salvia miltiorrhiza Bge. from fangling is the most scientific and suitable method.
  • 药物制剂与药品质量控制
    GUAN Shixia;LI Zhonggui;LI Haigang;CAO Liping;XU Shuqin;LI Dujun;YUAN Zhongwen;ZHOU Yubin;WU Liyuan
    2011, 30(5): 632-634.
    ObjectiveTo prepare doxycycline hydrochloride pellets by extrusion/spheronization technology and determine the pellets’ properties.MethodsDoxycycline hydrochloride pellets were prepared by using extrusion/spheronization. Influenitial factors and L9(34)orthogonal design was used to obtain optimal formulation.The pellets were coated with enteric coats by using the coated pot equipment.The micromeritic properties and in vitro dissolution of the pellets were determined.ResultsDoxycycline hydrochloride pellets obtained by extrusion/spheronization were round, smooth, even and on highyield.The release rate of the pellets coating weight at 15%,is lower 10% in the 0.1 mol•L1 HCl,while in buffer solution(pH 6.8)their release rate is over 80%.The dissolution test in vitro from the coated pellets was perfect.ConclusionThe process is easy and repeatable. The produced doxycycline hydrochloride pellets have an excellent intestinal solubility by a proper coating.
  • 药物制剂与药品质量控制
    LIU Ying;LIU Shumin;YU Donghua;LIU Lei;YANG Chao
    2011, 30(5): 635-637.
    ObjectiveTo research the isolate and purification craft of Consaponin of Dioscoreae Nipponicae, and provided the theoretical foundation and reference value to producing the beverage in industrialization.MethodsThe content of Protodioscin was chosen as index to the comprehensive assessment. To optimize the variety of macroreticular resin, different loading quantities, different sample concentration, eluent concentration ,elution volume.ResultsThe optimized craft was: D101 macroreticular resin, sample concentration 0.5 g•mL-1, loading quantities 2:1(macro reticular resin : crude drug of Dioscoreae Nipponicae), eluent concentration 50% alcohol, elution volume 14BV. ConclusionThis craft is simple and feasible with good reproducible and its active ingredients is more than 60%, and it can provide the basis for the production.
  • 药物制剂与药品质量控制
    ZHOU Wei;YU Yingjia;XIE Meifen;LI Xiaowen;LI Yan;DUAN Gengli
    2011, 30(5): 640-642.
    ObjectiveA method of microwave assisted extraction followed by HPLC was established for the determination of hesperidin of pericarpium citri reticulatae. MethodsThrough optimization of microwave assisted extraction method, the optimum conditions were as follows: extraction solvent of 50% DMSO aqueous solution, solidliquid ratio of 1:10, microwave power of 400 W, irradiation time of 3 min. A C18 column was used with the mobile phase of methanol0.2% trifluoroacetic acid solution (69:31, V/V) at the detection wavelength of 283 nm. ResultsThe calibration curve was linear in the range of 0.7-14.0 μg•mL-1. The average recovery was 101.75% with RSD of 2.53%. ConclusionThis method was simple, fast, accurate, and it is adapted to determine hesperidin of pericarpium citri reticulatae.
  • 药物制剂与药品质量控制
    SU Chi
    2011, 30(5): 642-643.
    ObjectiveTo establish a HPLC method for the determination of quercetin in rushu tablets.MethodsHPLC method was performed on Agilent Eclipse XDBC184.6 mm×250 mm5 μmcolumnwith mobile phase consisted of methanolwatercontaining 0.2% phosphotic acid)(4555.The flow rate was 1.0 mL·min1 and the detection wavelength was 370 nm.ResultsQuercetin showed a good linear over a range of 0.030.30 μgr0.999 9.The average recovery was 99.65% with the RSD of 1.85%n6.ConclusionThe determination method is simpleaccuratereliableand can be used to provide references for the quality control of rushu tablets.