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    药物研究
  • 药物研究
    FANG Ying;DUAN Xue-yun;WANG Hong-fei;FAN Heng;LIU Yan-wen
    2011, 30(10): 1259-1262. https://doi.org/10.3870/yydb.2011.10.001
    Objective To study effects of 8-hydroxy resin glycosides from Valeriana officinalis L.on Kv1.5 potassium channel currents. Methods The Kv1.5 HEK293 cells currents following the administration of 8-hydroxy resin glycosides at 10 and 30 μmol.L-1 were recorded by using the wholecell patch clamp recording technique. Results 8-hydroxy resin glycosides (10 and 30 μmol.L-1) decreased Kv1.5 HEK293 cells currents in a dosedependent manner.The peak currents (148.3±13.0) PA/PF was reduced to (109.4±4.4) PA/PF and (78.6±11.3) PA/PF, which resulted in the suppression ratio of 28.5% and 37.1% , respectively. Conclusion 8-hydroxy resin glycosides blocks Kv1.5 HEK293 cells currents dose dependently, which may contribute to the antiarrhythmic effects of Valeriana officinalis L..

  • 药物研究
    HUANG Shan;JIANG Chun-yan;LONG Fei
    2011, 30(10): 1262-1265. https://doi.org/10.3870/yydb.2011.10.002
    Objective To study the anti-inflammatory and analgesic effect of volatile oil from Nepeta angustifolia. Methods Fifty mouse or rats were randomly divided into five groups, as the control (treated with distilled water), positive control (with prednisone 5 mg or aspirin 8 mg), Nepeta angustifolia groups( with volatile oil of Nepeta angustifolia at 0.125, 0.250, 0.500 mL.kg-1 as highdose, medium-dose and low-dose).Models of mouse ear edema induced by xylene, rat paw edema induced by carrageena and mouse granuloma were used to study the anti-inflammatory effects.The acetic acid caused writhing and hot-plate test in mouse were taken to study the analgesic effects. Results The inhibitory rates of volatile oil from Nepeta angustifolia at high, medium and low doses and the prednisone group on the xylene-induced mouse ear edema were 24.73%, 21.45%, 15.83%, 27.63%, respectively, which on granuloma in mouse were 42.72%, 34.70%, 25.37%, 55.93%, respectively.With the inflammation prolonged, paw swelling increased continually and significantly in the control group, but not in the volatile oil of Nepeta angustifolia groups.The writhing were (13.08±4.64), (14.83±6.03), (17.75±4.35), (5.17±2.52) , (21.92±4.14) times in high-dose, medium-dose and low-dose group, aspirin group, the control group, respectively.And the pain threshold in the high-dose, medium-dose and low-dose group of volatile oil were extended at 30, 60, 90, 120 min after administration, compared with the control group (P<0.01). Conclusion The volatile oil from Nepeta angustifolia possesses obviously anti-inflammatory and analgesic effects.

  • 药物研究
    WANG Gang;CHANG Ming-quan;YANG Guang-yi;ZENG Nan;YE Fang
    2011, 30(10): 1266-1269. https://doi.org/10.3870/yydb.2011.10.003
    Objective To prepare long circulating nano-liposomes of quercetin(QUE-LCL) and investigate the physical and chemical properties and oral absorption in mice. Methods The QUE-LCL was prepared by the emulsified evaporationlow temperature solidification method with Glyceryl behenate(ATO) and Tween 80 as carriers and the optimum formulation selected by orthogonal test.Its morphology was examined by transmission electron microscope(TEM) and the particle diameter distribution was detected.The quereetin determination in nanoparticles and the mixture of gastrointestinal contents and feces by HPLC were established. Results QUE-LCL was spherical shape with mean diameter of 172.63 nm and entrapment efficiency was 91.77%.The oral absorption of QUE-LCL in mice was better than that of quercetin suspension and common liposomes. Conclusion The emulsified evaporationlow temperature solidification is suitable for preparing QUE-LCL,and the preparation of which made by orthogonal test promotes the oral absorption of quercetin in mice.
  • 药物研究
    HOU Yun-tian;HAO Guang-tao;ZHENG Zhuan-jie;LIANG Hai-xia;MA Meng;ZHU Li-jun;LIU Ze-yuan
    2011, 30(10): 1269-1272. https://doi.org/10.3870/yydb.2011.10.004
    Objective To establish a simple and sensitive high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method for determination of terazosin in human plasma. Methods The plasma samples were precipitated with the liquid extraction by tertbutyl ether and then were injected directly into the HPLC–MS/MS system.Inertsil C18 column (2.1 mm×150 mm,3.0 μm) was used, and methanol- 2 mmol.L-1ammonium acetate (90:10) was taken as the mobile phase by gradient elution.Terazosin and the internal standard (prazosin) were separated by HPLC and quantitated by MS/MS by using electrospray ionization (ESI) and multiple reaction monitoring (MRM) in the positive ion mode.The most intense [M-H]+ MRM transition of terazosin at m/z 388.4→m/z 247.4 was used for quantitation, and the transition at m/z 384.2→m/z 231.3 was used to monitor prazosin. Results The liner range of terazosin was 0.2-50 ng.mL-1(r= 0.9973), while the minimal detectable plasma concentration was 0.2 ng.mL-1.The average recovery was between 98.83% and 100.67%.Intra-day and inter-day RSD were less than 15%.Low, medium and high absolute recoveries were 75.40%, 70.28%, 67.39%, in line with biological sample analysis requirements. Conclusion This method is simple, sensitive and accurate, which is suitable for the study of pharmacokinetics of terazosin in human plasma and urine.
  • 药物研究
    PAN Hai-min;FANG Hui-hua;YAN Shi-hai
    2011, 30(10): 1273-1274. https://doi.org/10.3870/yydb.2011.10.005
    Objective To investigate the effects of total flavones from Bindens bipinnata L.on rabbit platelet aggregation. Methods Platelet aggregation was induced by adenosine diphoshate (ADP) or thrombase (Thr), the inhibitory effects and dose-dependent relationship of total flavones from Bindens bipinnata L.were observed in vitro by turbidimetric method. Results The high and middlle dose of total flavones from Bindens bipinnata L.significantly suppressed the maximum platelet agglutination induced by ADP (P<0.01), while the blocking rate of blood platelet aggregation was 45.82% and 28.65%, respectively.Additionally, these two doses of total flavones also demonstrated a strong restriction on the maximum platelet agglutination induced by Thr (P<0.01), in which the curbing rate of blood platelet aggregation was reached to 48.36% and 33.82%, respectively.Total flavones exhibit a dose dependent manner. Conclusion Total flavones from Bindens bipinnata L.possesses powerful inhibitory abilities against the platelet aggregation induced by ADP and Thr in vitro.

  • 药物研究
    SHAO Zhi-ling;HE Xue-xin;XIANG Jin-yi
    2011, 30(10): 1275-1278. https://doi.org/10.3870/yydb.2011.10.006
    Objective To observe effects of Urotensin Ⅱ (U Ⅱ) on phenotypic transition of cardiac fibroblasts. Methods In the primary culture of neonatal rat cardiac fibroblasts(CFs), as indexes of phenotypic transition, type I collagen was assessed by ELISA, α-SMA expression were assessed by immunoblotting and immunocytochemistry; ERK phosphorylation was determined by immunoblotting.Moreover, we evaluated the effect of ERK inhibitor PD98059 on the promotion of U Ⅱ in CFs phenotypic transition. Results U Ⅱ can enhance the type I collagen level, α-SMA and ERK phosphorylation.After PD98059 treatment, α-SMA expression was obviously depressed. Conclusion Urotensin Ⅱ can induce phenotypic transition of cardiac fibroblasts, the mechanisms are associated with enhancing ERK phosphorylation.
  • 药物研究
    HU Chun-ling;TANG Yin-ping;SHI Jing-ni;LIU Yan-wen
    2011, 30(10): 1278-1280. https://doi.org/10.3870/yydb.2011.10.007
    Objective To evaluate the synthesis of peptide of Carapax Trionycis and its effects on hepatic stellate cells (HSC). Methods Based on the sequence of active peptide of Carapax Trionycis, the peptide was produced by using solidphase synthesis method and purified by RP-HPLC.HSC cell line T6 was incubated with the synthetic peptide at different concentrations for 24 hours.Cell apoptosis was detected by flow cytometry with annexin V-FITC/PI double staining. Results Purity of the synthetic peptide obtained by RP-HPLC was over 98.0%, while its molecular weight was identical with theoretical value by massspectrum identification.The numbers of apoptotic cells and the necrotic cells were elevated when treated with 0.6 mg.mL-1 and 2.5 mg.mL-1 of synthetic peptide, respectively.The apoptotic cells showed more with the peptide in a dosedependent manner.The synthetic peptide at 1.2, 2.5 and 5.0 mg.mL-1 significantly upregulated the early apoptotic rate of HSC (P<0.05). Conclusion Peptide of Carapax Trionycis could be synthesized and induces early apoptosis of HSC.

  • 药物研究
    ZHOU Wu;ZHANG Jun-feng;WANG Tao
    2011, 30(10): 1281-1285. https://doi.org/10.3870/yydb.2011.10.008
    Objective To study the effects of propofol, a clinical commonly used sedative, on angiotensin Ⅱ (Ang Ⅱ)induced cardiomyocyte hypertrophy and ROS/JNK1/2 (c-Jun N-teminal kinase1/2, JNK1/2)signaling pathway. Methods In the primary culture of neonatal rat (1-2 d) cardiomyocytes, cell diameter was assessed by phase contrast microscope; protein synthesis rate was measured by [3H]Leucine incorporation as indicator of cardiomyocyte hypertrophy.The level of reactive oxygen species (ROS) was detected by 2,7dichlorofluorescein diacetate(DCFH-DA).NADPH oxidase (Nox) activity was tested by chromatometry.The phosphorylation of JNK1/2 were assessed by using Western blot. Results Ang Ⅱ significantly enhanced the cell size, total protein synthesis rate; increased the level of ROS and Nox activity; upregulated the JNK1/2 phosphorylation.The effects mentioned above were inhibited by propofol. Conclusion Propofol suppresses Ang Ⅱinduced cardiomyocyte hypertrophy in neonatal rats, which may be associated with downregulating ROS/JNK1/2 signaling pathway.

  • 药物研究
    HU Xue-lian;YU Tao;XING Mao;LEI Jian;CHEN Lin;ZHANG En-juan
    2011, 30(10): 1285-1287. https://doi.org/10.3870/yydb.2011.10.009
    Objective To establish a HPLC method for investigating the dissolution of lappaconitine hydrobromide dispersible tablets. Methods Dissolution of 3 batches of lappaconitine hydrobromide dispersible tablets was detected by using small cup method with distilled water as solvant, rotation rate at 50 r.min-1 and UVVis at 252 nm, which was compared with the commercial lappaconitine hydrobromide tablets. Results The linear range of lappaconitine hydrobromide was 9.76-73.20 μg.mL-1 (r=0.999 7).The average recovery was 100.3%.The same batch showed good uniformity, and the dissolution of different batches were all above 80.0% within 10 min. Conclusion This method is simple, sensitive and accurate, which can be used in the quality control of lappaconitine hydrobromide dispersible tablets.The dissolution rate of dispersible tablets is faster than the commercial lappaconitine hydrobromide ones.
  • 药物与临床
  • 药物与临床
    LI Ke-zhen;FANG Yong;GONG Mei;JIN Xin;FENG Ling
    2011, 30(10): 1301-1304. https://doi.org/10.3870/yydb.2011.10.016
    Objective To investgate the preventive effects of three frequently used 5-HT receptor antagonists for chemotherapyinduced gastrointestinal reactions and adverse effects, providing information for proper clinical use of antimetic drugs. Methods A total of 468 patients with ovarian cancer receiving TP chemotherapy were divided into group A of 172, group B of 138 and group C of 158 based on antimetics regimen accepted prior to chemotherapy.Patients of group A were intervenous drop infusion 2 mg of tropisetron 15-30 minutes before chemotherapy; patients of group B were intervenous drop infusion 50 mL of azaseron 15-30 minutes before chemotherapy; patients of group C were intervenous drop infusion 50 mL of granisetron 15-30 minutes before chemotherapy.Antemetic was intervenous drop infusioned slowly once a day during the whole duration of chemotherapy.Compare the condition of the curative effect and the adverse reaction after received different 5-HT receptor antagonists respectively. Results The effective rates of nausia inhibition between granisetron, tropisetron and azasetron were 84.30%,82.61% and 81.02%, respectively; The effective rates of vomiting inhibition between these three kinds of antemetics were 98.26%, 98.55%, 97.47% and the total incidence of adverse reactions were 13.37%, 13.04%, 13.29%, respectively.No significant difference was noted in nausea and vomiting inhibition and the total adverse reaction among three kinds of 5-HT receptor antagonists; for the vomiting complete remission rate, group B was much higher than group C; for the constipation reactions, the effect rate of azasetron and tropisetron were significantly higher than granisetron. Conclusion The effects of inhibiting nausea and vomiting among three kinds of 5-HT receptor antagonists were similar.For patiens with significant vomiting, azasetron is the best option.It should be noted that in the cause of the treatment of azasetron, patients should drink more water and take laxative treatment p.r.n.due to high incidence of constipation it caused.
  • 药物与临床
    NIU Ben;TIAN Yu-ke
    2011, 30(10): 1304-1307. https://doi.org/10.3870/yydb.2011.10.017
    Objective To study the effects of methoxamine plus ephedrine on preventing the hypotension following spinal anesthesia for cesarean delivery and on the neonate. Methods 100 patients undergoing elective cesarean section were randomly divided into two groups: intravenous injection (i.v.) of ephedrine 12 mg (group E) after spinal anesthesia; and i.v.methoxamine 1mg plus ephedrine 6 mg (group EM).The heart rate and blood pressure of the parturients were monitored continually; the anesthesia level, nausea and vomiting were recorded; collect umbilical artery for blood gas analysis.Umbilical artery blood pH, Apgar score of 1 min and 5 min were collected after delivery. Results The incidence of hypotension was 68.0% (group E) vs.46.0% (group EM) (P<0.05),respectively. Rate of tachycardia was 82.0% (group E) vs. 16.0% (group EM) (P<0.01), respectively. Rate of nausea and vomiting, umbilical artery blood pH and Apgar score showed no statistical significance between the two groups. Conclusion The combination of ephedrine and methoxamine is superior to ephedrine used alone in preventing or treating hypotension of healthy parturients undergoing cesarean delivery, and has no side effect on neonate.
  • 药物与临床
    CHEN Jing;CHEN Ye-shan;YANG Kun-yu;YIN Zhong-yuan;WANG Qiong
    2011, 30(10): 1307-1309. https://doi.org/10.3870/yydb.2010.10.018
    Objective To study the clinical effect of recombinant human epidermal growth factor solution in combination with crushed trimethoprimsulfamethoxazole tablet for external use on radiodermatitis in nasopharyngeal carcinoma patients. Methods The data of 62 patients with nasopharyngeal carcinoma, who had undergone radical radiotherapy and developed grade 3 to 4 radiodermatitis, were retrospectively analyzed. The treatment goup (n=32) were given recombinant human epidermal growth factor solution at 4 000 U.10 cm2)-1 plus application of crushed trimethoprimsulfamethoxazole onto the wound surface, while the patients in the control group (n=30) received only 4 000 U.(10 cm2)-1 of Genetime sprayed onto the wound surface twice a day in the morning and night. In both group, the medicines were used till the wound surface was dry and crust shed off. The change of the radiodermatitis and healing time were observed and recorded at fixed time points twice a day. The efficacy and side effects in the two groups were compared. Results The average healing time of skin desquamation was 3.2 days in the treatment group and 7.5 days in the control group, with difference being statistically significant (P<0.01). No obvious side effect was observed in both groups. Conclusion The treatment of recombinant human epidermal growth factor combined with trimethoprimsulfamethoxazole for radiodermatitis is safe and effective.
  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    ZHAO Peng;ZHANG Li-hua;LI Xiao-rong;LI Lin;LI Jin
    2011, 30(10): 1328-1332. https://doi.org/10.3870/yydb.2011.10.025
    Objective To screen the optimum method for deproteinationof polysaccharide from Limonium bicolor Kunze. Methods The proteins were removed from polysaccharide by four different Methods including trichloroacetic acid, Sevage, papain and papainSevage. Results PapainSevage method was the optimal one, in which deproteination rate was 83.72% while 80.25% of polysaccharide was remained.The optimum conditions for deproteinization were: hydrolysing the substrates with 2.0% papain (pH 7.0) at 75 ℃ for 2 hours, and repeated 3 times with Sevags method. Conclusion The PapainSevage is the best deproteination method for purifying polysaccharide.

  • 药物制剂与药品质量控制
    HOU Zhen-shan;CAI Lv-lv;PAN Jin-huo
    2011, 30(10): 1332-1334. https://doi.org/10.3870/yydb.2011.10.026
    Objective To establish a method for content determination of total alkaloids in ganershu by a purification progress. Methods The total alkaloids were determined by acidic dye colorimetry using synephrine as the reference.The detection wavelength was 415 nm. Results The linear range of synephrine was 117.5-352.4 μg, while the average recovery was 98.68% (RSD=1.60%). Conclusion This method is simple and reliable, which can be applied for the content determination of total alkaloids in ganershu.

  • 药物制剂与药品质量控制
    LI Yan
    2011, 30(10): 1335-1337. https://doi.org/10.3870/yydb.2011.10.027
    Objective To study the optimum preparation technology for barnidipine hydrochlorideβ-cyclodextrin(BN-β-CD) inclusion complexation. Methods Saturated aqueous solution method was used to prepare BN-β-CD inclusion complexation, orthogonal design was carried out to optimize the preparation technology by taking the drug loading capacity and inclusion efficiency as the evaluation index. Results The preparation conditions were optimized by orthogonal experiment as follows: barnidipine hydrochloride: β-cyclodextrin being 1:2, stirring speed was 200 r.min-1, inclusion temperature at 70 ℃, mixing time as 2 h. Conclusion The method can be used for preparation of BN-β-CD inclusion complexation, in which the dissolution rate of the inclusion complex made by the optimized preparation process increased significantly.

  • 药物制剂与药品质量控制
    WANG Wen-qing;LIN Meng;WANG Lin-zhi;WANG Qiu-lan;FANG Jian-guo;SHI Chun-yang
    2011, 30(10): 1338-1340. https://doi.org/10.3870/yydb.2011.10.028
    Objective To establish a HPLC method for quantitative determination of dihydroartemisin in tablets. Methods Shimadzu VPODS column (250 mm×4.6 mm, 5 μm) was used, and acetonitrilewater (60:40) was taken as the mobile phase with a flow at 0.8 mL.min-1 and a wavelength at 210 nm.The column temperature was 35 ℃. Results There was a good linear relationship of dihydroartemisin at the range from 500.2 to 2 501.0 μg.mL-1 (r=0.999 9).The average recovery was 99.5% (RSD=1.25%, n=9). Conclusion This method is accurate, sensitive and reproducible, which could be used for the quantitative determination of dihydroartemisinin tablets.

  • 药物制剂与药品质量控制
    MA Ya-zhong;WU Yan;LIU Li-ping;Lin Xiang-yang
    2011, 30(10): 1340-1343. https://doi.org/10.3870/yydb.2011.10.029
    Objective A simple sample pretreatment method was developed for the determination of clindamycin phosphate and tretinoin in Acne Gel by hollow fiberHPLC. Methods The gel sample pretreatment was carried out by hollow fiber.The chromatographic analysis was carried out on a Venusil XBP-C18 column(150 mm×4.6 mm,5 μm)with acetonitrile and potassium dihydrogen phosphate buffer solution(the pH value was adjusted to 3.0 by phosphoric acid)as the mobile phase by gradient elution at a flow rate of 1.0 mL.min-1.The column temperature was 30 ℃ and sample size was 20 μL.The detection wavelength of clindamycin phosphate and tretinoin in Acne Gel were set at 210 nm and 350 nm, respectively. Results The good resolution between peaks of main drugs and of the adjacent purity was obtained.Good linear relations in determination of clindamycin phosphate and tretinoin were obtained in the range of 48.00-480.00 μg.mL-1 (r= 0.999 8) and 1.00-20.00 μg.mL-1 (r=0.999 7),respectively.Meanwhile,the average recovery were 99.96%(RSD=0.69%,n=6)and 99.99%(RSD=1.24%,n=6). Conclusion This method is simple and accurate, and it’s suitable for the sample pretreatment and content determination of mian drugs in acne gel.
  • 药物制剂与药品质量控制
    2011, 30(10): 1345-1346. https://doi.org/10.3870/yydb.2011.10.031
  • 用药指南
  • 用药指南
    HU Dun-mei;DU Guang;WANG Zhen;DING Yu-feng
    2011, 30(10): 1357-1360. https://doi.org/10.3870/yydb.2011.10.037
    Objective To evaluate the rationality of clinical use of antimicrobial drugs according to application of antibiotics in outpatient prescriptions. Methods With a retrospective survey and antibiotics clinical application monitory network of the Ministery of Health, fixed number of outpatient prescriptions was randomly selected from the year of 2006-2009, and the ratio of different drug categories, consumption amount, combined usage of drugs, administration routes, DDDs and daily drug costs (DDC) were calculated. Results During the four years, only one antimicrobial drug was used in most prescriptions, and the ratio was kept over 85%. There was little change in the total consumption amount of the antimicrobial drugs, but there existd the elevating trend of consumption amount of antibiotics prescriptions. The antibiotics of β-lactam and quinolone were widely used, the ratio of these two was over 60% by years. The utilization rate of the generic names had increased from 19% to 52%. Conclusion The use of antibacterial drugs in our hospital is generally rational. The antibiotics monitoring should be kept on. At the same time, the use of generic names should be still enhanced and the supervision of drug costs should be enfored.