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    药物研究
  • 药物研究
    YANG Dan-li;LI Shu-hui;ZHANG Hai-gang;YANG Xiao-jiao;HAO Li-yun;JIANG Lin-lin;LI Xiao-hui
    Objective To study the effect and mechanisms of monocrotaline( MCT) on the pulmonary arterial pressure. Methods Eighteen SpragueDawley male rats were randomly divided into normal control group (n=7) and model group (n=11). Animals in the model group were given with a single dose of MCT (50 mg•kg-1) subcutaneously. Hemodynamic parameters such as pulmonary arterial systolic pressure (PASP), pulmonary artery diastolic pressure (PADP), mean pulmonary arterial pressure (MPAP) and right ventricular systolic pressure (RVSP) were measured by right catheterization with Powerlab on the 22nd day. The heart was separated into the right ventricle (RV) and left one with septum (LV+SEP) and weighed separately. RVHI was calculated as the weight ratio of RV/(LV+SEP). The weight ratio of lung to body weight was calculated. Immunohistochemical analysis was performed on paraffinembedded left lung tissue to detect the expression of αsmooth muscle actin (αSMA) and Ⅷ factor on pulmonary endangium. Results The PASP, PADP, MPAP and RVSP were elevated significantly (P<0.01) in the 50 mg•kg-1MCTtreated rats as compared with the normal control animals. The similar changes were observed for the values of LI and RVHI (P<0.01). Immunohistochemical analysis showed MCT effectively increased the expression of αSMA antigen in pulmonary arteries (PAs) and lead to PAs remodeling. In addition, MCT also could effectively decrease the expression of Ⅷ factor antigen in the endomembrane of PAs and lessen the number of pulmonary capillary. Conclusion MCT (50 mg•kg-1) can satisfactorily make the model of pulmonary artery hypertension and the mechanism of which may be related to the PA remodeling and the loss of pulmonary capillary.
  • 药物研究
    REN Xiu-hua;CAO Lei;SI Lu-qin;QIU Jun;LI Gao
    Objective To establish a HPLC method for determining 1’-hydroxymidazolam and optimize the incubated conditions for rCYP3A4. Methods 1’-hydroxymidazolam was determined by RPHPLC. Single effect experimental design was used to optimize the incubated conditions and the enzyme kinetics was evaluated by graphical analysis with LineweaverBurk double reciprocal plots (1/velocity vs. 1/ [substrate]). Results Calibration curves of 1’-hydroxymidazolam were linear in the range of 18.20-1 820.00 ng•mL-1 ( R2= 0.999 9). The optimal incubated conditions were 5 μmol•L-1, 10 pmol and 10 min for midazolam concentration, rCYP3A4 and incubation time, respectively. The enzymic kinetic parameters of rCYP3A4 were 0.96 μmol•L-1 for Km and 0.78 pmol•min-1 for Vmax. Conclusion The HPLC method is simple, accurate and rapid, suitable for the determination of 1’-hydroxymidazolam in rCYP3A4. The incubated conditions of rCYP3A4 and its kinetics can be applied for study on the drug interaction metabolized by CYP3A and effects of others on it.
  • 药物研究
    YU Jian-qiang;LI Yu-xiang;ZHAO Chen-jun;JIN Shao-ju;WANG Feng;JIANG Yuan-xu
    Objective To observe the effect of oxysophoridine (OSR) on the alterations of EEG and its power spectrums of amygdala in anaesthetized rat. Methods With the equipment of brain stereotactic apparatus, microelectrode was implanted into amygdala. Unipolar lead and computerized FFT technique were employed to record and analyze the effect of oxysophoridine on the bioelectricity change of amygdala in rats. Results The EEG of amygdala was mainly characterized with low amplitude and slow waves accompanied by spindleformed sleeping waves while the total power reduced remarkably(P<0.01) and the basic frequency shifted backward(P<0.05). The ratio of α and β waves to total frequency increased significantly(P<0.05) in rats administrated(icv) with oxysophoridine at the dose of 2.5,5.0,10.0 mg for each rat. Conclusion Oxysophoridine possesses central inhibitory effect and the mechanism may associate with reduction of bioelectricity in amygdala as well as alteration of frequency distribution.
  • 药物研究
    CHEN Sha-sha;LIU Xi-jiang;CAO Fei;XIAO Xing-peng;TIAN Xue-bi;TIAN Y-ke
    Objective To study the analgesic effects of local anesthetic ropivacaine by intracerebral injection in a rat model of bone cancer pain. Methods After the model of bone cancer pain was made, intracerebral guide cannula were implanted into the RVM (rostral ventromedial medulla). Von Frey filaments, Pin Prick test, Ambulatory pain were used to measure the pain thresholds before and after ropivacaine microinjection. Results Pain thresholds were significantly decreased in rats with bone cancer pain. After intra RVM administration of 0.5% ropivacaine, mechanical allodynia, mechanical hyperalgesia and ambulatory pain were attenuated and the pain behavior were significantly reversed. Conclusion Intra RVM administration of ropivacaine produces remarkable analgesic effects in a rat model of bone cancer pain. Thus, the RVM is critical for the development and maintenance of bone cancer pain.
  • 药物研究
    BU Shu-hong;ZHANG Jian;LU Xiao-tong;WANG Min;LIU Yan
    Objective To investigate the correlation between carbamazepine concentration, clinical therapeutic effect and CYP3A activity. Methods Hydrocortisone(HC) and 6hydroxy hydrocortisone (6β-OHC) in urine were detected by HPLC, 6β-OHC was used to test the activity of CYP3A. The concentration of carbamazepine in serum was assayed by FPIA, and the correlation of CYP3A activity, carbamazepine level and clinical effects was analyzed. Results The concentration of carbamazepine in serum showed a good correlation with lgCA, r= 0.846, and the patients with low activity of CYP3A showed better clinical therapeutic effect. Conclusion The activity of CYP3A in seizure patient could be helpful to predict the concentration of carbamazepine in serum and its clinical therapeutic effect, and guide individualization of drug therapy.
  • 药物研究
    CHEN Zhi-li;LUO Gao-jiang
    Objective To investigate the function of dendritic cells(DC)in patients with acute myocardial infarction (AMI)and the effects of simvastatin on it. Methods 32 patients with AMI were divided into two groups, who were treated regularly and with normal medicines plus simvastatin, respectively.PBMC from the AMI patients(before and 2 weeks after the treatment)and 12 healthy subjects were incubated and induced to mature DC in a completed medium containing GM-CSF an d IL-4.Flow cytometric analysis was used to detect the expression of co-stimulating factor CD86(B7-2)on DC.The stimulating capacity of DC was determined in allogenic mixed lymphocyte reaction(MLR).ELISA was used to analyze the level of cytokines(IL-1,IL-6,IL-10 and TNF-α)in the medium of MLR.Relationship of expression of CD86 to risk factors and blood hs-CRP level was also analyzed. Results Compared with normal group,CD86 on DC was much more expressed in AMI patinets;the stimulating capacity of DC in MLR was higher;T lymphoeytes in MLR secreted higher levels of pro-inflammation cytokines(IL-1β,IL-6 and TNF-α)and lower level of anti-inflammation cytokine(IL-10).Blood LDL-C before treatment was positively related to the expression of CD86.Simvastatin inhibited the function of DC and lowered blood level of hs-CRP and CD86,the levels of which were significantly positively correlated. Conclusion DC in AMI are activated, which may play an important role in initiating immune reaction in the plaque.LDL-C may be one of the activators of DC; inhibitory effect of simvastatin on inflammation in AMI may be due to inhibition on DC.
  • 药物研究
    WANG Xian-ying;YANG Jie;LI Xue-jing
    Objective To investigate anti-inflammatory, detumescent and analgesic effects of gubining capsule and provide the basis for its clinical application. Methods The anti-inflammatory and detumescent effects were studied by xyleneinduced swelling of ear in mice and carrageenaninduced swelling of voix pedis in rats. Twisting reaction times in mice induced by acetic acid and pain threshold after heat stimulation were investigated. Results Gubining capsule inhibited swelling of ear in mice and that of voix pedis in rats. It reduced twisting reaction times and prolonged pain threshold. Conclusion Gubining capsule has the antiinflammatory, detumescent and analgesic effects. It suggests that gubining capsule may have good effects on rheumatoid arthritis.
  • 药物与临床
  • 药物与临床
    LI Yan;MA Shu-mei
    Objective To investigate the effect of telmisartan on improving the artery flexibility in patients with hypertension and study whether consistently controlling of blood pressure will improve the flexibility of artery. Methods 84 patients with primary hypertension were treated with telmisartan 80 mg•d-1. The baPWV was measured before, onemonth and sixmonth after the treatment by PWV/ABI type instrument,respectively. Results SBP, DBP and PP were significantly decreased(P<0.01). There were no significant changes in HR(P>0.05). BaPWV was significantly decreased onemonth or sixmonth after the treatment, compared with that before the treatment (P<0.01). The change of baPWV was obviously greater in six months than in one month after treatment(P<0.01). Conclusion Telmisartan has the effect of improving the flexibility of artery in antihypertensive therapy, which could be continuous after the blood pressure decreased to normal.
  • 药物与临床
    GUO Hong-yu;DUAN Yong-ke;HONG Yan;CHENG Guan-chang;HE Rui-li;ZHENG Ya-xi;LIU Xiao-qiao
    Objective To investigate the shorttime effect of atorvastatin on anti-platelet function of clopidogrel in patients with acute coronary syndrome(ACS). Methods 100 ACS patients were randomly divided into four groups (every group included-15 UAP and-10 STEMI). All the patients were given with aspirin 300 mg•d-1 and clopidogrel 75 mg as the base treatment; then group I, II, III was given with atorvastatin 10 , 20 and 40 mg•d-1 ,qd,po in addition, respectively. Group Ⅳ was given with pravastatin 40 mg•d-1 qd,po. Venous blood was sampled for determining sofplasma (GMP-140) and max platelet aggregationrate (MPAR) pre and 3 days posttreatment. Results GMP-140 antigen in plasma and MPAR of all the four groups after treating were lower than those before treating (P<0.01), but no significant difference was found between the four groups before treating (P>0.05). Conclusion Atorvastatin does not interfere with the inhibitory effects of clopidogrel on platelet function in patients with acute coronary syndrome(ACS) in short period, which is safe combined with clopidogrel.
  • 药物与临床
    ZHAI Xi-ju
    Objective To investigate the clinical uses of doxepin on chemotherapy for patients with lung cancer. Methods 100 patients with lung cancer were enrolled into the study and all the patients were divided into two groups: therapeutic group and control group. 60 patients in the therapeutic group were given with chemotherapy, doxepin and routine psychological support; 40 other patients in the control group were given with chemotherapy and psychological support. The patients in both groups accepted questionnaires of selfrating anxiety scale (SAS) and selfrating depression scale (SDS) prior to treatment, 2 cycles, 4 cycles, 6 cycles after chemotherapy. Then we evaluated the clinical effects and side effects according to the changes of standard scales. Results The total effective rates after 2, 4, 6 cycles of chemotherapy were 90.0%, 85.0% and 80.0%, respectively. While in the control, the total effective rates were 65.0%, 40.0% and 36.0%, respectively. Compared with the control group, the total effective rates were significantly different(P<0.01), while not inner groups (P>0.05). In the control group, the total effective rate of 2, 4 cycles chemotherapy (P<0.05) and 2, 6 cycles of chemotherapy (P<0.01) were obviously different. But the total effective rates of 4 and 6 cycles of chemotherapy were not mardedly different (P>0.05). Conclusion During the course of chemotherapy for lung cancer, doxepin plus psychological support is an effective method and deserved for further study.
  • 药物与临床
    XIAO Yang;YAN Hong-liang;LAI Jiang;CHEN Ting
    Objective To investigate the clinical effect of diosmin tablets on postoperation complications of mixed hemorrhoid. Methods A total of 120 patients with mixed hemorrhoid were retrospectively analyzed. All patients were divided into two groups:diosmin treatment group (n=60)which were treated by diosmin tablets plus mayinglong musk hemorrhoids ointment and control group(n=60)which received vitamin C tablets instead of diosmin tablets. Results Diosmin tablets remarkably improved the postoperative symptoms in patients with mixed hemorrhoid, the effective rate of which was significantly higher than that of the control group (P<0.05 ). Conclusion Diosmin tablets have a significant effect on treating the postoperation complications of mixed hemorrhoid, and can be used as one of the clinical conventional methods in patients undergoing hemorrhoidectomy.
  • 药物与临床
    GAN Jian-guang;TIAN Guo-qiang;GAO Tian-lai
    Objective To compare the effects of venlafaxine retarder and clomipramine on cognition function of patients with depression. Methods 70 patients were divided into venlafaxine group (36 parients, using 75-300 mg•d-1 venlafaxine retarder) and clomipramine group (34 patinets, using 100-225 mg•d-1clomipramine) .The efficacy was evaluated with the Hamilton rating scale of depression(HAMD) and continuous performance Test(CPT), comparing with general population. Results The CPT scores of both groups before the treatment were significanthy lower than general population’s. After 6 weeks’ treatment, the HAMD scorereducing rate of both groups were similar, but significant differences appeared in the CPT scores of both groups. In the efficacions, the CPT scores of patients treated with venlafaxine retarder were similar with general population’s, but obvious differences existed in the clomipramine group and general population. Conclusion Venlafaxine retarder can improve cognition function of patients with depression, which is better than clomipramine.
  • 药物与临床
    CAO Tian-gao;LI Jing-nan;SHI Yun-zhen;LI Zhao-xia
    Objective To investigate the efficacy and safety of anti-virus and anti-fibrosis treatment on liver cirrhosis resulting from hepatitis B. Methods One hundred and twentysix patients with liver cirrhosis resulting from hepatitis B were randomly divided into A group(conventional therapy), B group(conventional therapy+anti-virus treatment) and C group(conventional therapy+anti-virus and anti-fibrosis treatment). Results Being treated for fourtyeight weeks, the liver function, Child-Pugh score and hepatic fibrosis in group A were not significantly improved compared with those before treatment. The liver function, ChildPugh score and hepatic fibrosis in group B were significantly improved compared with those before treatment (P<0.01). The Child-Pugh score and hepatic fibrosis in group C were significantly ameliorated compared with those in group B (P<0.01 or P<0.05). The serum albumin in group C was obviously raised compared with that in group B (P<0.05). Conclusion Anti-virus and anti-fibrosis treatment on liver cirrhosis caused by hepatitis B can significantly enhance the liver function and treat hepatic fibrosis. If combined with fuzheng huayu capsule, the therapeutic effect on hepatic fibrosis and the serum albumin elevation would be more manifest.
  • 药物与临床
    QI Xing-yi;HU Qiang-fu;HUANG Wei-qin
    Objective To observe the protective effects of ulinastatin(UTI) on myocardium during coronary artery bypass grafting(CABG) with cardiopulmonary bypass(CPB). Methods 60 patients scheduled for CABG with CPB were randomly divided into control group (group C) and ulinastatin group ( group U) , 30 in each. In group U, the patients received UTI 1 000 000 U in all, 300 000 U in which was given intravenously before anesthesia and 400 000 U was added into the primary solution, the last 300 000 U was given after declamping aorta. Control group (group C ) did not receive UTI intravenously or in the priming. Plasma levels of CK,CK-MB and cTnI were measured before induction(t1), 30 min following clamping (t2), reperfusion l h (t3) ,reperfusion 6 h (t4) and reperfusion24 h (t5). Results The plasma level of CK, CK-MB and cTnI increased significantly at t3, t4 and t5 in both groups compared with those at t1 (P<0.05) .The plasma cTnI level of group C at t3, t4 and t5 was significantly higher than that of group U( P<0.05) , and the plasma CK and CK- MB level of group C at t4,t5 was significantly higher than that of group U(P<0.05), respectively. Conclusion Ulinastatin can effectively protect myocardium from ischemia reperfusion injury during CPB.
  • 药物制剂
  • 药物制剂
    YANG Fang;LIU Gao-feng;ZHEN Li-mian
    Objective To optimize the preparation technics of wumeitougu oral liquid (WTOL). Methods The preparation technics of WTOL was optimized by L9 (34) orthogonal test with asperosaponin VI content as index, and the influencing factors of aqueous extracting and depositing in alcohol were investigated, respectively. Results The best preparation technic was as follows: adding 8 times of water, decocting for 3 times, 1.5 h for each time, with the relative density of water extracts at 1.12, concentration of depositing in alcohol at 65%, and keeping still at 4 ℃ for 2 days. Conclusion The optimized preparation technic was suitable and feasible.
  • 药物制剂
    WAN Chang-wei;FU Hong-xing;XU Yan-yan;ZHAO Ying-zheng;YANG Dong;CAO Gao-zhong
    Objective To prepare osmotic pump capsules and investigate the factors influencing release behavior, which provide a basis for the development of the capsule. Methods Using paracetamol as model drug, cellulose acetate(CA) as capsule materials,the shell of osmotic pump capsule was prepared by dip plastic method and mechanical drill treatment. By choosing different plasticizers, porogen, penetration promoting agents, the release behaviour of the capsules was studied, and fitted to linear equations; the surface structure was investigated by scanning the shell of capsule before and after the drug release. Results More than 90% of the loaded drug was released in 24 hours and the drug release behavior was best described by zeroorder kinetic equation, with 10% PEG-400 and 30% PEG-2000 or drug:PVP-K30=1:3, drug:PVPK30:Sodium chloride=2:1:2. Conclusion The osmotic pump capsules show potential to be a new controlledrelease drug delivery system.
  • 药物制剂
    HA Na;YANG Xi-jiang;ZHAO Yu-xin
    Objective To study the best preparation process for anshenning soft capsule. Methods The uniform design and multiple stepwise regression analysis were applied to investigate the influences of the ratio between extract and diluents, suspending agent and wetting agent on the physical stability of the content by using sedimentation ratio and the fluidity evaluation of the content suspension as test indexes. With the comprehensive evaluation about the disintegration and the disintegration under the accelerated trials of the soft capsule as the marker,the ratio between gelatin and glycerol, gelatin and water, the temperature of gelatin melting were investigated to test their influences on the solubility of capsule shell. Results The final formulation of anshenning soft capsule was ascertained as follows: the ratio of the medicine powder to soybean oil was 1:1.5, beeswax as the suspending agent accounting for 4% of the suspension, lecithin as the wetting agent accounting for 2% of the suspension. The final formulation of capsule shell was fixed as follows: gelatin: glycerol: water = 1:0.5:1(W/W). Conclusion The uniform design and regression model can be used to precisely predict the test results, and optimize the preparation process of anshenning soft capsule.
  • 药品质量控制
  • 药品质量控制
    CHENG Si-kun;WANG Jing;LI Jian;HUANG Guo-hai;ZHANG Xiao-nan;LUO Er-ping
    Objective Polarographic catalytic wave of morin in the presence of H2O2 was investigated, by which morin was determined in Morus Alba L. sensitively. Methods The determination was carried out by electroanalytical chemistry. Results In 0.2 mol•L-1 Hac-NaAc(pH 5.3±0.1)and 2.0×10-2 mol•L-1 H2O2 supporting electrolyte, the peak current was linearly proportional to morin’s concentration in the range from 6.0×10-8 mol•L-1 to 3.0×10-6 mol•L-1. Conclusion Compared with that of reported, this method is characterized as sensitivity, rapidness and convenience. Furthermore, the investigation of catalytic wave of morin is helpful in understanding its oxygen free radical scavenging ability.
  • 药品质量控制
    MA Yong-gui;LI Zi-ming;MIN Min;HE Guo-fang;WANG Qiu-lan;WANG Wen-qing
    Objective To establish a RP-HPLC method for determination of clonidine hydrochloride in compound clonidine hydrochloride tablets . Methods Chromatography was carried out on a column of the Hypersil C18(4.6 mm×250 mm,5 μm); mobile phase: 0.22% sodium 1octanesulfonatemethanolphosphoric acid(400:600:1,pH=3.0); flow rate: 0.9 mL•min-1 and the detection wavelength was 220 nm. Results A good linearity of clonidine hydrochloride was obtained within 1.37-6.85 μg•mL-1; the average recoveries of clonidine hydrochloride was 100.5%(RSD=0.76%),100.6%(RSD=2.66%),101.9%(RSD=0.92%) (n=9), respectively. Conclusion The method is simple, rapid, sensitive and accurate. It can be used to control quality of clonidine hydrochloride in compound clonidine hydrochloride tablets .
  • 药品质量控制
    MA Li;YAN Hui-juan;QU Jia-jia;ZHANG Yu
    Objective To establish a HPLC method for the determination of aesculin in Fraxinus hupehensis. Methods Aesculin was extracted from Fraxinus hupehensis by methanol. The Hypersil ODS column (4.6 mm×150 mm,5 μm) was employed as a stationary phase. The mobile phase was acetonitrile-water (25:75) ,the flow rate was 1 mL•min-1,the detection wavelength was 336 nm. Results The linear range was within 2-10 μg•mL-1. The average recovery was 100.19%, and RSD was 2.11%. Conclusion The method is efficient and accurate with a good repeatability ,and could be used for the determination of aesculin in Fraxinus hupehensis.