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    药物研究
  • 药物研究
    WANG Zhan-qing;WANG Jin-ping;XU Jing-feng;YANG Yong-ge;BIAN jia-ming
    2007, 26(4): 350-353.
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    Objective To probe into the protective effect of ferilnite(FLNT), a drug belonging to the class of ferulic acid nitric ester, on the myocardium submitted to ischemia/reperfusion injur in rats. Methods Sixty male adult SD rats were divided into 6 equal groups .Except for rats of the sham operation group(group ①) in which a thread was passed beneath the coronary artery but the vessel was not ligated, a model of ischemia/reperfusion injury of the myocardium was set up in each of the rats of the other 5 groups by ligating the left anterior descending branch of the coronary artery for 40 min followed by untying of the vessel for 3h. 10 min after the ligation of the artery, rats of group ②(model group),group ③④and⑤(FLNT treatment group ) and group ⑥(positive control group) were given each by gastragavage an equivalent amount of carboxymethylcellulose(CMC), 2,4 and 8 mg·kg-1 of FLNT and 2 mg·kg- 1 of nitroglycerine, respectively. Blood samples were taken from the common carotid artery at the termination of the 3 h reperfusion and the hearts extirpated for examination. ECG was recorded 10 min before and after the ligation of the artery and at different time points after the administration of the drugs. Results The size of myocardial infarction was much smaller, the activities of serum creatine kinase (CK) and lactate dehydrogenase (LDH) were significantly lower (P<0.05), the content of nitric oxide(NO) and activity of superoxide dismutase(SOD) in the myocardial tissue were strikingly higher, while the content of malonyldialdehyde(MDA) was dramatically lower in rats treated with different doses of FLNT(P<0.05) as composed with those parameters in rats of the model group. FLNT was also shown to prevent the elevation of T wave, depression of the R wave (P<0.05) and production of the pathological Q wave. ConclusionFLNT was shown to exert protective effects on the myocardium submitted to an ischemia/reperfusion injury in rats possibly by upregulating myocardial NO and strengthening the antioxidative mechanism of the organism.
  • 药物研究
    HUANG Sheng-wu;WU Zhi-hui;HU Xi-bo;LI Jun;FANG Jian-wen
    2007, 26(4): 353-355.
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    Objective To assess the in vitro antiCoxsackie virus activity of Anxinkang drop pills. Methods The antivirual activity of the Anxinkang drop pills were assayed in cultured rat myocardial cells infected with the Coxsackie virus (CVB3). The influence of the drug on the cytopathy of the myocardial cells, its effects on virus replication and the content of troponin in the supernatants of the cultured cells were kept under observation. Results Anxinkang drop pills were shown to effectively alleviate the cytopathy, depress virus replication and decrease the content of troponin in the supernatants. Conclusion Anxinkang drop pills were shown to be provided with a dramatic antiCoxsackie virus effect.
  • 药物研究
    QI Zhi;YU Qing-song;LI xiao-ai;GUO Min;ZhANG Hua-feng;XIANG Yi
    2007, 26(4): 356-359.
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    Objective To prepare chitosanCpG-ODN gene carriers with the use of chitosan (CS) as the material to carry oligodeoxyribonucleotide(ODN) containing CpG sequences and to study their immunological competence in mice. Methods -The CS CpG-ODN carriers were prepared with the method of complex coacervation. 24 male Balb/c mice were randomly divided into four equal groups : ①control group, ②CS group, ③CpG-ODN group and ④CS CpG-ODN group. Mice of the group ① to ④ were given each an I.M. injection of 200 μL of normal saline, 31.25 μg of CS, 15 μg of CpG-ODN and 15μg of CpG-ODN +31.25 μg of CS, respectively, as an initial immunization. A booster immunization was carried out 2 weeks later with the same method. 2 weeks thereafter, blood samples were taken from behind the orbit for examination. Lymphocyte proliferation was assayed with the MTT test. Serum IgG,IL-2 and IL-12 contents were determined with ELISA and peripheral blood T lymphocyte subsets CD+4 and CD+8 were detected with flow cytometry. ResultsEnhanced lymphocyte proliferation, striking increased serum contents of IL2 and IL12 , high levels of protective serum IgG as well as very effective upregulation of the percentage of CD+ 4 T cells and CD+4 / CD+8 ratio in the peripheral blood lymphocytes were demonstrated in the blood of mice immunized with CS CpGODN. Conclusion CS CpG-ODN gene carriers were shown to effectively improve the immunoenhancing effect of CpGODN.
  • 药物研究
    YIN Chun-ping;LIU Wen-tao;XU shun-qing;WU Ji-zhou
    2007, 26(4): 359-361.
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    Objective To seek after a new method for the identification of Fritillaria hupehensis and accurate distinguishment between Fritillaria hupehensis and Fritillaria unibracteata the certified product. Methods Random primers suitable for the distinguishment between Fritillaria hupehensis and Fritillaria unibracteata were screened out with the adoption of the random amplified polymorphic DNA (RAPD )technique . Results 20 random primers were screened out in total and one of which , the primers ,was shown to accurately distinguish between Fritillaria hupehensis and Fritillaria.unibracteata with very high specificity. Conclusion The results showed that RAPD marker technique could effectively distinguish between Fritillaria hupehensis and Fritillaria unibracteataKEY WORDS
  • 药物研究
    WANG Wen-qing;LI Ming;FANG Jian-guo;MA Yong-gui;TANG Jie;SHI Chunyang
    2007, 26(4): 364-366.
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    ABSTRACT Objective To study the anti-inflammatory and analgesic effects of dexibuprofen gel in murines. Methods Foodpad swelling in rats induced by subcutaneous injection of carrageenan , ear swelling in mice caused by topical smearing of xylene, signs of algesic reaction of the tail exposed to radiant heat in rats and writhing reflex induced by intraperitoneal injection of acetic acid in mice served as models of inflammation and sensation of pain in the murines, respectively. Relevant areas of the skin of the animals were smeared with dexibuprofen gel in different concentrations before the establishment of the models. In rats scheduled to carry the footpad swelling model, the part of the skin was smeared with the gel both before and after the setting up of the model. Results2.5% and 4.0% dexibuprofen gel smeared topically was shown to dramatically suppress the carrageenaninduced foot pad swelling in rats and ear swelling caused by xylene in mice. The drug could also strikingly heighten the pain threshold in response to radiant heat in rats, and decrease the writhing of the body induced by intraperitoneal injection of acetic acid in mice. Conclusion Dexibuprofen gel applied topically was shown to have notable antiinflammatory and analgesic effects.
  • 心血管系统用药专栏
  • 心血管系统用药专栏
    YE Ping-xian;FU Lu-hong;ZHU Jian-hua;CHEN Jun-zhu;ZHANG Fu-rong;ZHANG Liang-rong;TAO Qian-min
    2007, 26(4): 369-372.
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    Objective To study the effect of urokinase (UK) combined with liposomal alprostadil(Lipo-PG E1) in the treatment of acute myocardial infarction(AMI) and the influence of the management on the infarctrelated artery (IRA) and myocardial reperfusion. Methods Fiftytwo patients with AMI showing STsegment elevation were randomly divided into 2 equal groups: the trial group and the control group. Patients of both groups received thrombolytic treatment with UK. 10 min before the UK treatment, patients of the trial group were given each additionally 0.5 μg·kg-1 of Lipo-PG E1 dissolved in 0.9% sodium chloride solution administered intravenously within 2 h. Patients of the control group were given each an equivalent amount of solvent of Lipo-PG E1 administered in the same manner as described above. ECG and blood pressure were monitored in each of the patients in the 2 groups, including a 24 h continuous recording of the standard 12lead (or 18lead) ECG. The restoration rate of the STsegment in the ECG was determined 90 and 180 min after the thrombolytic treatment. Coronary angiography was performed 90 min after the beginning of the thrombolytic treatment to determine the grading of the forward blood flow of the infarctrelated artery(IRA) in the thrombolysis test in myocardial infarction(TIMI). Plasma levels of alpha granule membrane protein 140(GMP140) and endothelin(ET) were determined before and after the thrombolytic treatment. ResultsThe IRA patency rates in patients of the trial group and control group were 73.1% and 42.3%,respectively(P<0.05). The rate of complete (≥70%) STsegment restoration in patients of the trial group 90 and 180 min after the thrombolysis was also significantly higher than that in patients of the control group. The rates of complete restoration of the STsegment in patients of the trial group and control group showing grade 2 to grade 3 blood flow in the TIMI were 73.7% and 33.3%, respectively(P<0.05).The plasma levels of ET and GMP140 were significantly lower in patients of the trial group than those in patients of the control group. Conclusion Lipo-PG E1 combined with UK was shown to promote reperfusion of the infarctrelated artery (epicardial flow) and infarcted myocardium (microvasculature).
  • 心血管系统用药专栏
    FU Shen-wen;DU Yong-yuan;JIN Lie
    2007, 26(4): 372-375.
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    Objective To probe into the clinical therapeutic effectiveness of trimetazidine in the treatment of dilated cardiomyopathy(DCM) associated with moderate to severe chronic congestive heart failure(CHF). Methods 40 patients with DCM associated with moderate to severe chronic congestive heart failure were randomly divided into 2 groups: the control group(n=19) and the trial group(n=21). Patients of the control group were routinely treated with digitalis, diuretics, converting enzyme inhibitor β-receptor blocker etc.. On the basis of the routine treatment, patients of the trial group were given each additionally 20 mg of trimetazidine PO, t.i.d.. The course of treatment lasted 8 weeks. The grade of cardiac function, left ventricular ejection fraction(LVEF), left ventricular enddistolic diameter (LVDd)and the serum level of brain natriuretic peptide(BNP) were determined before and after the 8 week treatment in patients of both groups. Results The grade of cardiac function in patients of the trial group was greatly improved after the trimetazidine treatment. The overall effective rate in patients of the trial group was 90.5% while that in those of the control group was 52.6%. In patients of the trial group, the LVEF was dramatically increased, the LVDd greatly reduced, and the serum level of BNP significantly elevated after the treatment. However, the blood pressure and heart rate showed no apparent changes in patients treated with trimetazidine. Conclusion Trimetazidine was shown to have good therapeutic effects in the treatment of patients with DCM associated with congestive heart failure.
  • 心血管系统用药专栏
    MEI Jian-hua;HU Chang-sheng
    2007, 26(4): 375-377.
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    Objective To compare the therapeutic effects of puerarin injection and compound Radix Salvia Miltiorrhiza injection in the treatment of unstable angina pectoris(UAP). Methods Ninetyeight patients with unstable angina pectoris were randomly divided into two groups: the trial group (n=50) and control group (n=48). Patients of both group were treated routinely with isosorbide dinitrate, entericsoluble aspirin and nifedipine. Nitroglycerin to be sucked sublingually were administered during episodes of angina pectoris. On the basis of these conventional measures, patients of the trial group were given each 10 mL of puerarin injection added to 500 mL of 5%glucose solution administered by IV instillation q.d., while those of the control group were given each 40 mL of compound Radix Salvia Miltiorrhizae injection added to 500 mL of 5%glucose solution administered by IV instillation q.d .as well. The course of treatment in both groups lasted 14 days. Clinical symptoms, changes in electrocardiogram and parameters of hemorrheology were kept under observation before and after the treatment. Results The overall effective rates in patients of the trial group and control group were 96.0% and 81.2%, respectively, the difference being significant(P<0.05).The low shear value of the whole blood viscosity was sharply decreased(P<0.05), the erythrocyte deformability was apparently increased, while the hematocrit, erythrocyte aggregation index and platelet aggregation rate were markedly decreased in putients of the trial group. Differences between these parameters before and after the treatment in patients of the trial group were significant(P<0.01).Changes in these parameters after the treatment were much more pronounced in patients of the trial group than in those of the control group(P<0.01 or P<0.05). Conclusion Puerarin injection was shown to be superior to compound Radix Salvia Miltiorrhizae injection in the treatment of unstable angina pectoris.
  • 心血管系统用药专栏
    LIU Qing-yun;WU Rui-xia;ZHOU Li-qin;ZHOU Xiao-li;LIU Peng;HUANG Mei-song
    2007, 26(4): 378-379.
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    Objective To compare the therapeutic effects of sodium ozagrel and ligustrazine in the treatment of unstable angina pectoris(UA). Methods Ninetyseven patients with UA were randomly divided into 3 groups: the sodium ozagrel group (trial group 1,n=37), ligustrazine treatedgroup (trial group 2, n=31) and control group (n=29). Patients of all 3 groups were subjected to conventional treatment for angina pectoris. Patients of the trial group 1 and 2 were given each additionally an injection of sodium ozagrel (80 mg) and ligustrazine (100 mg) added to 500 mL of 5% glucose solution administered by IV instillation q.d., respectively. The course of treatment in all 3 groups lasted 2 weeks, indexes of clinical manifestations and laboratory examinations in patients of the 3 groups were compared after the two weeks treatment. Results The basic cure rates, excellent effective rates and overall effective rates in patients of the 2 trial groups were obviously higher than those in patients of the control group (P<0.05). However, the differences between patients of the trial group 1 and 2 were insignificant (P>0.05). Conclusion Sodium ozagrel and ligustrazine were shown to have notable effects to relieve myocardial ischemia in the treatment of UA .
  • 心血管系统用药专栏
    ZONG Wen-xia;LIN Li;HE Jing
    2007, 26(4): 380-382.
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    Objective To study the effect of telmisartan on the casual as well as dynamic blood pressure in patients with mild to moderate essential hypertension. MethodsAfter a week of washout period, 43 outpatients with mild to moderate essential hypertension were given each 40 mg of telmisartan PO, q.d. for 8 weeks. At the termination of the 2nd,4th and 8th week of the treatment course, casual blood pressure was taken in the morning. 24 h dynamic blood pressure was registered before and at the end of the treatment course. Results The overall effective rate of the telmisartan in the treatment was 79.1%. After the treatment, the average blood pressure in the whole day, day time and night time as well as 4 h following the medication were all lowered significantly (P<0.01), respectively. The trough/peak ratios of the systolic blood pressure and diastolic blood pressure were 68.4% and 79.3%, respectively.Conclusion Telmisartan was shown to be very effective in the treatment of patients with mild to moderate essential hypertension, its effect lasting 24 hours.

  • 药物与临床
  • 药物与临床
    LIN Cai;ZHANG Peng;XU Jian-jun;CHEN Geng-xin;LI Li-qun;LUO Xu;CHEN Xiao-qing;LIU Zheng-jun 
    2007, 26(4): 387-389.
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    Objective To survey the hemostatic effect of reptilase spraying upon the donor areas for autoskingrafting in patients with deep extensive burn. Methods Thirty patients with deep extensive burn chosen as subjects of the study, their unaffected skin of the bilateral thighs serving as donor areas of auto skingrafting. Skin grafts of the same size and thickness were taken from the bilateral unaffected thighs of the same patients for autoskingrafting. After the blood from the wounds had been swalled away, the wound surfaces of the left thigh and right thigh were sprayed with reptilase and 0.9% sodium chloride solution, respectively, followed by pressure bandaging covering layers of gauze. The hemostatic effect of the drugs was assessed by the average number of the layers of gauze stained with blood that was visible to the naked eye. Results In the wounds of the left thigh that had been treated with reptilase spraying, the average number of the layers of gauze stained with blood that was visible to the naked eye was (13.00±3.75), which was significantly smaller than that in the wounds of the right thigh that had been treated with normal saline spraying (16.00±3.12)(P<0.05)4 days after the operation. No adverse reactions were encountered in the treatment. Conclusion Reptilase spraying upon the donor areas in patients with extensive burn scheduled for autoskingrafting was shown to be an effective measure for local hemostasis.
  • 药物制剂
  • 药物制剂
    ZHONG Qiao-ni;ZHAO Li;LEI Yu-xia;CHENG Ming;ZHANG Chang-gong
    2007, 26(4): 408-410.
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    Objective To optimize the extraction technology for the total saponin of Radix Bupleuri. Methods The extraction technology for the total saponin of Radix Bupleuri was optimized by adopting a single factor experiment and an orthogonal design with the use of the extraction rate of the total saponin of Radix Bupleuri as the assessment index. Results The optimized extraction technology for the total saponin of Radix Bupleuri was as follows: powdered herb with a diameter less than 180 μm was subjected to reflux extraction for 3 times with 70% ethanol at 80 ℃, each extraction lasting 1h .For each extraction, 8 volumes of ethanol were added to 1 volume of the powdered drug. Conclusion It was shown by an approval test that the optimized technology was stable, feasible and suitable for the extraction of the total saponin of Radix Bupleuri.
  • 药品质量控制
  • 药品质量控制
    DING Shui-ping;DU Guang;LI Yong-jin
    2007, 26(4): 420-422.
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    Objective To set up a method for the quantitative determination of bacterial endotoxins in cefpirome sulfate for injection in order to replace the pyrogens test. Methods The limit value of bacterial endotoxin in the cefpirome sulfate was defined according to the turbidimetric kinetic method for the determination of bacterial endotoxin described in the Appendix of the Volume Ⅱof the Pharmacopoeia of the People’s Republic of China, 2005 edition. The interference of cefpirome sulfate for injection with the limulus reagent was also studied to determine whether the bacterial endotoxin test was suitable for the drug. Results Cefpirome sulfate for injection in several concentrations was in the quantitative determination of bacterial endotoxin showed no interference with the limulus reagent.The rate of recovery of bacterial endotoxin was between 50%200%. Conclusion It was shown that cefpirome sulfate can be quantitatively determined with the bacterial endotoxin test. 