目的 探讨重症肺炎患者应用头孢哌酮/舒巴坦的药代及药效动力学影响.方法 20例重症肺炎患者随机分为观察组和对照组,每组各10例,均接受头孢哌酮/舒巴坦抗感染治疗,对照组静脉给药输注30?min,观察组采用静脉给药输注3?h.分别于第1次治疗给药前及给药后的不同时间点采集患者动脉血2?ml,选择超高效液相色谱-电喷雾串联质谱分析方法测定头孢哌酮和舒巴坦的浓度,计算药动学数据(C?max、AUC0-∞、t1/2、CL、Vd等),结合不同细菌的MIC值进行计算％T>MIC比值.结果 对照组患者头孢哌酮的药动学参数为Cmax(83.85±15.44)mg/L、AUC0-∞(924.19±141.27)mg·?L-1·h-1、t1/2(3.30±0.64)h、CL(7.61±0.28)L/h、Vd(36.16±6.93)L/kg,舒巴坦的药动学参数为Cmax(66.97±1.54)mg/L、AUC0-∞(323.31±161.27)mg·?L-1·h-1、t1/2(1.74±0.07)h、CL(18.49±1.00)L/h、Vd(46.28±3.03)L/kg.观察组患者头孢哌酮的药动学参数为Cmax(68.19±3.95)mg/L、AUC0-∞(811.00±382.08)mg·?L-1·h-1、t1/2(4.02±1.18)h、CL(6.66±0.35)L/h、Vd(26.28±3.33)L/kg,舒巴坦的药动学参数为Cmax(22.28±2.74)mg/L,AUC0-∞(324.39±183.04)mg·?L-1·h-1、t1/2(1.49±0.34)h、CL(17.98±5.06)L/h、Vd(36.58±4.77)L/kg.观察组％T>MIC优于对照组.结论 头孢哌酮/舒巴坦临床应用于重症肺炎,可采取3?h延长输注时间抗感染.

Objective To investigate the changes of hepatic CYP450 activity and liver function in tramadol dependent rats. Methods Total 30 SD rats were divided into blank group, positive control group and experimental group, with 10 rats in each group. Each group was administered with saline, 80 mg/ ( kg·d) phenobarbital and 60 mg/ ( kg·d) tramadol. The rat model of tramadol dependent rats was established. Cocktail in vitro incubation method combined with liquid mass spectrometry ( LC-MS) technology were used to test the isozymes activities of CYP1 A2, CYP2 B1, CYP2 C11, CYP2 D2, CYP2 E1, CYP3 A1 in rat liver were measured, and RT-qPCR technique was used to detect the level of mRNA expression of the above isozymes, and the blood biochemical analyzer was used to analyze the liver function index. Results (1) Compared with the blank group, the activities of CYP1 A2, CYP2 B1, CYP2 C11, CYP2 E1 and CYP3 A1 in the positive control group were (190. 15 ± 33. 577), (98. 018 ± 36. 00), (1 348. 79 ± 40. 76), (3 214. 66 ± 133. 51) and (292. 76 ± 33. 32) μg/ml, which were significantly higher than those in the blank group (P ＜ 0. 05). The difference was statistically significant. (2) Compared with the blank group, the expression of CYP1 A2, CYP2 B1, CYP2 C11, CYP2 E1 and CYP3 A1 mRNA in the positive control group was significantly up, ( 89. 88 ± 14. 22) ％, ( 95. 12 ± 16) ％, (351. 25 ± 32. 33) ％, (556. 85 ± 42. 88) ％ and (52. 56 ± 11. 12) ％, and the difference was statistically significant, and there was no significant change in CYP2 D2 mRNA. The expression of CYP1 A2, CYP2 B1, CYP2 E1 and CYP2 D2 mRNA in the experimental group was up ( 75. 12 ± 21. 45) ％, ( 66. 32 ± 18. 14) ％, ( 81. 35 ± 23. 55) ％ and (382. 74 ± 33. 25) ％. The difference was statistically significant. There was no significant change in the expression of CYP2 C11 and CYP3 A1 mRNA. (3) In the liver biochemical index level, compared with the blank group, the content of ALT, AST and LDH in the positive control group and the experimental group increased significantly, and the results were statistically significant. Conclusion The abuse of tramadol may induce an increased activity of CYP1 A2, CYP2 B1, CYP2 E1 and CYP2 D2 and liver injury in rats.

Objective To investigate the pharmacokinetics of Cefoperazone/Sulbactam in intensive care unit patients with sepsis.Methods The patients with sepsis in intensive care unit of Ruian people's Hospital of Zhejiang Provincefrom January to September 2017 who was administered 2.0 g Cefoperazone/Sulbactam for the first time were inrolled.Serial serum samples were collected before the first antibiotic dose and at 0,0.25,0.5,1,2,3,4,6,8 h after Cefoperazone/Sulbactam was administered.Then the serum was separated and the concentration was determined by HPLC.Results Cefoperazone:half-life (t1/2:(1.575±0.325) h,clearance rate(CL):(0.095±0.023) L/(h· kg),apparent volume of distribution (Vd):(0.215±0.037) L/kg,peak concentration (Cmax):(83.633±19.324) mg/L,area under the curve AUC (0→∞):(190.213± 42.625) h·mg/L;Sulbactam:t1/2:(1.049±0.263) h,CL:(0.281±0.065) L/(h·kg),Vd:(0.424±0.103) L/kg,Cmax:(42.526±11.210) mg/L,AUC(0→∞):(64.394±15.435) h·mg/L.Conclusion The apparent volume of distribution of Cefoperazone in intensive care unit patients with sepsis is slightly larger than that reported in the literature,the peak concentration is slightly lower,and the half-life is shorter,while the change of Sulbactam is relatively small.Therefore,the dosage of Cefoperazone should be improved and the dosing interval should be shortened in those patients.

The geometric and electronic structures, energetics and spectroscopy of different complexes formed between cytosine and a molecule of [C(n)mim]Br (n = 2,4,6,8,10) are investigated in detail using the M06-2X and omega B97XD methods with 6-311 + + G(2d, p) basis set. A great number of stable C-[C(2)mim]Br and C-[C(4)mim]Br complexes were obtained, these structures are classified as three types: approximately coplanar, parallel and perpendicular. The BSSE-corrected binding energies of the most stable structures (C(n)1) at the M06-2X method are -108.3 to -97.3 kJ.mol(-1), which higher than the results of omega B97XD. The aqueous solvation environment has an extremely weaken impact on the cytosine interaction with imidazolium bromide ionic liquid.

Objective:To establish a mass spectrometry method for determination of blood concentration of cyclosporine A (CsA), and determine the blood concentration of cyclosporine A alone and in combination with lfuconazole.Methods:The blood concentration of cyclosporine A in rats was detected and compared when cyclosporine alone and combined with lfuconazole by using liquid chromatography-mass spectrometry. Chromatographic column Agilent Zorbax SB-C18 was used. Column temperature was 50℃. Mobile phase was acetonitrile-0.1% formic acid. Flow rate was 0.5 mL·min-1. Mass spectrometry condition was as follows: ESI (electrospray ion source) was used, positive ion detection was used, atomizing gas pressure was set to 20 psi.Results:The linear relationship of CsA was good in the range of 100 – 20 000 ng·mL-1 (r = 0.999 6). Intra-day RSD and inter-day RSD were less than 5%. The average extraction recovery was 90%. The average blood trough concentration of CsA when CsA combined with lfuconazole was higher (by 178.0%) than just cyclosporine alone in ifve days, and the peak concentration in combined utilization was higher (by 161.3%) than that of alone use.Conclusion: The method is simple, specific, accurate and high sensitivity, which can also be used for the determination of CsA blood concentration and pharmacokinetics study. Patients who are using CsA and lfuconazole will obviously have high blood concentrations of CsA, should reduce the dosage of CsA, and monitor the blood concentration.

INTRODUCTION:This study aimed to investigate the prevalence, clinical and radiographic features, and antibiotic responses of Mycoplasma pneumoniae (M. pneumoniae) infections in hospitalized adults with community-acquired pneumonia (CAP) in China.METHODOLOGY:Serum specimens collected from 189 CAP patients in both acute phase and convalescence were tested for IgG, IgA, and IgM mixed antibodies specific to M. pneumoniae. The clinical and radiographic characteristics and efficacy of three antibiotic regimens were compared between patients with M. pneumoniae infection and those without.RESULTS:Among 189 CAP patients, 88 (46.6%) were positive for M. pneumoniae infection. Compared to the negative patients, patients with M. pneumoniae infection were significantly younger, had higher rates of dry cough, and had white blood cell counts of <1010/L, but had less purulent sputum. Radiography further showed more centrilobular nodules, ground-glass opacities, tree-in-bud patterns and thickened bronchovascular bundles, but less pleural effusion and larger tracts of real opacities in patients with M. pneumoniae infections. Among the three regimens used, patients with moxifloxacin required significantly shorter fever abatement, treatment, and hospitalization times than those with azithromycin plus ceftriaxone and ceftriaxone only.CONCLUSIONS:M. pneumoniae infection was present in almost half of the CAP population in east China, with some distinct clinical and radiographic features. Moxifloxacin was an effective antibiotic for this infection.

Objective:To investigate perioperative prophylactic use of type Ⅰ incision in our hospital to provide a scientific evidence for making relevant policies and references for rational drug use.Methods;All the cases with type Ⅰ incision from March to June in 2011 in our hospital were retrospectively investigated and analyzed in respect of their basic information, surgery situation,incision healing information and antibiotic prophylaxis status.Results;Among 1 048 cases with type Ⅰ incision investigated,689 cases used antibiotic prophylaxis(the ratio was 65.7%) and 562 cases used rational antibiotics(the ratio was 81.6%).The healing grade of the 1 037 cases was A grade(the ratio was 99.9%) while that of 11 cases was B grade(the ratio was 1.0%).The time to give 319 cases(the ratio was 30.4%) antibiotic prophylaxis was from 30 minutes to 2 hours before operation,and 857 cases used antibiotic prophylaxis within 48 hours(the ratio was 81.8%).Conclusion; The perioperative prophylactic use of typelincision was still irrational,though it was more reasonable than before.It is suggested that perioperative prophylactic use in typelincision should be further supervised.

目的了解Ⅰ类切口患者切口处皮肤上的金黄色葡萄球菌带菌率、耐药情况和围手术期预防性使用抗菌药物现状,为我院和其它医院的围手术期预防用药提供参考。方法①采集I类切口患者切口处皮肤标本,对培养出的金黄色葡萄球菌进行药敏实验。②采用回顾性调查,抽取本院2011年5月及6月出院的Ⅰ类切口手术的所有病案,记录患者基本信息、手术信息和抗菌药物信息,对其进行统计分析。结果①共采集样本991份,检出23株SA,检出率为2.32%。②共调查1048例病案,围手术期预防性应用抗菌药物的有689例,占65.7%。结论我院Ⅰ类切口患者皮肤SA的检出率相对较低,Ⅰ类切口围手术期预防性用药的使用率相对于皮肤SA的带菌率仍较高。我院应继续加强抗菌药物的监管,建立健全合理应用抗菌药物管理制度。

耐甲氧西林金黄色葡萄球菌(MRSA)是医院感染和社区感染的重要病原菌之一。近年来MRSA的感染率不断上升,其耐药性也日益严重。本文主要针对MRSA的感染现状、有效的治疗药物进行综述。

目的分析螺内酯治疗原醛症致男性乳房发育的可能原因,以避免该不良反应的发生。方法回顾性分析1例螺内酯治疗原醛症致男性乳房发育的病例。结果螺内酯致男性乳房发育的因素包括年龄大小、服药剂量、服药时间长短等。结论临床药师应积极参与患者药物治疗的过程,密切监测药物不良反应的发生,真正做好药物使用过程中的药学监护计划。

OBJECTIVE: To prepare Fluconazole/moxifloxacin in situ forming eye gel,and to establish a quality control method for it.METHODS: The gel was prepared with different concentrations of poloxamer 407 as base,and the contents of fluconazole,moxifolxaein and ethylparaben were determined by HPLC.The determination was performed on Elite Hypersil ODS column with mobile phase consisted of triethylamine buffer solution(pH 3.3)-methanol(61 ∶ 39) at the flow rate of 1.0 mL·min-1.The column temperature was 30 ℃ and the detection wavelength was set at 260 nm.RESULTS: The gel was prepared using 15.5% poloxamer 407 as base and its gel-forming temperature was 32 ℃.The linear ranges were 100～600 μg·mL-1 for fluconazole(r=0.999 9),100～600 μg·mL-1 for moxifolxacin(r=0.999 9) and 10～60 μg·mL-1 for ethylparaben(r=0.999 8).Moreover,their average recovery rates were 99.75%(RSD=1.26%),99.89%(RSD=1.08%) and 100.10%(RSD=1.72%).CONCLUSION: The gel is reasonable in design,simple in preparation method and reliable in quality control.

Objective To understand the occurrence status of adverse drug reactions(ADR)in the elderly patients with chronic diseases and to increase the level of rational drug use.Methods The Chinese Journal Database and the medical journals published at home and abroad during 2002-2008 were retrieved for obtaining the information source.The conditions of ADR in the elderly patients were investigated and verified.The condition occurred after medication was recorded.The results were summarized and analyzed.Results 114 elderly patients were effectively investigated.Among them,16 cases showed adverse reactions.The incidence rate of ADR was 14.04%.Conclusion The elderly patients with chronic diseases usually suffered from several diseases,and took long-term combined medication,are prone to ADR.Therefore,doctors should remind the elderly patients to use drugs scientifically and rationally for avoiding the occurrence of ADR.

OBJECTIVE:To investigate the carrying rate and drug resistance of Staphylococcus aureus from the skin of type Ⅰincision and to provide reference for the rational use of antibiotic.METHODS:The specimen was taken by swabs from the skin of type Ⅰ incision,and susceptibility test of SA was carried out with K-B method under the guidance of Clinical Microbiology Laboratory Manual.RESULTS:A total of 991 samples were enrolled.23 strains of SA were isolated,including 17 strain of oxacillin sensitive Staphylococcus aureus,6 strains of oxacillin resistant Staphylococcus aureus.The carrying rate of MRSA was 0.61% while the rate of drug resistance was 26.09%.CONCLUSION:The detection rate of SA from the skin of type Ⅰ incision is low in our hospital while the rate of drug resistance is high.It is suggested that infection supervision and management should be further strengthened,and the spread of MRSA should be controlled in our hospital by adopting effective measures.

目的 建立高效液相色谱法测定氟康唑莫西沙星眼用即型凝胶含量,同时测定制剂中氟康唑、莫西沙星和羟苯乙酯的含量.方法 采用ODS-C18色谱柱,以三乙胺缓冲液-甲醇为流动相,流速1.0mL·min-1,检测波长260nm.结果 氟康唑、莫西沙星、羟苯乙酯的线性范围分别为25～250μg·mL-1(r=0.9999,n=6),25～250μg·mL-1(r=0.9999,n=6),2.5～25μg·mL-1(r=0.9997,n=6),平均回收率分别为99.6％,99.4％,99.3％.RSD分别为1.23％,1.20％,1.17％.结论 本方法操作简便,灵敏度高,重复性好,可用于该制剂的含量测定.

Objective:To analyze the usage of antibiotics in the patients with mycoplasmal pneumonia in Ruian People' s Hospital. Method:According to the "Guidelines for Clinical Use of Antibiotics" and "Diagnosis and Treatment Guidelines for Communityacquired Pneumonia",the types,application frequency,course of treatment,combination,cure rate and adverse drug reactions of antibiotics were statistically analyzed by the retrospective investigation in 97 patients with mycoplasma pneumonia in the year of 2010.Result: In the 97 cases,the percent of antibiotics usage was 100%with the reasonable rate before and after diagnosis of 35.0%and 50.5%,respectively.The used antibiotics included 6 categories and 21 species.Among them,the first 5 were moxifloxacin,azithromycin, azlocillin,ceftazidime and cefodizime.Two-kind drug combination was the main combination therapy.The percent of over-course treatment was 91.7%.The ratio of unreasonable usage was 4.1%.The cure rate was 66.0%.Conclusion:There is irrational application of antimicrobial drugs in the patients with mycoplasma pneumonia.It is necessary to strengthen the supervision and enhance the rational use of antibiotics according to the guidelines.

喹诺酮类药物具有抗菌活性强、抗菌谱广、体内分布广、半衰期长、口服吸收好、治疗敏感细菌所致感染具满意疗效等特点,在临床应用中具有重要地位,但细菌对该类药物的耐药性也逐渐增加,限制其临床的应用。本文综合国内外文献对其作用机制、抗菌特点、临床应用及不良反应进行综述;为喹诺酮类抗菌药的临床应用提供参考。

OBJECTIVE:To compare the efficacy of cefazolin and cefuroxime prevention of perioperative cesarean section wound infection. METHODS:291 cases of elective cesarean section surgery,according to the use of medicines are divided into group A(n=140)and group B(n=151),were retrospectively analyzed. Patients in group A,preoperative 30 min intravenous infusion of cefazolin 2.0 g;after surgery,2.0 g ivgtt,q12 h,continue to use 2～5 days. Patients in group B,preoperative 30 min intravenous infusion of cefuroxime 2.0 g;after surgery,2.0 g ivgtt,q12 h,continue to use 2～5 days. Comparison of the clinical effect of 2 groups patients. RESULTS:WBC,N%,Hb,complications,body temperature,wound healing had no statistical difference in postoperative between 2 groups. All patients were not the emergence of drug adverse reactions. CONCLUSION:cefazolin and cefuroxime has the same efficacy of prevention of cesarean section wound infection.

目的 头孢菌素类抗生素具有杀菌活性强、毒性低、治疗敏感细菌所致感染具满意疗效,在临床应用中具有非常重要地位.本文对其作用机制、抗菌特点及临床应用进行综述;为头孢菌素类抗生素的临床应用提供参考.

青霉素类抗生素具有杀菌活性、毒性低、治疗敏感细菌所致感染具满意疗效,在临床上仍占有重要地位。本文对其作用机制、抗菌特点及临床应用进行综述;为青霉素类抗生素的临床应用提供参考。

OBJECTIVE To establish a HPLC method for the simultaneous assaying of compound ofloxacin and ketotifen nasal sprays.METHODS The chromatographic column was Beckman ODS(4.6mm×25cm,5μm); the mobile phase was composed of acetonitrile-ammonium acetate(1%)with detection wavelength at 263nm and flow speed at 1.0mL·min-1.RESULTS The line range and Correlation coefficient of the ofloxacin were 30～300mg·L-1,r=0.999 9;and ketotifen fumarate were 20～200 mg·L-1,r=0.999 8;and ephedrine hydrochloride were 100-1000 mg·L-1,r=0.999 8;and ethylparaben were 3～30 mg·L-1,r=0.999 6.The average recoveries ofofloxacin were 98.14%,RSD=0.94%;and ketotifen fumarate were 98.33%,RSD=0.52%;and ephedrine hydrochloride were 98.83% RSD=1.22%;and ethylparaben were 98.91%,RSD=1.87%.CONCLUSION This methods accurate sensitive and fast.This methods is good at this nasal sprays.