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Role of Polyethylene Glycol and Silica for Dissolution Enhancement of Cefuroxime Axetil: In-Vitro Performance Evaluation and Characterization
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作者 Mst. Boby Aktar Bithy Milon Kumar Ghosh +3 位作者 Ashim Kumar Md. Rafiqul Islam Khan Mir Imam Ibne Wahed Ranjan Kumar Barman 《Pharmacology & Pharmacy》 CAS 2023年第5期156-175,共20页
Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therape... Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated Cefuroxime Axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy. 展开更多
关键词 Carplex-67 Cefuroxime axetil Improved Dissolution PEG-4000 Solid Dispersion Solvent Evaporation
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高效液相色谱法测定新菌灵片中头孢氨呋肟axetil的含量
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作者 王勇 吴信魏 丁寅芬 《海峡药学》 1994年第3期28-29,共2页
关键词 头孢氨呋肟 axetil 新菌灵 高效液相色谱法 流动相 精密量取 革兰氏阴性细菌 内标溶液 研磨成粉 甲醇超声
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Inclusion complexes of cefuroxime axetil with β-cyclodextrin:Physicochemical characterization, molecular modeling and effect of Larginine on complexation 被引量:3
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作者 Sarika Sapte Yogesh Pore 《Journal of Pharmaceutical Analysis》 SCIE CAS 2016年第5期300-306,共7页
The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We... The inclusion complexes of poorly water-soluble cephalosporin, cefuroxime axetil(CFA), were prepared with β-cyclodextrin(βCD) with or without addition of L-arginine(ARG) to improve its physicochemical properties. We also investigated the effect of ARG on complexation efficiency(CE) of βCD towards CFA in an aqueous medium through phase solubility behaviour according to Higuchi and Connors. Although phase solubility studies showed AL(linear) type of solubility curve in presence and absence of ARG, the CE and association constant(Ks) of βCD towards CFA were significantly promoted in presence of ARG,justifying its use as a ternary component. The solid systems of CFA with βCD were obtained by spray drying technique with or without incorporation of ARG and characterized by differential scanning calorimetry(DSC), X-ray powder diffractometry(XRPD), scanning electron microscopy(SEM), and saturation solubility and dissolution studies. The molecular modeling studies provided a better insight into geometry and inclusion mode of CFA inside βCD cavity. The solubility and dissolution rate of CFA were significantly improved upon complexation with βCD as compared to CFA alone. However, ternary system incorporated with ARG performed better than binary system in physicochemical evaluation. In conclusion, ARG could be exploited as a ternary component to improve the physicochemical properties of CFA via βCD complexation. 展开更多
关键词 CEFUROXIME axetil Β-CYCLODEXTRIN INCLUSION complex MOLECULAR modeling PHYSICOCHEMICAL characterization
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Development and evaluation of taste-masked dry suspension of cefuroxime axetil for enhancement of oral bioavailability 被引量:1
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作者 Yuqian Du Yinglei Zhai +4 位作者 Juhong Zhang Chunnuan Wu Cong Luo Jin Sun Zhonggui He 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2013年第5期287-294,共8页
Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared... Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared by means of wet granulation method and solid dispersion method.Binders,suspending agents and other compositions involved in the formulation were optimized.The differential scanning calorimetry(DSC)analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier,which contributed to an improvement of the dissolution rate.Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above.A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations,i.e.,two self-made dry suspensions and the commercial one.With a better release characteristic and a satisfying taste masking ability,the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs.The values of Cmax and AUC0e12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension,respectively.The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability. 展开更多
关键词 Cefuroxime axetil Taste masking Dry suspension Solid dispersion BIOAVAILABILITY
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Incompatibility of Paracetamol with Pediatric Suspensions Containing Amoxicillin, Azithromycin and Cefuroxime Axetil
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作者 Hamzah Maswadeh 《Pharmacology & Pharmacy》 2017年第11期355-368,共14页
The main objective of this work was to use the Differential Scanning Calorimetry (DSC) and FTIR spectroscopy to study the possible drug-drug or drug-excipient (s) interaction in case of concomitant oral administration... The main objective of this work was to use the Differential Scanning Calorimetry (DSC) and FTIR spectroscopy to study the possible drug-drug or drug-excipient (s) interaction in case of concomitant oral administration of paracetamol with the most common used antibiotics for children. Amoxicillin, azithromycin, cefuroxime axetil and their commercially available suspensions, Amoxil?, Azithromax? and Zinnat? were used. DSC curves for paracetamol, pure antibiotics, commercially available antibiotics and all binary mixtures used in this study showed drug-drug or drug-excipient (s) physical interaction and indicated a possible chemical interaction. To confirm chemical drug-drug or drug-excipient (s) interaction additional ATR-IR spectra for all samples used in this study were obtained. Results obtained from ATR-IR spectra showed drug-excipient (s) interaction in Zinnat?, Azithromax? and binary mixture Azithromax?-paracetamol, while chemical drug-drug interaction was not observed. From this study it can be concluded that the concomitant oral administration of paracetamol with commercially available antibiotics used in this study is not recommended and duration of two hours between the oral administrations of these drugs is strongly recommended to avoid drug-drug or drug-excipient (s) interaction. 展开更多
关键词 PARACETAMOL AMOXICILLIN AZITHROMYCIN CEFUROXIME axetil Compatibility DSC FTIR Drug-Drug Interaction
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Accelerated Aqueous Solubility and Antibacterial Activity of Cefuroxime Axetil Using Microcrystalline Cellulose as Carrier
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作者 Moushumi Tabassoom Salam Ashim Kumar +5 位作者 Akito Hata Hiromu Kondo Md. Abdus Salam Mir Imam Ibne Wahed Md. Rafiqul Islam Khan Ranjan Kumar Barman 《Pharmacology & Pharmacy》 2020年第8期159-173,共15页
This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a </span><i><span style="font-family:Verdana;">β</span>&l... This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a </span><i><span style="font-family:Verdana;">β</span></i><span style="font-family:Verdana;">-lactamase-stable broad spectrum second generation cephalosporin through solid dispersion (SD) technique. For this purpose, CA loaded SDs (CSDs) were prepared by solvent evaporation method using different concentrations of microcrystalline cellulose (MCC) as carrier. The CSDs were characterized by </span><i><span style="font-family:Verdana;">in-vitro</span></i><span style="font-family:Verdana;"> dissolution study, thermal analysis (DSC), crystallinity (PXRD), interactions (FTIR) and morphology (SEM). Among the formulations, CSD-2 showed the highest dissolution rate which was 2.59-fold higher than pure CA with a drug-carrier (CA: MCC) ratio of 1:3. Enhanced dissolution rate was attributed to conversion of drug from crystalline to amorphous state during preparation of SDs, which was validated by DSC, PXRD, FTIR and SEM analyses. Antibacterial activity of CSD-2 against </span><i><span style="font-family:Verdana;">Staphylococcus aureus</span></i><span style="font-family:Verdana;"> (ATCC 25923) and </span><i><span style="font-family:Verdana;">Escherichia coli</span></i><span style="font-family:Verdana;"> (ATCC 25922) showed 1.94- and 6.75-fold higher relative zone of inhibition (RZOI), respectively than pure CA. CSD-2 has been found to be the most effective optimized formulation in terms of both enhanced dissolution rate and antibacterial activity. Thus, it can be an effective alternative to conventional dosage forms of CA. However, further investigations are needed to validate its pharmacokinetic properties, </span><i><span style="font-family:Verdana;">in-vivo </span></i><span style="font-family:Verdana;">antibacterial efficacy and safety before recommending as a novel 展开更多
关键词 Cefuroxime axetil DISPERSION SOLUBILITY Antibacterial Activity
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Effect of flurbiprofen axetil analgesia after knee replacement on the cytokine contents in serum and joint fluid as well as HPA axis activity
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作者 Hao Lin Chun-Xia Liu 《Journal of Hainan Medical University》 2018年第12期25-28,共4页
Objective: To investigate the effect of flurbiprofen axetil analgesia after knee replacement on the cytokine contents in serum and joint fluid as well as HPA axis activity. Methods: Patients who underwent knee replace... Objective: To investigate the effect of flurbiprofen axetil analgesia after knee replacement on the cytokine contents in serum and joint fluid as well as HPA axis activity. Methods: Patients who underwent knee replacement in People's Hospital of Dongxihu District between April 2015 and January 2018 were selected as the research subjects and randomly divided into the experimental group who accepted flurbiprofen axetil combined with patient-controlled intravenous analgesia and the control group who accepted patient-controlled intravenous analgesia alone. The contents of cytokines and HPA axis-related hormones in serum were measured before surgery as well as 1 d and 3 d after surgery;the contents of cytokines in joint fluid were measured 1 d and 3 d after surgery. Results: Compared with those of same group before surgery, NGF, NPY, TNF-α, IL-2, IL-4, IL-10, ACTH, COR, INS, GH and PRL levels of both groups were increasing 1 d and 3 d after surgery, and NGF, NPY, TNF-α, IL-2, IL-4, IL-10, ACTH, COR, INS, GH and PRL levels in serum as well as PGE2, OPN, TGF-β1, FGF21, CXCL12 and YKL-40 in joint fluid of experimental group 1 d and 3 d after surgery were lower than those of control group. Conclusion: Flurbiprofen axetil analgesia after knee replacement can reduce the release of cytokines in serum and joint fluid, and inhibit the activity of HPA axis, and its analgesic effect is exact. 展开更多
关键词 KNEE replacement FLURBIPROFEN axetil CYTOKINE HPA axis
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Effect of flurbiprofen axetil intervention before induction on incision pain and inflammatory stress response after orthopedic surgery
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作者 Hong Liang Tai-Gong Jiang Bai-Zhan Lu 《Journal of Hainan Medical University》 2018年第24期73-76,共4页
Objective:To study the effect of flurbiprofen axetil intervention before induction on incision pain and inflammatory stress response after orthopedic surgery.Methods: A total of 86 cases of elderly patients who underw... Objective:To study the effect of flurbiprofen axetil intervention before induction on incision pain and inflammatory stress response after orthopedic surgery.Methods: A total of 86 cases of elderly patients who underwent operative treatment of femoral neck fracture in Guangyuan Hospital of Traditional Chinese Medicine between March 2014 and December 2017 were selected as the research subjects. All patients were randomly divided into the experimental group who accepted flurbiprofen axetil intervention before induction + routine anesthesia induction and maintenance, and the control group who accepted routine anesthesia induction and maintenance, and each group included 43 cases. The pain levels of the two groups were assessed 24 h after surgery;the levels of pain mediators and inflammatory stress molecules in serum as well as the expression intensity of inflammatory stress molecules in peripheral blood were determined before surgery and 24 h after surgery.Results:24 h after surgery, serum SP, NPY, PGE2, TNF-α, IL-1β, IL-18, ACTH, COR and NE levels as well as peripheral blood NF-κB, NLRP3, Caspase-1, GLUT4 and FOXP3 expression intensity of both groups were significantly higher than those before surgery, and NRS pain score, serum SP, NPY, PGE2, TNF- , IL-1β, IL-18, ACTH, COR and NE levels as well as peripheral blood NF-κB, NLRP3, Caspase-1, GLUT4 and FOXP3 expression intensity of experimental group 24 h after surgery were significantly lower than those of control group.Conclusions:Flurbiprofen axetil intervention before induction can improve and inhibit the incision pain and inflammatory stress response after orthopedic surgery. 展开更多
关键词 ORTHOPEDIC surgery FLURBIPROFEN axetil Pain MEDIATOR INFLAMMATORY RESPONSE Stress RESPONSE
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Effect of flurbiprofen axetil pretreatment on the pain degree as well as stress hormone and mediator secretion after abdominal surgery
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作者 Ying Chen 《Journal of Hainan Medical University》 2017年第14期37-41,共5页
Objective:To study the effect of flurbiprofen axetil pretreatment on the pain degree as well as stress hormone and mediator secretion after abdominal surgery.Methods: Patients undergoing abdominal surgery in our hospi... Objective:To study the effect of flurbiprofen axetil pretreatment on the pain degree as well as stress hormone and mediator secretion after abdominal surgery.Methods: Patients undergoing abdominal surgery in our hospital between May 2015 and March 2017 were selected and randomly divided into two groups, intervention group received flurbiprofen axetil pretreatment combined with routine intravenous anesthesia, and the control group only accepted conventional intravenous anesthesia. The levels of pain neurotransmitters and cytokines, stress hormones and mediators in serum were detected before operation as well as 12 h and 24 h after operation.Results: 12 h and 24 h after operation, serum NPY, SP, Glu, TNF-α, IL-2, IL-6, IL-10, ACTH, Cor, Ins, NE and E levels of both groups of patients were significantly higher than those before operation while SOD, GHS-Px and HO-1 levels were significantly lower than those before operation, and serum NPY, SP, Glu, TNF-α, IL-2, IL-6, IL-10, ACTH, Cor, Ins, NE and E levels of intervention group 12 h and 24 h after operation were significantly lower than those of control group while SOD, GHS-Px and HO-1 levels were significantly higher than those of control group.Conclusion:Flurbiprofen axetil pretreatment can reduce the pain degree and stress response after abdominal surgery. 展开更多
关键词 FLURBIPROFEN axetil PAIN CYTOKINE Stress
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利用计算模拟技术建立头孢呋辛酯片体内、外相关性溶出度评价方法
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作者 彭洁 洪建文 +6 位作者 肖慧 郭英豪 李佩 罗嘉琳 李何杏 丁子珊 陈涛 《中国抗生素杂志》 CAS CSCD 北大核心 2024年第3期325-332,共8页
目的利用计算模拟技术,探索建立前体药物头孢呋辛酯片的体内外相关性预测模型,用于仿制药生物等效性评估。方法参考文献中头孢呋辛酯片口服给药后的PK数据,结合参比制剂的血药浓度数据,利用GastroPlus TM软件搭建头孢呋辛酯片药代动力... 目的利用计算模拟技术,探索建立前体药物头孢呋辛酯片的体内外相关性预测模型,用于仿制药生物等效性评估。方法参考文献中头孢呋辛酯片口服给药后的PK数据,结合参比制剂的血药浓度数据,利用GastroPlus TM软件搭建头孢呋辛酯片药代动力学模型;结合原研制剂在不同溶出条件、4种溶出介质(pH1.2盐酸溶液、pH4.0醋酸盐缓冲溶液、pH6.8磷酸盐缓冲溶液和水)中的体外溶出行为,筛选适宜的溶出条件;将在不同溶出介质中得到的溶出曲线作为体内释放曲线,预测头孢呋辛酯片在体内PK参数并与参比制剂的临床实测数据进行比较,探讨头孢呋辛酯片体内外相关的溶出度方法。结果成功建立了头孢呋辛酯片体内外相关的溶出度方法:桨法,转速为55 r/min,以pH4.0醋酸盐缓冲液900 mL为溶出介质。结论所建立的头孢呋辛酯片药代动力学预测模型,可用于仿制药的生物等效性虚拟评估,为该药物的质量与疗效一致性评价提供了新思路。 展开更多
关键词 计算模拟技术 头孢呋辛酯片 溶出曲线 体内外相关性模型 仿制药
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氟比洛芬酯对胸腔镜右肺叶切除术患者单肺通气期间肺功能的影响
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作者 裴焕爽 于佳佳 +1 位作者 孟雨 付建峰 《临床麻醉学杂志》 CAS CSCD 北大核心 2024年第5期453-457,共5页
目的观察氟比洛芬酯对胸腔镜右肺叶切除术患者采用封堵器行单肺通气期间肺氧合功能、呼吸力学及肺部并发症的影响。方法选择择期全麻下行胸腔镜右肺叶切除术采用封堵器行单肺通气的患者60例,男25例,女35例,年龄35~64岁,BMI 18~28 kg/m^(... 目的观察氟比洛芬酯对胸腔镜右肺叶切除术患者采用封堵器行单肺通气期间肺氧合功能、呼吸力学及肺部并发症的影响。方法选择择期全麻下行胸腔镜右肺叶切除术采用封堵器行单肺通气的患者60例,男25例,女35例,年龄35~64岁,BMI 18~28 kg/m^(2),ASAⅠ或Ⅱ级。采用随机数字表法将患者分为两组:氟比洛芬酯组(F组)和对照组(C组),每组30例。F组在麻醉诱导前15 min静注氟比洛芬酯1.0 mg/kg,C组不予处理。于麻醉诱导前20 min(T_(0))、单肺通气30 min(T_(1))、单肺通气60 min(T_(2))、双肺通气15 min(T_(3))时抽取桡动脉血行血气分析,计算氧合指数(OI)并记录SpO_(2)。记录T_(1)、T_(2)时的气道峰压(Ppeak)、气道平台压(Pplat)、肺动态顺应性(Cdyn)和无效腔气量与潮气量之比(V_(D)/V_(T))。记录单肺通气期间低氧血症发生情况、补救例数、术后转ICU例数、术后72 h内肺不张、急性肺损伤和肺炎发生情况。结果与C组比较,F组T_(1)时SpO_(2)、T_(1)—T_(3)时PaO_(2)和OI、T_(1)、T_(2)时Cdyn明显升高(P<0.05);T_(1)、T_(2)时Ppeak和V_(D)/V_(T)、T_(2)时Pplat明显降低(P<0.05)。两组无一例单肺通气期间发生低氧血症和补救、术后转入ICU、术后72 h内发生肺不张、急性肺损伤和肺炎。结论对胸腔镜右肺叶切除术采用封堵器行单肺通气的患者,麻醉诱导前静注氟比洛芬酯有助于改善单肺通气期间肺氧合功能,优化呼吸力学参数。 展开更多
关键词 胸腔镜 肺叶切除术 封堵器 单肺通气 氟比洛芬酯 氧合 呼吸力学
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Preemptive analgesic effects of flurbiprofen axetil in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach 被引量:55
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作者 Wang Yan Zhang Hong-bin +2 位作者 Xia Bin Wang Gong-ming Zhang Meng-yuan 《Chinese Medical Journal》 SCIE CAS CSCD 2012年第4期579-582,共4页
Background Systemic non-steroidal anti-inflammatory drugs have been evaluated for their possible preemptive analgesic effects.The efficacy of flurbiprofen axetil for preemptive analgesia in patients undergoing radical... Background Systemic non-steroidal anti-inflammatory drugs have been evaluated for their possible preemptive analgesic effects.The efficacy of flurbiprofen axetil for preemptive analgesia in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach needs further investigation.The aim of this study was to research the preemptive analgesic effects of flurbiprofen axetil in thoracic surgery,and the influence of preoperative administration on postoperative respiratory function.Methods This randomized,double-blind,controlled trial enrolled 60 patients undergoing radical resection of esophageal carcinoma via the left thoracic approach.Anesthesia management was standardized.Each patient was randomly assigned to receive either 100 mg flurbiprofen axetil intravenously 15 minutes before incision (PA group) or intravenous normal saline as a control (C group).Postoperative analgesia was with sufentanil delivered by patient-controlled analgesia pump.Postoperative sufentanil consumption,visual analog scale pain scores,plasma levels of interleukin-8,and oxygenation index were measured.Results Compared with the preoperative baseline,postoperative patients in the PA group had no obvious increase in pain scores (P 〉0.05),but patients in the C group had significantly increased pain scores (P〈0.05).Pain scores in the C group were significantly higher at 24 hours postoperatively than preoperatively.Intergroup comparisons showed lower visual analog scale scores at 2-24 hours postoperatively in the PA group than the C group (P 〈0.05).Sufentanil consumption and plasma interleukin-8 levels at 2 and 12 hours postoperatively were significantly lower in the PA group than the C group (P 〈0.05).The oxygenation index at 2 and 12 hours postoperatively was significantly higher in the PA group than the C group (P〈0.05).Conclusions Intravenous flurbiprofen axetil appears to have a preemptive analgesic effect in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach,and appears to contribute to recovery of respiratorv function and to reduction of the postoperative inflammatory reaction. 展开更多
关键词 flurbiprofen axetil preemptive analgesia radical resection esophageal carcinoma
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Analgesic effect of parecoxib and flurbiprofen axetil for patients undergoing laparoscopic cholecystectomy and their influences on platelet aggregation 被引量:29
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作者 JI Fu-hai JIN Xin +1 位作者 YANG Jian-ping ZAN Li-li 《Chinese Medical Journal》 SCIE CAS CSCD 2010年第12期1607-1609,共3页
It is known that opioids produce postoperative analgesia, while it can also cause, especially in large doses, side effects like nausea, vomiting, constipation, syncope, skin itching, urinary retention and even respira... It is known that opioids produce postoperative analgesia, while it can also cause, especially in large doses, side effects like nausea, vomiting, constipation, syncope, skin itching, urinary retention and even respiratory inhibition. These factors have all greatly limited its clinical use for treating postoperative pain. Meanwhile, non-steroidal anti-inflammatory drugs (NSAIDs) play an increasingly important role in postoperative analgesia. Some studies suggest that NSAIDS may be neural protective in cerebral ischemic conditions. 展开更多
关键词 PARECOXIB flurbiprofen axetil cyclooxygenase inhibitor ANALGESIA
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Therapeutic time window of flurbiprofen axetil's neuroprotective effect in a rat model of transient focal cerebral ischemia 被引量:17
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作者 WANG Chen LIU Jun-le SANG Han-fei LU Yan DONG Hai-long XIONG Li-ze 《Chinese Medical Journal》 SCIE CAS CSCD 2008年第24期2572-2577,共6页
Background The neuroprotective effect of the cyclooxygenase (COX) inhibitor has been demonstrated in acute and chronic neurodegenerative processes. But its function under cerebral ischemic conditions is unclear. Thi... Background The neuroprotective effect of the cyclooxygenase (COX) inhibitor has been demonstrated in acute and chronic neurodegenerative processes. But its function under cerebral ischemic conditions is unclear. This study was designed to evaluate the neuroprotective efficacy of emulsified flurbiprofen axetil (FA, COX inhibitor) and its therapeutic time window in a model of transient middle cerebral artery occlusion (MCAO) in rats. Methods Forty-eight male SD rats were randomly assigned into six groups (n=8 in each group); three FA groups, vehicle, sham and ischemia/reperfusion (I/R) groups. Three doses of FA (5, 10 or 20 mg/kg, intravenous infusion) were administered just after cerebral ischemia/reperfusion (I/R). The degree of neurological outcome was measured by the neurologic deficit score (NDS) at 24, 48 and 72 hours after I/R. Mean brain infarct volume percentage (MBIVP) was determined with 2,3,5-triphenyltetrazolium chloride (TTC) staining at 72 hours after I/R. In three other groups (n=8 in each group), the selected dosage of 10 mg/kg was administrated intravenously at 6, 12 and 24 hours after I/R. Results The three different doses of FA improved NDS at 24, 48 and 72 hours after I/R and significantly reduced MBIVP. However, the degree of MBIVP in the FA 20 mg/kg group differed from that in FA 10 mg/kg group. Of interest is the finding that the neuroprotective effect conferred by 10 mg/kg of FA was also observed when treatment was delayed until 12-24 hours after ischemia reperfusion. Conclusion COX inhibitor FA is a promising therapeutic strategy for cerebral ischemia and its therapeutic time window could last for 12-24 hours after cerebral ischemia reperfusion, which would help in lessening the initial ischemic brain damage. 展开更多
关键词 cerebral ischemia flurbiprofen axetil NEUROPROTECTION neurologic deficit score therapeutic time window
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Flurbiprofen axetil promotes neuroprotection by activation of cerebral peroxisome proliferator-activated receptor gamma after focal cerebral ischemia in rats 被引量:13
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作者 LIU Jun-le JIN Jian-wen +1 位作者 PEI Shu-jun WANG Chen 《Chinese Medical Journal》 SCIE CAS CSCD 2012年第20期3719-3724,共6页
Background Our previous papers indicate that flurbiprofen axetil (FA), a cyclooxygenase inhibitor, is a promising therapeutic strategy for cerebral ischemia in rats. This study aimed to investigate whether FA could ... Background Our previous papers indicate that flurbiprofen axetil (FA), a cyclooxygenase inhibitor, is a promising therapeutic strategy for cerebral ischemia in rats. This study aimed to investigate whether FA could promote a neuroprotective effect by activation of peroxisome proliferator-activated receptor-y (PPAR-y) after focal cerebral ischemia in rats. Methods Totally 48 male Sprague-Dawley (SD) rats were randomly assigned into six groups (n=8 in each group): animals in group ischemia/reperfusion (I/R) only received 120-minute transient middle cerebral artery occlusion (tMCAO); animals in group I/R +FA were administered FA (10 mg/kg) by caudal vein just after 120-minute tMCAO; animals in group I/R +FA+GW9662 were administered GW9662 (a PPAR-Y inhibitor, 1 mg/kg) intraperitoneally 30 minutes before cerebral ischemia onset and FA (10 mg/kg) by caudal vein just after 120-minute tMCAO; animals in group I/R +GW9662 were administered GW9662 (1 mg/kg) intraperitoneally 30 minutes before cerebral ischemia onset; animals in group I/R +DMSO were administered 3% DMSO (vehicle of GW9662, 1 ml/kg) intraperitoneally 30 minutes before cerebral ischemia onset; animals in sham group experienced the identical surgery apart from the insertion of the nylon filament. The neurologic deficit score (NDS) were performed at 72 hours after reperfusion, and then mean brain infarct volume percentage (MBIVP) was determined with 2,3,5-triphenyltetrazolium chloride (TTC) 10 g/L staining. Results NDS was significantly increased in group I/R+FA (12.0 (10.0-15.0)), group I/R+FA+GW9662 (10.0 (8.0-12.0)), and in group I/R+FA+DMSO (12.0 (9.0-14.0)) at 72 hours after reperfusion compared with those in group I/R (7.5 (6.0-10.0)). NDS was conspicuously different between group I/R+FA (12.0 (10.0-15.0)) and group I/R+FA+GW9662 (10.0 (8.0-12.0)). MBIVP in group I/R ((45.82±8.83)%) was significantly greater than that in group I/R+FA ((23.52±9.90)%), group I/R+FA+GW9662 ((33.17±7.15)%); MBIVP in group I/R+FA ((23.52±9.90)%) was significantly smaller than that in group I/R+FA+GW9662 ((33.17±7.15)%). Conclusions FA confers the neuroprotective effect on tMCAO in rats and the selective PPAR-Y antagonist GW9662 attenuates the effect of FA. FA could promote a neuroprotective effect by, or in part, activation of PPAR-y after focal cerebral ischemia in rats. 展开更多
关键词 cerebral ischemia flurbiprofen axetil neuroprotection neurologic deficit score peroxisomeproliferator-activated receptor-8
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氟比洛芬酯与丙泊酚复合麻醉对老年肺癌肺叶切除术患者肺氧合功能、血流动力学及呼吸顺应性的影响
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作者 包萌萌 吴安石 《临床误诊误治》 CAS 2024年第1期99-104,共6页
目的分析氟比洛芬酯与丙泊酚复合麻醉对老年肺癌肺叶切除术患者围术期肺氧合功能、血流动力学及呼吸顺应性的影响。方法选取2020年1月—2022年6月行肺叶切除术的老年肺癌100例为研究对象,根据围术期麻醉方式的不同分为观察组和对照组,每... 目的分析氟比洛芬酯与丙泊酚复合麻醉对老年肺癌肺叶切除术患者围术期肺氧合功能、血流动力学及呼吸顺应性的影响。方法选取2020年1月—2022年6月行肺叶切除术的老年肺癌100例为研究对象,根据围术期麻醉方式的不同分为观察组和对照组,每组50例。观察组在单肺通气前实施氟比洛芬酯与丙泊酚复合麻醉,对照组在单肺通气前实施丙泊酚全凭静脉麻醉。比较2组术中丙泊酚用量,不同时间点[麻醉诱导前(T1)、单肺通气30 min(T2)、单肺通气60 min(T3)及术毕(T4)]肺氧合功能指标[氧分压(PaO_(2))、二氧化碳分压(PaCO_(2))、氧合指数(OI)]、血流动力学指标[平均动脉压(MAP)、心率(HR)]及呼吸顺应性指标[动态肺顺应性(Cdyn)]的变化情况,以及术后并发症发生情况。结果观察组术中丙泊酚用量(110.32±3.89)mg明显少于对照组(168.21±4.86)mg(P<0.01)。T1和T4时,2组PaO_(2)、PaCO_(2)、OI、MAP、HR、Cdyn比较差异均无统计学意义(P>0.05);与T1时比较,2组在T2和T3时PaO_(2)、PaCO_(2)、OI、HR及Cdyn均明显降低,MAP明显升高(P<0.05);其中观察组T2和T3时PaO_(2)、OI及Cdyn高于对照组,MAP、HR明显低于对照组(P<0.05,P<0.01)。观察组术后并发症总发生率18.00%(9/50)低于对照组54.00%(27/50)(P<0.01)。结论对行单肺通气下肺癌肺叶切除术的老年患者应用氟比洛芬酯与丙泊酚复合麻醉效果确切,可明显减少术中丙泊酚用量,改善患者围术期肺氧合功能及血流动力学,提高患者呼吸顺应性,有效保护肺功能,且安全性较好。 展开更多
关键词 肺肿瘤 老年人 肺叶切除术 麻醉 氟比洛芬酯 丙泊酚 氧合指数 血流动力学 呼吸顺应性 并发症
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氟比洛芬酯复合利多卡因用于妇科腹腔镜手术的麻醉效果研究
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作者 卓婷婷 肖丽 +1 位作者 马超 向睿 《中国医院用药评价与分析》 2024年第5期541-544,共4页
目的:探讨氟比洛芬酯复合利多卡因用于妇科腹腔镜手术的麻醉效果。方法:选取2020年10月至2022年10月于四川绵阳四〇四医院择期行腹腔镜手术的132例患者,采用单双号法分为对照组和联合组,各66例。麻醉诱导前10 min,对照组患者静脉注射0.9... 目的:探讨氟比洛芬酯复合利多卡因用于妇科腹腔镜手术的麻醉效果。方法:选取2020年10月至2022年10月于四川绵阳四〇四医院择期行腹腔镜手术的132例患者,采用单双号法分为对照组和联合组,各66例。麻醉诱导前10 min,对照组患者静脉注射0.9%氯化钠注射液10 mL,联合组患者双通道泵入氟比洛芬酯1.0 mg/kg+利多卡因1.0 mg/kg,术中持续输注利多卡因1.0 mg/(kg·h)至手术结束。比较两组患者术中用药剂量、脑电双频指数,术后(4、6和12 h)镇痛质量,术后12 h血清应激反应指标[肾上腺素(E)、去甲肾上腺素(NE)和皮质醇(Cor)]水平及术后24 h内不良反应发生情况。结果:联合组患者瑞芬太尼、丙泊酚总用量显著低于对照组;联合组患者插管前1 min、插管后1 min及插管后5 min的脑电双频指数显著低于对照组;术后4、6和12 h,联合组患者疼痛程度评分显著低于对照组,舒适度评分显著高于对照组;术后12 h,两组患者E、NE及Cor水平均较术前显著升高,但联合组患者的E、NE及Cor水平显著低于对照组,上述差异均有统计学意义(P<0.05)。术后24 h内,联合组、对照组患者的不良反应总发生率分别为4.55%(3/66)、7.58%(5/66),差异无统计学意义(P>0.05)。结论:氟比洛芬酯复合利多卡因预防性镇痛可有效提高妇科腹腔镜手术患者的麻醉镇痛质量,减轻机体围手术期应激反应,且使用安全。 展开更多
关键词 氟比洛芬酯 利多卡因 腹腔镜手术 预防性镇痛 镇痛质量 应激反应
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小儿解感颗粒联合头孢呋辛酯治疗小儿急性上呼吸道感染的效果及对患儿病情的影响
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作者 赵月华 《临床医学研究与实践》 2024年第11期99-102,共4页
目的分析小儿解感颗粒联合头孢呋辛酯治疗小儿急性上呼吸道感染(AURI)的效果。方法选择2019年1月至2021年12月我院收治的200例AURI患儿为研究对象,根据随机数字表法将其分为对照组(n=100,头孢呋辛酯)和研究组(n=100,小儿解感颗粒联合头... 目的分析小儿解感颗粒联合头孢呋辛酯治疗小儿急性上呼吸道感染(AURI)的效果。方法选择2019年1月至2021年12月我院收治的200例AURI患儿为研究对象,根据随机数字表法将其分为对照组(n=100,头孢呋辛酯)和研究组(n=100,小儿解感颗粒联合头孢呋辛酯)。比较两组的临床疗效、不良反应发生情况、血清指标和免疫功能指标。结果研究组的治疗总有效率为94.00%,高于对照组的80.00%(P<0.05)。两组的头晕、口干、腹泻、皮疹发生率及不良反应总发生率比较,差异无统计学意义(P>0.05)。治疗后,研究组的血清淀粉样蛋白A(SAA)、可溶性白细胞介素-2受体(sIL-2R)、白细胞介素-6(IL-6)、环氧化酶-2(COX-2)及细胞间黏附分子-1(ICAM-1)水平均低于对照组(P<0.05)。治疗后,研究组的CD4^(+)、CD4^(+)/CD8^(+)高于对照组,CD8^(+)低于对照组(P<0.05)。结论小儿解感颗粒联合头孢呋辛酯治疗小儿AURI能够改善患儿的血清指标和免疫功能,进而能够提高总体疗效,控制病情进展,且联合方案并未增加不良反应发生风险,临床可进一步推广运用。 展开更多
关键词 急性上呼吸道感染 小儿解感颗粒 头孢呋辛酯 免疫功能
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氟比洛芬酯预处理对于羟考酮复合丙泊酚在无痛纤维支气管镜检查术中应激反应的影响研究
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作者 兰竺霖 王昊 《中国实用医药》 2024年第5期1-5,共5页
目的研究氟比洛芬酯预处理对于羟考酮复合丙泊酚在无痛纤维支气管镜检查术中血流动力学以及应激反应的影响。方法90例无痛纤维支气管镜检查者,采用前瞻性研究方法,按随机数字表法分为A、B、C组,每组30例。A组:检查前5 min静脉滴注5 ml... 目的研究氟比洛芬酯预处理对于羟考酮复合丙泊酚在无痛纤维支气管镜检查术中血流动力学以及应激反应的影响。方法90例无痛纤维支气管镜检查者,采用前瞻性研究方法,按随机数字表法分为A、B、C组,每组30例。A组:检查前5 min静脉滴注5 ml生理盐水,检查前静脉注射羟考酮0.1 mg/kg,丙泊酚2 mg/kg;B组:检查前5 min静脉滴注5 ml生理盐水,检查前静脉注射羟考酮0.08 mg/kg,丙泊酚2 mg/kg;C组:检查前5 min静脉滴注50 mg氟比洛芬酯,检查前静脉注射羟考酮0.06 mg/kg,丙泊酚2 mg/kg。三组术中丙泊酚恒定输注,若术中患者体动则静脉追加丙泊酚30~50 mg。比较三组患者不同时间点[麻醉诱导前5 min(T0)、用药后即刻(T1)、喉罩置入后1 min(T2)、插入纤维支气管镜后1 min(T3)、纤维支气管镜取出后1 min(T4)、完成检查后5 min(T5)]血流动力学指标[经皮血氧饱和度(SpO_(2))、舒张压(DBP)、收缩压(SBP)、心率(HR)],不同时间点(T0、插入纤维支气管镜后3 min、T5)应激以及炎症反应指标[白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、肾上腺素(E)、去甲肾上腺素(NE)],不良反应(呛咳、低氧血症及喉、支气管痉挛)发生情况。结果T0、T4、T5时,三组SBP、DBP、HR、SpO_(2)比较差异无统计学意义(P>0.05);T2时,三组SpO_(2)比较差异无统计学意义(P>0.05);T1、T3时,三组SpO_(2)比较差异有统计学意义(P<0.05);T1、T2、T3时,三组SBP、DBP、HR比较差异有统计学意义(P<0.05)。T0时,三组NE、E、TNF-α、IL-6比较差异无统计学意义(P>0.05);插入纤维支气管镜后3 min、T5时,B组NE、E、TNF-α、IL-6均高于A组、C组,差异有统计学意义(P<0.05)。A组低氧血症、呛咳及喉、支气管痉挛发生率分别为20.00%、6.67%、3.33%,B组分别为3.33%、20.00%、6.67%,C组分别为3.33%、3.33%、3.33%。与A组比较,B组、C组低氧血症发生率明显降低,差异有统计学意义(P<0.05);与B组相比,C组呛咳发生率明显降低,差异有统计学意义(P<0.05);三组喉、支气管痉挛发生率比较,差异无统计学意义(P>0.05)。结论氟比洛芬酯预处理对羟考酮复合丙泊酚在无痛纤维支气管镜检查术中有助于缓解患者的应激反应,术中血流动力学更稳定,可使不良反应和麻醉药物剂量减少。 展开更多
关键词 氟比洛芬酯 无痛纤维支气管镜检查 羟考酮 丙泊酚 应激反应
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头孢呋辛酯联合小儿豉翘清热颗粒治疗儿童上呼吸道感染的效果
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作者 李中飞 黄艳春 胡晓玲 《中国医学创新》 CAS 2024年第8期11-15,共5页
目的:探究头孢呋辛酯联合小儿豉翘清热颗粒治疗儿童上呼吸道感染的临床效果。方法:选取2020年11月—2022年11月在当阳市人民医院治疗的上呼吸道感染患儿131例,应用随机数字表法将其分为对照组(n=65)及观察组(n=66),对照组接受头孢呋辛... 目的:探究头孢呋辛酯联合小儿豉翘清热颗粒治疗儿童上呼吸道感染的临床效果。方法:选取2020年11月—2022年11月在当阳市人民医院治疗的上呼吸道感染患儿131例,应用随机数字表法将其分为对照组(n=65)及观察组(n=66),对照组接受头孢呋辛酯治疗,观察组接受头孢呋辛酯联合小儿豉翘清热颗粒治疗。对比两组患儿临床症状消失时间、血清免疫球蛋白[免疫球蛋白G(IgG)、免疫球蛋白A(IgA)、免疫球蛋白M(IgM)、免疫球蛋白E(IgE)]、炎症指标[C反应蛋白(CRP)、血清淀粉样蛋白A(SAA)、降钙素原(PCT)]、症状积分(发热、咳嗽、鼻塞)、免疫功能指标(CD3^(+)、CD4^(+)、CD8^(+)、CD4^(+)/CD8^(+))。结果:对照组发热消失时间、咳嗽消失时间、咽痛消失时间、鼻塞消失时间均长于观察组,差异均有统计学意义(P<0.05)。治疗前,两组患儿IgG、IgA、IgM、IgE相较,差异均无统计学意义(P>0.05);治疗后,两组IgE均降低,IgG、IgA、IgM均升高,观察组IgE低于对照组,IgG、IgA、IgM均高于对照组,差异均有统计学意义(P<0.05)。治疗前,两组CRP、SAA、PCT相较,差异均无统计学意义(P>0.05);治疗后,两组CRP、SAA、PCT均降低,观察组均低于对照组,差异均有统计学意义(P<0.05)。治疗前,两组发热积分、咳嗽积分、鼻塞积分相较,差异均无统计学意义(P>0.05);治疗后,两组发热积分、咳嗽积分、鼻塞积分均降低,观察组均低于对照组,差异均有统计学意义(P<0.05)。治疗前,两组CD3^(+)、CD4^(+)、CD8^(+)、CD4^(+)/CD8^(+)相较,差异均无统计学意义(P>0.05);+治疗后,两组CD8均降低,CD3^(+)、CD4^(+)、CD4^(+)/CD8^(+)+均升高,观察组CD8低于对照组,CD3^(+)、CD4^(+)、CD4^(+)/CD8^(+)均高于对照组,差异均有统计学意义(P<0.05)。结论:头孢呋辛酯联合小儿豉翘清热颗粒治疗儿童上呼吸道感染效果显著,可改善免疫球蛋白水平及CRP、SAA、PCT表达水平,缩短症状消失时间,提升机体免疫功能。 展开更多
关键词 头孢呋辛酯 小儿豉翘清热颗粒 儿童 上呼吸道感染 C 反应蛋白 血清淀粉样蛋 A 降钙素原
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