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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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Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies
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作者 Zhining Ma Yuequan Wang +3 位作者 Huiyang He Tong Liu Qikun Jiang Xiaohong Hou 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2024年第3期177-189,共13页
Flurbiprofen(FB),a nonsteroidal anti-inflammatory drug,is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory effects.However,the racemic nature of its commercially available form... Flurbiprofen(FB),a nonsteroidal anti-inflammatory drug,is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory effects.However,the racemic nature of its commercially available formulation(Ocufen^(R))limits the full potential of its therapeutic activity,as the(S)-enantiomer is responsible for the desired antiinflammatory effects.Additionally,the limited corneal permeability of FB significantly restricts its bioavailability.In this study,we successfully separated the chiral isomers of FB to obtain the highly active(S)-FB.Subsequently,utilizing ion-pairing technology,we coupled(S)-FB with various counter-ions,such as sodium,diethylamine,trimethamine(TMA),and l-arginine,to enhance its ocular bioavailability.A comprehensive evaluation encompassed balanced solubility,octanol-water partition coefficient,corneal permeability,ocular pharmacokinetics,tissue distribution,and in vivo ocular anti-inflammatory activity of each chiral isomer salt.Among the various formulations,S-FBTMA exhibited superior water solubility(about 1–12 mg/ml),lipid solubility(1<lgP_(ow)<3)and corneal permeability.In comparison to Ocufen^(R),S-FBTMA demonstrated significantly higher in vivo antiinflammatory activity and lower ocular irritability(such as conjunctival congestion and tingling).The findings from this research highlight the potential of chiral separation and ion-pair enhanced permeation techniques in providing pharmaceutical enterprises focused on drug development with a valuable avenue for improving therapeutic outcomes. 展开更多
关键词 flurbiprofen ANTI-INFLAMMATORY Ophthalmic delivery Chiral resolution ION-PAIRING
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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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Synthesis of Flurbiprofen via Suzuki Reaction Catalyzed by Palladium Charcoal in Water 被引量:2
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作者 Gang LU Robert FRANZEN +1 位作者 Xiao Jing YU You Jun XU 《Chinese Chemical Letters》 SCIE CAS CSCD 2006年第4期461-464,共4页
Flurbiprofen 1, an excellent nonsteroidal antiinflammatory drug, was synthesized in 5 steps in 69% overall yield. The key step of constructing the biaryl fragment was successfully achieved via Pd/C-catalyzed Suzuki co... Flurbiprofen 1, an excellent nonsteroidal antiinflammatory drug, was synthesized in 5 steps in 69% overall yield. The key step of constructing the biaryl fragment was successfully achieved via Pd/C-catalyzed Suzuki coupling reaction in water using sodium tetraphenylborate as phenylation reagent. 展开更多
关键词 flurbiprofen Suzuki coupling PD/C sodium tetraphenylborate.
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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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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 被引量:1
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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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Preparation and characterization of solidified SMEDDS containing flurbiprofen by spray drying method
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作者 Yoo-Jeong Jang Kwan Hyung Cho 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2016年第1期108-109,共2页
Flurbiprofen, a non-steroidal anti-inflammatory agent, is used to treat rheumatoid arthritis and sore throat (1)However, it gave poor water solubility, and various solubilization technique such as self-microemulsifyin... Flurbiprofen, a non-steroidal anti-inflammatory agent, is used to treat rheumatoid arthritis and sore throat (1)However, it gave poor water solubility, and various solubilization technique such as self-microemulsifying drug delivery system(SMEDDS) has been used to improve the solubility, dissolution and oral bioavailability [2].The objective of this work was to develop redispersible solidified SMEDDS containing water-insoluble flurbiprofen with enhanced solubility. 展开更多
关键词 flurbiprofen SOLIDIFIED SMEDDS SOLUBILIZATION
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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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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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The Extent of Solubilization of Flurbiprofen and Ketoprofen by Cetyltrimethylammonium Micelles Using Semi-Equilibrium Dialysis
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作者 Jimmy D. Roach Ibrahim Laswi +2 位作者 Malik Mushannen Ali Chaari Mandy Bondaruk 《Advances in Materials Physics and Chemistry》 2020年第4期97-109,共13页
The partitioning of two non-steroidal anti-inflammatory drugs (NSAIDs), flurbiprofen and ketoprofen, into cationic cetyltrimethylammonium micelles was investigated using semi-equilibrium dialysis at 37℃ in phosphate ... The partitioning of two non-steroidal anti-inflammatory drugs (NSAIDs), flurbiprofen and ketoprofen, into cationic cetyltrimethylammonium micelles was investigated using semi-equilibrium dialysis at 37℃ in phosphate buffered saline. The micellar-water solubilization equilibrium constants for both NSAIDs, in their deprotonated forms, were observed to decrease linearly with increasing mole fraction of drug in micelles. For flurbiprofen, the solubilization constant in the limit as mole fraction of drug in micelles approaches zero was found to be 11,200 (co = 1 M), while for ketoprofen the value was 1950 (co = 1 M). Using 1H-NMR and UV spectroscopic techniques, the locus of solubilization for ketoprofen was found to be towards the charged exterior of the micelles, in the Stern layer, whereas flurbiprofen was found to solubilize more in the micellar interior. 展开更多
关键词 flurbiprofen KETOPROFEN CTAB MICELLE SOLUBILIZATION
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氟比洛芬酯联合纳布啡超前镇痛在腹腔镜胆囊切除术中的应用
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作者 刘涛 胡杰 《中外医疗》 2024年第22期26-31,共6页
目的评价氟比洛芬酯联合纳布啡超前镇痛应用于腹腔镜胆囊切除术(laparoscopic cholecystectomy,LC)中的临床效果。方法回顾性选取2022年8月—2023年10月于洛阳市中心医院接受LC的90例患者的临床资料,依据麻醉药物的不同分为纳布啡组(A组... 目的评价氟比洛芬酯联合纳布啡超前镇痛应用于腹腔镜胆囊切除术(laparoscopic cholecystectomy,LC)中的临床效果。方法回顾性选取2022年8月—2023年10月于洛阳市中心医院接受LC的90例患者的临床资料,依据麻醉药物的不同分为纳布啡组(A组,n=30)、氟比洛芬酯组(B组,n=30)和纳布啡联合氟比洛芬酯组(C组,n=30)。手术切皮前15 min给予超前镇痛药物,A组患者静脉输注纳布啡0.2 mg/kg,B组患者静脉输注氟比洛芬酯2 mg/kg,C组静脉输注纳布啡0.2 mg/kg和氟比洛芬酯2 mg/kg,比较3组患者术后2 h(T1)、术后4 h(T2)、术后12 h(T3)及术后24 h(T4)的视觉模拟评分法(Visual Analogue Scale,VAS)评分,Ramsay镇静评分,手术中使用丙泊酚和瑞芬太尼的剂量、停用药物后的苏醒时间、术后恢复质量评分[采用15项恢复质量(Quality of Recovery-15 Score,QoR-15)量表评估]、术后不良反应发生情况。结果3组患者丙泊酚用量、苏醒时间比较,差异无统计学意义(P均>0.05);C组患者瑞芬太尼用量低于A组和B组,差异有统计学意义(P<0.05)。C组患者T1、T2时间点VAS评分低于A组和B组,差异有统计学意义(P均<0.05);3组患者T3、T4时间点VAS评分比较,差异无统计学意义(P均>0.05)。3组患者T1~T4时间点的Ramsay评分比较,差异无统计学意义(P均>0.05)。C组患者术后第1天和术后第3天QoR-15评分显著高于A组和B组,差异有统计学意义(P均<0.05)。3组患者术后不良反应(恶心、呕吐、寒战、瘙痒和呼吸抑制)发生率比较,差异无统计学意义(P均>0.05)。结论氟比洛芬酯联合纳布啡超前镇痛在LC中可以提供良好的术中镇痛效果,并且能够抑制早期术后疼痛,提高患者术后生活质量,加速康复,联合应用安全性高,可以为腹腔镜下胆囊切除患者围术期镇痛管理提供参考。 展开更多
关键词 超前镇痛 氟比洛芬酯 纳布啡 腹腔镜胆囊切除术
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S(+)-Flurbiprofen Shows Potent PGE2 Inhibitory Activity in Inflammatory Cells, Superior Cell Transport Activity and Skin Permeability
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作者 Yoshihisa Toda Masanori Sugimoto +6 位作者 Hiromi Endo Miho Kamezawa Ichimaro Yamada Shogo Kawabata Shinsuke Kaku Noboru Otsuka Hideo Matsumoto 《Pharmacology & Pharmacy》 2016年第8期305-312,共8页
We developed a novel topical non-steroidal anti-inflammatory drug (NSAID)patch, S(+)-flurbiprofen plaster, (SFPP), containing S(+)-flurbiprofen (SFP), an enantiomer of flurbiprofen (FP). In a previous study conducted ... We developed a novel topical non-steroidal anti-inflammatory drug (NSAID)patch, S(+)-flurbiprofen plaster, (SFPP), containing S(+)-flurbiprofen (SFP), an enantiomer of flurbiprofen (FP). In a previous study conducted in an animal model, we showed good skin absorption and potent analgesic efficacy of SFPP. In this study, to examine the superior features, as an NSAID patch, of SFP as compared to FP and R(-)-flurbiprofen (RFP), we tested the stereospecificity of SFP actions on Prostaglandin E2 (PGE2) inhibition in rat inflammatory leukocytes and in the binding activity of the drug to cells, and also the in vitro skin permeability of the drug in the Yucatan micropig (YMP). SFP showed potent inhibitory activity on PGE2 production from peritoneal leukocytes stimulated with a bacterial suspension, as compared to RFP and FP. The half maximal (50%) inhibitory concentration (IC50) values were 14 nM for SFP, 52 nM for FP, and 17,000 nM for RFP. In the cell binding study, significant and rapid increase of SFP binding to polymorphonuclear leucocytes (PMNs) was observed at 5 min after incubation, eventually reaching a steady state. SFP showed significantly higher binding activity for the inflammatory leucocytes as compared to RFP, suggesting its superior transfer potency. The skin permeability profile of SFP, RFP and FP in the YMP model showed that the rank order of the cumulative amount of permeated compounds in the skin was SFP > RFP > FP. The steady-state permeation rate (Flux) of SFP was significantly higher than that of FP (4.89 and 1.55 mg/cm2/h, respectively, p = 0.0068), indicating the remarkably superior skin permeability of SFP. SFP exerted potent inhibitory activity on PGE2 production and superior binding activity to the PMNs and skin permeability, as compared to FP and RFP. These results suggest that SFP possesses favorable characteristics for use as an active ingredient in the NSAID patch. 展开更多
关键词 NSAIDS S(+)-flurbiprofen CYCLOOXYGENASE Skin Permeability
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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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不同剂量氟比洛芬酯复合地佐辛在老年宫腔镜手术超前镇痛中的应用效果 被引量:1
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作者 肖远航 《临床医学研究与实践》 2024年第7期98-101,共4页
目的探讨不同剂量氟比洛芬酯复合地佐辛在老年宫腔镜手术超前镇痛中的应用效果。方法选取2022年2月至2023年2月收治的136例拟行宫腔镜手术的老年患者为研究对象,以随机数字表法将其分为对照组和观察组,各68例。对照组采取50 mg氟比洛芬... 目的探讨不同剂量氟比洛芬酯复合地佐辛在老年宫腔镜手术超前镇痛中的应用效果。方法选取2022年2月至2023年2月收治的136例拟行宫腔镜手术的老年患者为研究对象,以随机数字表法将其分为对照组和观察组,各68例。对照组采取50 mg氟比洛芬酯复合地佐辛麻醉,观察组采取100 mg氟比洛芬酯复合地佐辛麻醉。比较两组的麻醉效果。结果术毕清醒时、术后10 min,观察组的呼吸频率、心率及平均动脉压均高于对照组(P<0.05)。术后4、8、12、24 h,观察组的视觉疼痛模拟量表(VAS)评分低于对照组(P<0.05);术后4、8、12 h,观察组的Ramsay镇静评分低于对照组(P<0.05)。术后4、8、12 h,观察组的舒适度量表(BCS)评分高于对照组(P<0.05)。术后12、24 h,观察组的白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)水平均低于对照组(P<0.05)。两组的不良反应总发生率比较,差异无统计学意义(P>0.05)。结论100 mg氟比洛芬酯+10 mg地佐辛在老年宫腔镜手术超前镇痛中的应用效果较好。 展开更多
关键词 氟比洛芬酯 地佐辛 宫腔镜手术 超前镇痛
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