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flurbiprofen microneedle patches for the management of acute postoperative pain

Nano Research 2024年第8期17卷 7493-7503页

作者： Huaqing Chu Yanyan Zhang Yuan Yang Jiangtao Xue Cong Li Wei Zhang Zhou Li Hui Zheng National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100021China Beijing Institute of Nanoenergy and Nanosystems Chinese Academy of SciencesBeijing 101400China Key Laboratory of Hunan Province for Integrated Traditional Chinese and Western Medicine on Prevention and Treatment of Cardio-Cerebral Diseases School of Integrated Chinese and Western MedicineHunan University of Chinese MedicineChangsha 410208China School of Life Science Institute of Engineering MedicineBeijing Institute of TechnologyBeijing 100081China Institute of Process Engineering Chinese Academy of SciencesBeijing 100190China

Acute postoperative pain is commonly treated with flurbiprofen(FBP),but conventional delivery methods are *** study prepared a new non-burst release microneedles(MNs)using genipin cross-linked gelatin(cGel).By adding varying amounts of genipin to modulate the crosslinking degree of cGel,the drug release behavior of the drug-loaded MNs in the skin can be *** crosslinking parameters that meet therapeutic requirements are selected,thus providing rapid and longlasting analgesic *** solutions were successfully cross-linked,altering matrix material microstructure,confirmed by scanning electron microscope imaging and fourier transform infrared *** demonstrated increasing mechanical strength with higher *** release rates were rapid initially,then slowed,exhibiting a characteristic of decreased release rates with increasing degrees of *** vivo,FBP/cGel MNs significantly reduced allodynia and hyperalgesia post-surgery,with the greatest effect observed at 2–3 h post-surgery,and can maintain analgesia for up to 6 *** tests confirmed good ***/cGel MNs effectively penetrate the stratum corneum,safely delivering drugs with significant analgesic effects,excellent mechanical properties,and good biocompatibility,representing a promising strategy for managing acute postoperative pain.

关键词： microneedle postoperative pain flurbiprofen non-steroid anti-inflammatory drug cross-linked gelatin

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Synthesis of flurbiprofen via Suzuki Reaction Catalyzed by Palladium Charcoal in Water

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Chinese Chemical Letters 2006年第4期17卷 461-464页

作者： Gang LU Robert FRANZEN Xiao Jing YU You Jun XU School of Pharmaceutical Engineering Shenyang Pharmaceutical University 103 Wenhua Road Shenyang 110016 Institute of Materials Chemistry Tampere University of Technology Korkeakoulunkatu 8 Tampere FIN-33720 Finland

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... 详细信息

关键词： flurbiprofen Suzuki coupling Pd/C sodium tetraphenylborate.

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Formulation and evaluation of co-prodrug of flurbiprofen and methocarbamol

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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 449-458页

作者： Neela Bhatia Kiran Katkar Snehal Ashtekar Department of Quality Assurance Bharati Vidyapeeth College of Pharmacy Near Chitranagari Shivaji University

The current work envisages synthesis of an ester prodrug of flurbiprofen whereby its carboxylic group was condensed with a skeletal muscle relaxant methocarbamol, with the aim of synergistic activity of two drugs, avoid flurbiprofen mediated gastro-intestinal damage and minimize the ulceration tendency of flurbiprofen. The synthesized prodrug was characterized and confirmed by physicochemical and spectroscopic studies. Solubility and partition coefficient studies indicated an increased lipophilicity and thus better suitability for oral administration than the parent drugs and the protein binding studies revealed a low protein binding capacity of the mutual prodrug. Subsequently, in-vitro hydrolysis was studied in different pH, simulated gastric fluid, simulated intestinal fluid and plasma and quantitative evaluation was performed by high performance liquid chromatography. It was found that the prodrug remained unhydrolyzed in the stomach after absorption however, underwent rapid cleavage by the esterases in blood to give the parent drug. Furthermore, the mutual ester prodrug was evaluated for its anti-inflammatory, analgesic, skeletal muscle relaxation, ulcerogenic and total acid content activity and was found to possess comparable activity with that of the parent drugs. Microscopic structures of the stomach tissues revealed significant reduction in gastric ulcer formation of mice gastric mucosa as compared to parent carboxylic acid drug.

关键词： NSAIDs flurbiprofen Skeletal muscle relaxant Methocarbamol, Ester prodrug RP-HPLC Ulcerogenicity

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Preparation and characterization of solidified SMEDDS containing flurbiprofen by spray drying method

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 108-109页

作者： Yoo-Jeong Jang Kwan Hyung Cho College of Pharmacy Inje University

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.

关键词： flurbiprofen Solidified SMEDDS Solubilization

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flurbiprofen and its attenuating effect on intracranial ischemic injury as well as ischemia in other systemic organs

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Chinese Medical Journal 2013年第3期126卷 553-553页

作者： Shailendra Kapoor 7487 Sherwood Crossing place #302 USA MechanicsvilleVA

To the＇ editor： I read with great interest the recent article by Liu et al.1 The article provided highly interesting data on the mitigating effect of flurbiprofen on ischemia related injury. Interestingly, besides affording neuroprotection by activation of cerebral peroxisome proliferator activated receptor gamma, flurbiprofen also affords cerebral protection after ischemia/reperfusion injury by modulating the Akt/GSK-3[3 pathway.^2 It also up regulates Bcl-2 expression.

关键词： flurbiprofen attenuating effect on intracranial ischemic injury systemic organs

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The Extent of Solubilization of flurbiprofen and Ketoprofen by Cetyltrimethylammonium Micelles Using Semi-Equilibrium Dialysis

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Advances in Materials Physics and Chemistry 2020年第4期10卷 97-109页

作者： Jimmy D. Roach Ibrahim Laswi Malik Mushannen Ali Chaari Mandy Bondaruk Pre-Medical Education Unit Weill Cornell Medical College-Qatar Doha Qatar

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.

关键词： flurbiprofen Ketoprofen CTAB Micelle Solubilization

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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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Journal of Hainan Medical University 2017年第14期23卷 37-41页

作者： Ying Chen Anesthesiology Department Combine Traditional Chinese and Western Medicine Hospital of Liangshan Prefecture in Sichuan ProvinceLiangshanSichuan Province615000

Objective:To study the effect of flurbiprofen axetil pretreatment on the pain degree as well as stress hormone and mediator secretion after abdominal ***: 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 ***: 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 ***:flurbiprofen axetil pretreatment can reduce the pain degree and stress response after abdominal surgery.

关键词： flurbiprofen axetil Pain Cytokine Stress

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(S)-（+）-flurbiprofen的制备

(S)-（+）-Flurbiprofen的制备

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“以岭医药杯”第八届全国青年药学工作者最新科研成果交流...

作者：梁美好王尊元马臻沈正荣浙江省医学科学院浙江省医学科学院浙江省医学科学院浙江省医学科学院

目的: 采用新的方法合成非甾体抗炎镇痛药flurbiprofen并拆分得到S-异构体。方法以国内价格较低廉的2-氟苯胺为起始原料,经1,3-二溴-5,5-二甲基海因溴代、与苯缩合、再与2-溴丙酸钠进行格氏反应,酸化后得到外消旋的flurbiprofen, 再经... 详细信息

目的: 采用新的方法合成非甾体抗炎镇痛药flurbiprofen并拆分得到S-异构体。方法以国内价格较低廉的2-氟苯胺为起始原料,经1,3-二溴-5,5-二甲基海因溴代、与苯缩合、再与2-溴丙酸钠进行格氏反应,酸化后得到外消旋的flurbiprofen, 再经葡辛胺拆分,得（S）-（+）-flurbiprofen。结果成功制备得到目标产物,其结构经mp、NMR等确证。结论该制备方法具有工艺简单、得率高、试剂价格低廉等特点,适合于工业化生产。

关键词： flurbiprofen 合成拆分

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