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[PMID]:29443767
[Au] Autor:Xiang X; Yuan X; Lian Y; Fang J; Wu Y
[Ti] Título:Effect of oxycodone hydrochloride combined with flurbiprofen axetil for intravenous patient-controlled analgesia in lower abdominal patients: A randomized trial.
[So] Source:Medicine (Baltimore);97(7):e9911, 2018 Feb.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Problems like postoperative pain are still common phenomena after general anesthesia. Oxycodone hydrochloride is a semisynthetic opioid with a safe and excellent therapeutic effect on visceral pain. Flurbiprofen axetil has the efficacy of targeted analgesia. We hypothesize that different doses of oxycodone hydrochloride combined with flurbiprofen axetil would generate great results on postoperative intravenous analgesia in lower abdominal patients. METHODS: In the clinical trial, 90 American Society of Anesthesiologists I or II patients scheduled for elective general anesthesia were randomly divided into 3 groups, 30 cases in each group. Group I: oxycodone hydrochloride 0.5 mg/kg + flurbiprofen axetil 150 mg, group II: oxycodone hydrochloride 0.75 mg/kg + flurbiprofen axetil 150 mg, group III: oxycodone hydrochloride 1.0 mg/kg + flurbiprofen axetil 150 mg. Dilute them with 0.9% saline to 150 mL, respectively, with the background dose of 2 mL/h, patient-controlled analgesia 2 mL per time, with an interval of 10 min, and the loading dose of 0.1 mL/kg. Record the preoperative situation, 24 h (T0) before surgery, postoperative situation, 1 h (T1), 4 h (T2), 8 h (T3), 12 h (T4), 24 h (T5), 48 h (T6), 72 h (T7) after the surgery, including the mean arterial pressure, heart rate, saturation of pulse oximetry, static and dynamic pain rating (NRS) and Ramsay sedation score, effective pressing and total pressing ratio (referred to as the pressing ratio), patient satisfaction, and occurrence of adverse reactions. RESULTS: There was no significant statistic difference in mean arterial blood pressure, heart rate, arterial oxygen saturation, and adverse reactions among the 2 groups at each time point (P > .05). Compared with group I, the static NRS rating in group II and group III were significantly lower than that in group I (P < .05) from T1 to T5. The dynamic NRS rating of group II from T1 to T4 and that of group III from T1 to T5 were significantly lower (P < .05). The effective pressing and total pressing ratio was significantly higher (P < .05). There was no significant statistic difference between group II and group III in NRS rating and the effective pressing and total pressing ratio (P > .05). Compared with group III, the Ramsay sedation scores of group I and group II were significantly lower from T1 to T4 (P < .05). CONCLUSION: The dose of 0.75 mg/kg oxycodone hydrochloride combined with flurbiprofen axetil can provide safe and effective postoperative analgesia for lower abdominal patients, with fewer adverse reactions.
[Mh] Termos MeSH primário: Dor Abdominal
Flurbiprofeno/análogos & derivados
Oxicodona
Dor Pós-Operatória
[Mh] Termos MeSH secundário: Dor Abdominal/diagnóstico
Dor Abdominal/tratamento farmacológico
Dor Abdominal/etiologia
Administração Intravenosa
Idoso
Analgésicos Opioides/administração & dosagem
Analgésicos Opioides/efeitos adversos
Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/efeitos adversos
Relação Dose-Resposta a Droga
Monitoramento de Medicamentos/métodos
Quimioterapia Combinada/métodos
Feminino
Flurbiprofeno/administração & dosagem
Flurbiprofeno/efeitos adversos
Seres Humanos
Masculino
Meia-Idade
Oxicodona/administração & dosagem
Oxicodona/efeitos adversos
Medição da Dor/métodos
Dor Pós-Operatória/diagnóstico
Dor Pós-Operatória/tratamento farmacológico
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Anti-Inflammatory Agents, Non-Steroidal); 5GRO578KLP (Flurbiprofen); CD35PMG570 (Oxycodone); I0OU31PUI5 (flurbiprofen axetil)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180215
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000009911


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[PMID]:28450165
[Au] Autor:Liu N; Higashi K; Ueda K; Moribe K
[Ad] Endereço:Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan.
[Ti] Título:Effect of guest drug character encapsulated in the cavity and intermolecular spaces of γ-cyclodextrins on the dissolution property of ternary γ-cyclodextrin complex.
[So] Source:Int J Pharm;531(2):543-549, 2017 Oct 15.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Various ternary Guest 2/(Guest 1/γ-cyclodextrin (CD)) complexes were prepared using a cogrinding and subsequent heating method, wherein Guest 1 was incorporated in the cavity of γ-CD and Guest 2 was incorporated into the intermolecular spaces between γ-CD columns. Dissolution fluxes of Guest 1 and Guest 2 from all ternary complexes were almost identical. The dissolution flux of flurbiprofen (Guest 1) from the ternary complexes depended on the solubility of Guest 2 drugs (naproxen
[Mh] Termos MeSH primário: Portadores de Fármacos/química
gama-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Química Farmacêutica
Flurbiprofeno/química
Cetoprofeno/química
Naproxeno/química
Salicilamidas/química
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Salicylamides); 0 (gamma-Cyclodextrins); 57Y76R9ATQ (Naproxen); 5GRO578KLP (Flurbiprofen); 90Y4QC304K (Ketoprofen); KZJ0BYZ5VA (gamma-cyclodextrin); L929ZCK4BF (ethenzamide)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180109
[Lr] Data última revisão:
180109
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE


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[PMID]:28516471
[Au] Autor:Wakai A; Lawrenson JG; Lawrenson AL; Wang Y; Brown MD; Quirke M; Ghandour O; McCormick R; Walsh CD; Amayem A; Lang E; Harrison N
[Ad] Endereço:Emergency Care Research Unit (ECRU), Division of Population Health Sciences (PHS), Royal College of Surgeons in Ireland (RCSI), 123 St. Stephen's Green, Dublin 2, Ireland.
[Ti] Título:Topical non-steroidal anti-inflammatory drugs for analgesia in traumatic corneal abrasions.
[So] Source:Cochrane Database Syst Rev;5:CD009781, 2017 05 18.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Traumatic corneal abrasions are relatively common and there is a lack of consensus about analgesia in their management. It is therefore important to document the clinical efficacy and safety profile of topical ophthalmic non-steroidal anti-inflammatory drugs (NSAIDs) in the management of traumatic corneal abrasions. OBJECTIVES: To identify and evaluate all randomised controlled trials (RCTs) comparing the use of topical NSAIDs with placebo or any alternative analgesic interventions in adults with traumatic corneal abrasions (including corneal abrasions arising from foreign body removal), to reduce pain, and its effects on healing time. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (which contains the Cochrane Eyes and Vision Trials Register) (2017, Issue 2), MEDLINE Ovid (1946 to 30 March 2017), Embase Ovid (1947 to 30 March 2017), LILACS (Latin American and Caribbean Health Sciences Literature Database) (1982 to 30 March 2017), OpenGrey (System for Information on Grey Literature in Europe) (www.opengrey.eu/); searched 30 March 2017, ZETOC (1993 to 30 March 2017), the ISRCTN registry (www.isrctn.com/editAdvancedSearch); searched 30 March 2017, ClinicalTrials.gov (www.clinicaltrials.gov); searched 30 March 2017 and the WHO International Clinical Trials Registry Platform (ICTRP) (www.who.int/ictrp/search/en); searched 30 March 2017. We did not use any date or language restrictions in the electronic searches for trials.We checked the reference lists of identified trials to search for further potentially relevant studies. SELECTION CRITERIA: RCTs comparing topical NSAIDs to placebo or any alternative analgesic interventions in adults with traumatic corneal abrasions. DATA COLLECTION AND ANALYSIS: Two review authors independently performed data extraction and assessed risks of bias in the included studies. We rated the certainty of the evidence using GRADE. MAIN RESULTS: We included nine studies that met the inclusion criteria, reporting data on 637 participants.The studies took place in the UK, USA, Israel, Italy, France and Portugal. These studies compared five types of topical NSAIDs (0.1% indomethacin, 0.03% flurbiprofen, 0.5% ketorolac, 1% indomethacin, 0.1% diclofenac) to control (consisting of standard care and in four studies used placebo eye drops). Overall, the studies were at an unclear or high risk of bias (particularly selection and reporting bias). None of the included studies reported the primary outcome measures of this review, namely participant-reported pain intensity reduction of 30% or more or 50% or more at 24 hours. Four trials, that included data on 481 participants receiving NSAIDs or control (placebo/standard care), reported on the use of 'rescue' analgesia at 24 hours as a proxy measure of pain control. Topical NSAIDs were associated with a reduction in the need for oral analgesia compared with control (risk ratio (RR) 0.46, 95% confidence interval (CI) 0.34 to 0.61; low-certainty evidence). Approximately 4 out of 10 people in the control group used rescue analgesia at 24 hours. No data were available on the use of analgesia at 48 or 72 hours.One trial (28 participants) reported on the proportion of abrasions healed after 24 and 48 hours. These outcomes were similar in both arms of the trial. (at 24 hours RR 1.00 (0.81 to 1.23); at 48 hours RR 1.00 (0.88 to 1.14); low-certainty evidence). In the control group nine out of 10 abrasions were healed within 24 hours and all were healed by 48 hours. Complications of corneal abrasions were reported in 6 studies (609 participants) and were infrequently reported (4 complications, 1 in NSAID groups (recurrent corneal erosion) and 3 in control groups (2 recurrent corneal erosions and 1 corneal abscess), very low-certainty evidence). Possible drug-related adverse events (AEs) were reported in two trials (163 participants), with the number of adverse events low (4 AEs, 3 in NSAID group, including discomfort/photophobia on instillation, conjunctival hyperaemia and urticaria, and 1 in the control group, corneal abscess) very low-certainty evidence. AUTHORS' CONCLUSIONS: The findings of the included studies do not provide strong evidence to support the use of topical NSAIDs in traumatic corneal abrasions. This is important, since NSAIDs are associated with a higher cost compared to oral analgesics. None of the trials addressed our primary outcome measure of participant-reported pain intensity reduction of 30% or more or 50% or more at 24 hours.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/administração & dosagem
Lesões da Córnea/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Tópica
Anti-Inflamatórios não Esteroides/efeitos adversos
Lesões da Córnea/complicações
Diclofenaco/administração & dosagem
Flurbiprofeno/administração & dosagem
Seres Humanos
Indometacina/administração & dosagem
Cetorolaco/administração & dosagem
Medição da Dor
Ensaios Clínicos Controlados Aleatórios como Assunto
Cicatrização
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 144O8QL0L1 (Diclofenac); 5GRO578KLP (Flurbiprofen); XXE1CET956 (Indomethacin); YZI5105V0L (Ketorolac)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170809
[Lr] Data última revisão:
170809
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170519
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD009781.pub2


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[PMID]:28430684
[Au] Autor:Zhao H; Feng Y; Jiang Y; Lu Q
[Ad] Endereço:From the *Department of Anesthesiology and †Reproductive Medical Center, Peking University People's Hospital, Beijing, China.
[Ti] Título:Flurbiprofen Axetil Provides Effective Analgesia Without Changing the Pregnancy Rate in Ultrasound-Guided Transvaginal Oocyte Retrieval: A Double-Blind Randomized Controlled Trial.
[So] Source:Anesth Analg;125(4):1269-1274, 2017 Oct.
[Is] ISSN:1526-7598
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: In this prospective double-blind randomized study, we evaluated the analgesic effect and potential effect on pregnancy rate of the nonsteroidal anti-inflammatory drug flurbiprofen axetil in patients undergoing ultrasound-guided transvaginal oocyte retrieval under propofol-remifentanil anesthesia. METHODS: A total of 200 patients scheduled to undergo ultrasound-guided transvaginal oocyte retrieval were randomly allocated to receive 1.5 mg/kg of flurbiprofen axetil (FA group) or placebo (control group) 30 minutes before the procedure. Postoperative pain scores, embryo implantation rate, and pregnancy rate were recorded. Neuroendocrine biomarkers and prostaglandin E2 levels in follicular fluid were tested after oocyte retrieval. RESULTS: Patients in the FA group awakened earlier after surgery than patients in the control group (3.3 ± 2.6 vs 5.3 ± 3.4 minutes, P < .05) and had lower pain scores than patients in the control group (2.0 [0.0, 2.8] vs 5.0 [3.0, 5.0], P< .001). The difference in pregnancy rates between the 2 groups (44%-44%) was 0% (conventional 2-sided 95% confidence interval, -13.8% to 13.8%). The lower limit of the 90% 1-sided confidence interval for this difference was -9.0%, which was within the predefined noninferiority margin of -15.0%. The concentration of prostaglandin E2 in follicular fluid was decreased in the FA group (24.51 ± 1.52 vs 25.15 ± 1.49 pg/mL, P = .039), although the difference does not appear to be clinically important. CONCLUSIONS: Flurbiprofen axetil given before ultrasound-guided transvaginal oocyte retrieval for patients under propofol-remifentanil general anesthesia relieves pain without any detrimental effect on clinical pregnancy rate.
[Mh] Termos MeSH primário: Analgesia/métodos
Flurbiprofeno/análogos & derivados
Recuperação de Oócitos/métodos
Taxa de Gravidez/tendências
Ultrassonografia de Intervenção/métodos
Vagina
[Mh] Termos MeSH secundário: Adulto
Anestesia Geral/métodos
Método Duplo-Cego
Implantação do Embrião/efeitos dos fármacos
Implantação do Embrião/fisiologia
Feminino
Flurbiprofeno/administração & dosagem
Seres Humanos
Gravidez
Estudos Prospectivos
Vagina/efeitos dos fármacos
Vagina/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
5GRO578KLP (Flurbiprofen); I0OU31PUI5 (flurbiprofen axetil)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170422
[St] Status:MEDLINE
[do] DOI:10.1213/ANE.0000000000002025


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[PMID]:28421196
[Au] Autor:Xin JY; Sun LR; Chen SM; Wang Y; Xia CG
[Ad] Endereço:Key Laboratory for Food Science & Engineering, Harbin University of Commerce, Harbin 150076, China.
[Ti] Título:Synthesis of L-Ascorbyl Flurbiprofenate by Lipase-Catalyzed Esterification and Transesterification Reactions.
[So] Source:Biomed Res Int;2017:5751262, 2017.
[Is] ISSN:2314-6141
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The synthesis of L-ascorbyl flurbiprofenate was achieved by esterification and transesterification in nonaqueous organic medium with Novozym 435 lipase as biocatalyst. The conversion was greatly influenced by the kinds of organic solvents, speed of agitation, catalyst loading amount, reaction time, and molar ratio of acyl donor to L-ascorbic acid. A series of solvents were investigated, and tert-butanol was found to be the most suitable from the standpoint of the substrate solubility and the conversion for both the esterification and transesterification. When flurbiprofen was used as acyl donor, 61.0% of L-ascorbic acid was converted against 46.4% in the presence of flurbiprofen methyl ester. The optimal conversion of L-ascorbic acid was obtained when the initial molar ratio of acyl donor to ascorbic acid was 5 : 1. kinetics parameters were solved by Lineweaver-Burk equation under nonsubstrate inhibition condition. Since transesterification has lower conversion, from the standpoint of productivity and the amount of steps required, esterification is a better method compared to transesterification.
[Mh] Termos MeSH primário: Ácido Ascórbico/química
Flurbiprofeno/química
Lipase/química
[Mh] Termos MeSH secundário: Esterificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5GRO578KLP (Flurbiprofen); EC 3.1.1.- (Novozyme 435); EC 3.1.1.3 (Lipase); PQ6CK8PD0R (Ascorbic Acid)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170501
[Lr] Data última revisão:
170501
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170420
[St] Status:MEDLINE
[do] DOI:10.1155/2017/5751262


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[PMID]:28402193
[Au] Autor:Essa EA; Elmarakby AO; Donia AMA; El Maghraby GM
[Ad] Endereço:a Department of Pharmaceutical Technology, Faculty of Pharmacy , Tanta University , Tanta , Egypt.
[Ti] Título:Controlled precipitation for enhanced dissolution rate of flurbiprofen: development of rapidly disintegrating tablets.
[So] Source:Drug Dev Ind Pharm;43(9):1430-1439, 2017 Sep.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: The aim of this work was to investigate the potential of controlled precipitation of flurbiprofen on solid surface, in the presence or absence of hydrophilic polymers, as a tool for enhanced dissolution rate of the drug. The work was extended to develop rapidly disintegrated tablets. SIGNIFICANCE: This strategy provides simple technique for dissolution enhancement of slowly dissolving drugs with high scaling up potential. METHODS: Aerosil was dispersed in ethanolic solution of flurbiprofen in the presence and absence of hydrophilic polymers. Acidified water was added as antisolvent to produce controlled precipitation. The resultant particles were centrifuged and dried at ambient temperature before monitoring the dissolution pattern. The particles were also subjected to FTIR spectroscopic, X-ray diffraction and thermal analyses. RESULTS: The FTIR spectroscopy excluded any interaction between flurbiprofen and excipients. The thermal analysis reflected possible change in the crystalline structure and or crystal size of the drug after controlled precipitation in the presence of hydrophilic polymers. This was further confirmed by X-ray diffraction. The modulation in the crystalline structure and size was associated with a significant enhancement in the dissolution rate of flurbiprofen. Optimum formulations were successfully formulated as rapidly disintegrating tablet with subsequent fast dissolution. CONCLUSIONS: Precipitation on a large solid surface area is a promising strategy for enhanced dissolution rate with the presence of hydrophilic polymers during precipitation process improving the efficiency.
[Mh] Termos MeSH primário: Portadores de Fármacos/metabolismo
Excipientes/química
Flurbiprofeno/química
Polímeros/química
Comprimidos/química
[Mh] Termos MeSH secundário: Química Farmacêutica
Portadores de Fármacos/química
Interações Hidrofóbicas e Hidrofílicas
Solubilidade
Espectroscopia de Infravermelho com Transformada de Fourier
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Excipients); 0 (Polymers); 0 (Tablets); 5GRO578KLP (Flurbiprofen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170413
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1318905


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[PMID]:28402143
[Au] Autor:Wang HB; Yang FF; Gai XM; Cheng BC; Li JY; Pan H; Yang XG; Pan WS
[Ad] Endereço:a Department of Pharmaceutics, School of Pharmacy , Shenyang Pharmaceutical University , Liaoning , China.
[Ti] Título:A pH-independent instantaneous release of flurbiprofen: a study of the preparation of complexes, their characterization and in vitro/in vivo evaluation.
[So] Source:Drug Dev Ind Pharm;43(9):1460-1471, 2017 Sep.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In this study, furbiprofen/hydroxypropyl-ß-cyclodextrin (HPßCD) inclusion complexes were prepared to improve the drug dissolution and facilitate its application in hydrophilic gels. Inclusion complexes were prepared using a supercritical fluid processing and a conventional optimized co-lypholization method was employed as a reference. The entrapment efficacy and drug loading of both methods were investigated. Evaluation of drug dissolution enhancement was conducted in deionized water as well as buffer solutions of different pH. Carbopol 940 gels of both flurbiprofen and flurbiprofen/HPßCD inclusion complexes, with or without penetration enhancers, were prepared and percutaneous permeation studies were performed using rat abdominal skin samples. Formation of flurbiprofen/HPßCD inclusion complexes was confirmed by Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. The results obtained showed that SCF processing produced a higher EE (81.91 ± 1.54%) and DL (6.96 ± 0.17%) compared with OCL with values of 69.11 ± 2.23% and 4.00 ± 1.01%, respectively. A marked instantaneous release of flurbiprofen/HPßCD inclusion complexes prepared by SCF processing (103.04 ± 2.66% cumulative release within 5 min, a 10-fold increase in comparison with flurbiprofen alone) was observed. In addition, this improvement in dissolution was shown to be pH-independent (the percentage cumulative release at pH 1.2, 4.5, 6.8 and 7.4 at 5 min was 95.19 ± 1.71, 101.75 ± 1.44, 105.37 ± 4.58 and 96.84 ± 0.56, respectively). Percutaneous permeability of flurbiprofen-in-HPßCD-in-gels could be significantly accelerated by turpentine oil and was related to the water content in the system. An in vivo pharmacokinetic study showed a 2-fold increase in C and a shortened T as well as a comparable relative bioavailability when compared with the commercial flurbiprofen Cataplasms (Zepolas ). With their superior dissolution, these flurbiprofen/HPßCD inclusion complexes prepared by SCF processing could provide improved applications for flurbiprofen.
[Mh] Termos MeSH primário: Flurbiprofeno/química
Flurbiprofeno/farmacocinética
beta-Ciclodextrinas/química
beta-Ciclodextrinas/farmacocinética
[Mh] Termos MeSH secundário: 2-Hidroxipropil-beta-Ciclodextrina
Animais
Disponibilidade Biológica
Varredura Diferencial de Calorimetria
Química Farmacêutica
Liberação Controlada de Fármacos
Concentração de Íons de Hidrogênio
Interações Hidrofóbicas e Hidrofílicas
Microscopia Eletrônica de Varredura
Ratos
Espectroscopia de Infravermelho com Transformada de Fourier
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (beta-Cyclodextrins); 1I96OHX6EK (2-Hydroxypropyl-beta-cyclodextrin); 5GRO578KLP (Flurbiprofen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170413
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1318908


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[PMID]:28259191
[Au] Autor:Vayá I; Jiménez MC; Miranda MA; Chatterjee A; Gustavsson T
[Ad] Endereço:Departamento de Química/Instituto de Tecnología, Química UPV-CSIC, Universitat Politècnica de València Camino de Vera s/n, 46022 Valencia, Spain, School of Chemistry, University of East Anglia, Norwich Research Park NR4 7TJ, Norwich, United Kingdom;, Email: i.vaya-perez@uea.ac.uk.
[Ti] Título:Ultrafast Fluorescence Dynamics in Flurbiprofen-Amino Acid Dyads and in the Supramolecular Drug/Protein Complex.
[So] Source:Chimia (Aarau);71(1-2):18-25, 2017 Feb 22.
[Is] ISSN:0009-4293
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The interaction dynamics between the drug flurbiprofen (FBP) and human serum albumin (HSA) has been investigated by time-resolved fluorescence spectroscopy, combining femtosecond fluorescence upconversion and picosecond time-correlated single photon counting. In order to obtain additional information on the drug/ protein interaction, several covalently linked model dyads, composed of FBP and tryptophan or tyrosine, were also studied. For all systems, the main feature was a remarkable dynamic FBP fluorescence quenching, more prominent in the dyads than in the protein complex. All systems also displayed a clear stereoselectivity depending on the (S)- or (R)-form of FBP, that was strongly influenced by the conformational arrangement of the investigated chromophores.
[Mh] Termos MeSH primário: Aminoácidos/química
Fluorescência
Flurbiprofeno/química
Albumina Sérica/química
[Mh] Termos MeSH secundário: Seres Humanos
Substâncias Macromoleculares/química
Modelos Moleculares
Estrutura Molecular
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acids); 0 (Macromolecular Substances); 0 (Serum Albumin); 5GRO578KLP (Flurbiprofen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170904
[Lr] Data última revisão:
170904
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170306
[St] Status:MEDLINE
[do] DOI:10.2533/chimia.2017.18


  9 / 1767 MEDLINE  
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[PMID]:28147361
[Au] Autor:Uwai Y; Matsumoto M; Kawasaki T; Nabekura T
[Ad] Endereço:Department of Pharmaceutics, School of Pharmacy, Aichi Gakuin University, Nagoya, Japan.
[Ti] Título:Enantioselective Effect of Flurbiprofen on Lithium Disposition in Rats.
[So] Source:Pharmacology;99(5-6):236-239, 2017.
[Is] ISSN:1423-0313
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:AIMS: Lithium is administered for treating bipolar disorders and is mainly excreted into urine. Nonsteroidal anti-inflammatory drugs inhibit this process. In this study, we examined the enantioselective effect of flurbiprofen on the disposition of lithium in rats. METHODS: Pharmacokinetic experiments with lithium were performed. RESULTS: Until 60 min after the intravenous administration of lithium chloride at 30 mg/kg as a bolus, 17.8% of lithium injected was recovered into the urine. Its renal clearance was calculated to be 1.62 mL/min/kg. Neither creatinine clearance (Ccr) nor pharmacokinetics of lithium was affected by the simultaneous injection of (R)-flurbiprofen at 20 mg/kg. (S)-flurbiprofen impaired the renal function and interfered with the urinary excretion of lithium. The ratio of renal clearance of lithium to Ccr was decreased by the (S)-enantiomer. CONCLUSION: This study clarified that the (S)-flurbiprofen but not (R)-flurbiprofen inhibited the renal excretion of lithium in rats.
[Mh] Termos MeSH primário: Flurbiprofeno/farmacologia
Cloreto de Lítio/farmacocinética
[Mh] Termos MeSH secundário: Animais
Cloreto de Lítio/sangue
Cloreto de Lítio/urina
Masculino
Ratos
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5GRO578KLP (Flurbiprofen); G4962QA067 (Lithium Chloride)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170516
[Lr] Data última revisão:
170516
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170202
[St] Status:MEDLINE
[do] DOI:10.1159/000455917


  10 / 1767 MEDLINE  
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[PMID]:28106772
[Au] Autor:Porrini V; Sarnico I; Benarese M; Branca C; Mota M; Lanzillotta A; Bellucci A; Parrella E; Faggi L; Spano P; Imbimbo BP; Pizzi M
[Ad] Endereço:Department of Molecular and Translational Medicine, University of Brescia, Viale Europa 11, 25123 Brescia, Italy. v.porrini@unibs.it.
[Ti] Título:Neuroprotective and Anti-Apoptotic Effects of CSP-1103 in Primary Cortical Neurons Exposed to Oxygen and Glucose Deprivation.
[So] Source:Int J Mol Sci;18(1), 2017 Jan 18.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:CSP-1103 (formerly CHF5074) has been shown to reverse memory impairment and reduce amyloid plaque as well as inflammatory microglia activation in preclinical models of Alzheimer's disease. Moreover, it was found to improve cognition and reduce brain inflammation in patients with mild cognitive impairment. Recent evidence suggests that CSP-1103 acts through a single molecular target, the amyloid precursor protein intracellular domain (AICD), a transcriptional regulator implicated in inflammation and apoptosis. We here tested the possible anti-apoptotic and neuroprotective activity of CSP-1103 in a cell-based model of post-ischemic injury, wherein the primary mouse cortical neurons were exposed to oxygen-glucose deprivation (OGD). When added after OGD, CSP-1103 prevented the apoptosis cascade by reducing cytochrome c release and caspase-3 activation and the secondary necrosis. Additionally, CSP-1103 limited earlier activation of p38 and nuclear factor κB (NF-κB) pathways. These results demonstrate that CSP-1103 is neuroprotective in a model of post-ischemic brain injury and provide further mechanistic insights as regards its ability to reduce apoptosis and potential production of pro-inflammatory cytokines. In conclusion, these findings suggest a potential use of CSP-1103 for the treatment of brain ischemia.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Ciclopropanos/farmacologia
Flurbiprofeno/análogos & derivados
Glucose/deficiência
Neurônios/patologia
Fármacos Neuroprotetores/farmacologia
Oxigênio/farmacologia
[Mh] Termos MeSH secundário: Animais
Caspase 3/metabolismo
Núcleo Celular/efeitos dos fármacos
Núcleo Celular/metabolismo
Córtex Cerebral/patologia
Citocromos c/metabolismo
Ativação Enzimática/efeitos dos fármacos
Flurbiprofeno/farmacologia
Glicogênio Sintase Quinase 3 beta/metabolismo
Ibuprofeno/farmacologia
Camundongos Endogâmicos C57BL
Necrose
Neurônios/efeitos dos fármacos
Neurônios/metabolismo
Fator de Transcrição RelA/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(3',4'-dichloro-2-fluoro(1,1'-biphenyl)-4-yl)cyclopropanecarboxylic acid); 0 (Cyclopropanes); 0 (Neuroprotective Agents); 0 (Transcription Factor RelA); 5GRO578KLP (Flurbiprofen); 9007-43-6 (Cytochromes c); EC 2.7.11.1 (Glycogen Synthase Kinase 3 beta); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); EC 3.4.22.- (Caspase 3); IY9XDZ35W2 (Glucose); S88TT14065 (Oxygen); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170424
[Lr] Data última revisão:
170424
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170121
[St] Status:MEDLINE



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