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1.
Pharm Res ; 37(3): 42, 2020 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-31989335

RESUMO

PURPOSE: The design of biorelevant conditions for in vitro evaluation of orally administered drug products is contingent on obtaining accurate values for physiologically relevant parameters such as pH, buffer capacity and bile salt concentrations in upper gastrointestinal fluids. METHODS: The impact of sample handling on the measurement of pH and buffer capacity of aspirates from the upper gastrointestinal tract was evaluated, with a focus on centrifugation and freeze-thaw cycling as factors that can influence results. Since bicarbonate is a key buffer system in the fasted state and is used to represent conditions in the upper intestine in vitro, variations on sample handling were also investigated for bicarbonate-based buffers prepared in the laboratory. RESULTS: Centrifugation and freezing significantly increase pH and decrease buffer capacity in samples obtained by aspiration from the upper gastrointestinal tract in the fasted state and in bicarbonate buffers prepared in vitro. Comparison of data suggested that the buffer system in the small intestine does not derive exclusively from bicarbonates. CONCLUSIONS: Measurement of both pH and buffer capacity immediately after aspiration are strongly recommended as "best practice" and should be adopted as the standard procedure for measuring pH and buffer capacity in aspirates from the gastrointestinal tract. Only data obtained in this way provide a valid basis for setting the physiological parameters in physiologically based pharmacokinetic models.


Assuntos
Bicarbonatos/química , Ácidos e Sais Biliares/química , Líquidos Corporais/química , Líquidos Corporais/metabolismo , Trato Gastrointestinal Superior/química , Trato Gastrointestinal Superior/metabolismo , Tampões (Química) , Famotidina/administração & dosagem , Famotidina/metabolismo , Absorção Gastrointestinal , Humanos , Concentração de Íons de Hidrogênio , Ibuprofeno/administração & dosagem , Ibuprofeno/metabolismo , Intestino Delgado , Sais/química , Estômago
2.
Medicine (Baltimore) ; 98(51): e18473, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31861028

RESUMO

BACKGROUND: The aim of this study is to determine the efficacy of preemptive analgesia with paracetamol and ibuprofen to reduce the intensity and incidence of headache and myalgia after electroconvulsive therapy (ECT). METHODS: Sixty patients with major depression who were treated with ECT were randomized to receive ECT 3 times a week. The first 3 sessions were included in the study. The patients were divided into 3 groups; Group C (Control, Saline, n = 20), Group P (Paracetamol, n = 20), and Group I (Ibuprofen, n = 20). Demographics, duration of seizure, visual analog scale (VAS) for headache and myalgia and nausea, vomiting and pruritus were evaluated at postoperative 24 hours period. RESULTS: Duration of seizure after ECT was similar in all groups (P = .148). In the study, heart rate and mean arterial pressure were found to be some changes in some of the sessions. There were no significant differences in any comparison for all groups in all sessions regarding VAS scores for headache and myalgia. Incidence of headache and myalgia in Group I was lower than the other groups (P = .233, P = .011, respectively). But, there was no significant difference between the other groups. There was no significant difference in vomiting, intergroups, and intragroup. CONCLUSIONS: The findings of our study indicate that pain intensity of headache and myalgia did not show a significant change between groups and within groups. While pain intensity of myalgia between the groups reached no statistical significance, ibuprofen was significantly lowered the incidence of myalgia at postoperative 24 hours period.


Assuntos
Analgésicos não Entorpecentes/administração & dosagem , Eletroconvulsoterapia/efeitos adversos , Cefaleia/prevenção & controle , Mialgia/prevenção & controle , Acetaminofen/administração & dosagem , Adulto , Transtorno Depressivo Maior/terapia , Método Duplo-Cego , Feminino , Cefaleia/etiologia , Humanos , Ibuprofeno/administração & dosagem , Masculino , Pessoa de Meia-Idade , Mialgia/etiologia , Adulto Jovem
3.
Int J Mol Sci ; 20(20)2019 Oct 11.
Artigo em Inglês | MEDLINE | ID: mdl-31614502

RESUMO

A desirable multi-functional nanofibrous membrane (NFM) for prevention of postoperative tendon adhesion should be endowed with abilities to prevent fibroblast attachment and penetration and exert anti-inflammation effects. To meet this need, hyaluronic acid (HA)/ibuprofen (IBU) (HAI) NFMs were prepared by electrospinning, followed by dual ionic crosslinking with FeCl3 (HAIF NFMs) and covalent crosslinking with 1,4-butanediol diglycidyl ether (BDDE) to produce HAIFB NFMs. It is expected that the multi-functional NFMs will act as a physical barrier to prevent fibroblast penetration, HA will reduce fibroblast attachment and impart a lubrication effect for tendon gliding, while IBU will function as an anti-inflammation drug. For this purpose, we successfully fabricated HAIFB NFMs containing 20% (HAI20FB), 30% (HAI30FB), and 40% (HAI40FB) IBU and characterized their physico-chemical properties by scanning electron microscopy, Fourier transformed infrared spectroscopy, thermal gravimetric analysis, and mechanical testing. In vitro cell culture studies revealed that all NFMs except HAI40FB possessed excellent effects in preventing fibroblast attachment and penetration while preserving high biocompatibility without influencing cell proliferation. Although showing significant improvement in mechanical properties over other NFMs, the HAI40FB NFM exhibited cytotoxicity towards fibroblasts due to the higher percentage and concentration of IBU released form the membrane. In vivo studies in a rabbit flexor tendon rupture model demonstrated the efficacy of IBU-loaded NFMs (HAI30FB) over Seprafilm® and NFMs without IBU (HAFB) in reducing local inflammation and preventing tendon adhesion based on gross observation, histological analyses, and biomechanical functional assays. We concluded that an HAI30FB NFM will act as a multi-functional barrier membrane to prevent peritendinous adhesion after tendon surgery.


Assuntos
Ácido Hialurônico/administração & dosagem , Ibuprofeno/administração & dosagem , Traumatismos dos Tendões/cirurgia , Aderências Teciduais/prevenção & controle , Células 3T3 , Animais , Proliferação de Células , Células Cultivadas , Modelos Animais de Doenças , Ácido Hialurônico/química , Ácido Hialurônico/farmacologia , Ibuprofeno/química , Ibuprofeno/farmacologia , Membranas Artificiais , Camundongos , Microscopia Eletrônica de Varredura , Nanofibras , Coelhos , Espectroscopia de Infravermelho com Transformada de Fourier , Traumatismos dos Tendões/complicações , Aderências Teciduais/etiologia
4.
Cochrane Database Syst Rev ; 9: CD001505, 2019 09 09.
Artigo em Inglês | MEDLINE | ID: mdl-31499593

RESUMO

BACKGROUND: Progressive lung damage causes most deaths in cystic fibrosis. Non-steroidal anti-inflammatory drugs (such as ibuprofen) may prevent progressive pulmonary deterioration and morbidity in cystic fibrosis. This is an update of a previously published review. OBJECTIVES: To assess the effectiveness of treatment with oral non-steroidal anti-inflammatory drugs in cystic fibrosis. SEARCH METHODS: We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group Trials Register comprising references identified from comprehensive electronic database searches, hand searches of relevant journals and abstract books of conference proceedings. We contacted manufacturers of non-steroidal anti-inflammatory drugs and searched online trials registries.Latest search of the Group's Trials Register: 21 November 2018. SELECTION CRITERIA: Randomized controlled trials comparing oral non-steroidal anti-inflammatory drugs, at any dose for at least two months, to placebo in people with cystic fibrosis. DATA COLLECTION AND ANALYSIS: Two authors independently assessed trials for inclusion the review and their potential risk of bias. Two authors independently rated the quality of the evidence for each outcome using the GRADE guidelines. MAIN RESULTS: The searches identified 17 trials; four are included (287 participants aged five to 39 years; maximum follow-up of four years) and one is currently awaiting classification pending publication of the full trial report and two are ongoing. Three trials compared ibuprofen to placebo (two from the same center with some of the same participants); one trial assessed piroxicam versus placebo.The three ibuprofen trials were deemed to have good or adequate methodological quality, but used various outcomes and summary measures. Reviewers considered measures of lung function, nutritional status, radiological assessment of pulmonary involvement, intravenous antibiotic usage, hospital admissions, survival and adverse effects. Combined data from the two largest ibuprofen trials showed a lower annual rate of decline for lung function, % predicted forced expiratory volume in one second (FEV1), mean difference (MD) 1.32 (95% confidence interval (CI) 0.21 to 2.42) (moderate-quality evidence); forced vital capacity (FVC), MD 1.27 (95% CI 0.26 to 2.28) (moderate-quality evidence); forced expiratory flow (FEF25%-75%), MD 1.80 (95% CI 0.15 to 3.45). The post hoc analysis of data from two trials split by age showed a slower rate of annual decline of FEV1 % predicted and FVC in the ibuprofen group in younger children, MD 1.41% (95% CI 0.03 to 2.80) (moderate-quality evidence) and MD 1.32% (95% CI 0.04 to 2.60) (moderate-quality evidence) respectively. Data from four trials demonstrated the proportion of participants with at least one hospitalization may be slightly lower in the ibuprofen group compared to placebo, Peto odds ratio 0.61 (95% CI 0.37 to 1.01) (moderate-quality evidence). In one trial, long-term use of high-dose ibuprofen was associated with reduced intravenous antibiotic usage, improved nutritional and radiological pulmonary status. No major adverse effects were reported, but the power of the trials to identify clinically important differences in the incidence of adverse effects was low.We did not have any concerns with regards to risk of bias for the trial comparing piroxicam to placebo. However, the trial did not report many data in a form that we could analyze in this review. No data were available for the review's primary outcome of lung function; available data for hospital admissions showed no difference between the groups. No analyzable data were available for any other review outcome. AUTHORS' CONCLUSIONS: High-dose ibuprofen can slow the progression of lung disease in people with cystic fibrosis, especially in children, which suggests that strategies to modulate lung inflammation can be beneficial for people with cystic fibrosis.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Fibrose Cística/tratamento farmacológico , Administração Oral , Adolescente , Adulto , Anti-Inflamatórios não Esteroides/administração & dosagem , Criança , Feminino , Humanos , Ibuprofeno/administração & dosagem , Ibuprofeno/uso terapêutico , Masculino , Piroxicam/administração & dosagem , Piroxicam/uso terapêutico , Ensaios Clínicos Controlados Aleatórios como Assunto , Adulto Jovem
5.
Medicine (Baltimore) ; 98(31): e16689, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31374055

RESUMO

Paracetamol (acetaminophen) has been proposed as an alternative medication for closing hemodynamically significant patent ductus arteriosus (PDA). However, the clinical outcomes remain inconclusive in very low birth weight (VLBW) and extremely low birth weight (ELBW) infants.The aim of this study was to compare the efficacy and safety of oral paracetamol and ibuprofen for pharmacological closure of PDA in premature infants from a real-world study.This retrospective study enrolled 255 preterm infants with birthweights of ≤1.5 kg, and echocardiographically confirmed significant PDA. Subjects were classified into 3 groups: Group I (standard-dose ibuprofen group) received 10 mg/kg oral ibuprofen followed by 5 mg/kg/day for 2 days. Group II (high-dose ibuprofen group) received 10 mg/kg/day oral ibuprofen for 3 days. Group III (paracetamol group) received 15 mg/kg/6 h oral paracetamol for 3 days.On day 9 after medication start, PDA closure was achieved in 61 (71.7%) patients assigned to the high-dose ibuprofen group, (63.8%) in the standard-dose ibuprofen group, and 33 (37.9%) of those in the oral paracetamol group (P <.001). Oral standard-dose ibuprofen was more effective than oral paracetamol (P = .001). The ductus closed faster in the high-dose ibuprofen group than in the standard-dose group (median closure time 3.9 ± 1.0 versus 4.4 ±â€Š1.0 days, P = .009). Total bilirubin significantly increased in the high-dose ibuprofen group (P = .02). No gastrointestinal, renal, or hematological adverse effects were reported. Subgroup analyses indicated paracetamol was minimally effective in ELBW infants (PDA closure 13%).This study demonstrated that paracetamol may be a poor medical alternative for PDA management in VLBW and ELBW infants. High dosage ibuprofen was associated with a faster clinical improvement and higher rate of PDA closure.


Assuntos
Acetaminofen/administração & dosagem , Inibidores de Ciclo-Oxigenase/administração & dosagem , Permeabilidade do Canal Arterial/tratamento farmacológico , Ibuprofeno/administração & dosagem , Administração Oral , Relação Dose-Resposta a Droga , Feminino , Idade Gestacional , Humanos , Recém-Nascido de Peso Extremamente Baixo ao Nascer , Lactente Extremamente Prematuro , Recém-Nascido , Masculino , Estudos Retrospectivos , Resultado do Tratamento
6.
Int J Pharm ; 569: 118549, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31394188

RESUMO

Trial-and-error approach to formulation development is long and costly. With growing time and cost pressures in the pharmaceutical industry, the need for computer-based formulation design is greater than ever. In this project, emulgels were designed and optimized using Formulating for Efficacy™ (FFE) for the topical delivery of ibuprofen. FFE helped select penetration enhancers, design and optimize emulgels and simulate skin penetration studies. pH, viscosity, spreadability, droplet size and stability of emulgels were evaluated. Franz cell studies were performed to test in vitro drug release on regenerated cellulose membrane, drug permeation in vitro on Strat-M® membrane and ex vivo on porcine ear skin, a marketed ibuprofen gel served as control. Emulgels had skin compatible pH, viscosity and spreadability comparable to a marketed emulgel, were opaque and stable at 25 °C for 6 months. Oleyl alcohol (OA), combined with either dimethyl isosorbide (DMI) or diethylene glycol monoethyl ether (DGME) provided the highest permeation in 24 h in vitro, which was significantly higher than the marketed product (p < 0.01). OA + DGME significantly outperformed OA ex vivo (p < 0.05). The computer predictions, in vitro and ex vivo penetration results correlated well. FFE was a fast, valuable and reliable tool for aiding in topical product design for ibuprofen.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Ibuprofeno/administração & dosagem , Ibuprofeno/química , Absorção Cutânea , Animais , Química Farmacêutica , Simulação por Computador , Composição de Medicamentos , Etilenoglicóis/administração & dosagem , Etilenoglicóis/química , Álcoois Graxos/administração & dosagem , Álcoois Graxos/química , Técnicas In Vitro , Isossorbida/administração & dosagem , Isossorbida/análogos & derivados , Isossorbida/química , Pele/metabolismo , Solubilidade , Suínos
7.
Pharm Dev Technol ; 24(9): 1144-1154, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31298072

RESUMO

Ibuprofen is a non-steroidal anti-inflammatory drug for the treatment of Rheumatoid Arthritis and osteoarthritis. In this study, we prepared topical gel network for enhancement of ibuprofen penetration, maintenance of controlled release and increased patient compliance. Nanoparticles containing ibuprofen were prepared by means of emulsion formation/solvent diffusion method using synthesized copolymer. Nanoparticles were then conjugated with aminoethylmethacrylate, resulting in ibuprofen-loaded nanoparticles in PLGA-b-PEG-MA structure. Ibuprofen-loaded gel networks were developed by crosslinking nanoparticles via UV exposure. Suitability for topical application has been assessed through characterization of particle size, zeta potential, morphology, encapsulation efficiency, in vitro release, cytotoxicity and enhancement of in vitro wound healing. The mean diameter of nanoparticles was measured as 230 ± 20 nm. Gel network formulations with higher particle size (2800 ± 350 nm) and zeta potential (39.8 ± 9.2 mV), depending on conjugation of methacrylate within copolymeric structure, and having encapsulation efficacy of 73.6 ± 2.8% were prepared. The in vitro release of ibuprofen was sustained for more than 7 hours. Gel network improved collagen synthesis, type I collagen mRNA expression and fibrosis in dose dependent manner. Based on this, we can conclude that PLGA-b-PEG gel network might be a promising systems for the local delivery of ibuprofen in RA patients.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Géis/química , Ibuprofeno/administração & dosagem , Metacrilatos/química , Nanocápsulas/química , Polietilenoglicóis/química , Poliglactina 910/química , Administração Tópica , Animais , Anti-Inflamatórios não Esteroides/farmacocinética , Anti-Inflamatórios não Esteroides/farmacologia , Linhagem Celular , Colágeno/metabolismo , Preparações de Ação Retardada/química , Ibuprofeno/farmacocinética , Ibuprofeno/farmacologia , Camundongos , Raios Ultravioleta
8.
Int J Pharm ; 567: 118478, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31260782

RESUMO

To encapsulate and deliver poorly water-soluble drugs, castor oil/silica hybrid microparticles (HMP)s were synthesized. Green chemistries were used to silylate the oil and further cross-link it into solid microparticles by sol-gel reaction. Silylated castor oils (ICO)s at various silylation ratios were prepared and allowed the solubilization of ibuprofen at several concentrations up to 16 wt%. The HMPs were formulated by ThermoStabilized Emulsion (TSE) process which permits to "freeze" the oil-in-water emulsion while the sol-gel reaction occurs. The hybrid mineral/organic composition and the morphology (spherical shape and micrometric size) of these HMPs were determined by complementary technics (SEM, TGA, EDX, 29Si NMR and FTIR spectroscopies). The HMPs reached a good ibuprofen loading efficiency regardless to the formulation used while the release kinetics in simulated oral administration exhibited a tunable release during 3 h according to the silylation ratio. The ibuprofen rate also influenced its own amorphous or crystalline character within the HMPs. For subcutaneous conditions, ibuprofen release took place over 15 days. Finally, biodegradability assays in simulated digestion medium suggested a surface-limited hydrolysis of the particles and cytocompatibility studies on NIH-3T3 and Caco-2 cells demonstrated an excellent cellular viability.


Assuntos
Óleo de Rícino/administração & dosagem , Portadores de Fármacos/administração & dosagem , Dióxido de Silício/administração & dosagem , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Células CACO-2 , Óleo de Rícino/química , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Humanos , Ibuprofeno/administração & dosagem , Ibuprofeno/química , Camundongos , Células NIH 3T3 , Dióxido de Silício/química , Solubilidade , Água/química
9.
Int J Pharm ; 569: 118564, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31352049

RESUMO

Control of infection and inflammation is crucial for the success of periodontal treatment. In this study, in-situ forming implants (ISFI) loaded with chlorhexidine dihydrochloride (CHX) and ibuprofen (IBU) were developed and tested to optimize periodontal treatment outcomes. Release profiles were promising. Exposure to 1.5% and 5.3% CHX-IBU loaded ISFI's release media decreased significantly the P. gingivalis growth up to 20-fold and 35-fold, respectively, after 48 h (p < 0.05). The metabolic activity assay of gingival epithelial cells (EC) demonstrated 1.5% CHX-IBU-loaded ISFI to be non-toxic, therefore, it was selected for further experimentation. Furthermore, significant down-regulation of TNF-α release (34% at 6 h and 43% at 24 h, p < 0.05) in P. gingivalis lipopolysaccharide (Pg-LPS) stimulated EC exposed to 1.5% CHX-IBU ISFI release medium was demonstrated by ELISA. In vivo, 1.5% CHX-IBU ISFI was injected into the periodontal pocket in an experimental periodontitis mouse model and the reduction in inflammation and improvement in periodontal wound healing was evaluated through inflammatory cell scoring and histomorphometry at 7- and 15-days post-treatment. The results indicate that CHX-IBU loaded ISFI could be efficient as adjuvant to periodontal therapy for the control of infection and inflammation. Moreover, other (e.g., pro-regenerative) drugs could be incorporated into ISFI to further improve periodontal treatment outcomes.


Assuntos
Anti-Infecciosos Locais/administração & dosagem , Anti-Inflamatórios não Esteroides/administração & dosagem , Clorexidina/administração & dosagem , Ibuprofeno/administração & dosagem , Periodontite/tratamento farmacológico , Animais , Anti-Infecciosos Locais/química , Anti-Inflamatórios não Esteroides/química , Linhagem Celular , Clorexidina/química , Implantes de Medicamento , Liberação Controlada de Fármacos , Células Epiteliais/efeitos dos fármacos , Gengiva/citologia , Humanos , Ibuprofeno/química , Lipopolissacarídeos , Masculino , Camundongos Endogâmicos C57BL , Estudo de Prova de Conceito , Cicatrização/efeitos dos fármacos
10.
Curr Pharm Biotechnol ; 20(13): 1122-1133, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31333124

RESUMO

BACKGROUND: Periodontal disease is the most common oral condition that affects the tissue surrounding the teeth. The oral cavity is colonized by an impressive array of micro-organisms, many of which can colonize the implants such as Guided Tissue Regeneration (GTR) often utilized in recovering procedures that result in inflammation interfering with the bone regeneration. METHODS: In the current study, a nano-hybrid GTR membrane is developed as a heliacal structure scaffold with localized drug delivery function (Ibuprofen) as an anti-inflammatory agent. Polycaprolactone (PCL) and a blend of Polyvinyl alcohol (PVA)/collagen (Col) (50/50) were electrospun by electrospinning. Ibuprofen (Ibu) was loaded once in the PCL context and once in the hydrophilic portion (PVA/Col). RESULTS: The in vitro release behavior was investigated in each case. Chemical and physical properties were studied for each item. Morphology investigation indicated a heliacal structure with the total average diameter of 1266 nm consististing of porous pores with the average diameter of 256nm. CONCLUSION: The membranes indicated proper mechanical properties and appropriate biodegradation rate as a potential GTR membrane. The controlled and sustained release of Ibu was obtained from both PCL and PVA/COL loaded membranes. Kinetic model study indicated the following zero-order and Higuchi models for the optimum case of PCL loaded and PVA/Col Ibu loaded scaffolds respectively.


Assuntos
Anti-Inflamatórios/administração & dosagem , Regeneração Tecidual Guiada/métodos , Ibuprofeno/administração & dosagem , Membranas Artificiais , Poliésteres/química , Tecidos Suporte/química , Anti-Inflamatórios/farmacologia , Regeneração Óssea , Colágeno/química , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Humanos , Ibuprofeno/farmacologia , Nanofibras/química , Álcool de Polivinil/química , Porosidade , Próteses e Implantes
11.
Int J Pharm ; 568: 118553, 2019 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-31344444

RESUMO

Blending two polymers is an effective technique to obtain a novel material with desirable properties. Chitosan (CH) has limited applications in tissue engineering owing to its poor mechanical strength in a wet state. Polycaprolactone (PCL) has low toxicity with good mechanical strength and controlled release properties, but lack cell recognition signals. Thus, the blending of CH and PCL (CH/PCL) polymers would provide a better biomaterial required for the management of chronic osteomyelitis (OM) after surgical debridement possessing superior physicomechanical and controlled release properties. Herein, blend sponges using different ratios of CH and PCL, i.e., 100%CH/00%PCL, 75%CH/25%PCL, 50%CH/50%PCL and 25%CH/75%PCL were prepared, which are denoted as 100CH/00PCL, 75CH/25PCL, 50CH/50PCL and 25CH/75PCL, respectively. These blend sponges were characterized using FTIR, XRD, DSC, SEM, and contact angle. The results revealed that CH and PCL polymers were well dispersed in a blend at a molecular level without any chemical interactions. Blend sponges were loaded with ciprofloxacin hydrochloride (CIP) and ibuprofen. Further, in vitro efficacy of drug-loaded blend sponges was evaluated for drug release, antibacterial potential, and anti-inflammatory activity. Amongst four blend sponges, the 75CH/25PCL sponge demonstrated the controlled release of ibuprofen and an ideal release profile of CIP along with potential antibacterial as well as anti-inflammatory activity over the study period. Thus, it can be concluded that the 75CH/25PCL sponge is a promising candidate for the management of chronic OM after surgical debridement.


Assuntos
Quitosana/administração & dosagem , Sistemas de Liberação de Medicamentos , Osteomielite/tratamento farmacológico , Poliésteres/administração & dosagem , Animais , Antibacterianos/administração & dosagem , Antibacterianos/química , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Materiais Biocompatíveis/administração & dosagem , Materiais Biocompatíveis/química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Quitosana/química , Doença Crônica , Ciprofloxacino/administração & dosagem , Ciprofloxacino/química , Liberação Controlada de Fármacos , Eritrócitos/efeitos dos fármacos , Humanos , Ibuprofeno/administração & dosagem , Ibuprofeno/química , Camundongos , Poliésteres/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento
13.
Early Hum Dev ; 135: 16-22, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31212222

RESUMO

BACKGROUND: Infants born at 23-24 weeks' gestation have the highest risk of developing a hemodynamically significant patent ductus arteriosus (hsPDA), that is refractory to pharmacological closure requiring surgical ligation. Thus, these patients might have the greatest benefits from hsPDA closure, although previous studies on PDA closure were not focused on this population. AIM: To compare the occurrence of hsPDA, failure rate of the first course of ibuprofen in closing hsPDA, and need of surgical closure in infants born at 23+0-24+6 weeks' gestation to those in infants born at 25+0-28+6 weeks' gestation. STUDY DESIGN: This is a retrospective multicenter study including infants born at 23+0-28+6 weeks of gestation admitted to the neonatal care units from January 2013 to December 2017. All infants underwent echocardiographical assessment for hsPDA diagnosis and eventually pharmacological treatment, and surgical closure. RESULTS: We studied a total of 842 infants of which 562 (67%) developed a PDA. Among those with PDA, 511 (91%) received a pharmacological treatment for a hsPDA. We found that a hsPDA occurred in 70% (106/151) of infants born at 23-24 weeks and in 59% (405/691) of infants born at 25-28 weeks of gestation (P < 0.001). Failure of closure with the first-treatment cycle (69 vs. 40%; P < 0.001) and need of surgical closure (19 vs 10%) were more frequent (P < 0.011) in infants born at 23-24 than 25-28 gestational weeks. Paracetamol vs. ibuprofen treatment and gestational age of 23-24 versus 25-28 weeks increased closure failure, while less severe RDS and maternal clinical chorioamnionitis decreased it. CONCLUSIONS: Among extremely preterm infants, infants born at 23-24 weeks of gestation have the highest risk of developing a hsPDA refractory to pharmacological treatment requiring surgical closure. Our findings support the need of individualized more careful strategies for hsPDA management in this special population.


Assuntos
Gerenciamento Clínico , Permeabilidade do Canal Arterial/epidemiologia , Lactente Extremamente Prematuro , Procedimentos Cirúrgicos Cardíacos , Permeabilidade do Canal Arterial/diagnóstico por imagem , Permeabilidade do Canal Arterial/tratamento farmacológico , Permeabilidade do Canal Arterial/cirurgia , Ecocardiografia , Feminino , Hemodinâmica , Humanos , Ibuprofeno/administração & dosagem , Ibuprofeno/uso terapêutico , Recém-Nascido , Masculino
14.
Eur Arch Otorhinolaryngol ; 276(8): 2243-2249, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31055640

RESUMO

PURPOSE: To evaluate the efficacy of single low dose (75 mg) preoperative pregabalin in reducing post-operative pain of septorhinoplasty. METHODS: A double blind single center Randomized controlled trial based on block randomization. In the pregabalin group (PG) 34 participants received 75 mg pregabalin orally one hour before anesthesia induction while in control group (CG) 34 participants received a placebo. Pain and sedation were repeatedly measured with Visual Analouge Scale (VAS) and Riker Sedation-Agitation Scale (RSAS) respectively, 0.5, 1, 2, 6, 24 hours postextubation. Cumulative doses of fentanyl and ibuprofen received in both groups were compared. RESULTS: Thirty-two of the participants in PG and 33 of the participants in CG completed the study. The Mean VAS pain score was less in PG versus CG 30 min postoperatively (2.30 ± 1.30 vs. 4.85 ± 1.17), one hour (2.28 ± 0.92 vs. 4.27 ± 0.78), two hours (2.11 ± 0.88 vs. 3.60 ± 0.61) and six hours (1.47 0.62 vs. 2.76 ± 0.91) but not 24-hours postoperatively (0.84 ± 0.62 vs. 1.09 ± 0.92). Participants in the PG were less agitated during early post-extubation period (at 10 min: RSAS 3.93 ± 0.43 vs. 4.42 ± 0.50) and more alert during the first hour post-extubation (at 60 min: RSAS 3.90 ± 0.29 vs. 3.36 ± 0.69). The total dose of rescue fentanyl and ibuprofen was lower in the PG compared to the CG. CONCLUSIONS: A single dose of 75 mg pregabalin is very effective for pain control after septorhinoplasty procedure when administered one hour before anesthesia induction. Side effects are rare and opioid sparing was noted. TRIAL REGISTRATION: Clinical trial number: IRCT2017043033706N1.


Assuntos
Dor Pós-Operatória , Pregabalina/administração & dosagem , Rinoplastia , Analgésicos/administração & dosagem , Analgésicos/efeitos adversos , Analgésicos Opioides/administração & dosagem , Método Duplo-Cego , Feminino , Fentanila/administração & dosagem , Humanos , Ibuprofeno/administração & dosagem , Masculino , Pessoa de Meia-Idade , Medição da Dor/métodos , Dor Pós-Operatória/etiologia , Dor Pós-Operatória/prevenção & controle , Pregabalina/efeitos adversos , Rinoplastia/efeitos adversos , Rinoplastia/métodos , Fatores de Tempo , Resultado do Tratamento
15.
Int J Pharm ; 565: 70-82, 2019 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-31054878

RESUMO

Post-operative adhesion is a common cause of several complications including intestinal obstruction, chronic pelvic pain and/or infertility. Adhesions are fibrous bands that result from the inflammatory reactions due to peritoneum damage. The current study focused on designing an effective anti-inflammatory loaded barrier for the prevention of post-operative adhesions. The proposed method is based on the use of polyvinyl alcohol (PVA), cryobarrier loaded with Ibuprofen (Ibu). Anti-adhesive Ibu-cryobarriers were prepared in different forms, and subjected to in-vitro evaluation comprising; drug release rate, maximum swelling index, morphological examination using scanning electron microscope (SEM), fourier-transform infrared spectroscopy (FTIR) and mechanical properties. Optimized cryobarriers were further investigated for their in-vivo effectiveness in preventing post-operative adhesions in female Sprague-Dawley rats. All formulations showed appropriate physical and morphological characteristics, in-vitro controlled sustained drug release profiles during a period of seven days with acceptable maximum swelling index. Invivo, all cryobarriers were equivalent to each other concerning serum or tissue parameter. However, morphological and histopathological evaluations revealed that both xerocryogel and lyophilized cryofilms are more effective than the cryogel in prevention of post-operative peritoneal adhesions. The current study showed the possibility of preparing drug loaded cryobarriers using simple technique with an effective in vivo post-operative adhesion prevention.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Criogéis/administração & dosagem , Ibuprofeno/administração & dosagem , Álcool de Polivinil/administração & dosagem , Complicações Pós-Operatórias/prevenção & controle , Aderências Teciduais/prevenção & controle , Parede Abdominal/cirurgia , Animais , Ceco/cirurgia , Preparações de Ação Retardada/administração & dosagem , Feminino , Ratos Sprague-Dawley
16.
Acta Odontol Scand ; 77(7): 552-558, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31094614

RESUMO

Objective: To assess the effect of preoperative administration of ibuprofen and acetaminophen on the efficacy of buccal infiltration for pulp therapy in mandibular primary molars. Materials and methods: A randomized controlled trial with an ID no. NCT03423329 in Clinical-Trials.gov was conducted in the outpatient clinic of Paediatric Dentistry Department at Ain Shams University. The study was designed with two test arms where either ibuprofen or acetaminophen was administered to children whereas in the control arm a multivitamin placebo was used. Children's self-reported pain responses were recorded using Wong-Baker FACES pain scale. For statistical analysis, Chi-square test or Fisher's exact test was used to compare between the three groups whereas Friedman's test was used to study changes within each group. Results: In a sample of 60 children, a significant decrease in the mean pain rating scores was detected in all groups where success rates ranged from 40% with ibuprofen to 55% and 65% with acetaminophen and placebo, respectively. However, there was no statistically significant difference between the three groups regarding severity of pain during access cavity preparation. Conclusions: Both analgesics have no clinical advantage over the placebo in increasing the efficacy of buccal infiltration during pulp therapy in mandibular primary molars.


Assuntos
Acetaminofen/administração & dosagem , Analgesia/métodos , Ibuprofeno/administração & dosagem , Dor/prevenção & controle , Pulpotomia , Criança , Método Duplo-Cego , Humanos , Dente Molar , Extração Dentária , Resultado do Tratamento
17.
Niger J Clin Pract ; 22(4): 503-510, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30975954

RESUMO

Aim: The objective of this study was to compare the efficacy of different doses of pregabalin and intravenous ibuprofen with regard to pain management and analgesic consumption after third molar surgery. Materials and Methods: Ninety patients who had been scheduled for third molar surgery were assigned to four different treatment groups. The inclusion criteria consisted of the presence of fully or partially bony retentive asymptomatic mandibular third molars. These groups are included the following: (Group 1) premedicated with oral placebo and intravenous (IV) placebo, (Group 2) premedicated with oral placebo and 400-mg IV Ibuprofen, (Group 3) premedicated with 75-mg oral pregabalin and 400-mg IV ibuprofen, and (Group 4) premedicated with 150-mg oral pregabalin and 400 mg IV ibuprofen. Postoperative pain was assessed with visual analog scale (VAS) every hour for the first 12 hs following the surgery. Pain was then assessed at different time intervals during 7 days following the surgery. Kruskal-Wallis tests were used to compare the four groups in terms of VAS pain scores, analgesic consumption, and first rescue analgesic request time after the surgery. Results: At the end of the study, the results of 80 patients (20 patients per group) were analyzed. The group 4 had lower pain intensity compared with other groups at various time intervals. This difference is statistically significant in between the first 3-10 h (first day) and single-time intervals in second, third, fifth, and sixth postoperative days. Postoperative analgesic consumption was not statistically different between the groups. The first rescue analgesic request time after surgery was different between the pregabalin combination groups and group 2. No significant difference in the side effects was observed. Conclusion: These findings suggest that preoperative coadministration of 150-mg pregabalin and IV ibuprofen may be useful in improving pain control after third molar surgery.


Assuntos
Analgésicos/administração & dosagem , Ibuprofeno/administração & dosagem , Dente Serotino/cirurgia , Dor Pós-Operatória/prevenção & controle , Pregabalina/administração & dosagem , Administração Intravenosa , Administração Oral , Adolescente , Adulto , Método Duplo-Cego , Feminino , Humanos , Masculino , Manejo da Dor , Período Pré-Operatório , Extração Dentária , Resultado do Tratamento , Escala Visual Analógica
19.
Eur J Anaesthesiol ; 36(5): 351-359, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30946703

RESUMO

BACKGROUND: NSAIDs and paracetamol are the cornerstones of pain treatment after day case surgery. However, NSAIDs have numerous contraindications and consequently are not suitable in up to 25% of patients. Metamizole is a non-opioid compound with a favourable gastro-intestinal and cardiovascular profile compared with NSAIDs. OBJECTIVES: The study aimed to assess if a combination of metamizole and paracetamol is noninferior to a combination of ibuprofen and paracetamol in treating pain at home after painful day case surgery. DESIGN: A double-blind randomised controlled trial. SETTING: Single centre. PATIENTS: Two hundred patients undergoing elective ambulatory haemorrhoid surgery, arthroscopic shoulder or knee surgery, or inguinal hernia repair. INTERVENTION: Patients were randomly allocated to receive either metamizole and paracetamol (n = 100) or ibuprofen and paracetamol (n = 100) orally for four days. MAIN OUTCOME MEASURES: Average postoperative pain intensity using a numerical rating scale and use of rescue medication were measured in the postanaesthesia care unit (PACU) and on postoperative days (POD) 1 to 3. A difference in mean numerical rating scale score of 1 point or less was considered noninferior. Adverse effects of study medication and satisfaction with study medication were measured on PODs 1 to 3 by telephone follow-up. RESULTS: In the PACU, the difference in mean ±â€ŠSD pain score between metamizole and paracetamol and ibuprofen and paracetamol was 0.85 ±â€Š0.78. From POD 1 to 3, this difference was lower than 1, resulting in noninferiority. Rescue opioid consumption in the PACU and on PODs 1 and 3 was not significantly different between treatment groups. Rescue opioid consumption on POD2 was significantly higher in the ibuprofen and paracetamol group (P = 0.042). Adverse effects of study medication and overall patient satisfaction were similar in both groups. CONCLUSION: Paracetamol/metamizole and paracetamol/ibuprofen are equally effective in treatment of acute postoperative pain at home after ambulatory surgery with comparable patient satisfaction levels. TRIAL REGISTRATION: European Union Clinical Trials Register 2015-003987-35.


Assuntos
Dor Aguda/tratamento farmacológico , Analgésicos não Entorpecentes/administração & dosagem , Dipirona/administração & dosagem , Ibuprofeno/administração & dosagem , Dor Pós-Operatória/tratamento farmacológico , Acetaminofen/administração & dosagem , Acetaminofen/efeitos adversos , Dor Aguda/diagnóstico , Dor Aguda/etiologia , Administração Oral , Adulto , Procedimentos Cirúrgicos Ambulatórios/efeitos adversos , Dipirona/efeitos adversos , Método Duplo-Cego , Quimioterapia Combinada/métodos , Feminino , Humanos , Ibuprofeno/efeitos adversos , Masculino , Pessoa de Meia-Idade , Medição da Dor , Dor Pós-Operatória/diagnóstico , Dor Pós-Operatória/etiologia , Satisfação do Paciente , Autoadministração , Resultado do Tratamento
20.
Mol Biol Rep ; 46(3): 3093-3100, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30929160

RESUMO

In this study we are presenting the development of technetium-99m (99mTc) labeled ibuprofen for the imaging of aseptic inflammation. 99mTc-Ibuprofen complex was developed by optimizing the radiolabeling conditions such as reaction time, ligand and reducing agent concentration, pH, reaction time and temperature. Following the addition of 600 µg of ibuprofen, 4 µg of stannous chloride as reducing agent and 300 MBq 99mTc radioactivity; the pH of reaction mixture was adjusted to 11 and allowed to react for 15 min at room temperature. Chromatography analysis revealed > 94% 99mTc-ibuprofen complex formation with promising stability in saline and blood serum up to 6 h. Biodistribution study using normal and sterile inflammation induced mice indicated low accumulation of labeled compound in key body organs; however, kidneys (14.76 ± 0.87% ID/g organ) and bladder (31.6 ± 3.0% ID/g organ) showed comparatively higher radioactivity due to main excretory path. Inflamed to normal tissues ratio (T/NT), at 1 h post-injection, showed promising value (4.57 ± 0.56). The SPECT imaging of artificially inflammation induced rabbit model also verified the biodistribution results. In conclusion, radiochemical purity and biological evaluation of 99mTc-ibuprofen complex indicates the agent can be utilized for imaging of deep seated aseptic inflammation.


Assuntos
Ibuprofeno/administração & dosagem , Cintilografia , Compostos Radiofarmacêuticos/administração & dosagem , Tecnécio , Animais , Cromatografia , Estabilidade de Medicamentos , Humanos , Concentração de Íons de Hidrogênio , Ibuprofeno/química , Ibuprofeno/farmacocinética , Marcação por Isótopo , Ligantes , Modelos Animais , Estrutura Molecular , Cintilografia/métodos , Compostos Radiofarmacêuticos/química , Compostos Radiofarmacêuticos/farmacocinética , Ratos , Distribuição Tecidual , Tomografia Computadorizada de Emissão de Fóton Único
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