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1.
J Pharm Biomed Anal ; 215: 114758, 2022 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-35421777

RESUMO

Three disposable stochastic sensors based on maltodextrin (dextrose equivalent = 4-7) and nanostructures (copper monolayer, carbon monolayer and carbon-copper composite layer) deposited using cold plasma on copy paper were proposed for the fast analysis of ibuprofen, ketoprofen and flurbiprofen in pharmaceutical formulation samples. The widest linear concentration ranges recorded were: for ibuprofen 1 fmol/L - 1 mmol/L when the disposable stochastic sensor based on carbon monolayer was used, for ketoprofen 1 fmol/L - 1 mmol/L when the disposable stochastic sensors based on copper monolayer and carbon-copper composite layer were used, and for flurbiprofen 1 fmol/L - 10 mmol/L when the disposable stochastic sensor based on carbon-copper composite layer was used. The lowest limit of detection recorded for each non-steroidal anti-inflammatory drug was 1 fmol/L.


Assuntos
Flurbiprofeno , Cetoprofeno , Anti-Inflamatórios não Esteroides , Carbono , Cobre , Composição de Medicamentos , Ibuprofeno/química , Cetoprofeno/química
2.
Molecules ; 27(7)2022 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-35408503

RESUMO

The synthesis of derivatives of three nonspecific COX-1 and COX-2 inhibitors, ibuprofen, ketoprofen, naproxen is presented. These acids were connected via an amide bond with an amino acid (L-proline, L-tyrosine, and beta-alanine) used as a linker. The amino acid carboxylic group was esterified with 3,4,5 trimethoxybenzyl alcohol. The activity of the novel derivatives was examined in vivo on carrageenan-induced inflammation, and in vitro, as cyclooxygenase and lipoxygenase inhibitors. It was found that the new compounds were more potent anti-inflammatory agents than the parent drugs. Thus, the ibuprofen (21) and ketoprofen (16) derivatives reduced rat paw edema by 67 and 91% (the reduction by the relevant NSAIDs was 36 and 47%, respectively). They inhibited COX-2 more than the starting drugs (21 by 67%, ibuprofen 46%, 19 by 94%, ketoprofen 49%). Docking of compounds on the active sites of COX-1 and COX-2 reflects their in vitro activity. Thus, 19 adopts an unfavorable orientation for COX-1 inhibition, but it binds effectively in the binding pocket of COX-2, in agreement with the absence of activity for COX-1 and the high inhibition of COX-2. In conclusion, the performed structural modifications result in the enhancement of the anti-inflammatory activity, compared with the parent NSAIDs.


Assuntos
Anti-Inflamatórios não Esteroides , Cetoprofeno , Aminoácidos/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios não Esteroides/química , Carragenina/efeitos adversos , Ciclo-Oxigenase 1 , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Edema/induzido quimicamente , Edema/tratamento farmacológico , Ibuprofeno/farmacologia , Ibuprofeno/uso terapêutico , Simulação de Acoplamento Molecular , Ratos
3.
Carbohydr Polym ; 288: 119389, 2022 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-35450650

RESUMO

A novel physically and chemically double-crosslinked hydrogel derived from chitosan oligosaccharide/alginate (COS/Alg) was developed by using norbornene (Nb)-tetrazine (Tz) click reaction for ketoprofen delivery. The properties of the hydrogel were evaluated by rheological, FTIR, TGA, XRD, SEM, swelling and drug release studies. The Nb-Tz chemical cross-linking facilitated outstanding hydrophobic drug loading (44% wt/wt of ketoprofen) and sustained release through a hydrophobic interaction mechanism between the drug and the used polysaccharides. The COS/Alg electrostatics network (10/10 of NH2/COOH molar ratio) generated the pH responsiveness, suppressing the release in simulated gastric fluid (below 10% for 2 h) and enhancing the release in simulated intestinal fluids (up to 84% for 24 h). The prepared hydrogel was non-toxic to human HEK-293 cells (95% cell viability). This work opens up a potential approach for preparing hydrophilic hydrogels from natural polysaccharides that can be used in the delivery of hydrophobic drugs.


Assuntos
Quitosana , Cetoprofeno , Alginatos/química , Quitosana/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Células HEK293 , Humanos , Hidrogéis/química , Concentração de Íons de Hidrogênio , Nióbio , Norbornanos
4.
AAPS PharmSciTech ; 23(4): 101, 2022 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-35348937

RESUMO

The present piece of research work is framed for improving the solubility of ketoprofen by forming co-crystal using fumaric acid as a coformer. Co-crystal of ketoprofen and fumaric acid was prepared by simple solvent-assisted grinding method, containing drug and coformer as independent variables and solubility and % drug release were assumed to be dependent variables. Differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, nuclear magnetic resonance and scanning electron microscopy techniques were used to characterize the preparation of optimized batch of co-crystal and further, evaluated for in vitro and in vivo anti-inflammatory and analgesic activities. Based on results of solubility and dissolution rate studies the formulation showed magnified improvement in both the properties on co-crystallization. The values of Gibbs free energy are negative at all levels of carrier demonstrating spontaneity of the drug solubilization process. The IC50 value of optimized batch of co-crystal formulation and the pure drug was observed as 327.33 µg/ml and 556.11 µg/ml, respectively, demonstrating that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. In vivo (anti-inflammatory and analgesic) activities revealed that optimized batch of co-crystal formulation delivered a rapid pharmacological response in Wistar rats and albino mice when compared with standard drug.


Assuntos
Cetoprofeno , Animais , Varredura Diferencial de Calorimetria , Camundongos , Ratos , Ratos Wistar , Solubilidade , Difração de Raios X
5.
Biomed Pharmacother ; 149: 112819, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35299123

RESUMO

Dexketoprofen is an enantiomer of ketoprofen (S+) that belongs to nonsteroidal anti-inflammatory drugs and has analgesic, anti-inflammatory, and antipyretic properties. Dexketoprofen has a stronger effect than ketoprofen, which makes it a readily used preparation. The review aims to find in recent original publications data about dexketoprofen and its comparison with other painkilling medications. The systematic literature review was conducted in November 2021 (2018 onwards). We selected 12 articles from PubMed, Google Scholar, Medline Complete databases. In the last 4 years, there have been many publications that shed a new light on dexketoprofen. The article is a comparative analysis of dexketoprofen's action vs other nonsteroidal anti-inflammatory drugs and the combination of dexketoprofen with tramadol vs paracetamol with tramadol. The findings of the review confirm that dexketoprofen is a very good pain reliever more potent than paracetamol. Dexketoprofen produces similar effects to lidocaine and dexmedetomidine. Complex preparations containing dexketoprofen and tramadol are very effective painkilling tandem and are more effective than tramadol and paracetamol therapy in the treatment of acute pain.


Assuntos
Cetoprofeno , Tramadol , Acetaminofen , Anti-Inflamatórios não Esteroides/uso terapêutico , Cetoprofeno/análogos & derivados , Cetoprofeno/farmacologia , Cetoprofeno/uso terapêutico , Trometamina/uso terapêutico
7.
J Phys Chem B ; 126(10): 2098-2107, 2022 03 17.
Artigo em Inglês | MEDLINE | ID: mdl-35142495

RESUMO

Ketoprofen (KP) is one of the most popular nonsteroidal anti-inflammatory drugs; however, drug-induced photosensitivity of KP has been reported as a serious adverse effect. KP incorporated into a protein can produce an allergen under UV irradiation, which causes drug-induced photosensitivity. The photochemistry of KP with 20 kinds of proteinogenic amino acids in phosphate buffer solutions at pH 7.4 was studied by transient absorption spectroscopy. The KP carboxylate anion (KP-) gave rise to a carbanion via a decarboxylation within a laser pulse, and the carbanion yielded 3-ethylbenzophenone ketyl biradical (3-EBPH) through a proton transfer reaction. Twelve kinds of proteinogenic amino acids obviously accelerated the reaction. Structural information on the complexes of KP docked in the binding sites of human serum albumin (HSA) was obtained by molecular mechanics (MM) and molecular dynamics (MD) calculations. The photochemical reaction of KP- with amino acid residues in HSA was discussed on the basis of the experimental and calculational results. The information on the reactivity of KP with the amino acids and the stable structures of the KP-HSA complexes should be essential for understanding of the initial step for drug-induced photosensitivity.


Assuntos
Cetoprofeno , Aminoácidos , Ânions , Anti-Inflamatórios não Esteroides/química , Humanos , Cetoprofeno/química , Fotoquímica , Prótons
8.
J Control Release ; 343: 443-456, 2022 03.
Artigo em Inglês | MEDLINE | ID: mdl-35124130

RESUMO

The objective of this study was to develop a novel extended in vitro in vivo correlation (IVIVC) model combined with design of experiment (DoE) that integrates the DoE into IVIVC, which can predict the pharmacokinetics of sustained-release (SR) tablets from their formulation compositions, and vice versa. To develop the extended IVIVC model, ketoprofen was used as a model drug. Nineteen types of ketoprofen SR tablets with different formulation compositions were prepared based on the mixture design and used to derive mathematical relationships between the formulation composition and the in vitro dissolution profiles for DoE. The predictability of the DoE equation was externally validated by using additional seven types of SR formulations with prediction errors (%PE) of less than 11.45%. For the development of IVIVC model, three SR formulations that have fast, medium, and slow drug-releasing rates were selected, and the in vivo pharmacokinetics were assessed in Beagle dogs. The pharmacokinetic properties of ketoprofen SR tablets were described by a population pharmacokinetics (POP-PK) model which incorporated the pH-dependent dissolution of ketoprofen by a time-dependent Hill-type equation. The final POP-PK model could describe the overall in vivo pharmacokinetic profiles and allowed estimation of the in vivo dissolution parameters. The POP-PK model estimated in vivo dissolution parameter, Kdiss, in vivo were then correlated with the in vitro dissolution parameter, Kdiss, in vitro by linear regression (R2 = 0.9989), establishing IVIVC. Finally, the equation derived from DoE was introduced to the IVIVC model to develop the extended IVIVC, which connects the formulation composition, in vitro dissolution, and in vivo pharmacokinetic profiles. The average %PE of the final extended IVIVC model was 4.24% for Cmax and 4.46% and AUC. Finally, the final extended IVIVC was applied to predict the in vivo PK profiles of SR tablets from their formulation compositions as well as to design the optimal formulation to achieve certain target PK profiles. The %PE of the final extended IVIVC model was less than 14.67% for Cmax and 12.41% for AUC, satisfying the FDA criteria of conventional IVIVC. The present extended IVIVC model may provide a useful tool towards rationalized design and development of new SR formulations.


Assuntos
Cetoprofeno , Animais , Preparações de Ação Retardada/farmacocinética , Cães , Liberação Controlada de Fármacos , Solubilidade , Comprimidos
9.
Contact Dermatitis ; 86(4): 300-307, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35089601

RESUMO

BACKGROUND: Allergic contact dermatitis (ACD) and photoallergic contact dermatitis (PACD) to benzophenone present in printing ink have been reported. However, precise chemical analyses and extended photo-patch tests have not been performed in these cases. OBJECTIVES: To determine which components present in a magazine cover are responsible for a patient's skin reaction, to determine the primary sensitizer, and precisely diagnose ACD and PACD. METHODS: After initial photo-patch tests were performed on a patient with a history of reaction to magazine covers after sun exposure, gas chromatography-mass spectrometry and high-performance liquid chromatography analyses of the magazine covers, and additional photo-patch tests were performed. RESULTS: The first photo-patch test results confirmed PACD to ketoprofen and fenofibrate and evoked PACD to the magazine covers. 4-methyl benzophenone (4-MBP) and 1-hydroxy-cyclohexyl-phenyl-ketone (1-HCPK) were found in the magazine cover. Additional photo-patch tests confirmed PACD to 1-HCPK and to benzophenone, and photo-aggravated ACD to 4-MBP. The primary sensitizer was ketoprofen. CONCLUSIONS: Benzophenones are present in a wide variety of products, without always being listed on the packaging. Patients previously sensitized to other ketones, such as ketoprofen, may react to benzophenones without being able to avoid contact with these molecules. New regulations may be needed for more efficient eviction advice.


Assuntos
Dermatite Alérgica de Contato , Dermatite Fotoalérgica , Cetoprofeno , Anti-Inflamatórios não Esteroides , Benzofenonas/efeitos adversos , Dermatite Alérgica de Contato/complicações , Dermatite Alérgica de Contato/etiologia , Dermatite Fotoalérgica/diagnóstico , Dermatite Fotoalérgica/etiologia , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Cetoprofeno/efeitos adversos , Cetoprofeno/química , Testes do Emplastro
10.
Environ Sci Pollut Res Int ; 29(21): 31085-31098, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35000165

RESUMO

In this work, buckwheat husks (Fagopyrum esculentum) were modified by acid treatment and posteriorly employed to remove the ketoprofen in batch adsorption. The characterization results indicated that a more irregular surface with new empty spaces was generated after acid treatment. The adsorptive process was favored at acidic pH = 3. The dosage of 0.85 g L-1 was fixed for the kinetic and isothermal tests, obtaining good removal and capacity indications. The kinetic studies were better represented by pseudo-second-order, obtaining an experimental capacity of 74.3 mg g-1 for 200 mg L-1 of ketoprofen. An increase in temperature negatively affected the adsorption isotherm curves, resulting in a maximum capacity of 194.1 mg g-1. Thermodynamic results confirmed the exothermic nature of the process with physical forces acting. The adsorbent presented high efficiency in treating a synthetic effluent containing different drugs and salts, 71.2%. Therefore, adsorbent development from buckwheat husks treated with a strong acid is an excellent alternative, given the good removal results and the low cost for its preparation.


Assuntos
Fagopyrum , Cetoprofeno , Poluentes Químicos da Água , Adsorção , Anti-Inflamatórios não Esteroides , Concentração de Íons de Hidrogênio , Cinética , Termodinâmica , Águas Residuárias/química
13.
Ultrason Sonochem ; 82: 105906, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34979456

RESUMO

The present study comparatively investigated the ultrasonic degradation of ketoprofen (KET) and paracetamol (PCT) in water. Ultrasonic irradiation at 555 kHz achieved rapid degradation of KET and PCT in water, the removal efficiencies of KET (2.5-80 µM) and PCT (2.5-80 µM) reached 87.7%-100% and 50.6%-86.9%, respectively, after 10 min of reaction under an ultrasonic power of 60 W. The degradation behaviors of both KET and PCT followed the Langmuir-Hinshelwood model. KET was eliminated faster than PCT because of its higher hydrophobicity. Acidic media favored ultrasonic degradation of KET and PCT. Organic compounds in water matrices exerted a great negative effect on the ultrasonic degradation rates of KET and PCT major by competing with target compounds with the generated radicals at the bubble/water interfacial region. The effects of anions were species dependent. The introduction of ClO4- and Cl- enhanced KET and PCT degradation to different extents, while the introduction of HCO3- posed a negative effect on both KET and PCT. KET and PCT degradation are accompanied by the generation of several transform intermediates, as identified via LC/MS/MS analysis, and corresponding reaction pathways have been proposed. A human umbilical vein endothelial cell (HUVEC) toxicity evaluation indicated that ultrasonic treatment was capable of controlling the toxicity of KET or PCT degradation. Of note, the enhanced formation of disinfection byproducts (DBPs), i.e., trichloromethane (TCM) and trichloronitromethane (TCNM), was found due to chlorination after ultrasonic treatment for both KET and PCT.


Assuntos
Ultrassom , Acetaminofen , Desinfecção , Humanos , Cetoprofeno , Cinética , Espectrometria de Massas em Tandem , Água , Poluentes Químicos da Água/análise , Purificação da Água
14.
Appl Spectrosc ; 76(2): 216-227, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35001646

RESUMO

The molecular structure and solution-state molecular interactions in the popular non-steroidal anti-inflammatory drug, ketoprofen, are extensively studied with the aim of gaining a better understanding of the chemical behavior of its solution state and its connection to its nucleation pathway and crystallization outcome. Using as reference solid-state X-ray structures of enantiomeric and racemic forms of ketoprofen, a set of self-assembly models underpinned by density functional theory calculations has been considered for the analysis of spectroscopic data, infrared (IR) and vibrational circular dichroism (VCD), obtained for solutions of the samples as a function of composition and solvent. From our results it can be concluded that, contrary to the general belief for generic carboxylic acids, there are no cyclic dimeric structures of ketoprofen present in solution, but rather linear arrays made up of two (in high polar or diluted media) or more units (in low polar or low dilution media). This observation is in line with the idea that the weak contacts (other than H-bonding) would hold the key to molecular self-assembly, in agreement with recent studies on other aromatic carboxylic acids.


Assuntos
Cetoprofeno , Dicroísmo Circular , Espectroscopia de Infravermelho com Transformada de Fourier , Estereoisomerismo
15.
J Vet Pharmacol Ther ; 45(1): 126-132, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34719792

RESUMO

The aim of the study was to determine the effect of ketoprofen (2 mg/kg) on the intravenous pharmacokinetics of ganciclovir (10 mg/kg) in chukar partridges (Alectoris chukar). Eight clinically healthy partridges were used in the study. The study was performed in two periods using a cross-over design following a 15-day drug washout period. Plasma concentrations of ganciclovir were determined using the high-pressure liquid chromatography-ultraviolet detector and analyzed by non-compartmental analysis. The elimination half-life (t1/2ʎz ), area under the concentration-time curve (AUC0-∞ ), total body clearance, and volume of distribution at steady state of ganciclovir were 1.63 h, 33.22 h*µg/ml, 0.30 L/h/kg, and 0.53 L/kg, respectively. Ketoprofen administration increased the t1/2ʎz and AUC0-∞ of ganciclovir by 78% and 108%, respectively, and while decreased ClT by 53%. The increased plasma concentration and prolonged elimination half-life of ganciclovir caused by ketoprofen may result in the prolonged duration of action and therapeutic effect of ganciclovir. However, the concomitant use requires determination of the pharmacokinetics of ketoprofen and the safety of both drugs.


Assuntos
Galliformes , Cetoprofeno , Administração Intravenosa/veterinária , Animais , Área Sob a Curva , Ganciclovir , Meia-Vida
16.
Br Poult Sci ; 63(1): 14-20, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34633873

RESUMO

1. The aim of this study was to determine the pharmacokinetics of meloxicam (MLX, 1 mg/kg body weight (BW)), ketoprofen (KETO, 2 mg/kg BW), and tolfenamic acid (TA, 2 mg/kg BW) in chukar partridge (Alectoris chukar) following intravenous (IV) administration.2. Twenty-four healthy chukar partridges were randomly divided into three equal groups (n = 8) as MLX, KETO and TA. Plasma concentrations of MLX, KETO and TA were measured using high-performance liquid chromatography-ultraviolet detection and analysed using non-compartmental analysis.3. No adverse effects were determined in chukar partridges after IV administration of MLX, KETO and TA. MLX, KETO and TA were detected in plasma up to 10, 12 and 12 h, respectively. The terminal elimination half-life of MLX, KETO and TA was 1.22, 1.77 and 1.95 h, respectively. MLX, KETO and TA exhibited volumes of distribution at a steady-state of 0.03, 0.23 and 0.41 l/kg BW, respectively. The total plasma clearance of MLX, KETO and TA was 0.02, 0.11 and 0.15 l/h/kg, respectively. The extraction ratios for MLX, KETO and TA were calculated as 0.002, 0.011 and 0.016, respectively.4. MLX, KETO and TA offer treatment in chukar partridges for various conditions with an absence of adverse reactions and properties such as short elimination half-life and low volume of distribution. However, there is a need to establish the safety and adverse effects of repeated administration, pharmacokinetics of other administration routes and pharmacological efficacy of MLX, KETO and TA in chukar partridges.


Assuntos
Galliformes , Cetoprofeno , Animais , Galinhas , Meloxicam , ortoaminobenzoatos
17.
Vet Rec ; 190(6): e977, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34617277

RESUMO

BACKGROUND: The objective of this study was to evaluate the benefits of administering ketoprofen to cows suffering from active digital dermatitis (DD). METHODS: 158 cows presented with active DD (M1, M2 or M4.1 stage) were randomly allocated to either the control or the treatment group. All cows were treated with topical application of oxytetracycline spray. The treatment group also received an intramuscular injection of ketoprofen (3 mg/kg, Ketofen 10%, Ceva Animal Health). Cows were mobility scored just before they were treated and then again one week later. Information regarding their daily milk production was also collected. RESULTS: Animals in the control group were at 2.57 (95% confidence interval (CI): 0.82-8.01, p = 0.10) times higher odds to be lame at the second evaluation compared to those that received ketoprofen as well. This was a numeric but not statistically significant difference. When only cows that were lame prior to treatment were considered, cows that did not receive ketoprofen were at 20.20 (95% CI: 1.40-291.29, p = 0.03) higher odds of remaining lame week post-treatment comparing to cows that did receive ketoprofen. Freshly calved and lame at enrolment cows in the treatment group produced 58.38 ± 1.85 kg per day the week after treatment comparing to freshly calved and lame at enrolment controls that produced 47.89 ± 1.81 kg per day (p < 0.05). CONCLUSION: The addition of ketoprofen in the treatment of active DD lesions may be beneficial for animal welfare and for animal productivity.


Assuntos
Doenças dos Bovinos , Dermatite Digital , Cetoprofeno , Animais , Bovinos , Doenças dos Bovinos/tratamento farmacológico , Dermatite Digital/tratamento farmacológico , Feminino , Cetoprofeno/uso terapêutico , Lactação , Coxeadura Animal
18.
Environ Sci Pollut Res Int ; 29(15): 21860-21875, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34773238

RESUMO

Schizolobium parahyba species can be found in all of South America, producing several residues that can be a major opportunity to develop activated carbon. This work presents the investigation regarding the development of a high specific surface activated carbon (981.55 m2 g-1) and its application in the adsorption of ketoprofen from the aqueous media. The ketoprofen molecules were better adhered to the adsorbent surface under acidic conditions (pH = 2), being the ideal adsorbent dosage determined as 0.7 g L-1, resulting in satisfactory values. It was found that the system reached equilibrium in 200 to 250 min depending on the initial concentration studied, achieving an adsorption capacity of 229 mg g-1. The general order was the most suitable model for describing the experimental data, with an R2 ≥ 0.9985 and MSR ≤ 63.40 (mg g-1)2. The equilibrium adsorption found that the temperature increases the adsorption capacity, achieving 447.35 mg g-1 at 328 K. Besides that, the Tóth model was the most suitable for describing the isotherms R2 ≥ 0.9990 and MSR ≤ 25.67 (mg g-1)2, indicating a heterogeneous adsorbent. The thermodynamic values found that the adsorption of ketoprofen is spontaneous (average ΔG0 of - 32.79 kJ mol-1) and endothermic (ΔH0 10.44 kJ mol-1). The treatment of simulated effluent with the developed adsorbent was efficient, removing 90% of ketoprofen, ibuprofen, and salts. It was found that the adsorbent is reaming its adsorption capacity up to the 5th cycle, progressively decreasing the adsorption capacity until the adsorption does not occur past the 12th cycle. Overall, the results demonstrated that the activated carbon from residual biomass of the Schizolobium parahyba species could be an excellent alternative in obtaining an effective adsorbent to treat wastewater-containing drugs.


Assuntos
Cetoprofeno , Poluentes Químicos da Água , Adsorção , Carvão Vegetal/química , Concentração de Íons de Hidrogênio , Cinética , Termodinâmica , Poluentes Químicos da Água/análise
19.
J Vet Pharmacol Ther ; 45(1): 69-82, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34387365

RESUMO

The current studies aimed to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) profile and to establish a PK-PD model for ketoprofen in a new fixed combination product containing tulathromycin (2.5 mg/kg) and ketoprofen (3 mg/kg) to treat bovine respiratory disease associated with pyrexia in cattle. Firstly, the effect of different ketoprofen doses as mono-substance (1, 3, and 6 mg/kg subcutaneous) on lipopolysaccharide-induced fever was evaluated which indicated that rectal temperature reduction lasted longer in the calves receiving 3 and 6 mg/kg ketoprofen. Secondly, the PK profile of the combination product was compared with mono-substance products (3 mg/kg subcutaneous and intramuscular). The PK profile of ketoprofen in the combination product was characterized by longer t1/2 , lower Cmax and increased AUC in comparison with mono-substance products. Due to prolonged ketoprofen exposure in the combination product, the pyrexia reducing effect of the combination product lasted longer in a second lipopolysaccharide challenge study in comparison with mono-substance products. Finally, a PK-PD model for the anti-pyretic effect of ketoprofen was developed based on the data from the different studies. The PK-PD model eliminated the need for additional animal experiments and indicated that a 3 mg/kg ketoprofen dose in the combination product provided optimal efficacy.


Assuntos
Doenças dos Bovinos , Compostos Heterocíclicos , Cetoprofeno , Animais , Bovinos , Dissacarídeos
20.
Environ Sci Pollut Res Int ; 29(2): 2122-2135, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34363168

RESUMO

This study used the bark of the forest species Campomanesia guazumifolia modified with H2SO4 to absorb the anti-inflammatory ketoprofen from aqueous solutions. FTIR spectra confirmed that the main bands remained after the chemical treatment, with the appearance of two new bands related to the elongation of the carbonyl group present in hemicellulose. Micrographs confirmed that the surface started to contain a new textural shape after acid activation, having new pores and cavities. The drug adsorption's optimum conditions were obtained by response surface methodology (RSM). The adsorption was favored at acidic pH (2). The dosage of 1 g L-1 was considered ideal, obtaining good indications of removal and capacity. The Elovich model very well represented the kinetic curves. The isotherm studies indicated that the increase in temperature negatively affected the adsorption of ketoprofen. A maximum adsorption capacity of 158.3 mg g-1 was obtained at the lower temperature of 298 K. Langmuir was the best-fit isotherm. Thermodynamic parameters confirmed the exothermic nature of the system (ΔH0 = -8.78 kJ mol-1). In treating a simulated effluent containing different drugs and salts, the removal values were 35, 50, and 80% at 15, 30, and 180 min, respectively. Therefore, the development of adsorbent from the bark of Campomanesia guazumifolia treated with H2SO4 represents a remarkable alternative for use in effluent treatment containing ketoprofen.


Assuntos
Cetoprofeno , Myrtaceae/química , Casca de Planta , Poluentes Químicos da Água , Adsorção , Sulfeto de Hidrogênio , Concentração de Íons de Hidrogênio , Cetoprofeno/isolamento & purificação , Cinética , Casca de Planta/química , Soluções , Termodinâmica , Poluentes Químicos da Água/isolamento & purificação
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