Anti-inflammatory effect of rosmarinic acid isolated from Blechnum brasiliense in adult zebrafish brain.

Neuroinflammation has been associated to neurodegenerative disease development, with evidence suggesting that high levels of proinflammatory cytokines promote neuronal dysfunction and death. Therefore, it is necessary to study new compounds that may be used as adjuvant treatments of neurodegenerative diseases by attenuating the inflammatory response in the central nervous system (CNS). The aim of this study was to utilize the lipopolysaccharide (LPS) induction model of neuroinflammation to evaluate the modulation of inflammation by rosmarinic acid (RA) isolated from Blechnum brasiliense in adult zebrafish.

Amazonia Products in Novel Lipid Nanoparticles for Fucoxanthin Encapsulation.

Lipid nanoparticles (LNs) are traditional systems able to effectively increase skin hydration. However, due to its reduced viscosity, LNs suspensions are less attractive for skin administration. To overcome this disadvantage, the LN were incorporated in the semi-solid formulation is easy manipulation.

In vitro toxic evaluation of two gliptins and their main impurities of synthesis.

Background: The presence of impurities in some drugs may compromise the safety and efficacy of the patient's treatment. Therefore, establishing of the biological safety of the impurities is essential. Diabetic patients are predisposed to tissue damage due to an increased oxidative stress process; and drug impurities may contribute to these toxic effects.

Stability in clinical use and stress testing of meropenem antibiotic by direct infusion ESI-Q-TOF: Quantitative method and identification of degradation products.

An ESI-MS/MS method through direct infusion was validated for quantitative analysis of meropenem powder for injection. The validation parameters were established in a rapid analysis of 30 s. Drug stability was studied through the submission to stress testing, resulting on four degradation products.

Biological Safety Studies and Simultaneous Determination of Linagliptin and Synthetic Impurities by LC-PDA.

A stability-indicating LC method was developed for quantification of linagliptin (LGT) and three synthetic impurities. The method utilizes a Thermo Scientific® RP-8 column (100 mm × 4.6 mm; 5 m) with the PDA detector for quantitation of impurities.

Application of Quality by Design to optimize a stability-indicating LC method for the determination of ticagrelor and its impurities.

Simultaneous analysis of drug compounds and their impurities of degradation and synthesis became constant in the modern pharmaceutical analysis. Likewise, analytical techniques must improve sensitivity and selectivity for the monitoring of pharmaceutical products, allowing a full assessment of impurities in drug products and, therefore, ensure safety and efficacy of pharmacological treatments. The application of Quality by Design (QbD) principles has proved to be feasible on the elaboration of analytical methods, allowing the comprehensive evaluation and measurement of different analytical parameters and their effects on critical properties of the methodology in development.

Stability of doripenem in reconstituted solution - thermal and oxidative decomposition kinetics and degradation products by LC-MS.

A ultra-fast liquid chromatography method applied to quantitation of doripenem in powder for injection was validated. Validation parameters were assayed and a rapid analysis was established by a reversed-phase system comprising a C column endcapped (50 × 4.0 mm, 2.

HPLC method for simultaneous analysis of ticagrelor and its organic impurities and identification of two major photodegradation products.

A simple, fast and sensitive analytical method by high-performance liquid chromatography (HPLC) was developed and validated for the simultaneous determination of ticagrelor and two synthesis impurities. The HPLC method was established using an Agilent 1200 Series equipment coupled to photodiode array detector (PDA) at 270nm with a Zorbax Plus C column (150×4.6mm, 5.

Hydrogel containing adapalene- and dapsone-loaded lipid-core nanocapsules for cutaneous application: development, characterization, in vitro irritation and permeation studies.

Lipid-core polymeric nanocapsule suspensions containing adapalene and dapsone (AD-LCNC) were developed and incorporated in a Carbopol 940® hydrogel (AD-LCNC HG). A nanoemulsion (AD-NE), similarly prepared but omitting the polymer, was developed and also incorporated in a Carbopol 940 hydrogel (AD-NE HG) to evaluate the polymer effect. Physicochemical characteristics were evaluated.

Quantitative determination of the β-methyl carbapenem doripenem in powder for injection by a stability-indicating capillary zone electrophoresis method.

A capillary zone electrophoresis method for quantitative determination of doripenem in synthetic matrix was developed. The stability-indicating capability was performed applying stress testing protocols. The selected analytical conditions include 100 mM sodium borate buffer (pH 8.

Structural elucidation of gemifloxacin mesylate degradation product.

Gemifloxacin mesylate (GFM), chemically (R,S)-7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid methanesulfonate, is a synthetic broad-spectrum antibacterial agent. Although many papers have been published in the literature describing the stability of fluorquinolones, little is known about the degradation products of GFM. Forced degradation studies of GFM were performed using radiation (UV-A), acid (1 mol L(-1) HCl) and alkaline conditions (0.

Determination of quinolones and fluoroquinolones, tetracyclines and sulfonamides in bovine, swine and poultry liver using LC-MS/MS.

Antibacterials are widely used in veterinary medicine. Residues of these drugs can remain in food of animal origin, including bovine liver. This paper describes a fast and simple analytical method for the determination of quinolones and fluoroquinolones, tetracyclines and sulfonamides in bovine liver samples.

A simple, fast and cheap non-SPE screening method for antibacterial residue analysis in milk and liver using liquid chromatography-tandem mass spectrometry.

In routine laboratory work, screening methods for multiclass analysis can process a large number of samples in a short time. The main challenge is to develop a methodology to detect as many different classes of residues as possible, combined with speed and low cost. An efficient technique for the analysis of multiclass antibacterial residues (fluoroquinolones, tetracyclines, sulfonamides and trimethoprim) was developed based on simple, environment-friendly extraction for bovine milk, cattle and poultry liver.

HPLC-DAD for the determination of three different classes of antifungals: method characterization, statistical approach, and application to a permeation study.

This study describes and characterizes methods for high-performance liquid chromatography diode array detection (HPLC-DAD) analysis of formulations containing molecules with antifungal activity of three different classes: terbinafine and butenafine (allylamines), miconazole and fluconazole (azoles), and geraniol, neral and geranial (monoterpenes). All methods used the same chromatographic column (RP18 ), enabling the analysis to be performed in a single batch. The specificity was extensively discussed through the establishment of purity peak methods.

Highly selective colorimetric method to determine gemifloxacin mesylate in the presence of a synthetic impurity.

A simple visible spectrophotometric method was developed for the determination of gemifloxacin mesylate (GFM) in tablets. The method was based on the formation of a yellow ion-pair complex between the basic nitrogen of the drug and the sulfonphthalein acid dye in phthalate buffer. The method was validated by the study of its specificity, linearity, precision, accuracy, and robustness.

Capillary zone electrophoresis for determination of vildagliptin (a DPP-4 inhibitor) in pharmaceutical formulation and comparative study with HPLC.

A stability-indicating capillary zone electrophoresis (CZE) method was validated for the determination of vildagliptin (VLG) in pharmaceutical dosage forms using ranitidine hydrochloride (RH) as internal standard. The CZE method was carried out in a fused silica capillary (64.5 cm total length and 56.

Gemifloxacin mesylate (GFM): dissolution test based on in vivo data.

Gemifloxacin mesylate (GFM) is a synthetic, broad-spectrum, fluoroquinolone antibacterial agent. It is different from other class members because it achieves adequate plasma concentrations to inhibit both topoisomerase IV and gyrase. The aim of this study was to develop and validate a dissolution test for GFM in coated tablets, using a simulated absorption profile based on in vivo data obtained from the literature.

Quantitative evaluation of besifloxacin ophthalmic suspension by HPLC, application to bioassay method and cytotoxicity studies.

Besifloxacin (BSF) is a synthetic chiral fluoroquinolone developed for the topical treatment of ophthalmic infections. The present study reports the development and validation of a microbiological assay, applying the cylinder-plate method, for determination of BSF in ophthalmic suspension. To assess this methodology, the development and validation of the method was performed for the quantification of BSF by high performance liquid chromatography (HPLC).

Influence of penetration enhancers and molecular weight in antifungals permeation through bovine hoof membranes and prediction of efficacy in human nails.

This work aimed to evaluate the effect of different substances on the permeation of geraniol through bovine hoof membranes. Different penetration enhancers were able to increase the permeability up to 25 times compared to control. It was demonstrated that acetilcysteine in association with ascorbic acid increased the permeation, even in acid formulations.

Biological safety studies of gemifloxacin mesylate and related substances.

Purpose: The aim of this study was to evaluate the cytotoxic, phototoxic, genotoxic and photogenotoxic potential of gemifloxacin mesylate (GFM), its main synthetic impurity (SI) and one isolated and structurally elucidated degradation product (DP).

Methods: The neutral red uptake (NRU) and reduction of 2,5-diphenyl-3,-(4,5-dimethyl-2-thiazolyl)tetrazolium bromide (MTT) assays were performed as in vitro endpoints to evaluate cytotoxicity and phototoxicity in a 3T3 cell line, and predict toxicity and/or phototoxicity after systemic administration of the drug. The in vitro alkaline single-cell electrophoresis (comet) assay was used to evaluate the genotoxic and photogenotoxic potential of the substances using the same cell line.

Micellar electrokinetic chromatographic method for mianserin hydrochloride and analysis of degradation products by mass spectrometry.

A simple, stability-indicating micellar electrokinetic chromatography (MEKC) method was developed and validated for the analysis of mianserin hydrochloride in coated tablets. The method employed (hydroxymethyl)aminomethane (TRIS) 50 mM to which sodium dodecyl sulfate (SDS) 50 mM was added at pH 10.6 as the electrolyte and the voltage applied was 25 kV.

Levodopa microparticles for pulmonary delivery: photodegradation kinetics and LC stability-indicating method.

Levodopa, (S)-2-amino-3-(3,4-dihydroxyphenyl) propanoic acid, is still considered the gold standard treatment for Parkinson's disease. However, oral levodopa shows poor pharmacokinetics and its efficacy becomes problematic with the progression of the disease. Pulmonary delivery using the association of the polymers: chitosan, hyaluronic acid and HPMC, represents a novel approach to overcome this problem.

Photodegradation kinetics, cytotoxicity assay and determination by stability-indicating HPLC method of mianserin hydrochloride.

A stability-indicating HPLC method for the determination of mianserin hydrochloride in coated tablets was developed and validated. Also, drug photodegradation kinetics and cytotoxicity were determined. Chromatographic analyses were performed in an Ace RP-18 octadecyl silane column (250 mm x 4.

Stability-indicating RP-LC method for the determination of vildagliptin and mass spectrometry detection for a main degradation product.

A simple, precise and stability-indicating reversed-phase liquid chromatography method was developed and validated for the determination of vildagliptin (VLG) in pharmaceutical dosage form. The chromatographic separation was obtained within 6 min and was linear in the range of 20-80 µg/mL (r(2) = 0.9999).

Identification, characterization and cytotoxicity in vitro assay of nitazoxanide major degradation product.

Stress studies of the broad-spectrum antiparasitic nitazoxanide were conducted in order to isolate and elucidate the major degradation product involved in thermal, acid, alkaline, oxidative and photolytic decomposition of the drug in solution and solid state. The major degradation product was identified and characterized using techniques namely LC-DAD, (1)H NMR, (13)C NMR, IR, and MS/MS. The stability of nitazoxanide raw material and nitazoxanide in tablets and in suspension powder was studied under different conditions and the results suggest the formation of the same deacetylated degradation product occur in all cases.