The present study investigated the febrile response in zymosan-induced arthritis, as well increase PGE(2) concentration cerebrospinal fluid (CSF), along with effects of antipyretic drugs on these responses rats. Zymosan intra-articularly injected at dose 0.5 mg did not affect body core temperature (Tc) compared saline (control), whereas doses 1 and 2 mg, zymosan promoted a flattened Tc declined thereafter. 4 was selected for further experiments because it elicited marked long-lasting...

The antipyretic and hypothermic prodrug dipyrone prevents PGE2 -dependent -independent fever induced by LPS from Escherichia coli Tityus serrulatus venom (Tsv) respectively. We aimed to identify the metabolites responsible for effects.Male Wistar rats were treated i.p. with indomethacin (2 mg·kg(-1) ), dipyrone, 4-methylaminoantipyrine (4-MAA), 4-aminoantipyrine (4-AA) (60-360 4-formylaminoantipyrine, 4-acethylaminoantipyrine (120-360 ) or vehicle 30 min before injection of (50 μg·kg(-1) Tsv...

An enantioselective method based on capillary electrophoresis (CE) using cyclodextrin (CD) as chiral selector was developed and validated for determination of lercanidipine (LER) enantiomers, a drug calcium channel blocker which exerts antihypertensive effects long duration, in pharmaceutical formulation. Optimum separation LER enantiomers obtained 50 cm × μ m id sodium acetate buffer solution 200 mmol/L pH 4.0 containing 10 2,3,6-o-methyl- β -cyclodextrin (TM- -CD) background electrolyte....

In general, Passiflora species have been reported for their folk medicinal use as sedative and anti-inflammatory. However, P. caerulea has already to treat pulmonary diseases. Severe tuberculosis, generally caused by Mycobacterium tuberculosis strains resistant multiple drugs, can lead deleterious inflammation high mortality, encouraging new approaches in drug discovery. Thus, the aim of this work was evaluate mucronata Lam., Passifloraceae, potential treatment. Specifically, related...

Abstract A simple enantioselective method based on CE using CD as chiral selector was developed and validated for the determination of isradipine (IRD) enantiomers in a pharmaceutical formulation IRD degradation studies. After optimization, best results were obtained 15 mM borate buffer at pH 9.3 sulfobutyl ether‐β‐cyclodextrin (2.5%, w/v) selector. The applied voltage +30 kV, sample injection performed hydrodynamic mode. All analyses carried out fused‐silica uncoated capillary with an id 50...

The aim of this research was to perform a phytochemical study the methanol leaves extract T. guianensis (MET) guided by vasodilatory and antioxidant activities. chemical profile MET ethyl acetate fraction (EA fraction) determined HPLC-UV-MS EA fractionation reverse-phase chromatography. vasorelaxant effects MET, fractions, sub-fractions constituents were assessed on rat aorta pre-contracted with phenylephrine. Antioxidant activity evaluated using DPPH assay. results show that MET-induced...

Pharmaceuticals can exist in many solid forms, which have different physical and chemical properties. These forms include polymorphs, solvates, amorphous, hydrates. Particularly, hydration process be quite common since pharmaceutical solids contact with water during manufacturing also exposed to storage. In the present work, it is proved that NQR technique capable of detecting hydrated not only pure raw material but final product (tablets), being this way a useful for quality control. This...

The aim of this study was to perform the isolation and characterization vasodilatory flavonoids from Tapirira guianensis Aubl. (Annacardiaceae) leaves. In context, ethyl acetate fraction (EA fraction) obtained subjected fractionation batches by HSCCC affording: myricetin 3-O-α-L-rhamnopyranoside (myricitrin, 1); quercetin 3-O-(6"-O-galloyl)-β-D-galactopyranoside (2); 3-O-α-L-arabinofuranoside (avicularin, 3); (quercitrin, 4). Myricitrin (1) induced a relaxation 56.07 ± 13.04% at 300 μM (P <...

Dihydroergotamine is a semisynthetic natural product derived from ergotamine, an ergot alkaloid. It used to treat migraines, neurological disease characterized by recurrent moderate severe headaches. In this work, the in vitro metabolism of dihydroergotamine was evaluated biomimetic phase I reaction, aiming verify all possible formed metabolites. submitted assay using rat liver microsomes, and metabolites were analyzed HPLC-MS/MS. The reactions performed with Jacobsen catalyst for scaling up...

After oral administration dipyrone is rapidly hydrolyzed to 4-methylaminoantipyrine, which absorbed and further metabolized 4-formylaminoantipyrine 4-aminoantipyrine, acetylated by a polymorphic N-acetyltransferase system 4-acetylaminoantipyrine. To evaluate the presence of metabolites in different rat matrices after intraperitoneal administration, an analytical method was developed validated.The four main were extracted from plasma, cerebrospinal fluid hypothalamus samples LLE prior...

Fever is considered an important component of the acute phase response body in defence against invading organisms such as bacteria. Quercetin, representative flavonoid class, has been extensively studied anti-inflammatory agent. In present study, we investigated effect quercetin, administered orally (5, 25 and 50 mg kg(-1)) or intraperitoneally (50 kg(-1)), on febrile induced by either mug intravenously (5 injected lipopolysaccharide (LPS from Escherichia coli) rats. contrast with well known...

The genus Erythrina, Fabaceae, is widely distributed in tropical and subtropical regions. Their flowers, fruits, seeds bark are frequently used folk medicine for its effects on the central nervous system such as anticonvulsant, antidepressant, analgesic, sedative, hypnotic effects. Erythraline has been reported one of active compounds from but until now there no pharmacokinetics data about this compound only few results showing a putative metabolism were reported. To improve information...

A simple CE based method was developed and validated for the determination of interferon alpha-2a in a pharmaceutical formulation. After optimization, best results were obtained using 30 mmol L−1 tetraborate buffer at pH 8.50 with 50 sodium dodecyl sulfate, diode array detector 200 nm. The applied voltage +25 kV, sample injection performed hydrodynamic mode. All analyses carried out fused-silica uncoated capillary an i.d. 75 μm effective length 50.0 cm. Under these conditions, analysis...

Abstract Introduction: Ductal carcinoma in situ (DCIS) represents around 20% of early breast cancer diagnoses globally. Some studies evaluated risk factors associated with DCIS recurrence. Among these, age, surgical margins, comedonecrosis (CN), high nuclear grade, negative hormone receptors and HER2 expression stand out. Recent approaches have been evaluating the role immune microenvironment its association recurrence progression DCIS. Objective: To evaluate between Tumor Infiltrating...

This paper presents simple, rapid, precise and accurate stability-indicating HPLC CE methods, which were developed validated for the determination of nitrendipine, nimodipine nisoldipine. These drugs are calcium channel antagonists 1,4-dihydropyridine type used in treatment cardiovascular diseases. Experimental results showed a good linear correlation between area concentration covering relatively large domain all cases. The linearity analytical procedures was range 2.0–120.0 μg mL−1...

Diclofenac sodium (DS) is a non-steroidal anti-inflammatory drug that widely prescribed for the treatment of rheumatoid arthritis and post-surgery analgesia. The active pharmaceutical ingredient anhydrous form; however, it can also exist in hydrate form. In this context, knowing properties solid state important relevant area because they have significant impact on solubility, bioavailability, chemical stability drugs. present study, data from XRPD, FTIR spectroscopy, thermal analysis were...

Abstract Introduction: Radiation therapy (RT) plays an important role in the management of patients with ductal carcinoma situ (DCIS) breast, treated by breast conserving surgery (BCS). RT reduces significantly risk local recurrences (LR). Efforts are being, currently, to de-escalate this scenario individualized decision-makings. Several biomarkers and clinical tools were developed predict probability LR aid a tailored decision. The aim study is assess potential MSKCC DCIS Nomogram, which...

Metamizole, or dipyrone (DIP), is a widely used prodrug (bioprecursor class) with powerful analgesic and antipyretic effects. In the gastrointestinal tract DIP first hydrolyzed to 4-methylaminoantipirine (4- MAA), which then absorbed metabolized in liver corresponding 4-aminoantipyrine AA) 4-formylamino-antipyrine (4-FAA) derivatives. Furthermore, 4-AA suffers an acylation reaction afford 4- acetylaminoantipyrine (4-AAA). Despite some authors have proposed that 4-MAA are active metabolites...

INTRODUCTION: The understanding of the transition between preinvasive and invasive stage in breast carcinomas is key to more efficient strategies for early diagnosis treatment, as well it expands knowledge about complex mechanisms carcinogenesis. In this study our aim was compare prognostic predictive pathological features situ components ductal carcinomas. MATERIAL AND METHODS: We selected 146 consecutive samples with DCIS associated carcinoma. age patients ranged from 29 87 years (median =...

INTRODUCTION: The prevalence of DCIS has been rising in the last decades, probably due to better screening programs. This increase diagnosed cases shows heterogeneity group, particularly risk associated invasive disease and recurrences, most these as cancer. We investigated role basal cytokeratin 5/6 (CK5/6) invasion ductal carcinoma situ (DCIS). MATERIAL AND METHODS: Tissue microarrays from 236 samples, consisting 90 without (IDC) (group 1) 146 with IDC 2), both groups having similar...