Showing 1-30 of 99 resultados for "P0847"
Takao Komasaka et al.
Chemical & pharmaceutical bulletin, 62(11), 1073-1082 (2014-11-05)
The present study aimed to develop a practical method for preparing nanosuspension formulations of poorly water-soluble compounds for enhancing oral absorption in toxicology studies in the discovery stage. To obtain a suitable nanosuspension formulation for the intended purpose, formulations were...
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds...
K Kogermann et al.
International journal of pharmaceutics, 444(1-2), 40-46 (2013-02-02)
The main purpose of this study was to investigate the effect of different polymers, with varying physicochemical properties and molecular weight on the stability and dissolution of co-milled amorphous solid dispersions (ASDs) of piroxicam (PRX). The stability of amorphous PRX...
Mark C Wenlock et al.
Bioorganic & medicinal chemistry letters, 21(12), 3550-3556 (2011-05-24)
In drug discovery projects the ability to show a relationship between a compound's molecular structure and its pharmacokinetic, in vivo efficacy, or toxicity profile is paramount for the design of better analogues. To aid this understanding the measurement of distribution...
P Pfitzenmeyer et al.
The Journal of rheumatology, 21(8), 1573-1577 (1994-08-01)
We describe 2 patients who developed pulmonary infiltrates while being treated with piroxicam. There was no satisfactory explanation other than drug induced lung disease for their illness. They had no exposure to pneumotoxic drugs or aerocontaminants. Microorganisms were not cultured...
Aurélien Vidal et al.
European journal of medicinal chemistry, 45(1), 405-410 (2009-10-13)
A series of new oxicam derivatives bearing a quaternary ammonium (QA) moiety was synthesized and evaluated in vitro for antiosteoarthritis properties. Propyltrimethyl ammonium 3 and propyldiethylmethyl ammonium 11 stimulated aggrecan expression and mitigated the inhibitory action of IL-1. QA derivative...
Gianpaolo Chiriano et al.
European journal of medicinal chemistry, 48, 206-213 (2012-01-03)
In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as β-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising...
Francisco J Prado-Prado et al.
Bioorganic & medicinal chemistry, 18(6), 2225-2231 (2010-02-27)
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against...
Jianjun Zhang et al.
The Journal of pharmacy and pharmacology, 65(1), 44-52 (2012-12-12)
The aim of the study was to prepare and to characterize two polymorphs of lornoxicam, a water-insoluble non-steroidal anti-inflammatory drug, which has thus far received no exploration of its polymorphs. Form I and form II of lornoxicam were prepared by...
Önder Ersan et al.
Acta orthopaedica et traumatologica turcica, 46(6), 411-415 (2013-02-23)
The aim of this study was to compare the analgesic effects of intra-articular levobupivacaine alone, intra-articular levobupivacaine in combination with lornoxicam, and intra-articular levobupivacaine in combination with lornoxicam and morphine on patients following arthroscopic surgery. The study included 60 ASA...
Michael A Kron et al.
Clinical and vaccine immunology : CVI, 20(2), 276-281 (2012-12-21)
The therapeutic effects of a controlled parasitic nematode infection on the course of inflammatory bowel disease (IBD) have been demonstrated in both animal and human models. However, the inability of individual well-characterized nematode proteins to recreate these beneficial effects has...
Mariana P Arce et al.
Journal of medicinal chemistry, 52(22), 7249-7257 (2009-10-28)
Novel multifunctional compounds have been designed, synthesized, and evaluated as potential drugs for the treatment of Alzheimer's disease (AD). With an L-glutamic moiety as a suitable biocompatible linker, three pharmacophoric groups were joined: (1) an N-benzylpiperidine fragment selected to inhibit...
R E Lister et al.
European journal of rheumatology and inflammation, 12(4), 6-11 (1993-01-01)
Piroxicam-beta-cyclodextrin is a novel NSAID; it is a supermolecular inclusion complex designed to improve the risk:benefit ratio of piroxicam. In animal studies it has been shown to be as effective as piroxicam as an anti-inflammatory and analgesic agent but with...
Nursyamsyila Mat Hadzir et al.
AAPS PharmSciTech, 14(1), 456-463 (2013-02-07)
Fatty acid esters are long-chain esters, produced from the reaction of fatty acids and alcohols. They possess potential applications in cosmetic and pharmaceutical formulations due to their excellent wetting behaviour at interfaces and a non-greasy feeling when applied on the...
Miriam Redondo et al.
European journal of medicinal chemistry, 47(1), 175-185 (2011-11-22)
A simple and efficient synthetic method for the preparation of quinazoline type phosphodiesterase 7 (PDE7) inhibitors, based on microwave irradiation, has been developed. The use of this methodology improved yields and reaction times, providing a scalable procedure. These compounds are...
Nelilma C Romeiro et al.
European journal of medicinal chemistry, 43(9), 1918-1925 (2008-01-29)
This paper describes molecular docking studies of a series of classical NSAIDs with PPARgamma receptor, which has been pointed as a new target for the design of anti-cancer and anti-inflammatory drugs, and has been found to be responsible for some...
C R Lee et al.
Drugs, 48(6), 907-929 (1994-12-01)
Piroxicam-beta-cyclodextrin is a complex of the established nonsteroidal antiinflammatory drug (NSAID) piroxicam and an inert cyclic macromolecule, beta-cyclodextrin. In clinical trials in patients with rheumatic diseases or pain arising from other conditions, it was as effective an analgesic as standard...
Wei Li Lee et al.
PloS one, 9(12), e114284-e114284 (2014-12-04)
Floating dosage forms with prolonged gastric residence time have garnered much interest in the field of oral delivery. However, studies had shown that slow and incomplete release of hydrophobic drugs during gastric residence period would reduce drug absorption and cause...
The piroxicam enigma.
B Ljunggren
Photo-dermatology, 6(4), 151-153 (1989-08-01)
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential...
D Gerber
Drug intelligence & clinical pharmacy, 21(9), 707-710 (1987-09-01)
During the approximately five years (1981-86) that piroxicam has been available in South Africa, the Medicines Safety Centre has received 31 reports of adverse reactions associated with this drug. Among these are two reactions not previously recorded in the literature...
Anima Vats et al.
Therapeutic delivery, 3(11), 1281-1295 (2012-12-25)
In recent years, nonsteroidal anti-inflammatory drugs have been found to be cogent as an adjuvant therapeutic agent in mitigating colorectal cancer. Thus, this present investigation was aimed to formulate an oral, targeted tablet of piroxicam microspheres for sustained and targeted...
M L de Carli et al.
Journal of oral rehabilitation, 40(3), 171-178 (2012-12-21)
This study aimed to evaluate the efficacy of piroxicam associated with low-level laser therapy compared with single therapies in 32 patients presenting temporomandibular joint arthralgia in a random and double-blind research design. The sample, divided into laser + piroxicam, laser...
Prem Shankar Gupta et al.
Expert opinion on drug delivery, 10(1), 17-32 (2012-10-30)
The present study investigates the effect of particle engineering technique on powder properties and pharmacokinetics of piroxicam (PXM). PXM was subjected to melt sonocrystallization to obtain product designated as MSCPXM and characterized for various pharmacotechnical parameters, performance characteristics and pharmacokinetic...
A Guerra et al.
European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising...
Pelayo Camps et al.
Journal of medicinal chemistry, 52(17), 5365-5379 (2009-08-12)
Two isomeric series of dual binding site acetylcholinesterase (AChE) inhibitors have been designed, synthesized, and tested for their ability to inhibit AChE, butyrylcholinesterase, AChE-induced and self-induced beta-amyloid (Abeta) aggregation, and beta-secretase (BACE-1) and to cross blood-brain barrier. The new hybrids...
Dennis J Pelletier et al.
Journal of chemical information and modeling, 47(3), 1196-1205 (2007-04-13)
The identification of phospholipidosis (PPL) during preclinical testing in animals is a recognized problem in the pharmaceutical industry. Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process....
David Buttar et al.
Bioorganic & medicinal chemistry, 18(21), 7486-7496 (2010-09-28)
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been used to assign a primary binding site for these compounds...
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this...
Bram Baert et al.
Bioorganic & medicinal chemistry, 15(22), 6943-6955 (2007-09-11)
A set of 116 structurally very diverse compounds, mainly drugs, was characterized by 1630 molecular descriptors. The biological property modelled in this study was the transdermal permeability coefficient logK(p). The main objective was to find a limited set of suitable...

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