Search results for "ROMA"
showing 10 items of 13919 documents
PLS-UV spectrophotometric method for the simultaneous determination of paracetamol, acetylsalicylic acid and caffeine in pharmaceutical formulations
1997
A simple and fast analytical procedure is proposed for the simultaneous determination of paracetamol, acetylsalicylic acid and caffeine in pharmaceuticals by means the partial least square treatment of the spectrophotometric absorbance data between 216 and 300 nm, taken at 5 nm intervals. The method involves the use of 8 standard mixtures of the three compounds assayed, considered at two concentration levels, and the measurement of the absorbance of samples in a 20% (v/v) ethanol in water solution previously filtered. In the analysis of real and synthetic samples precise and accurate values were obtained by the aforementioned procedure, providing in all cases variation coefficients and accu…
Improving Dissolution Behavior and Oral Absorption of Drugs with pH-Dependent Solubility Using pH Modifiers: A Physiologically Realistic Mass Transpo…
2021
Orally dosed drugs must dissolve in the gastrointestinal (GI) tract before being absorbed through the epithelial cell membrane. In vivo drug dissolution depends on the GI tract's physiological conditions such as pH, residence time, luminal buffers, intestinal motility, and transit and drug properties under fed and fasting conditions (Paixao, P. et al. Mol. Pharm. 2018 and Bermejo, et al. M. Mol. Pharm. 2018). The dissolution of an ionizable drug may benefit from manipulating in vivo variables such as the environmental pH using pH-modifying agents incorporated into the dosage form. A successful example is the use of such agents for dissolution enhancement of BCS class IIb (high-permeability,…
Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro ex…
2014
Concomitant food intake can diminish oral absorption of drugs with limited permeability and an absorption window in the proximal intestine, due to viscosity-mediated decrease in dosage form disintegration time and drug dissolution rate. Three poorly-permeable drugs (atenolol, metformin hydrochloride, and furosemide) exhibiting negative food effect, and one highly-soluble and highly-permeable (metoprolol tartrate), serving as a negative control, were selected for the study. In vitro and in silico tools were used to evaluate the influence of media viscosity on drug bioperformance under fasted and fed conditions. The obtained results demonstrated that increased medium viscosity in the presence…
Micellar liquid chromatography for prediction of drug transport.
2000
Abstract The vast majority of well absorbed drugs are transported passively across the cell membranes. Physicochemical descriptors of drug molecules that are believed to influence transcellular transport are routinely used to predict drug absorption by means of complex mathematical models. In this paper, a new in vitro method, based on the retention data in micellar liquid chromatography (MLC), is validated for the prediction of passive drug absorption. The retention of a heterogeneous drugs set in MLC using Brij 35 as surfactant in the mobile phase is compared with the retention data reported in literature obtained in red cell membrane lipid liposomes, human red cell membranes vesicles (ve…
Influence of gamma-aminobutyric acid on baclofen intestinal absorption.
1994
Since previous studies suggested that baclofen absorption in the rat middle intestine was inhibited by beta-alanine and therefore mediated, at least in part, by the beta-aminoacid carrier, we focused our new studies on the analysis of the possible inhibition of the drug by a gamma-aminoacid model compound, gamma-aminobutyric acid (GABA). A rat jejunum in situ study was undertaken in order to evaluate the effect of GABA on baclofen absorption and to establish the inhibition model. Assays using isotonic perfusion solutions of 0.5 mM baclofen with starting GABA concentrations ranging from 0 to 100 mM are reported. The results show that the absorption rate pseudoconstants of the drug decrease a…
Partially competitive inhibition of intestinal baclofen absorption by beta-alanine, a nonessential dietary aminoacid.
1991
In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption rate pseudoconstants of the spasmolytic drug decrease as beta-alanine concentration increases, until a limiting value is obtained (36.8 per cent of that found for baclofen alone). A computer method was developed in order to calculate parameters governing baclofen absorption in the presence of beta-aminoacid, with the following results: Vm = 11.22 mM h-1; Km = 7.42 mM; Ki = 2.4…
Intestinal absorption pathway of gamma-aminobutyric acid in rat small intestine.
1994
Intestinal absorption of gamma-aminobutyric acid (GABA), as a model compound for gamma-aminoacids, has not been extensively studied from the kinetic viewpoint. Since data from our laboratory suggested that some competition arises between intestinal absorption of beta-alanine and GABA and since our intent was to maintain the aqueous stagnant diffusion layer in order to approach absorption tests to in vivo physiological conditions, a rat jejunum in situ study was undertaken in order to gain an insight into the mechanism of GABA absorption. In the present paper, results from assays using isotonic perfusion solutions with starting GABA concentrations ranging from 1 to 50 mM are reported. They s…
Quantitative analysis of the effect of controlled-release formulation on nonlinear gastrointestinal absorption of P-glycoprotein substrate talinolol …
2020
Abstract Oral absorption of talinolol, a substrate of P-glycoprotein (P-gp), from a sustained-release (SR) formulation was reportedly decreased compared to that from an immediate-release (IR) formulation. The aim of this study was to predict and understand the effect of controlled-release formulation on the oral absorption of P-gp substrates by developing a physiologically based pharmacokinetic (PBPK) absorption model incorporating multiple kinetic parameters obtained from in vitro studies, using talinolol as a model substrate. Simulation analysis using the developed PBPK absorption model indicated that the clinically observed marked decrease in the plasma concentration of talinolol adminis…
Effect of simulated gastrointestinal digestion on plant sterols and their oxides in enriched beverages
2013
Abstract This study evaluates the bioaccessibility (percentage of soluble compound available for absorption) of plant sterols (PS) and their oxides (phytosterol oxidation products, POPs) after simulated gastrointestinal digestion in fruit (Fb), milk (M) and fruit-based milk beverages with (FbM a ) or without (FbM b ) tangerine juice. In beverages and their bioaccessible fraction (BF), campesterol, campestanol, stigmasterol, β-sitosterol and sitostanol were detected. Bioaccessibility of total PS ranged between 2.62 and 6.48%, FbM b yielding the highest value, followed by FbM a > Fb > M. Campesterol/campestanol were the most bioaccessible PS. Only oxides of β-sitosterol were detected in beve…
Effect of cooking on oxalate content of pulses using an enzymatic procedure.
2003
An enzymatic method proposed for the determination of oxalate in urine is adapted for the estimation of soluble oxalate content in beans, chickpeas and lentils. Oxalates were extracted in water by refluxing for 2 h. The method is based on the oxidation of oxalate by the oxidase and the determination of the resulting hydrogen peroxide, which in presence of peroxidase, 3-methyl-2 benzotiazinolone and 3-dimethylamino benzoic, gives an indamine compound with an absorption maximum at 590 nm. The linearity (from 0.015 to 0.6 mM) of the method is adequate to the analysis of oxalate contents in pulses, and the inter-day precision of the method expressed as relative standard deviation was good (3.01…