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Biomedical subjects

F Alhaique

Publications and source records attributed to F Alhaique.

32 records · Page 2Linked to original sources

A polymeric film responding in diffusion properties to environmental pH stimuli: a model for a self-regulating drug delivery system.

A new polymeric film, ethylene-vinyl-NN-diethylglycinate random copolymer, has been studied to evaluate possible applications of such a material to produce controlled release dosage forms. Protonation of the substituted amino groups took place to different extents according to environmental pH conditions. The polymeric film proved to be permeable only to uncharged species, the rate of diffusion of which increased with the increasing charge of the membrane. This effect might be related to strong polymer-proton interactions affecting structure and transport properties of the film and enhancing the solvation process. The charged form of a number of barbituric acid derivatives did not diffuse through the membrane. The uncharged forms permeated the polymeric sheeting at rates consistent with their partition coefficients and which increased with the increasing charge of the polymer.

Chemical Phenomena↗

Effect of a second solubilizate on the partition coefficient of drugs in micellar solution and their permeation rate across an artificial membrane.

The distribution of a solubilizate between micelles and the aqueous phase does not obey a simple partition law when a second solubilizate species is present. Alterations of the apparent partition coefficient cannot be explained in terms of a simple displacement mechanism, following the interaction of both solubilizates with the same site of the micelle. A non linear increase in solubilizate association to micelles following an increase in surfactant concentration is observed in the presence of a second solubilizate. A depression in the cloud point temperature follows the addition of a second species and is such that cannot be interpreted as a simple additive effect. Alteration of the apparent partition coefficient in a miscellar solution has an effect on the permeation rate of the solubilizate across an artificial membrane. Biopharmaceutical implications are discussed.

Benzoates↗

O- and N-alkylation with "Meerwein's reagent": the unusual behaviour of two lactams.

Usually tertiary oxonium salts are excellent O-alkylating agents of lactams; in some cases indiscriminate O- and N-alkylations have been described. In this paper the particular behaviour towards Meerwein's reagent of two isomers with a lactamic structure is pointed out: in one case the usual O-alkylation occurs, in the other N-alkylation is the only reaction that takes place.

Alkylation↗

Effect of surfactant monomers on chloramphenicol association to an albumin-lecithin complex: a model for modified drug absorption.

The binding of chloramphenicol to an albumin-lecithin complex in the presence or absence of premicellar concentrations of both ionic and non-ionic surfactants has been examined. Long chain, strong ionic detergents, such as sodium dodecyl sulphate or cetyltrimethylammonium bromide, severely perturb protein structure and eventually allow full separation of the complex into lecithin and albumin-detergent complexes. The dissociation process is reversible upon the removal of the detergent by exhaustive dialysis. After the splitting of the complex, the amount of antibiotic associated with the lipid-protein mixture increases. Structural alteration of the albumin-lecithin complex and the increase in the binding of chloramphenicol have an effect on the transfer rate of this antibiotic across an artificial barrier consisting of an aqueous dispersion of the same complex, as observed in a model system. It is suggested that a reversible alteration in membrane structure, and consequently in membrane permeability, might be easily effected, at the molecular level, through a reversible dissociation of structural lipoproteins into their components, operated by premicellar concentrations of ionic surfactants. This represents a tentative picture of the possible events taking place within the membrane and modifying the absorption rate of a drug, when it is associated with surfactants in a pharmaceutical preparation.

Absorption↗

Effect of surfactants on diffusion of calcium in mucin: a possible mechanism affecting enamel remineralization.

By means of in vitro experiments, performed with a three compartment diffusion cell, we show how the presence of surfactants, often present in the formulation of dentifrices and mouthrinses, may affect the availability of calcium and its permeation rate through the proteic layer covering dental enamel (acquired pellicle). Mucin was the protein used to simulate the pellicle. Experiments were performed at different surfactant concentrations (i.s. below and above CMC) and also in the presence of fluoride ions that are capable of enhancing enamel remineralization. The mechanisms involved, mainly related to the interaction of surfactant monomers with the model protein, are discussed in this paper.

Calcium↗