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Biomedical subjects

E Doelker

Publications and source records attributed to E Doelker.

At least 55 records · Page 3Linked to original sources

Long-term histopathological study of new polypeptidic biomaterials.

The long-term histopathological evaluation of a new class of synthetic polypeptides, the poly(tert-butyloxycarbonylmethyl glutamates), as implantable drug delivery systems is addressed. This evaluation was performed in rat muscles over one year. The histological analysis included the measurement of many parameters, such as the type and thickness of the collagen capsule. The influence of the presence of progesterone, the selected active drug, could also be monitored over time.

Animals↗

Acute histopathological response to a new biodegradable polypeptidic polymer for implantable drug delivery system.

This article deals with the in vivo evaluation of a new class of synthetic polypeptides, the poly[(tert-butyloxycarbonylmethyl) glutamates], POMEG, as an injectable or implantable drug delivery system. Three different polymers, varying in their degree of esterification, were extruded either with or without progesterone, and finally implanted in rats up to 14 days. Histologic evaluation of the implant sites show evidence of the good biocompatibility of these polymers. In addition, the description of their in vivo behavior, based on microscopic observation of the implanted POMEG rods, enables one to appreciate their potential as a drug delivery system for short- or long-term therapy.

Animals↗

Effect of polymeric network structure on drug release from cross-linked poly(vinyl alcohol) micromatrices.

Three types of poly(vinyl alcohol) were cross-linked by glutaraldehyde to form water-swellable materials possessing a three-dimensional, molecular network. Proxyphylline and theophylline were incorporated into the polymer networks during the cross-linking reaction. The firm hydrogels formed were dried and reduced to a particle size of 400-630 microns. The molecular structure of the gels was characterized by equilibrium swelling measurements which allowed the determination of the average distance between two cross-links and, hence, the macromolecular mesh size. The sulfate and glutaraldehyde residues contained in the purified and nonpurified cross-linked polymers were analyzed, and methods for their elimination and inactivation were developed. Drug release from the highly cross-linked gels could be controlled over more than 12 hr, as the diffusion process in these very dense macromolecular networks is rather slow. The extent of branching and entanglement of the polymeric chains appeared to have an important effect. In addition, the release rate was influenced greatly by the amount and, to a lesser extent, by the type of drug in the network.

Aminophylline↗

Methodology for a better evaluation of the relation between mechanical strength of solids and polymorphic form.

In order to evaluate the role played by polymorphism in the mechanical strength of solid dosage forms (e.g. compressed tablets) and minimize the influence of other factors (such as compaction force, porosity, particle size, and possibly crystal habit), a melted disc technology was developed. With this technique, tablet-shaped discs of zero porosity were prepared by melting powder and subsequent crystallization in the desired modifications. Taking phenobarbitone as a model drug, different methods were used to get discs of forms I, II and III and the amorphous form. Mechanical properties of the discs were assessed, primarily through their bending strength. The Vickers hardness number was also determined for some specimen discs and monocrystals. Results showed that the amorphous form and form III of phenobarbitone gave the toughest discs and would therefore the most suitable materials to manufacture coherent tablets. Moreover, the various preparation methods used resulted in discs of different internal structures. Both crystal size and crystal habit significantly affected the physical properties of the tested materials.

Chemistry, Pharmaceutical↗

[Use of principles of iontophoresis and electrophoresis for controlled release of medical substances].

The present review describes work done over the past twenty years on the controlled release of drugs using iontophoresis or electrophoresis techniques. Following a description of therapeutic applications, in vivo and in vitro studies have been discussed with emphasis on the potentials of such techniques to control drug release. Different mathematical models have been reviewed and an attempt has been made to combine them to explain the various configurations of systems currently used.

Chemistry, Pharmaceutical↗

Osmotic water transport through cellulose acetate membranes produced from a latex system.

The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by casting or spraying. The osmotic water permeability of both kinds of films was measured, as well as their loss of leachable materials and degree of swelling in a saturated solution of potassium chloride. The permeabilities varied over a wide range depending on the physicochemical properties of the plasticizer and its initial concentration in the latex, and on the conditions for coating (temperature, rate of spraying, and drying duration). High boiling point plasticizers gave more permeable films. Films prepared by casting were found to be sensitive to their sodium dodecyl sulfate content.

Cellulose↗

Mechanically strong films produced from cellulose acetate latexes.

Mechanically strong films, comparable with those obtained from organic solutions, can be produced from cellulose acetate latexes, a new type of dispersion, both by casting and spraying. The prerequisite conditions for high strength, which include choice of water-soluble plasticizers possessing some degree of volatility, are discussed.

Cellulose↗

Mechanisms of potassium chloride release from compressed, hydrophilic, polymeric matrices: effect of entrapped air.

The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air entrapped in the matrix during preparation. Removal of the air prior to release restored the traditional t1/2 behavior.

Air↗

Modelling of sustained release of water-soluble drugs from porous, hydrophobic polymers.

The release behaviour of water-soluble drugs from hydrophobic, porous polymeric matrices is complicated by the dissolution of the drug in the water-filled pores under quiescent conditions. Mathematical models are presented for drug release above and below the solubility limit of the drug in the dissolution medium, for constant void fraction (porosity). Experimental studies of KCl release from the porous ethyl cellulose tablets in water at 37 degrees C are explained in terms of dissolution-controlled and diffusion-controlled steps of the release mechanism.

Delayed-Action Preparations↗

Comparative in vitro evaluation of six commercial vincamine prolonged-release dosage forms.

This study consisted of a comparison of the release rates of six commercial brands of prolonged-release vincamine. The pH of the dissolution medium was found to be highly significant. Due to the low solubility of vincamine in media close to the neutral point, all of the preparations tested, with the exception of one, showed highly variable release curves under the three pH conditions chosen.

Delayed-Action Preparations↗