0000000001096035
AUTHOR
Y. Pourcelot
showing 23 related works from this author
On the difficulty of assessing the specific surface area of magnesium stearate
2001
Abstract The water content of as-received commercial magnesium stearate batches from animal and vegetable sources have been modified by ageing in humid air at room temperature or by vacuum treatment. The complete adsorption–desorption isotherms of nitrogen and krypton vapours by samples of these as received and modified materials have been measured at liquid nitrogen temperature after standardised vacuum degassing. They are greatly affected by the initial water content of the material. In particular: (a) the BET surface area values computed from the adsorption branch vary widely and is increasing with increasing water content; (b) anomalous hysteresis of varying amplitude is observed in all…
Dry adsorbed emulsion: 2. Dissolution behaviour of an intricate formulation
2002
The behaviour of a pharmaceutical form, called dry adsorbed emulsion (DAE), containing a sparingly soluble drug (i.e. theophylline) was studied for dissolution drug release kinetic, in relation with DAE structure characterisation. In vitro dissolution testings were performed under different experimental conditions (medium at pH 1.2 and 7.4, medium with or without surfactant addition, different particle sizes, discrete or densified particles). Discrete DAE particles showed an extended release, in comparison with the native drug powder, depending on both drug solubility in the medium and particle size. The relevance of dissolution data was not improved by surfactant addition (0.1% sodium laur…
Dry adsorbed emulsion: 1. Characterization of an intricate physicochemical structure
2000
Abstract A recent solid pharmaceutical form called “Dry Adsorbed Emulsion” (DAE) was characterized in morphological and structural fields. A DAE is an intricate system initiated by a water‐in‐oil emulsion including the active drug (i.e., theophylline). Each emulsion phase is adsorbed on pulverulent adsorbents with a suitable polarity (silica) to obtain a free‐flowing powder with nonporous particles of size from 125 to 710 μm, with small specific surface area and a spherical shape. Different methods, such as scanning electron microscopy combined with chemical microanalysis, dying tests, and electron spin resonance studies, allow the formulator to follow the behavior of DAE aqueous and oily p…
Comparative study of the lubricant performance of Compritol® HD5 ATO and Compritol® 888 ATO: effect of polyethylene glycol behenate on lubricant capa…
2003
The aim of this paper is to study the lubricant capacity of Compritol HD5 ATO, a glyceryl and polyethylene glycol dibehenate, obtained by atomization. This material is compared to Compritol 888 ATO, constituted only by glyceryl dibehenate. First, this study verifies that Compritol HD5 ATO and Compritol 888 ATO present the same granular characteristics and that their mixes with Lactopress present no structural differences. Secondly, in term of compressibility and cohesiveness, the use of Compritol 888 ATO or Compritol HD5 ATO with Lactopress does not involve any significant modification. Finally, the minor difference of lubricant capacity between Compritol HD5 ATO and Compritol 888 ATO has n…
Colonic drug delivery: influence of cross-linking agent on pectin beads properties and role of the shell capsule type.
2006
For colonic delivery, pectin beads obtained by ionotropic gelation method have been already reported as an interesting approach. This study investigated the influence of the cross-linking agent (calcium or zinc) and the type of shell capsule used (classical or enteric capsules) on pectin beads properties and on their performance to target the colon (in vitro dissolution studies with subsequent pH change to mimic overall gastro-intestinal tract). Zinc pectinate beads seemed to be relatively similar to calcium's ones in morphological point, except on the surface aspect. When beads were introduced in classical hard capsules, ketoprofen release was not significantly different between CPG and ZP…
Effects of different cellulose derivatives on drug release mechanism studied at a preformulation stage
2003
As a matter of fact, in vitro dissolution is well known to be the method of choice for the pharmaceutical industry to develop effective medicines. However, many experiments must be performed all along a new product life and they represent an overcharge of work for researchers. The purpose of this paper was to assess the relevance of new parameters obtained during preformulation stage by Nuclear Magnetic Resonance (NMR) experiments to better understand drug release mechanism. This study was carried out with three cellulose derivatives currently used as carrier matrices (Microcrystalline cellulose (MCC), Hydroxypropylmethyl cellulose (HPMC) and Ethyl cellulose (EC)). Granules and tablets were…
Thermal analyses of commercial magnesium stearate pseudopolymorphs
2005
Abstract Two commercial magnesium stearate powders in two well-characterised structural states are investigated using DSC and coupled TGA–DTA under dry nitrogen flow. They consist of either a mixture of crystalline hydrates or a poorly crystallised so-called anhydrate. Following the degassing of unbound water, 1 or 3 weight-loss peaks are observed below about 100 °C, each associated with one heat loss peak at the same temperature. The present results and a review of graphical data from literature show that the so-called anhydrate always contains a significant amount of water. At the beginning of the dehydration process, the heat loss is the same as the standard heat of vaporisation of water…
Influence of drug polarity upon the solid-state structure and release properties of self-emulsifying drug delivery systems in relation with water aff…
2009
To overcome low oral bioavailability of poorly water-soluble drugs, self-emulsifying drug delivery systems (SEDDS) have been noted as a promising strategy. However, incorporation of drugs into SEDDS composed of Gelucire44/14 could induce interactions not yet well understood. The aim of this study was to investigate the influence of drug polarity upon the solid-state structure of SEDDS formulation, particularly in terms of wettability, thermal behaviour and microscopic aspects and their effect upon the release properties of the SEDDS. Model drugs were naproxen and sodium naproxen (10% w/w), two drugs with similar chemical structure but different water solubilities. Both drugs had an effect o…
Influence of cryogenic grinding on properties of a self-emulsifying formulation
2003
Abstract Recently, self-emulsifying drug delivery systems (SEDDS) have been developed as a method to deliver lipophilic drugs. Gelucire® 44/14 is an excipient, from the lauroyl macrogolglycerides family, producing a fine oil-in-water emulsion when introduced into an aqueous phase under gentle agitation as SEDDS, improving thereby solubility of poorly water-soluble drugs and their bioavailability. The aims of this study were to process Gelucire® 44/14 into a powder by cryogenic grinding to produce solid oral dosage forms and to investigate influence of this process on different properties of a formulation made of Gelucire® 44/14 and ketoprofen (90/10). Cryogenic grinding produced Gelucire® 4…
Comparative study of the lubricant performance of Compritol 888 ATO either used by blending or by hot melt coating.
2003
Compritol 888 ATO is used as a lubricant in oral solid dosage formulations. It can also be used as a hot melt coating agent sprayed onto a powder. In this study, we compare the lubricant performance of Compritol 888 ATO either used by classical blending or by hot melt coating onto Lactopress by compression tests. In physical mix, the Compritol concentration does not affect the compressibility. The same compressibility is obtained with lactose coated by 0.5 or 1% of Compritol, but a higher compressibility can be observed with 2 and 3%. Cohesiveness of lactose depends on the process: hot melt coating induces a decrease of tablet tensile strength. In terms of forces transmission during compres…
Study of Morphology of Reactive Dissolution Interface Using Fractal Geometry
1996
J. Pharm. Sci. ISI Document Delivery No.: VF662 Times Cited: 7 Cited Reference Count: 15 Tromelin, A Gnanou, JC Andres, C Pourcelot, Y Chaillot, B; International audience; The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q(0))(DR/3) and -d Q/dt = K' R(DR-3) using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways of calculation allows proposal of the hypothesis that dissolution begins on a specific population of reactive sites and probably promotes the formation of microporous volumes or cracks.
Assessing the particle size of a broadly dispersed powder by complementary techniques
1998
The experimental determination of reliable particle size distribution curves and statistical parameters of broad distributions is known to be a difficult task. This problem is addressed here in an attempt to characterize the granularity of three distinct batches of a pharmaceutical powder (fenofibrate from Fournier Laboratories). The methodology consists in comparing the results, expressed in terms of surface based mean diameter, as obtained by three complementary techniques, namely optical microscopy image analysis, laser light low angle diffraction and surface area measurement by krypton physisorption. These techniques are applied in parallel to the material of interest and to a certified…
Influence of the parameters molecular structure and granularity on the compactibility of a powder
1995
Drug Dev. Ind. Pharm. ISI Document Delivery No.: RP128 Times Cited: 3 Cited Reference Count: 14 Andres, c ndiaye, a thomas, c tromelin, a chaillot, b pourcelot, y; International audience; The aim of this study was to determine whether it is possible to obtain better characterization of materials in order to find out if these one are suitable in Quality Assurance for direct tableting. We tried to show that a methodological approach combining chemical, physical and technological aspects could control the direct compression process. We chose orthoboric acid as a study model for the direct compression. From a chemical point of view, our findings show only one crystalline molecular structure (RX…
Colon-specific drug delivery: Influence of solution reticulation properties upon pectin beads performance.
2006
In this study, pectinate gel beads were produced by ionotropic gelation method with different solutions of cross-linking agents and ketoprofen was entrapped as model drug. The influence of these formulation parameters was investigated upon bead properties and upon their performance to target the colon. Zinc pectinate beads obtained with 10% of counter-ions solution at pH 1.6 exhibited the strongest gel network due to "egg-box" dimmer formation helped by hydrogen bonding. Furthermore the gel network formed at low pH was arranged in a compact three-fold conformation. Thus, this matrix structure in enteric capsules induced the lowest drug release in the upper gastro-intestinal tract (pH 1.2 fo…
Performance of Multilayered Particles: Influence of a Thin Cushioning Layer
2005
Nowadays, oral dosage forms with controlled release kinetics have known an increasing interest. The polymer coating of drug-loaded particles is one of the most common methods used for controlling drug delivery. Such multilayered particles could be either filled into capsules or compressed into tablets for their oral administration. However, many studies have noticed that coating films are damaged during the compression process, leading to significant changes in drug release profiles. The aims of this study were to investigate the effects of a thin cushioning layer [made of HydroxyPropylMethyl Cellulose (HPMC)] applied on coated theophylline particles upon particle characteristics, tablet pr…
Preformulation: Effect of Moisture Content on Microcrystalline Cellulose (Avicel PH-302) and Its Consequences on Packing Performances
1999
This study evaluates the influence of moisture content on the packing performances of a new grade of microcrystalline cellulose (MCC) (Avicel PH-302) either by classical method or by an unconventional compression technique (constant volume reduction of powder bed). An increase in moisture content decreases the apparent density of the powder bed, resulting from interparticulate friction enhancement. This modification of apparent density seems to be the main effect caused by the presence of humidity, which explains the variations of compression properties, like an increase of powder plasticity generally observed in the experimental conditions.
Affinity scale between a carrier and a drug in DPI studied by atomic force microscopy.
2002
The dry powder inhalers (DPIs) consist, in the most cases, of ordered mixture where the particles adhesion results of interactions between the drug and the carrier. Generally, one step of production process is the micronization of the drug particles in order to reduce the size for ordered mixing optimization. But this operation is known to partially create an amorphous surface. In this case, surrounding storage conditions, like relative humidity (RH), are able to modify the percentage of amorphous drug surface. The aim of this study was to investigate surface reactivity, surface energy and direct force measurements by atomic force microscopy (AFM) between lactose (carrier) and zanamivir (dr…
Relationship between particle size and dissolution rate of bulk powders and sieving characterized fractions of two qualities of orthoboric acid
1996
Drug Dev. Ind. Pharm. ISI Document Delivery No.: VN279 Times Cited: 1 Cited Reference Count: 22 Tromelin, A Habillon, S Andres, C Pourcelot, Y Chaillot, B; International audience; We have carried out a study of the particle size distribution and aqueous dissolution rate of two commercially available qualities of orthoboric acid, labeled ''crystal'' (ABC) and ''powder'' (ABP). In a previous work, we have shown that the two commercial qualities of orthoboric acid chosen as model compound (''powder'' and ''crystal'') are related to the same crystal network in spite of their different names. However, these two qualities have very different size particle distributions, as previously determined b…
Application of fractal geometry to dissolution kinetic study of a sweetener excipient
2001
Abstract In the context of relationship study between dissolution kinetic and particle morphology using the fractal geometry tool, we use a commercially available quality of saccharin powder. The characterization of molecular feature and image analysis study allows us to conclude to the statistic self-similarity of particles of four sieved particles size fractions, permitting the fractal approach. Calculation of reactive fractal dimension is performed using two forms of mass transfer equation: −d Q /d t = kQ D R /3 Δ C and −d Q /d t = k′R D R −3 Δ C , with Δ C ={ C f /[ln C s /( C s − C f )]}. Based on comparison of the surface fractal dimension D S on the two values of reactive fractal di…
Formation des agrégats à partir d'une phase cristalline d'acide orthoborique. Intérêt pour la technologie des poudres pharmaceutiques
1994
National audience
Etude de la morphologie de l'interface reactive de dissolution en utilisant le concept de géométrie fractale
1995
National audience
Use of fractal geometry to dissolution study of a sweetener excipient
2002
International audience
Aptitude à la comprimabilité : structure moléculaire - état particulaire
1994
International audience