Pierre Fabre Medicament

Galderma Research & Development

Bernard Freiss

Hubert Lochard

Florence Marciacq

Martial Sauceau

Christophe Joussot-Dubien

Jacques Fages

Jean-Jacques Letourneau

Florence Marciaçq

Mathieu Soulayres

The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, using the following successive stages: (a) bringing one or several active substances into contact with one or several host molecules; (b) initiating a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in (a) in a static mode in the presence of one or several diffusing agents; (c) recovering the active substance-host molecule molecular complex formed; (d) adding and mixing an interaction agent with the active substance-host molecule molecular complex; (e) recovering the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound obtained by the method, particularly a piroxicam-cyclodextrin-arginine compound.

Inclusion complexes containing piroxicam, a cyclodextrin and arginine

The present invention relates to a batch method for impregnating a nonporous polymer pharmaceutical carrier with an active substance, characterized in that said method includes the following consecutive steps: a) mixing the active substance and the nonporous polymer pharmaceutical carrier, the pharmaceutical carrier being in a solid form and insoluble in supercritical COand not being non-crosslinked polyvinylpyrrolidone; b) performing a step of molecular diffusion in the absence of water by contacting, in a static mode without agitation, the mixture obtained in step a) with supercritical COat a pressure of 80 to 170 bars, at a temperature of 31 to 90&#xb0; C. for 1 to 6 hours; c) recovering the polymer pharmaceutical carrier impregnated with the active substance obtained in step b), the impregnated pharmaceutical carrier being nonporous and being in a solid form and the active substance being in an amorphous form, the method being implemented in the absence of an additional solvent. The invention further relates to a polymer pharmaceutical carrier in a nonporous solid form impregnated with an active substance characterized in that said carrier can be obtained by the method according to the present invention, in that the active substance is in an amorphous form and is water-soluble, and in that the polymer pharmaceutical carrier is not non-crosslinked polyvinylpyrrolidone and is insoluble in supercritical CO.

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The invention relates to a method for the preparation of soluble molecular complexes, comprising one or more active substances which are poorly-soluble in an aqueous medium, included within one or more host molecules, characterized in comprising the following steps: (a) bringing one or more active substances into contact with one or more host molecules, (b) carrying out a molecular diffusion step by bringing a dense fluid into contact, under pressure, with the mixture obtained in (a), in static mode, in the presence of one or more diffusion agents and (c) recovery of the molecular complex thus formed.

Method for the preparation of molecular complexes

A method for preparing molecular complexes between Adapalene and cyclodextrins using the technology of dense fluids under pressure, especially that of CO2 is described.

Method for preparing molecular complexes between adapalene and cyclodextrins

The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, characterised in that it comprises the following succesive stages: (a) one or several active substances are brought into contact with one or several host molecules; (b) initiation of a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in stage (a) in a static mode in the presence of one or several diffusing agents; (c) recovery of the active substance- host molecule molecular complex thus formed; (d) initiation of a stage wherein an interaction agent is added to and mixed with the active substance host molecule molecular complex; (e) recovery of the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound which can be obtained by said method, particularly a piroxicam-cyclodextrin-arginine compound.

Inclusion complexes containing an active substance, a cyclodextrin and an agent for interaction

The present invention relates to a continuous process of DHA enrichment of a solution of fatty acids or derivatives thereof comprising less than 50% of DHA relative to the total fatty acids of the solution or to derivatives thereof, wherein the process comprises the steps of (a) simultaneous countercurrent injection, into a fractionation column, of the flow of the solution of fatty acids or of derivatives thereof and of a flow of supercritical COat a temperature of less than or equal to 70&#xb0; C. and at a pressure of between 100&#xd7;10Pa and 160&#xd7;10Pa, wherein the level of supercritical COis between 30 and 70, and (b) recovery of the residue comprising at least 50% of DHA relative to the total fatty acids of the residue or to derivatives thereof, wherein the DHA yield is greater than or equal to 60%.

DHA enrichment process

The present invention relates to a complex that includes mequitazine, a cyclodextrin, and an interaction agent wherein the rate of solubilization in water of complexed mequitazine, measured for a 2 g/l mixture of mequitazine in water at 35&#xb0; C. after 15 minutes of stirring, is greater than 50% at pH 9. The present invention also relates to a method of preparing the aforementioned complex and a pharmaceutical composition of which the complex is a part.

Complex containing mequitazine, a cyclodextrin and an interaction agent

The invention concerns a method for preparing compounds for interaction of an active substance hardly soluble in an aqueous medium with a porous support. The invention is characterized in that it comprises the following steps: (a) mixing the active substance generated by supercritical fluid and the specific amount of porous support; (b) carrying out a molecular diffusion step by contacting in static mode a supercritical fluid with the mixture obtained at step (a) for the time required to improve the dissolution in the aqueous medium of the mixture obtained at step (a); (c) washing the interactive compound obtained at step (b) with a supercritical fluid flow; (d) recuperating the particles of the interactive compound thus formed. The invention also concerns a compound obtainable by said method.

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Castres, France

Bernard Freiss