Alliance Pharmaceutical Corp.

Novartis Ag

Produits Chimiques Ugine Kuhlmann

Other

Application Et Transferts De Technologies Avancees

Jean G Riess

Leila Zarif

Bernard Pucci

Marie-Pierre Krafft

Andre A Pavia

Luis A Dellamary

Thomas E Tarara

Ernest George Schutt

Jeffry G Weers

Pierre Vierling

Jacques Greiner

Maurice Le Blanc

Camille Guedj

Alain Milius

Nicholas Simon Faithfull

Peter E Keipert

Duane J Roth

Frederic Guillod

Thomas F Zuck

Francois Jeanneaux

Nathalie Garelli

Sylvie Gaentzler

Andre Lantz

Aime Cambon

Stephen F Flaim

Leo A Trevino

Francoise Giulieri

Georges Santini

Raphael Pastor

Michele Postel

Brigitte Charpiot

Claude Giovannoni

Luis Sole-Violan

Alexandre Manfredi

Chantal Cornelus

Catherine Santaella

Veronique Sanches

Phospholipid based powders for drug delivery applications are disclosed. The powders comprise a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Phospholipid-based powders for drug delivery

Phospholipid based powders for drug delivery applications are disclosed. The powders may include a polyvalent cation in an amount effective to increase the gel-to-liquid crystal transition temperature of the particle compared to particles without the polyvalent cation. The powders are hollow and porous and are preferably administered via inhalation.

Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature (T) of at least 20&#xb0; C. above the recommended storage temperature (Tst) for drug delivery.

Stable metal ion-lipid powdered pharmaceutical compositions for drug delivery and methods of use

Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature Tof at least 20&#xb0; C. above the recommended storage temperature (Tst) for drug delivery.

Preparations comprising a fluorocarbon or highly fluorinated compound and a lipophilic/fluorophilic organic compound, and their uses

Amphiphilic fluorine derivatives with telomeric structures; preparation procedure and biomedical applications

Multiple emulsions comprising a discontinuous emulsified phase incorporating a highly polar liquid, a second component selected from the group consisting of fluorocarbons and hydrocarbons and a continuous hydrophobic phase are disclosed. In preferred embodiments, the hydrophobic phase may comprise a fluorocarbon or hydrocarbon. Additionally, the stable multiple emulsions of the present invention may further incorporate a bioactive agent and are particularly suitable for drug delivery including pulmonary drug delivery.

Multiple emulsions comprising a hydrophobic continuous phase

Microstructures formed from fluorinated amphiphiles and mixed fluorinated and non-fluorinated amphiphiles and having the geometry of tubules, helixes and fibers and methods for preparing them. Tubular forms are capable of encapsulating or incorporating bioactive agents or other useful substances for controlled release in vivo.

Elongated microstructures from perfluoroalkylated amphiphiles

Stable reverse water-in-fluorocarbon emulsions and water-in-fluorocarbon-in-water multiple emulsions comprising the reverse fluorocarbon emulsions. The reverse emulsions comprise a continuous phase which is a highly fluorinated or perfluorinated compound, a discontinuous aqueous phase and a fluorinated surfactant or mixture of surfactants. The multiple emulsions comprise an aqueous continuous phase and a discontinuous phase comprising globules formed of aqueous droplets dispersed into a highly fluorinated or perfluorinated compound. The emulsions can contain pharmacologically active agents, and are particularly suitable for pulmonary drug delivery.

Stable reverse and multiple fluorocarbon emulsions

New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1. These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Amphiphilic fluorine derivatives with telomeric structures; preparation

Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;

Perfluoroalkylated amphiphilic phosphorus compounds: preparation and

Novel hydrocarbon oil/fluorochemical preparations and methods for their use are provided. The preparations, which preferably comprise a fluorophilic dispersing agent, may be in the form of hydrocarbon oil-in-fluorochemical dispersions or in the form of a multiple emulsion comprising a polar liquid continuous phase and are particularly useful for administering bioactive agents. In particular the preparations of the present invention may be used to control the bioavailability and improve the efficacy of lipophilic bioactive agents having limited solubility in an aqueous physiological environment.

Hydrocarbon oil/fluorochemical preparations and methods of use

Biocompatible fluorocarbon emulsions are utilized to inhibit the removal of endogenously produced nitric oxide from the bloodstream, and to thereby inhibit vascular stenosis, vasoconstriction, and any other physiological condition or disorder arising in whole or in part from a deficiency of endogenous nitric oxide.

Liquid fluorocarbon emulsion as a vascular nitric oxide reservoir

Fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1. These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Amphiphilic fluorine derivatives with telomeric structures

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Falicon, France

Jean G Riess