GALENIC APPLICATIONS OF SELF-EMULSIFYING MIXTURES OF LIPIDIC EXCIPIENTS
First Claim
Patent Images
1. A method of enhancing the absorption of an active principle by a mechanism involving inhibition of efflux pumps, comprising orally administering a pharmaceutical composition, wherein the pharmaceutical composition comprises:
- a self-emulsifying mixture, said self-emulsifying mixture comprisingone or more lipid excipients in an amount of 40 to 85%, the one or more lipid excipients being selected from the group consisting of glyceryl linoleate, glyceryl mono-oleate, glyceryl oleate/linoleate, glyceryl laurate, polyglyceryl-3 oleate, soybean oil, capric/caprylic/lauric acid triglycerides, and oleic acid,one or more surfactants in an amount of 15 to 50%, andoptionally one or more cosurfactants; and
one or more active principles.
1 Assignment
0 Petitions
Accused Products
Abstract
A subject-matter of the invention is novel pharmaceutical formulations which make it possible to improve the intestinal absorption of orally administered active principles, their process of preparation and the application of lipid excipients in combination with one or more surfactants and one or more cosurfactants for inhibiting efflux pumps.
-
Citations
38 Claims
-
1. A method of enhancing the absorption of an active principle by a mechanism involving inhibition of efflux pumps, comprising orally administering a pharmaceutical composition, wherein the pharmaceutical composition comprises:
a self-emulsifying mixture, said self-emulsifying mixture comprising one or more lipid excipients in an amount of 40 to 85%, the one or more lipid excipients being selected from the group consisting of glyceryl linoleate, glyceryl mono-oleate, glyceryl oleate/linoleate, glyceryl laurate, polyglyceryl-3 oleate, soybean oil, capric/caprylic/lauric acid triglycerides, and oleic acid, one or more surfactants in an amount of 15 to 50%, and optionally one or more cosurfactants; and one or more active principles. - View Dependent Claims (2, 3, 4, 5, 6, 7, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 36)
-
8. (canceled)
-
9. (canceled)
-
24. Pharmaceutical composition comprising:
-
an active principle; a self-emulsifying mixture (SEEDS) of one or more lipid excipients in an amount of 40 to 85%, the one or more lipid excipients being selected from the group consisting of glyceryl linoleate, glyceryl mono-oleate, glyceryl oleate/linoleate, glyceryl laurate, polyglyceryl-3 oleate, soybean oil, capric/caprylic/lauric acid triglycerides, and oleic acid; and one or more surfactants in an amount of 15 to 50%; and optionally comprising one or more co-surfactants. - View Dependent Claims (25, 26, 27, 28, 29, 30, 32, 33, 37, 38)
-
-
31. (canceled)
-
34. A method for inhibiting to P-glycoprotein of cancer cells and to enhance the cellular penetration of the active principle into the tumour cells comprising administering by injection an injectable solution that inhibits P-glycoprotein of cancer cells and enhances the cellular penetration of the active principle into the tumour cells;
wherein the injection solution comprises a self-emulsifying mixture comprising one or more lipid excipients, one or more surfactants, and, optionally, one or more cosurfactants.
-
35. Process for the preparation of self-emulsifying mixtures (SEEDS), the self emulsifying mixtures comprising:
-
one or more lipid excipients in an amount of 40 to 85%, the one or more lipid excipients being selected from the group consisting of glyceryl linoleate, glyceryl mono-oleate, glyceryl oleate/linoleate, glyceryl laurate, polyglyceryl-3 oleate, soybean oil, capric/caprylic/lauric acid triglycerides, and oleic acid, one or more surfactants in an amount of 15 to 50%, and optionally one or more cosurfactants, the process comprising; adding of the lipid excipient, of the surfactant and, if appropriate, of the cosurfactant, semisolid excipients requiring preheating; mixing by stirring until a homogeneous solution is obtained; dissolving the active principle in a solvent, such as DMSO, glycofurol or one of the excipients participating in the composition of the emulsions and of the microemulsions; adding the dissolved active principle to the mixture of lipid excipient, surfactant and, if appropriate, cosurfactant; if appropriate, performing heating or ultrasound treatment until a homogeneous solution is obtained.
-
Specification