Camurus Ab

Camarus Ab

Goddard, Christopher Robert

Fredrik Joabsson

Fredrik Tiberg

Markus Johnsson

Krister Thuresson

Ian Harwigsson

Markus Johansson

Margareta Linden

Catalin Nistor

Andreas Norlin

The present invention relates to formulation precursors (pre-formulations) for the in situ generation of compositions for the controlled release of the salts of peptide active agents, including somatostatin analogues. The invention also relates to pre-formulations of amphiphilic components and at least one salt of a peptide active agent (e.g., somatostatin analogue) for parenteral application.

Peptide slow-release formulations

The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of:

Topical bioadhesive formulations

The present invention relates to compositions forming a low viscosity mixture of: a) at least one diacyl glycerol; b) at least one phosphatidyl choline; c) at least one oxygen containing organic solvent; d) at least one GnRH analog; Wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, pre-filled administration devices and kits containing the formulations.

GnRH analogue formulations

The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

The present invention provides a method for the production of amphiphile particles having incorporated therein at least one active agent. The method comprises forming a dispersion of particles comprising at least one amphiphilic structuring agent in a solution of at least one active agent, heating said dispersion to an elevated temperature, followed by cooling to around ambient temperature. The loading provided thereby is typically at least 130% of the loading provided by equilibration of the particles in a solution of active agent. The invention also provides corresponding amphiphile particles.

Method for loading amphiphile particles with active agents

The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Pre-formulations of a low viscosity mixture containing: a) at least one diacyl glycerol; b) at least one phosphatidyl choline; c) at least one oxygen containing organic solvent; d) at least one somatostatin analog are described. The pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The pre-formulations are useful for generating depot composition far the controlled release of somatostatin analogs such as octreotide. Methods of treatment comprising the administration of such formulations are also provided, as are pre-filled administration devices and kits containing the formulations.

Somatostatin analogue formulations

The present invention relates to compositions containing at least one cationic peptide active agent, at least one neutral structure forming amphiphile, at least one anionic structure forming amphiphile and optionally at least one solvent wherein the composition is in the form of a non-lamellar phase structure and/or forms a nonlamellar phase structure on exposure to body fluids. The invention also relates to methods for protecting peptides from enzymic degredation in vivo and to compositions in which the peptide active agent is so protected.

Compositions of lipids and cationic peptides

The present invention relates to compositions forming a low viscosity mixture of: a) at least one neutral diacyl lipid, such as a diacyl glycerol; b) at least one phospholipid, such as a phosphatidyl choline; c) at least one biotolerable solvent, such as an oxygen containing solvent; d) at least one GLP-1 analogue; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, especially in treating diabetes, and to pre-filled administration devices and kits containing the formulations.

Glp-1 analogue formulations

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Lipid depot formulations

The present invention relates to compositions containing a) at least one monoacyl lipid; b) at least one diacyl glycerol and/or tochopherol; and c) at least one fragmentation agent; and optionally an active agent. The compositions are capable of self-dispersing to provide colloidal non-lamellar particles upon contact with an aqueous fluid. The invention additionally provides a method for forming non-lamellar particles from such compositions, and pharmaceutical formulations containing the compositions, plus non-lamellar particles formable from the compositions.

Compositions forming non-lamellar dispersions

Liquid depot formulations

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of:

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Lund, Sweden

Fredrik Joabsson