Abstract: The present invention relates to a particulate composition containing; a) 5 to 90% of at least one phosphatidyl choline component b) 5 to 90% of at least one diacyl glycerol component, at least one tocopherol, or mixtures thereof, and c) 1 to 40% of at least one non-ionic stabilizing amphiphile, where all parts are by weight relative to the sum of the weights of a+b+c and where the composition contains particles of at least one non-lamellar phase structure or forms particles of at least one non-lamellar phase structure when contacted with an aqueous fluid. The invention additionally relates to pharmaceutical formulations containing such compositions, methods for their formation and methods of treatment comprising their administration.

Abstract: The present invention relates to compositions forming a low viscosity mixture of: a) 20-50 wt. % of at least one diacyl glycerol; b) 20-54 wt. % of at least one phosphatidyl choline (PC); c) 5-15 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) 1 to 20 wt. % polar solvent e) 5 to 150 mg/ml of at least one peptide somatostatin receptor agonist comprising pasireotide; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to compositions forming a low viscosity mixture of: a) 20-80 wt. % of at least one diacyl glycerol and/or a tocopherol; b) 20-80 wt. % of at least one phosphatidyl choline (PC); c) 5-20 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) up to 20 wt. % polar solvent e) at least one peptide active agent; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.

Abstract: A pharmaceutical composition comprising a pharmaceutically effective amount of a pharmaceutically active substance and a pharmaceutically acceptable carrier including a cationic excipient, wherein said cationic excipient is a labile ester of betaine and a lipophilic alcohol having at least one primary hydroxyl group. Also, the use of a labile ester of betaine and a lipophilic alcohol having at least a primary hydroxyl group as a cationic excipient in a carrier for a pharmaceutical composition comprising a pharmaceutically active substance.

Abstract: 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.

Abstract: 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.

Abstract: A high bioavailability opioid depot precursor formulation comprising: a) a controlled-release matrix; b) at least oxygen containing organic solvent; c) at least one active agent selected from buprenorphine and salts thereof. Typically such a precursor formulation will form a depot composition upon administration to the body of a subject.

Abstract: 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.

Abstract: 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.

Abstract: 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 opioid 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.

Abstract: The present invention relates to particulate compositions comprising at least 50% of dioleoyl phosphatidyl ethanolamine (DOPE) and 1 to 50% of Polysorbate 80 (P80). All parts are by weight relative to the sum of the weights of a+b and the compositions comprise non-lamellar particles or form non-lamellar particles when contacted with an aqueous fluid. The compositions have advantageous stability and low toxicity and the invention also relates to pharmaceutical compositions thereof.

Abstract: The present invention provides a particulate composition including; a) at least 50% of at least one structure forming amphiphile, b) 0 to 40% of at least one structure swelling amphiphile, and c) 2 to 20% of at least one dispersion stabilizing polymeric amphiphile, where all parts are by weight relative to the sum of the weights of a+b+c and wherein the composition comprises non-lamellar particles or forms non-lamellar particles when contacted with an aqueous fluid. Where component b) is 0% then component a) comprises at least two structure forming amphiphiles. The invention also provides pharmaceutical compositions of the compositions and kits containing the compositions for establishing a pharmaceutical formulation of an active agent.

Abstract: The present invention relates to compositions forming a low viscosity mixture of: i) a non-polymeric slow-release matrix ii) at least one biocompatible, (preferably oxygen containing) organic solvent; iii) at least one peptide active agent; and iv) at least one lipid soluble acid. 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.

Abstract: The present invention relates to formulations of a lipid based controlled-release matrix, a polyhydroxy component and a bioactive agent. Such formulation are useful in the delivery of the bioactive compounds. The invention also relates to the use of a polyhydroxy component for increasing the solubility of a bioactive compound, especially a peptide in a lipid-based controlled-release matrix.