Abstract: The present invention provides a formulation comprising a lipid matrix; at least one thiolated antioxidant; at least one bioactive agent; and optionally at least one chelating agent. The bioactive agent may be a gonadotrophin-releasing hormone (GnRH) agonist; a gonadotrophin-releasing hormone (GnRH) antagonist; a luthenizing hormone releasing hormone (LHRH); and/or a luthenizing hormone releasing hormone (LHRH) related peptide.

Abstract: The present invention relates to pre-formulations comprising: a) at least one di-acyl lipid; b) at least one phospholipid; c) at least one biocompatible, organic solvent; d) an alkyl ammonium EDTA salt; and e) at least one somatostatin receptor agonist; wherein the pre-formulation has a water content in the range of 0 to 1.0 wt %. The invention further relates to methods of treatment comprising administration of such pre-formulations, to pre-filled administration devices and kits containing the formulations, to the use of an alkylammonium EDTA salt to reduce the decomposition of the lipid components and/or any active agent contained within the pre-formulation.

Abstract: The present invention relates to an injectable pre-formulation comprising: a) at least one of a mono-, di-, or tri-acyl lipid and/or a tocopherol; b) optionally at least one phospholipid; c) at least one biocompatible, organic solvent; and d) at least one prostacyclin analogue or a salt thereof; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. Such compositions may additionally comprise polar co-solvents. Methods of treatment, particularly for management of pulmonary artery hypertension (PAH), severe PAH, Raynard's disease ischemia and related conditions are provided, as well as corresponding uses of the compositions. Administration devices comprising the formulations and kits comprising the devices are also provided.

Abstract: A composition for the delayed delivery of a peptide active agent comprising: i) a salt of said peptide active agent comprising at least one positively charged peptide ion and at least one negatively charged counter-ion ii) a sustained-release delivery vehicle. Wherein said at last one negatively charged counter-ion is a halide ion, preferably a chloride or bromide ion.

Abstract: The present invention relates to an injectable pre-formulation comprising a low viscosity mixture of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one oxygen containing organic solvent; d) at least one 5HT3 antagonist; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. Such compositions may additionally comprise polar solvents and/or further active agents such as opioid agonists and/or antagonists. Methods of treatment, particularly for management of nausea and vomiting such as for post-operative nausea and vomiting and/or therapy induced nausea and vomiting are provided, as well as corresponding uses of the compositions. Administration devices comprising the formulations and kits comprising the devices are also provided.

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 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.

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: A depot precursor formulation comprising: a) a controlled-release matrix; b) at least oxygen containing organic solvent; c) at least 12% by weigh of at least one active agent selected from buprenorphine and salts thereof, calculated as buprenorphine free base. Corresponding depot compositions and methods of treatment in pain management, by opioid maintenance and related methods are provided.

Abstract: 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 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, pre-filled administration devices and kits containing the formulations.

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 provides a formulation comprising a lipid matrix; at least one thiolated antioxidant; at least one bioactive agent; and optionally at least one chelating agent. The bioactive agent may be a gonadotrophin-releasing hormone (GnRH) agonist; a gonadotrophin-releasing hormone (GnRH) antagonist; a luthenizing hormone releasing hormone (LHRH); and/or a luthenizing hormone releasing hormone (LHRH) related peptide.

Abstract: 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.

Abstract: The present invention provides a formulation comprising: i) a lipid matrix; ii) at least one thiolated antioxidant; iii) optionally at least one bioactive agent; and iv) optionally at least one chelating agent.

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. at least one diacyl glycerol and/or at least one tocopherol; b. at least one phospholipid component comprising phospholipids having i. polar head groups comprising more than 50% phosphatidyl ethanolamine, and ii. two acyl chains each independently having 16 to 20 carbons wherein at least one acyl chain has at least one unsaturation in the carbon chain, and there are no more than four unsaturations over two carbon chains; c. at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein optionally 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 non-lamellar liquid crystalline phase structure upon contact with an aqueous fluid.

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 provides a method for forming a dispersion comprising non-lamellar amphiphile particles having improved phase behavior, particle size distribution and/or storage stability, said method comprising forming a dispersion of lamellar and optionally non-lamellar particles comprising at least one structuring agent in a polar solvent, heating said particles to an elevated temperature, followed by cooling, wherein said heating is to a temperature and for a period sufficient to provide, after cooling, a measurable improvement in phase behavior, particle size distribution and/or storage stability.

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 stabilising 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 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.