An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations aprepitant is dissolved at high concentrations and remains dissolved and stable even over prolonged periods of time.

An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations aprepitant is dissolved at high concentrations and remains dissolved and stable even over prolonged periods of time.

The present invention relates to a controlled release sterile injectable formulation in the form of solution, suspension or sol-gel formulation for intramuscular or subcutaneous administration comprising a therapeutically effective amount of a neurokinin 1 receptor antagonist, in particular Aprepitant or Fosaprepitant or pharmaceutical acceptable salt, derivative or metabolite thereof. It also relates to a process for developing such formulations.

The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenypethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharm...

The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer namely 5-[2(S)-[1(RS)-[35-bis(trifluoromethyl)-phenypethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-34-dihydro-2H-124-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant a process for its preparation and to a pharmaceuti...

An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations aprepitant is dissolved at high concentrations and remains dissolved and stable even over prolonged periods of time.

An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations, aprepitant is dissolved at high concentrations and remains dissolved and stable, even over prolonged periods of time.

An aqueous stable and ready-to-use formulation of aprepitant is prepared. Especially preferred formulations comprise a synergistic combination of a co-solvent and a surfactant and may further include a secondary co-solvent. Among other advantages of contemplated formulations, aprepitant is dissolved at high concentrations and remains dissolved and stable, even over prolonged periods of time.

A molecule with neuro activities, especially 4-substituent-2-hydroxylmorpholine-3-one, as a new intermediate of neurokinin-1 receptor antagonist Aprepitant, and preparation method thereof.