Abstract: The present invention relates to an efficient and environmentally friendly process for preparing (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethylpyrrolidinium bromide with high yield and purity suitable for industrial scale applications.

Abstract: This invention relates to a an orally disintegrating tablet obtainable by direct compression of a dry powdered mixture, said mixture comprising up to 15% by weight of calcium silicate, at least 50% of a diluent, a disintegrant agent and an active ingredient. It also relates to a process for preparing the tablets by homogeneous blending the specific excipients in powder form and subsequent direct compression of the mixture. Said tablets disintegrate quickly in the cavity of the mouth, in particular in less than 15 seconds.

Abstract: A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 ?m or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60° C.; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.

Abstract: New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterized by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.

Abstract: A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 ?m or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60° C.; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.

Abstract: New polymorphic form of a long-acting beta-2 adrenoceptor agonist A new polymorphic form of arformoterol tartrate, designated as form D, is provided and which is characterised by at least one of the following: (i) a powder X-ray diffraction pattern having peaks at approximately 6.8, 13.3, 13.6, 3.8, 14.1, 18.2, 18.7, 20.0±0.2 degrees two theta; or (ii) a DSC thermogram showing an endothermic peak with an onset at approximately 19-120° C., and a maximum at approximately 129-131° C., followed by an exothermic peak with a maximum at approximately 137-138° C.; wherein the DSC thermogram of form D has a further endothermic peak with an onset at approximately 168-170° C.1 Processes for preparing the new polymorphic form, uses thereof and intermediates for the preparation thereof, are also provided.

Abstract: The invention relates to a solid formulation for the oral administration of olanzapine that comprises a core of anhydrous olanzapine Form I or a pharmaceutically acceptable salt thereof and, optionally, pharmaceutically acceptable excipients, said core being coated with a functional polymer that acts as filmogenic agent. The method for obtaining it comprises: i) providing anhydrous olanzapine Form I or a salt thereof and, optionally, pharmaceutically acceptable excipients in solid form; ii) providing a functional polymer that acts as filmogenic agent; iii) preparing a dispersion of said functional polymer in an aqueous medium,—and applying the dispersion obtained in step iii) onto the solid form of step i).

Abstract: The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.

Abstract: The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.

Abstract: A stable micronised monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 ?m. Processes for preparing the stable micronised monoclinic form of asenapine maleate are also described. Formula (I).

Abstract: The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.

Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).

Abstract: The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.

Abstract: The present invention refers to an improved method for the preparation of compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid substantially free of its 3H-I isomer. The invention also refers to the use of said intermediate for the preparation of Rufinamide and for obtaining a new polymorphic form of Rufinamide, designed as Form R-5. The invention also refers to said new polymorph of Rufinamide, and to the composition containing it and its use as medicament. The new polymorph of Rufinamide shows good stability and appropriate physico-chemical properties for its manipulation on industrial scale. Polymorph Form R-5 will be suitable to use as pharmaceutical for the treatment of convulsions, especially for the treatment of epilepsy.

Abstract: The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.

Abstract: The present invention relates to pharmaceutical compositions and formulations for the oral administration of Irbesartan, one of its pharmaceutically acceptable salts or its polymorphs, optionally combined with a diuretic and to a process for the manufacture of said composition.

Abstract: This invention relates to a an orally disintegrating tablet obtainable by direct compression of a dry powdered mixture, said mixture comprising up to 15% by weight of calcium silicate, at least 50% of a diluent, a disintegrant agent and an active ingredient. It also relates to a process for preparing the tablets by homogeneous blending the specific excipients in powder form and subsequent direct compression of the mixture. Said tablets disintegrate quickly in the cavity of the mouth, in particular in less than 15 seconds.

Abstract: The present invention relates to a composition comprising a pharmaceutically acceptable salt of Clopidogel and isomalt as a diluent, to the use of said composition in the elaboration of an oral pharmaceutical formulation, as well as to an oral pharmaceutical formulation comprising said composition.

Abstract: The present invention refers to a solid pharmaceutical composition of entacapone, levodopa and carbidopa or pharmaceutically acceptable salts thereof characterized in that entacapone is in the form of granules and it is added separately to levodopa and carbidopa. In addition, this invention provides the process for its preparation.

Abstract: The present invention relates to pharmaceutical compositions and formulations for the oral administration of Irbesartan, one of its pharmaceutically acceptable salts or its polymorphs, optionally combined with a diuretic and to a process for the manufacture of said composition.