Abstract: A method for enlarging the particle size of crystalline microparticles of active substance by providing a first suspension prepared from crystalline microparticles of active substance with a first d50 value of 0.5-5 ?m, solvent and antisolvent for the active substance, wherein the solubility of the active substance in the solvent-antisolvent mixture of the first suspension is 0.001-0.5 wt. %, such that the average particle diameter (d50 value) at the end or the method is at least 0.03 ?m larger than the starting d50 value. The d50 values of a first batch can also serve to control the particle coarsening of a second batch. In addition, particles of fluticasone propionate having an average particle size d50 of 1.0-1.5 ?m and simultaneously a narrow particle size distribution with a span <1.35 and high crystallinity with an amorphous fraction of <0.5 wt. % can be prepared.

Abstract: A method and device for producing crystalline active ingredient particles. The active ingredient is crystallized from a supersaturated solution on the surface of particles of the active ingredient. A suspension of active ingredient particles is subjected to wet grinding in a supersaturated solution of the active ingredient in a first module. At least a part of the suspension is fed from the first module into the second module where it is cooled and simultaneously subjected to ultrasound. The suspension is fed back into the first module after cooling and being subjected to ultrasound. Active ingredient solution and optionally antisolvent are added to the suspension and active ingredient particles and liquid phase are extracted. A relative supersaturation of the active ingredient in the liquid phase of the suspension, relative to the entire liquid phase, is ?90%, and the extracted active ingredient particles comprise a mean particle size of 10-500 ?m.

Abstract: A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare are highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.

Abstract: An arrangement and a method for producing high-purity crystals, such as temperature-sensitive pharmaceutical agents, in a countercurrent crystallization process. The arrangement comprises a plurality of crystallizers, mother liquor lines, each of which has a shut-off valve, and crystallization product lines, each of which has a shut-off valve, so that a mother liquor flow can be generated which is directed from a crystallizer to the second-next crystallizer in the direction of decreasing purity, and a crystallization product flow can be generated which is directed from a to dissolved crystallization product that is about to crystallize to the next crystallizer in the direction of higher purity.

Abstract: A method and device for producing crystalline active ingredient particles. The active ingredient is crystallized from a supersaturated solution on the surface of particles of the active ingredient. A suspension of active ingredient particles is subjected to wet grinding in a supersaturated solution of the active ingredient in a first module. At least a part of the suspension is fed from the first module into the second module where it is cooled and simultaneously subjected to ultrasound. The suspension is fed back into the first module after cooling and being subjected to ultrasound. Active ingredient solution and optionally antisolvent are added to the suspension and active ingredient particles and liquid phase are extracted. A relative supersaturation of the active ingredient in the liquid phase of the suspension, relative to the entire liquid phase, is ?90%, and the extracted active ingredient particles comprise a mean particle size of 10-500 ?m.

Abstract: The present invention relates to a method for the reliable and reproducible preparation of 4-[17?-methoxy-17?-methoxymethyl-3-oxoestra-4,9-dien-11?-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

Abstract: The present invention relates to a method for the reliable and reproducible preparation of 4-[17?-methoxy-17?-methoxymethyl-3-oxoestra-4,9-dien-11?-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

Abstract: A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.

Abstract: An arrangement and a method for producing high-purity crystals, such as temperature-sensitive pharmaceutical agents, in a countercurrent crystallization process. The arrangement comprises a plurality of crystallizers, mother liquor lines, each of which has a shut-off valve, and crystallization product lines, each of which has a shut-off valve, so that a mother liquor flow can be generated which is directed from a crystallizer to the second-next crystallizer in the direction of decreasing purity, and a crystallization product flow can be generated which is directed from a to dissolved crystallization product that is about to crystallize to the next crystallizer in the direction of higher purity.

Abstract: The invention relates to novel solid body forms of mesoprogestin 11?-[4E-(hydroxyiminomethyl)-phenyl]-17?-methoxymethyl-17?-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.

Abstract: The present invention relates to a method for the reliable and reproducible preparation of 4-[17?-methoxy-17?-methoxymethyl-3-oxoestra-4,9-dien-11?-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

Abstract: The process for making crystals of a 11 ?-benzaldoxim-estra-4,9-diene derivative having an average particle size of from 3 ?m to 25 ?m and a maximum particle size of 100 ?m, includes subjecting a supersaturated solution containing a special 11?-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, In order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described and are part of the invention.

Abstract: The process for making steroid crystals having a predetermined average particle size of from 1 ?m to 25 ?m and a maximum particle size that does not exceed a predetermined maximum value of 100 ?m, includes subjecting a supersaturated solution containing a steroid to a wet milling by wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.

Abstract: The method of isolating an anhydrous etidronate disodium particulate includes preparing a liquid-liquid dispersion consisting of an aqueous-organic phase and an etidronate-disodium-salt-containing aqueous phase; adjusting a temperature of the liquid-liquid dispersion to between 0 and 30° C. and intensely agitating so that a coarse-particle fraction precipitates from the liquid-liquid dispersion, then drawing off a fine-particle suspension and allowing a fine-particle fraction to precipitate from it and filtering and drying the coarse particle fraction. In a preferred embodiment the fine-particle fraction is separated from the fine-particle suspension for recycling The resulting anhydrous etidronate disodium particulate has a grain size of from about 0.1 to 1 mm and a bulk density of 0.4 to 0.6 g/cm2 with good properties for pharmaceutical applications.

Abstract: The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.

Abstract: The invention relates to the isolation of etidronate disodium whereby

Abstract: The invention relates to novel solid body forms of mesoprogestin 11&bgr;-[4E-(hydroxyiminomethyl)-phenyl]-17&agr;-methoxymethyl-17&bgr;-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.

Abstract: The process for making crystals of a 11&bgr;-benzaldoxim-estra-4,9-diene derivative having a predetermined average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, includes subjecting a supersaturated solution containing a special 11&bgr;-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.

Abstract: The process for making steroid crystals having a predetermined average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, includes subjecting a supersaturated solution containing a steroid to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.

Abstract: The process for making crystals of a medicinally effective ingredient having a predetermined average particle size in a predetermined size range and a maximum particle size that does not exceed a predetermined maximum value, includes subjecting a supersaturated solution containing the medicinally effective ingredient to a wet milling by a wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.