Ciba Specialty Chemicals Corporation

Novartis Ag

Ciba-geigy Corporation

Basf Se Corporation

Andreas Burkhard

Martin Szelagiewicz

Claudia Marcolli

Paul Adriaan Van Der Schaaf

Josef Zelger

Robert Portmann

Urs Christoph Hofmeier

Walter Scherrer

Erwin Marti

Franz Schwarzenbach

Heinz Wolleb

Peter Rohringer

Annemarie Wolleb

Werner Schreiber

Hans-Jörg Kirner

Andre Geoffroy

Thomas Ehlis

Stefan Hari

Hans Jürg Kirner

Paul Van Der Schaaf

Serge Schroeder

Beat Freiermuth

Arnold Grubenmann

Bernard Schultz

Andr&eacute; Geoffroy

Karlheinz Franke

Regine Peter

André Geoffroy

The invention relates to dosage forms and formulations comprising the novel crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide, wherein crystal modification A is characterized by characteristic lines with interplanar spacings (d values) of 10.5 &#x212b;, 5.14 &#x212b;, 4.84 &#x212b;, 4.55 &#x212b;, 4.34 &#x212b;, 4.07 &#x212b;, 3.51 &#x212b;, 3.48 &#x212b;, 3.25 &#x212b;, 3.19 &#x212b;, 3.15 &#x212b;, 3.07 &#x212b;, and 2.81 &#x212b;, determined by means of an X-ray powder pattern. Dosage forms of crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide may be for oral or parenteral administration, in the form of a solid or liquid, and in a dosage range of 20 mg to less than 500 mg. Solid dosage forms comprise a tablet or capsule, and further comprise a pharmaceutically-acceptable carrier and film-coat.

Crystal modification A of 1-(2,6-difluorobenzyI)-1 H-1,2,3-triazole-4-carboxamide and dosage forms and formulations thereof

The invention relates to the novel modifications B and C of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of the formula its use and pharmaceutical preparations comprising this crystal modifications.

Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1, 2,3-triazole-4-carboxamide

Sertraline hydrochloride polymorphic form II is conveniently prepared by adding hydrogen chloride to solution of sertraline free amine in a ketone. In preferred processes, the solution of sertraline free amine seeded with some crystals of polymorphic form II and/or the solution is heated before addition of the hydrogen chloride.

Polymorphic forms of sertraline hydrochloride

A crystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.

A cystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.

Crystalline forms of the (3R,5S)- and the (3S,5R)-enantiomers of fluvastatin, referred to as polymorphic Forms A, B1, B2, C, D and E, processes for the preparation of these crystalline forms and pharmaceutical compositions comprising them are disclosed.

Crystalline forms of Fluvastatin sodium

Crystal modification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide and its use as antiepileptic

Novel crystalline forms of Fluvastatin sodium hydrates were found, referred to hereinafter as polymorphic Forms C, D, E and F. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms, a process for the preparation of highly crystalline Fluvastatin sodium Form A, and pharmaceutical compositions comprising the crystalline forms.

Crystalline forms

Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide

The present invention provides a hydrate of the 4,4&prime;-di-triazinylamino-2,2&prime;-di-sulfostilbene compound having the formula:

Triazinylaminostilbene compounds

The present invention provides a hydrate of the 4,4'-di-triazinylamino-2,2'-di-sulfostilbene compound having the formula: ##STR1## in which M and M.sub.1 independently represent hydrogen, an alkaline-, an alkaline earth metal or ammonium, x is a number within the range of from 1 to 30, and the crystal form of the hydrate (I) being characterized by an X-ray diffraction pattern which is essentially as set out in the accompanying FIGS. 1 to 11; or a mixture containing one or more of the hydrates of the 4,4'-di-triazinylamino-2,2'-di-sulfostilbene compound having the formula (I); processes for the preparation of the new hydrates; and the use of the new hydrates for the preparation of concentrated aqueous formulations of fluorescent whitening agents.

There is provided a white crystal form of the compound having the formula: ##STR1## whose crystal form is characterised by an X-ray diffraction diagram which is essentially as shown in Table I, II or III. Also provided is a formulation comprising from 10 to 85% by weight of the white crystal form of compound having the formula (1) and from 90 to 15% by weight of a polyhydroxy compound, preferably glycerine.

Fluorescent whitening agent

The present invention relates to novel hydrates of the disodium salt or dipotassium salt of 4,4'-bis(2-sulfostyryl)biphenyl characterized by their water of hydration content, to the crystal forms associated therewith, characterized by their X-ray diffraction pattern, to processes for the preparation, and to their use for the preparation of concentrated formulations of fluorescent whitening agents.

Hydrates of the disodium salt or dipotassium salt of

Mixed crystals of at least two different compounds of formula I ##STR1## wherein R is --CH.sub.3, phenyl, --COOCH.sub.3, --COOCH.sub.3, --COOC.sub.2 H.sub.5, --NHCO--C.sub.1 -C.sub.4 alkyl or --CONH--C.sub.1 -C.sub.4 alkyl, M.sup.+ and M.sub.1.sup.+ are each independently of the other an alkali metal cation, an alkaline earth metal cation or a heavy metal cation or NH.sub.4.sup.+ ; wherein X, Y, X' and Y' are each independently hydrogen, halogen, --CH.sub.3, --C.sub.2 H.sub.5, --OCH.sub.3, --OC.sub.2 H.sub.5, --NO.sub.2 or the group of formula --NHCO--C.sub.1 -C.sub.4 alkyl, wherein at least two of the cations M.sup.+ and M.sub.1.sup.+ in the compounds forming the mixed crystals of formula I are different and the X-ray diffraction patterns of the mixed crystals differ from the X-ray diffraction patterns of the individual components and of their sum. Such mixed crystals are most suitable as pigments for coloring high molecular organic material and are distinguished in particular by surprisingly high color strength and pure shade.

Growing community of inventors

Basel, Switzerland

Andreas Burkhard