Takeda Pharmaceutical Company Limited

Tadashi Urai

Hideo Hashimoto

Hiroki Ito

Muneo Nonomura

It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer.

Stable solid preparations

Provided is a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole showing an X-ray powder diffraction pattern having characteristic peaks at interplanar spacings (d) of 10.06&#xb1;0.2, 8.70&#xb1;0.2, 6.57&#xb1;0.2, 5.59&#xb1;0.2 and 4.00&#xb1;0.2 Angstroms. The present invention provides a stable antiulcer drug superior in the absorbability.

Crystal of benzimidazole compound

The present invention relates to a production method of a crystal of (R)-lansoprazole or (S)-lansoprazole, which includes crystallization at a temperature of about 0&#xb0; C. to about 35&#xb0; C. from a Calkyl acetate solution containing (R)-lansoprazole or (S)-lansoprazole at a concentration of about 0.1 g/mL to about 0.5 g/mL and the like. According to the production method of the present invention, a crystal of (R)-lansoprazole or (S)-lansoprazole superior in preservation stability can be produced efficiently on an industrial large scale.

Process for the crystallization of (R)- or (S)-lansoprazole

The present invention relates to a production method of an optically active form of a compound represented by formula (II)wherein ring A is a benzene ring optionally having substituent(s); Ris H, a hydrocarbon group optionally having substituent(s), an acyl group or an acyloxy group; R, Rand Rare each H, an alkyl group optionally having substituent(s), an alkoxy group optionally having substituent(s) or an amino group optionally having substituent(s); X is N or CH; Y is N or CH; and * shows an asymmetric center, or a salt thereof, which includes reacting a compound represented by the formula (I)wherein each symbol is as defined above, or a salt thereof, with an excess amount of an oxidizing agent in the presence of a catalyst for asymmetric induction, and provides an efficient production method of an optically active sulfoxide derivative in high yield on an industrial large scale by a convenient method, while achieving an extremely high enantiomer excess.

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Osaka, Japan

Tadashi Urai