Abstract: A method is used in the production of a disintegrative particulate composition including three components consisting of a first disintegrator component having sedimentation volume in water of 4.0 cm3/g or more, and a second disintegrator component other than the first disintegrator component and an excipient. The method includes a first wet granulation step using any two of the three components, and a second wet granulation step using the granules obtained in the first wet granulation step and at least the component not used in the first wet granulation step; thus the disintegrative particulate composition is produced. Moreover, an orally disintegrating tablet contains a medicinal ingredient and the disintegrative particulate composition.

Abstract: The purpose of the present invention is to provide a new disintegrative particulate composition having an optimal balance between the tablet hardness and disintegrability that are mutually opposing properties, and disintegrating tablets for pharmaceuticals and various kinds of foods comprising said composition. The present invention relates to a disintegrative particulate composition comprising milled lactose and/or granulated lactose as an excipient, and to a disintegrating tablet for pharmaceuticals or foods, comprising the disintegrative particulate composition, especially the tablet having tablet hardness of from 20 to 200 N, and disintegration time in water of from 1 to 60 sec.

Abstract: An object of the present invention is to provide a disintegrative particulate composition that can be used for an orally disintegrating tablet having both excellent tablet hardness and disintegrability. This invention relates to a method for the production of a disintegrative particulate composition including three components consisting of a first disintegrator component having sedimentation volume in water of 4.0 cm3/g or more, a second disintegrator component other than the first disintegrator component and an excipient, which comprises a first wet granulation step using any two of the three components and a second wet granulation step using the granules obtained in the first wet granulation step and at least the remaining one component not used in the first wet granulation step; the disintegrative particulate composition thus produced; and an orally disintegrating tablet comprising a medicinal ingredient and the disintegrative particulate composition.

Abstract: An object of the present invention is to provide an orally disintegrating tablet having both an excellent tablet hardness and disintegrability even when the content of a medicinal ingredient is high. This invention relates to an orally disintegrating tablet comprising a medicinal ingredient having distribution coefficient (log P) in a range of from ?6.0 to 10.0 and a disintegrative particulate composition produced by granulation consisting of at least two stages, especially to said orally disintegrating tablet having tablet hardness of from 30 to 100 N, and disintegration time in water of from 10 to 30 sec.

Abstract: An object of the present invention is to provide an orally disintegrating tablet (ultrafast-disintegrating tablet) having an extremely high disintegrability (short disintegration time), and a high tablet hardness, and to provide a simple method for the production of said ultrafast-disintegrating tablet without such a complicated process as freeze-drying. This invention relates to an orally disintegrating tablet comprising a first disintegrator component of an acid-type carboxymethylcellulose, and having a tablet hardness of 10 N or more and a disintegration time in water of less than 15 seconds, a method for the production of said orally disintegrating tablet, and to a disintegrative particulate composition for use in said method.

Abstract: An object of the present application is to provide an orally-disintegrating tablet having excellent tablet hardness and disintegrability, and including a disintegrative particulate composition. This invention relates to a disintegrative particulate composition comprising the four components consisting of a first disintegrator component of an acid-type carboxymethylcellulose, a second disintegrator component other than the acid-type carboxymethylcellulose, an excipient of a sugar or sugar alcohol, and crystalline cellulose; and to an orally-disintegrating tablet, including the disintegrative particulate composition and a medicinal ingredient.

Abstract: An object of the present application is to provide an orally-disintegrating tablet having excellent tablet hardness and disintegrability and a disintegrative particulate composition by which the orally-disintegrating tablet can be obtained with a relatively low tablet compression force and which can provide excellent moldability, as well as a method of producing the same, etc.

Abstract: The present application provides an orally-disintegrating tablet having excellent tablet hardness and disintegrability. The present application further provides a method of producing a disintegrative particulate composition including three components consisting of a first disintegrator component of an acid-type carboxymethylcellulose, a second disintegrator component and an excipient. The method includes a first wet granulation step using any two of the three components, and a second wet granulation step using granules obtained in the first wet granulation step and the remaining one component of the three components not used in the first wet granulation step. The production method may further includes a crystalline cellulose as a fourth component or a third step of mixing a crystalline cellulose into granules obtained in the second wet granulation step. Disintegrative particulate compositions obtained by these methods are also disclosed.

Abstract: Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.

Abstract: A novel indole derivative or a salt thereof is provided, which is represented by the formula: wherein R1 represents an aryl lower alkyl group, said aryl group may be substituted with one or more groups selected from the group consisting of a halogen atom, an aryl group, a heterocyclic group, an aryl lower alkyl group, an aryl lower alkenyl group, a halo-lower alkyl group, a lower cycloalkyl-lower alkoxy group, a lower cycloalkoxy-lower alkyl group, an aryl lower alkynyl group, an aryloxy lower alkyl group, an aryl lower alkoxy group, a lower alkylthio group, a lower alkoxy group, and an alkenyl group; and R2 represents a lower alkyl group, a lower alkenyl group, an aryl group, or a heterocyclic group, each of which may be substituted with a hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aryl group. The compound of the present invention has blood sugar level-depressing activity and PDE5-inhibiting activity, and is useful as medicine.

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2??(I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract: The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.

Abstract: The present invention provides novel benzimidazole derivatives of the following formula (I) and salts thereof: wherein R1 represents a lower alkyl group or a lower alkyloxy-lower alkyl group; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an aryl group, and such; R3 represents a lower alkyl group, a lower alkenyl group, an aryl group, a lower alkylaryl group, an aryl-lower alkenyl group, a halothienyl group, a lower alkylamino group, or an aryl-lower alkylamino group; A represents a benzene ring, a naphthalene ring, or a pyridine ring; and X represents a halogen atom. The derivatives and their salts have blood sugar level-depressing activity or PDE5-inhibiting activity, and are useful as pharmaceutical preparations.

Abstract: The present invention provides novel benzimidazole compounds of the formula (I): wherein each symbol is as defined in the specification, salts thereof and prodrugs thereof, which are useful in treating, for example, the diseases curable through decrease in blood sugar level.

Abstract: A sulfonamide compound of the formula (I):

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2  (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract: The present invention relates to a sulfonamide compound of the formula (I): 1

Abstract: The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.

Abstract: A sulfonamide compound of the formula (I):

Abstract: A novel benzimidazole derivative or a salt thereof is provided, which is represented by the formula: wherein R1 represents an alkyl group, etc., R2 represents a substituted or unsubstituted aromatic lower alkyl group, R3 represents an alkyl group, etc., and -X- is represented by the following formula (V): etc. This derivative or a salt thereof is useful as medicine.