Sumitomo Dainippon Pharma Co., Ltd.

Dainippon Sumitomo Pharma Co., Ltd.

Sumitomo Pharmaceuticals Company Limited

Yasushi Ochiai

Yuki Ikeda

Hiroyuki Nishii

Takafumi Matsumoto

Maki Sasaki

Keiichi Fujiwara

Teruko Ariyama

Yasuhiro Matsui

Yuka Kato

Hirohisa Kobayashi

Kazuhiko Tomomura

Kouji Wakisaka

The present invention relates to a stable ophthalmic suspension formulation comprising (R)-(&#x2212;)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3'-pyrrolidine-1,2&#x2032;,3,5&#x2032;-tetrone, which is useful for treating a disease in posterior eye segment and the like, avoiding side-effects due to systemic exposure.

Ophthalmic suspension formulation

The purpose of the invention is to provide a press-coated orally-disintegrating tablet having a powder/granular material with poor formability in its inner core, which has an excellent disintegrability and a suitable hardness as a whole tablet. Furthermore, the invention is a press-coated orally-disintegrating tablet with an outer layer surrounding an inner core wherein the inner core has a thickness in the range of 30 to 80% per that of the whole tablet, and the outer layer comprises (a) microcrystalline cellulose, (b) a sugar or a sugar alcohol, and (c) one or more particular ingredients selected from the group consisting of crospovidone, starches, low-substituted hydroxypropylcellulose and carmellose.

Press-coated orally-disintegrating tablets

A tablet containing droxidopa as an active ingredient in a proportion of 20-80 wt % relative to the total weight of the tablet, and characteristically containing at least one excipient selected from mannitol, lactose, erythritol, glucose, sucrose, crystalline cellulose, and corn-derived starch is provided. In addition, a preparation containing corn-derived processed starch or polyvinyl alcohol as a binder and the like, which is a stable tablet containing droxidopa as an active ingredient, is provided.

Stable tablet containing droxidopa

The purpose of the present invention is to provide a press-coated orally-disintegrating tablet characterized by containing an inner core which has an excellent disintegratability in oral cavity and a suitable hardness as a whole tablet. The present invention relates to a press-coated orally-disintegrating tablet with an outer layer surrounding an inner core wherein the inner core has a thickness in the range of 10 to 90% per that of the whole tablet, and the outer layer comprises (a) microcrystalline cellulose, (b) an inorganic excipient, and (c) one or more particular ingredients selected from the group consisting of crospovidone, starches, low substituted hydroxypropylcellulose and carmellose.

Dry-coated orally-disintegrating tablet

The invention provides an orally disintegrating tablet that has both adequate tablet hardness and rapid disintegrability in the oral cavity, and that undergoes minor hardness reduction and maintains good oral disintegrability even when preserved under moist conditions. In particular, the invention relates to an orally disintegrating tablet containing (a) crystalline cellulose, (b) a calcium hydrogen phosphate compound, (c) a natural starch and (d) a lubricant, wherein the blending ratio to 100 wt % of the disintegrating tablet is (a) 9 to 60 wt %, (b) 16 to 60 wt %, (c) 3 to 40 wt % and (d) 0.01 to 1.8 wt %.

Orally disintegrating tablet

A granular preparation containing a biguanide compound and a solidification-preventive agent does not solidify during storage and can avoid the difficulty in dosing.

Granular preparation containing biguanide compound

Crystalline 3-[(1S)-1-(2-fluorobiphenyl-4-yl)ethyl]-5-{[amino(morpholin-4-yl)methylene]amino}-isoxazole that exhibits the following angle of diffraction (2&#x3b8;) and relative intensity in a powder X-ray diffraction pattern, is very easy to handle and stable in a process of its formulation into a pharmaceutical preparation. 

Crystalline isoxazole derivative and medical preparation thereof

The present invention provides coated granules using drug granules containing a water soluble drug as an active ingredient at a high density, which is superior in uniform content and stability, and which is capable of providing a pharmaceutical preparation superior in drug release control and having a smaller size than conventional preparations, and a production method of the granules, and further, a pharmaceutical preparation using the drug granules.

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Ibaraki, Japan

Yasushi Ochiai