Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Hiroyoshi Koyama

Naoru Hamaguchi

Masahiko Koike

Shin-Ichiro Hirai

Hiroshi Matoba

Toshio Kashihara

Shunichi Itoh

Kazuhiro Ohkouchi

Tadashi Makino

Kazumichi Yamamoto

Tetsuya Kawano

Jun-ichi Kikuta

Arisa Maeda

Kazuhiro Okochi

Kazuhiro Doken

Shinji Ohmori

The present invention can retain the volume of a tablet large without increasing the thickness of the tablet or the like dimension and prevents a plurality of tablets from sticking to each other even if they are subjected to a film-coating or the like treatment, so as to improve the yield. The tablet is a tablet () longer in one direction when seen in plan. The tablet () has side edges () each of which extends in a longitudinal direction and is formed in the shape of a curve projecting outwardly in plan view. The curve has a radius of curvature (R) set to at least 1.5 times a length (L) of the tablet. This makes a projected area of the tablet () in plan view at least 97% with respect to a projected area of a standard elliptical tablet having opposite end portions each of which is formed by a semi-circle having a diameter of a width (W) of the tablet.

Tablet

The present invention provides a solid preparation containing an insulin sensitizer and an active ingredient (except insulin sensitizers), which is useful as a therapeutic drug for diabetes and the like, and which is superior in preparation characteristics such as content uniformity and dissolution property of the insulin sensitizer and the active ingredient (except insulin sensitizers), preparation hardness and the like.

Solid preparation

The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.

Solid preparation comprising alogliptin and metformin hydrochloride

The present invention provides an oral preparation sufficiently masking the bitter taste of pioglitazone and a salt thereof. The present invention provides an oral preparation containing pioglitazone or a salt thereof and alkali metal chloride.

Oral preparation comprising pioglitazone

The present invention provides a solid preparation containing an insulin sensitizer and an active ingredient (except insulin sensitizers), which shows in vivo dissolution behavior of an insulin sensitizer, which is similar to the dissolution behavior of an insulin sensitizer from 'a solid preparation containing an insulin sensitizer alone as an active ingredient'. The present invention provides a solid preparation containing (1) a layer containing an insulin sensitizer, and (2) a layer containing (a) an active ingredient (except insulin sensitizers), (b) microcrystalline cellulose having a mean particle size of 5-25 &#x3bc;m, (c) microcrystalline cellulose having a mean particle size of 30-100 &#x3bc;m and (d) polyvinylpyrrolidone K-90.

Solid pharmaceutical preparation

The present invention provides a production method of a preparation coated with pioglitazone hydrochloride, which is useful as a therapeutic agent for diabetes and the like, and which is superior in the characteristics of the preparation such as dissolution property of pioglitazone hydrochloride.

Process for producing coated preparation

A solid preparation useful as a diabetes-treating agent or the like and excellent in the dissolution properties of an insulin sensitizer and an insulin secretagogue, which comprises an insulin sensitizer, an insulin secretagogue and a polyoxyethylene sorbitan fatty acid ester is provided.

Solid preparation comprising an insulin sensitizer, an insulin secretagogue and a polyoxyethylene sorbitan fatty acid ester

Quickly disintegrating solid preparations which contain: a) an active ingredient; b) D-mannitol having an average particle size of 30 &mgr;m to 300 &mgr;m; c) a disintegrating agent; and d) celluloses.

Quickly disintegrating solid preparations

Granules having a core are produced by spraying core granules with a dispersion of a low substituted hydroxypropylcellulose (L-HPC), and, if necessary, simultaneously applying a dusting powder. The granules having a core thus obtained exhibit increased granule strength and improved disintegrating property as compared with those produced by known methods. An active ingredient such as a drug can be contained in the dispersion, dusting powder or core granules.

Granules having core and their production

(A) A clad powdery or granular preparation of a medicinally active ingredient and (B) a powdery or granular ion exchanger such as a cation exchange resin are blended to prepare a solid preparation. The active ingredient includes .beta.-lactam antibiotics having a basic group. The clad powdery or granular preparation includes not only coated preparation wherein the active ingredient or preparation is coated but also a variety of preparations in which the contact of the active ingredient with the ion exchanger is suppressed or inhibited. Polymers such as a water-soluble polymer, an enteric polymer and so on can be used as the coating agent for the coated preparation. The using amount of the ion exchanger is about 10 to 5,000 parts by weight per 100 parts by weight of the active ingredient. Said solid preparation can remarkably decrease the unpleasant taste and odor of the active ingredient such as bitterness, being excellent in dissolution property and absorbability of the active ingredient.

Solid preparation comprising ion exchanger and active agent

A compression-moldable composition comprising an active ingredient, an excipient and an oily or fatty substance having a lower melting point of about 20.degree. to 90.degree. C. is compression-molded into uncoated tablets without coating to improve the abrasion resistance. The oily or fatty substance includes a higher fatty acid or a salt thereof, a wax, a fatty acid ester, a hardened oil, a polyalkylene oxide, etc., and the amount thereof is about 0.01 to 10% by weight. The composition may comprise (1) a granulated powder containing the active ingredient and the excipient, and the powdery or granular oily or fatty substance having a lower melting point, or (2) a granulated powder containing the active ingredient, the excipient and said oily or fatty substance. Compression-molding of the composition improves the abrasion resistance of the tablet and significantly inhibits the development of powder by wearing or abrasion even when the oily or fatty substance is used in a small amount of about 0.1 to 0.5% by weight.

Uncoated tablets and method of producing the same

An enteric film is produced by spraying on a material a mixed solution of (a) hydroxypropylmethylcellulose phthalate exhibiting a viscosity of about 136 to 204 centistokes as 10% methanol/dichloromethane (1:1 by weight) solution at 20.degree. C., (b) polyethylene glycol presenting solid state at ambient temperature and (c) shellac, wherein respective ratios of (b) and (c) to (a) are 0.1 to 20 weight percent and 5 to 40 weight percent; and then drying the solution. The enteric film excels in film strength and acid resistance, and can be employed in pharmaceutical preparations.

Enteric film and preparatoin thereof

This invention relates to an antibacterial solid composition for oral administration which comprises a lipid soluble cephalosporin compound and a cyclodextrin. The said composition provides much increased in vivo absorbability of a non-ester form of the cephalosporin compound. This composition is useful for prevention and treatment of bacterial infections.

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Osaka, Japan

Hiroyoshi Koyama