Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Teikoku Hormone Mfg. Co., Ltd.

Advance Co., Ltd.

Masafumi Misaki

Yutaka Yamagata

Susumu Iwasa

Shigeyuki Takada

Kenji Nakamura

Maiko Harada

Ikurou Yamane

Mitsuru Shiraishi

Yasutaka Igari

Katsumi Iga

Shoji Fukumoto

Keiichiro Okabe

Tetsuya Kawano

Yuki Tsushima

Kayoko Okamoto

Kenichiro Kiyoshima

Emi Kyo

Masahiro Niwa

Wataru Hoshina

Yoshihiro Ohmachi

The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part.

Solid preparation

The present invention relates to an enteric tablet with improved bioavailability, which is rapidly disintegrated after reaching the intestine to allow dissolution of the active ingredient, and which characteristically reduces the amount of talc to be used and is free of an alkali component.

Enteric tablet

Sustained release preparations, which show suppressed initial release of a physiologically active substance and can release a constant amount of the physiologically active substance over a long period of time, and dispersion vehicle thereof can be obtained by adding a cationic substance or polyols to the outside of a matrix or dispersion vehicle thereof. Thus, sustained release preparations, which show suppressed initial release of a physiologically active substance immediately after the administration and can release a constant amount of the physiologically active substance over a long period of time and dispersion vehicle thereof can be provided.

Sustained-release preparation

The present invention intends to provide a solid preparation which contains an insulin sensitizer and an active ingredient other than an insulin sensitizer, and exhibits dissolution behavior of an insulin sensitizer similar to that of an insulin sensitizer from 'a solid preparation containing only an insulin sensitizer as an active ingredient'. The solid preparation comprises 'a part containing coated particles in which the particles containing an insulin sensitizer are coated with lactose or a sugar alcohol' and &#x201c;a part containing an active ingredient other than an insulin sensitizer&#x201d;.

A method for producing a preparation containing a bioactive substance, characterized in that it comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with a high pressure gas. The method allows the production of a preparation which is suppressed in excessive initial release of the bioactive substance immediately after the administration thereof, is capable of releasing a predetermined amount of the bioactive substance over a long period of time, and is extremely reduced in the deterioration of the bioactive substance and in the amount of a residual organic solvent.

Method for producing preparation containing bioactive substance

Nasal preparation of guanidinoimino quinoline derivatives

A method for producing a sustained-release preparation, which comprises dispersing a physiologically active polypeptide into an organic solvent solution of a biodegradable polymer and removing the organic solvent, wherein the polypeptide is a powder obtained by lyophilizing an aqueous solution of the polypeptide which solution has a water-miscible organic solvent and/or a volatile salt; which improves the ease of handling of the physiologically active polypeptide powder in the process for producing the preparation; which makes it possible to industrially produce the sustained-release preparation in large scale; which provides a sustained-release preparation showing high and stable concentration of the active component in blood in long term, low initial release ratio of the physiologically active polypeptide, and high entrapment ratio of the polypeptide into the sustained-release preparation.

Sustained-release preparation of physiologically active polypeptide and production thereof

The present invention provides a complex of human growth hormone and zinc containing human growth hormone and zinc at a molar ratio of about 1:1.6 to about 1:2.4, and a sustained-release preparation which comprises the complex of human growth hormone and zinc and a biodegradable polymer and which has a high entrapment ratio of human growth hormone and exhibits a stable sustained-release suppressing the initial burst.

Complex of human growth hormone and zinc and use

A method of producing sustained-release microcapsules which comprises dispersing a physiologically active polypeptide into a solution of a biodegradable polymer and zinc oxide in an organic solvent, followed by removing the organic solvent; which provides a sustained-release preparation showing a high entrapment ratio of the physiologically active polypeptide and its constant high blood concentration levels over a long period of time.

Method of producing a sustained-release preparation

This invention provides a sustained-release preparation comprising a biodegradable polymer metal salt and broactive polypeptide, with enhanced entrapment of the bioactive polypeptides, a suppression of initial burst, and a constant long-term release of the bioactive polypeptides.

Method of producing sustained-release preparation

Complex of human growth hormone and zinc

An interface is formed by incorporating (1) a mixture comprising a water-soluble protein and a drug into a matrix, or preferably (2) a mixture comprising a water-soluble protein and a drug to a porous matrix coated with a cationic surfactant or other ionic surfactant. The coating amount of the ionic surfactant is about 0.1 to 50 .mu.g, and the content of the water-soluble protein is about 0.1 to 1,500 .mu.g, each per 1 cm.sup.2 of the matrix. The water-soluble protein includes an albumin and the drug includes a physiologically active peptide or protein, for example. The use of the stabilized interface inhibits decrease of the drug retaining amount, and insures an effective transdermal drug delivery with a high repeatability and accuracy.

Growing community of inventors

Takarazuka, Japan

Masafumi Misaki