Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Wako Pure Chemical Industries, Inc.

Yoshio Hata

Kazumichi Yamamoto

Akiko Yamada

Yasutaka Igari

Jun Sato

Akira Saikawa

Tsutomu Tani

Satoshi Iinuma

Hikaru Taira

Takashi Aoki

Kohei Yamamoto

Kazumichi Yamatomo

A Yamada

K Yamamoto

Akiko c/o Takeda Pharmaceutical Company Ltd Yamada

Takashi c/o Wako Pure Chemical Ind Ltd Aoki

Kohei c/o Wako Pure Chemical Ind Ltd Yamamoto

Tsutomu c/o Wako Pure Chemical Ind Ltd Tani

Akiko 313-501 Sashimono-Cho Yamada

Kazumichi 341-11-1109 Shimizu-Cho Yamamoto

A controlled release composition containing a physiologically active substance in high content, suppressing the initial excess release, and achieving a stable release speed over a long period of time is provided. A controlled release composition comprising (1) a physiologically active substance or salt thereof in an amount of about 14% (w/w) to about 24% (w/w) based on the total composition weight, (2) hydroxynaphthoic acid selected from the group consisting of 3-hydroxy-2-naphthoic acid and 1-hydroxy-2-naphthoic acid or salt thereof, and (3) a lactic acid polymer or salt thereof having a weight-average molecular weight of 15000 to 50000 in which the content of polymers having molecular weights of 5000 or less is about 5% by weight or less, wherein the molar ratio of said hydroxynaphthoic acid or salt thereof to said physiologically active substance or salt thereof is from 3:4 to 4:3.

Controlled release composition and method of producing the same

Present invention is to provide a sustained-release composition which contains a physiologically active substance in high content even when gelatin is not included, and suppresses its initial excessive release and, thus, can achieve a stable release rate over about one month. A sustained-release composition containing a lactic acid-glycolic acid polymer having a ratio or weight average molecular weight and number average molecular weight of about 1.90 or lower, or a salt thereof, and a physiologically active substance.

Sustained-release composition and process for producing the same

A process for producing a lactic acid polymer of 15,000 to 50,000 in weight-average molecular weight, the content of polymeric materials having not more than about 5,000 in weight-average molecular weight therein being not more than about 5% by weight, characterized by hydrolyzing a high molecular weight lactic acid polymer, placing the resultant solution comprising the hydrolyzed product under a condition capable of precipitating the objective lactic acid polymer, separating the precipitated lactic acid polymer and collecting them. The lactic acid polymer is useful as a matrix for sustained-release preparations. The sustained-release microcapsule preparation encapsulating a physiologically active substance can fully prevent the initial excessive release of the physiologically active substance from the microcapsules and keep a stable release rate over a long period of time.

Lactic acid polymer and process for producing the same

A sustained-release composition containing a hydroxynaphthoic acid salt of a biologically active substance and a biodegradable polymer, a method of its production, and a pharmaceutical composition containing said sustained-release composition.

Sustained release compositions, process for producing the same and utilization thereof

Sustained release compositions containing a physiologically active substance or its salt, hydroxynaphthoic acid or its salt and a lactic acid-glycolic polymer or its salt, wherein the product of the weight-average molecular weight of the lactic acid-glycolic acid polymer by the amount (&#x3bc;mol) of the terminal carboxyl group per unit mass (g) of the lactic acid-glycolic acid polymer is from 1,200,000 to 3,000,000 (inclusive); and their production; medicaments containing these sustained release compositions, etc.

Sustained release compositions, process for producing the same and use thereof

A process for producing a biodegradable polymer having free carboxyl at the &ohgr;-end charcterized by polymerizing a cyclic ester compound in the presence of a hydroxymonocarboxylic acid derivative having protected carboxyl or a hydroxydicarboxylic acid derivative having protected carboxyl, and then deprotecting the thus obtained polymer having protected carboxyl at the &ohgr;-end. Use of the above process makes it easy to control the molecular weight of the target biodegradable polymer and the content of free carboxyl therein, thereby enabling the efficient production of a polymer having a high purity and being contaminated with littel catalyst remaining therein.

Process for producing polymer

A sustained-release preparation comprising a bioactive substance having an acidic group and a biodegradable polymer having an optionally protected basic group which improves the rate of incorporation of the bioactive substance, suppresses its leakage early after adminstration, and exhibits constantly suppressed release for an extended period of time.

Sustained-release preparation

A sustained-release preparation comprising a bioactive substance having an acidic group and a biodegradable polymer having an optionally protected basic group which improves the rate of incorporation of the bioactive substance, suppresses its leakage early after administration, and exhibits constantly suppressed release for an extended period of time.

Growing community of inventors

Hokkaido, Japan

Yoshio Hata