Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Tomomichi Futo

Kazuhiro Saito

Tetsuo Hoshino

Masuhisa Hori

Muneo Nonomura

Kazumichi Yamamoto

Hisayoshi Shimizu

Jiichi Arai

Kei Mukai

Koichi Maedera

Sustained-release compositions wherein a water-soluble physiologically active peptide is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, and the physiologically active substance is contained in an amount of 15 to 35 wt/wt % to the total microcapsules and weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, which is characterized by having a high content of the physiologically active substance, and suppression of the initial excessive release within one day after the administration and a stable drug sustained-release over a long period of time, and method for producing the same.

Sustained-release composition and method for producing the same

This invention provides a production method for a solid sustained-release preparation, characterized in that a sustained-release preparation (a sustained-release preparation suspension) is freeze-dried in a freeze-drying container whose inner face is partially or totally coated with an ice layer or water-repelling base material.

Producing a sustained-release preparation

A sustained release preparation comprising a combination of a microcapsule which gradually releases a GnRH agonist or a salt thereof for a long term, and a microcapsule which gradually releases a GnRH agonist or a salt thereof for a short term.

Sustained-release preparations

A drug comprising either a peptide having the LH-RH action or an LH-RH antagonist is carried on an intrauterine contraceptive device (IUD) so as to be able to provide controlled release. Once the IUD is put in the uterus, the carried drug is gradually released over such a prolonged period of treatment time as, for example, several months to be continuously absorbed through the uterus mucosa or the vagina mucosa. This construction makes it possible to reduce the patient's pain and such a troublesomeness as frequent drug administration and continuously administer a necessary drug over a prolonged period of time while taking a contraceptive measures.

Pharmaceutical product for application to uterus mucosa

There is provided a process for producing microcapsules of a water-soluble drug by in-water drying process, which comprises carrying out the process in the presence of an osmotic pressure adjustor present in the external aqueous phase. This process improves the drug take up into microcapsules.

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Osaka, Japan

Tomomichi Futo