Takeda Chemical Industries, Inc.

Satoshi Iinuma

Hiroaki Okada

Yoshio Hata

Jun Sato

Hikaru Taira

Yasutaka Igari

Yutaka Yamagata

Kazumichi Yamamoto

Makoto Fukuta

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

According to a first embodiment, there is provided a sustained-release preparation comprising a water-insoluble or slightly water-soluble polyvalent metal salt of a water-soluble physiologically active substance which is not an endothelin antagonist, and a biodegradable polymer. The sustained-release preparation of the first embodiment is highly efficient in incorporating the water-soluble physiologically active substance and suppresses the initial burst of the water-soluble physiologically active substance. The sustained-release preparation of the present invention is capable of releasing the water-soluble physiologically active substance while retaining its bioactivity after administration in vivo. Furthermore, the water-soluble physiologically active substance in the sustained-release preparation is kept stable for a long period of time, with little loss of bioactivity. According to a second embodiment, there is provided a sustained-release preparation comprising an anti-endothelin substance and a biodegradable polymer. The sustained-release preparation of the present invention sustainedly releases an anti-endothelin substance, serving well in the treatment of endothelin-associated diseases.

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.

The present invention provides a conjugate capable of passing the blood-brain barrier comprising a bioactive peptide or protein incapable of passing the blood-brain barrier and a carrier peptide which exhibits substantially no bioactivity and which is capable of passing the blood-brain barrier. The conjugate makes it possible to allow a bioactive peptide or protein incapable of passing the blood-brain barrier to easily pass the blood-brain barrier for uniform transport to the brain without any side effect of the carrier peptide.

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Kobe, Japan

Satoshi Iinuma