Abstract: 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.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula 1

Abstract: A method of production of sustained-release microcapsules that comprises obtaining microcapsules comprising a bioactive substance that are encapsulated with a biodegradable polymer, and thermally drying the obtained microcapsules at a temperature not lower than the glass transition temperature of the biodegradable polymer for about 24 to about 120 hours to produce the sustained-release microcapsules comprising, relative to the weight of the sustaind-release microcapsule, not less than 60% (w/w) of the biodegradable polymer, possessing pharmaceutical characteristics clinically excellent in that a bioactive substance is released at constant rate over a very long period of time from just after administration with dramatically suppressed initial release of the bioactive substance in excess just after administration and with minimum remaining organic solvent.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: A method of production of sustained-release microcapsules that comprises obtaining microcapsules comprising a bioactive substance that are encapsulated with a biodegradable polymer, and thermally drying the obtained microcapsules at a temperature not lower than the glass transition temperature of the biodegradable polymer for about 24 to about 120 hours to produce the sustained-release microcapsules comprising, relative to the weight of the sustained-release microcapsule, not less than 60% (w/w) of the biodegradable polymer, possessing pharmaceutical characteristics clinically excellent in that a bioactive substance is released at constant rate over a very long period of time from just after administration with dramatically suppressed initial release of the bioactive substance in excess just after administration and with minimum remaining organic solvent.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group;R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group;R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted;R.sub.7 represents a D-amino acid residue or an azaglycyl residue; andQ represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.

Abstract: The present invention is to provide a prophylactic/therapeutic composition for the secondary cataract comprising a polypeptide having an inhibitory activity of cell adhesion and a lactic acid-glycolic acid polymer.The composition of the present invention inhibits adhesion and extension of lens epithelial cells onto the posterior lens capsule after extraction of lens and is useful as a prophylactic/therapeutic composition for the secondary cataract in the clinical point of view.

Abstract: A transmucosal therapeutic composition comprising a physiologically active peptide or protein and a cytidine nucleotide derivative was produced. The above composition results in a satisfactory transmucosal absorption of physiologically active peptides or proteins which are otherwise hardly absorbed from the mucosa. Since it allows self-administration to the mucosa, such as the nasal, vaginal or digestive tract mucosa, in lieu of injection which causes pain, the invention is of great utility as a pharmaceutical dosage form for physiologically active peptides or proteins which must be administered over a protracted time.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group; R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group;R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted;R.sub.7 represents a D-amino acid residue or an azaglycyl residue; andQ represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.

Abstract: The present invention relates to a matrix for sustained-release preparation comprising an ester formed at a terminal carboxyl group of a straight-chain polyester which essentially consists of an .alpha.-hydroxymonocarboxylic acid. The matrix is stable to light, heat, moisture, coloring etc., and is of low toxicity. The sustained-release preparation produced by using the ester of the present invention offers stable drug release over an extended period of time, ensuring sustained stable effect. Furthermore, the sustained-release preparation does not show excess drug release just after administration.

Abstract: The present invention relates to a matrix for sustained-release preparation comprising an ester formed at a terminal carboxyl group of a straight-chain polyester which essentially consists of an .alpha.-hydroxymonocarboxylic acid. The matrix is stable to light, heat, moisture, coloring etc., and is of low toxicity. The sustained-release preparation produced by using the ester of the present invention offers stable drug release over an extended period of time, ensuring sustained stable effect. Furthermore, the sustained-release preparation does not show excess drug release just after administration.

Abstract: (1) A composition which comprises erythropoietin and hyaluronic acid shows a sustained-release of the medicine in a living body, and(2) A water-soluble composition which comprises (a) a pharmacologically active polypeptide secreted by an animal body or its derivative or a chemically synthesized pharmacologically active substance, (b) a water-soluble species' of hyaluronic acid or its nontoxic salt and (c) a water-soluble protein injectable into body fluids without showing any substantial pharmacological activity brings about a prolonged action in vivo of a pharmacologically active substance. In addition, the composition can be administered using a small-gauge needle and thereby contributes to relieving pain in patients.

Abstract: A method of producing a sustained-release preparation which includes permitting a water-soluble polypeptide to permeate into a biodegradable matrix in the aqueous solution. The production method of the present invention makes possible the permeation of a water-soluble polypeptide into a biodegradable matrix without bringing the water-soluble polypeptide into contact with an organic solvent. Hence the water-soluble polypeptide is prepared without affecting the water-soluble polypeptide bioactivity and is thus effective for use as a pharmaceutical.

Abstract: A transmucosal therapeutic composition comprising a physiologically active peptide or protein and a cytidine nucleotide derivative is described. The above composition results in a satisfactory transmucosal absorption of physiologically active peptides or proteins which are otherwise hardly absorbed from the mucosa. Since it allows self-administration to the mucosa, such as the nasal, vaginal or digestive tract mucosa, in lieu of injection which causes pain, the invention is of great utility as a pharmaceutical dosage form for physiologically active peptides or proteins which must be administered over a protracted time.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group; R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group;R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted;R.sub.7 represents a D-amino acid residue or an azaglycyl residue; andQ represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.

Abstract: (1) A composition which comprises erythropoietin and hyaluronic acid shows a sustained-release of the medicine in a living body, and(2) A water-soluble composition which comprises (a) a pharmacologically active polypeptide secreted by an animal body or its derivative or a chemically synthesized pharmacologically active substance, (b) a water-soluble species of hyaluronic acid or its nontoxic salt and (c) a water-soluble protein injectable into body fluids without showing any substantial pharmacological activity brings about a prolonged action in vivo of a pharmacologically active substance. In addition, the composition can be administered using a small-gauge needle and thereby contributes ot relieving pain in patients.

Abstract: A water soluble composition is described which comprises (a) a water soluble pharmacologically active peptide selected from the group consisting of cytokines or haematopoietic factors and (b) a sulfate group-containing acidic mucopolysaccharide and/or a desulfated modification of a naturally occurring sulfate group containing acidic mucopolysaccharide, and which brings about prolonged action of pharmacologically active peptides in a living body.