Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3? is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5? wherein n is 2 or 3, and R5? is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6? wherein n is 2 or 3, and R6? is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

Abstract: Medicinal preparations for treating sex hormone-dependent diseases which comprise a combination of a compound having a luteinizing hormone-releasing hormone agonistic effect or its salt with a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt for administering the compound having a luteinizing hormone-releasing hormone agonistic effect or its salt followed by the compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt. By using these preparations, the concentration of a sex hormone (for example, testosterone, LH, FSH, estrogen) can be quickly recovered after the medicable period of a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt or a preparation containing the same (preferably a sustained-release preparation), which makes it possible to definitely determine the drug cessation period in an intermittent treatment.

Abstract: 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.

Abstract: 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 (?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.

Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.

Abstract: 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 (?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.

Abstract: The agent for preventing the postoperative recurrence of premenopausal breast cancer comprising a GnRH agonist or antagonist of the present invention can prevent the postoperative recurrence of premenopausal breast cancer without severe side effects. In addition, by using the agent of the present invention in the form of a long term sustained-release type microcapsule, the drug action can be maintained for a long time without frequently administering the drug, and thus, prevention of the postoperative recurrence of premenopausal breast cancer having a long recurrence-preventing term and having high convenience becomes possible.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3? is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5? wherein n is 2 or 3, and R5? is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6? wherein n is 2 or 3, and R6? is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

Abstract: 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.

Abstract: The agent for preventing the postoperative recurrence of premenopausal breast cancer comprising a GnRH agonist or antagonist of the present invention can prevent the postoperative recurrence of premenopausal breast cancer without severe side effects. In addition, by using the agent of the present invention in the form of a long term sustained-release type microcapsule, the drug action can be maintained for a long time without frequently administering the drug, and thus, prevention of the postoperative recurrence of premenopausal breast cancer having a long recurrence-preventing term and having high convenience becomes possible.

Abstract: 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.

Abstract: 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.

Abstract: A composition prepared by containing or blending a physiologically active non-peptide substance and a biodegradable polymer having two or more carboxylic groups at its end or a salt thereof features: (1) larger content of the physiologically active non-peptide substance can be contained, as well as release of the same can be controlled or accelerated, whereby secure pharmaceutical effect is achieved; (2) when the physiologically active non-peptide substance causes subcutaneous stimulation, an activity of canceling the stimulation by strongly acidic group at its end is expected; and (3) high glass transition point and high stability.

Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity with maintaining circadian rhythm of blood pressure for a long time.

Abstract: Medicinal preparations for treating sex hormone-dependent diseases which comprise a combination of a compound having a luteinizing hormone-releasing hormone agonistic effect or its salt with a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt for administering the compound having a luteinizing hormone-releasing hormone agonistic effect or its salt followed by the compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt. By using these preparations, the concentration of a sex hormone (for example, testosterone, LH, FSH, estrogen) can be quickly recovered after the medicable period of a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt or a preparation containing the same (preferably a sustained-release preparation), which makes it possible to definitely determine the drug cessation period in an intermittent treatment.

Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.

Abstract: A sustained-release preparation containing a physiologically active compound slightly soluble in water, a component obtained by treating with water a polyvalent metal compound slightly soluble in water, and a biodegradable polymer which are improved in the release-control and stabilization of the physiologically active compound slightly soluble in water and can be produced by a process suitable for mass production.

Abstract: A sustained-release preparation which comprises a physiologically active peptide of general formula: wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula: wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.

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

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