Abstract: The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic polymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably releases compound (I) or a salt thereof over a long period of time and exerts medicinal effects of compound (I) or a salt thereof over a long period of time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing frequency of administration, is an excellent formulation as a clinical medicine.

Abstract: The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic acid-glycolic acid copolymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably release compound (I) or a salt thereof for a long time and exerts a medicinal effect of compound (1) or a salt thereof for a long time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing the number of administration times, is an excellent formulation as a clinical medicine.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic polymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably releases compound (I) or a salt thereof over a long period of time and exerts medicinal effects of compound (I) or a salt thereof over a long period of time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing frequency of administration, is an excellent formulation as a clinical medicine.

Abstract: The present invention relates to a sustained-release formulation comprising a metastin derivative and a lactic acid-glycolic acid copolymer having a weight average molecular weight of about 5,000 to about 40,000 or a salt thereof. The sustained-release formulation of the present invention slowly and stably release compound (I) or a salt thereof for a long time and exerts a medicinal effect of compound (I) or a salt thereof for a long time. Furthermore, the sustained-release formulation of the present invention, which improves patient's convenience by reducing the number of administration times, is an excellent formulation as a clinical medicine.

Abstract: 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.

Abstract: 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.

Abstract: The present invention provides a pharmaceutical composition, wherein solubility and stability of a water-insoluble or slightly water-soluble compound represented by formula (I): wherein each symbol is as defined in the specification, are improved, by combination of the above-mentioned compound and a cyclodextrin derivative and a method for improving solubility, stability and the like of the above-mentioned compound.

Abstract: 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.

Abstract: A sustained-release composition which comprises (i) a physiologically active substance and (ii) a lactic acid-glycolic acid copolymer in which the weight-average molecular weight (Mw) is about 8,000 to about 11,500, the ratio of the weight-average molecular weight (Mw) to the number-average molecular weight (Mn) is greater than 1.9, and the compositional molar ratio of lactic acid to glycolic acid is 99.9/0.1 to 60/40, or a salt thereof, and which does not contain a drug retaining substance is provided and said sustained-release composition has improved spherical property and/or needle penetrating property.

Abstract: 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.

Abstract: 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.

Abstract: A provision of a method for producing a microsphere improved in dispersibility. A method for producing a microsphere improved in dispersibility, characterized in that during the production of microspheres by an in-water drying method, an osmotic pressure regulating agent is added to an outer water phase.

Abstract: 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.

Abstract: 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.