Abstract: Sustained release preparations, which show suppressed initial release of a physiologically active substance and can release a constant amount of the physiologically active substance over a long period of time, and dispersion vehicle thereof can be obtained by adding a cationic substance or polyols to the outside of a matrix or dispersion vehicle thereof. Thus, sustained release preparations, which show suppressed initial release of a physiologically active substance immediately after the administration and can release a constant amount of the physiologically active substance over a long period of time and dispersion vehicle thereof can be provided.

Abstract: A method for producing a preparation containing a bioactive substance, characterized in that it comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with a high pressure gas. The method allows the production of a preparation which is suppressed in excessive initial release of the bioactive substance immediately after the administration thereof, is capable of releasing a predetermined amount of the bioactive substance over a long period of time, and is extremely reduced in the deterioration of the bioactive substance and in the amount of a residual organic solvent.

Abstract: A method for producing a preparation containing a bioactive substance, characterized in that it comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with a high pressure gas. The method allows the production of a preparation which is suppressed in excessive initial release of the bioactive substance immediately after the administration thereof, is capable of releasing a predetermined amount of the bioactive substance over a long period of time, and is extremely reduced in the deterioration of the bioactive substance and in the amount of a residual organic solvent.

Abstract: A process for conveniently producing a stable protein powder retaining the higher-order structure at a high level which comprises freezing a protein-containing solution at a cooling rate of about −300 to −10° C./min. and then drying.

Abstract: Sustained release preparations, which show suppressed initial release of a physiologically active substance and can release a constant amount of the physiologically active substance over a long period of time, and dispersion vehicle thereof can be obtained by adding a cationic substance or polyols to the outside of a matrix or dispersion vehicle thereof. Thus, sustained release preparations, which show suppressed initial release of a physiologically active substance immediately after the administration and can release a constant amount of the physiologically active substance over a long period of time and dispersion vehicle thereof can be provided.

Abstract: A nasal preparation comprising a compound represented by the formula: wherein Ring A is an optionally substituted 5- or 6-membered aromatic heterocyclic ring, Ring B is an optionally substituted 5- or 6-membered aromatic homocyclic or heterocyclic ring, R1 is a hydrogen atom, a hydroxyl group or a lower alkyl group, and n is 0 or 1, which has an Na—H exchange inhibiting activity, or a salt thereof exhibits excellent bioabsorbability and an Na—H exchange inhibiting activity superior to that of an oral preparation, thus being useful as a prophylactic and/or therapeutic agent for ischemic heart diseases such as myocardial infarct and arrhythmia.

Abstract: A method for producing a preparation containing a bioactive substance, characterized in that it comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with a high pressure gas. The method allows the production of a preparation which is suppressed in excessive initial release of the bioactive substance immediately after the administration thereof, is capable of releasing a predetermined amount of the bioactive substance over a long period of time, and is extremely reduced in the deterioration of the bioactive substance and in the amount of a residual organic solvent.

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: The present invention is to provide sustained-release microcapsules which contains high amount of a drug, suppresses initial release and shows stable release, and the production method of which comprises adding a physiologically active substance to biodegradable polymer in an organic solvent containing a fat and oil (in particular, vitamin E) and dispersing and emulsifying the mixture.

Abstract: Disclosed is a sustained-release preparation characterized in that it is produced by dispersing in an oil phase a rapidly dried product containing a bioactive polypeptide and a surfactant, and subsequent shaping, and a method of its production.

Abstract: A sustained-release preparation containing a bioactive polypeptide is prepared using a starting material containing a lyophilized product of an aqueous solution or suspension of the bioactive polypeptide in a non-ionic surfactant. The lyophilized product is dispersed in an oil phase, which further contains a biocompatible, biodegradable polymer.

Abstract: A sustained-release microcapsule contains an amorphous water-soluble pharmaceutical agent having a particle size of from 1 nm-10 .mu.m and a polymer. The microcapsule is produced by dispersing, in an aqueous phase, a dispersion of from 0.001-90% (w/w) of an amorphous water-soluble pharmaceutical agent in a solution of a polymer having a wt. avg. molecular weight of 2,000-800,000 in an organic solvent to prepare an s/o/w emulsion and subjecting the emulsion to in-water drying.

Abstract: A pharmaceutical preparation is provided by a microcapsule containing a physiologically active substance which is water-soluble only at a pH of about 3 or below, and a polymer which is biodegradable upon oral administration. A process for producing the microcapsule is also provided.

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 microcapsule contains a pharmaceutically effective amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof and a polymer binder and a method of preparing said microcapsule. The microcapsule is produced by dispersing in an aqueous phase a dispersion of the amorphous water-soluble 2-piperazinone-1-acetic acid compound or salt thereof in a solution of a polymer in an organic solvent to give an s/o/w type emulsion and subjecting the emulsion to in-water drying. The sustained-release microcapsule entraps 2-piperazinone-1-acetic acid compound or the salt thereof, as a drug, in high concentration, and in reducing the initial release of the drug, thereby reducing undesirable side effects of the drug.

Abstract: A novel microparticle preparation comprising microparticles of a polymer which contain a drug and are coated with a film of an agent for preventing aggregation of the microparticles is disclosed. The preparation is produced by spraying a solution of a polymer containing a drug and an aqueous solution of an agent for preventing aggregation of the microparticles separately from different nozzles and contacting them with each other in a spray dryer.

Abstract: A novel microparticle preparation comprising microparticles of a polymer which contain a drug and are coated with a film of an agent for preventing aggregation of the microparticles is disclosed. The preparation is produced by spraying a solution of a polymer containing a drug and an aqueous solution of an agent for preventing aggregation of the microparticles separately from different nozzles and contacting them with each other in a spray dryer.

Abstract: A pharmaceutical composition containing a physiologically active peptide or protein which is poorly absorbable through the gastrointestinal tract and heat-labile enterotoxin B subunit brings an increased absorbability of said peptide or protein into the mammalian body when administered through mucosa.

Abstract: Microcapsules are advantageously produced with high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/O emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.

Abstract: Microcapsules are advantageously produced with high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/O emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.