Abstract: This invention provides a method for producing a microparticle which comprises pulverizing a solid preparation comprising a compound represented by the formula: ##STR1## wherein ring A is an optionally substituted benzene ring; R is a hydrogen atom or an optionally substituted hydrocarbon group; B is an optionally esterified or amidated carboxyl group; X is --CH(OH)-- or --CO--; k is 0 or 1; and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof and a biodegradable polymer of .alpha.-hydroxycarboxylic acid in the presence of a pulverizing auxiliary, which can provide microparticles which are less adhesive and involve less aggregation and are thus excellent in drug entrapment ratio and control of drug-release in a desired particle size.

Abstract: A two-compartment type prefilled syringe includes a first rubber stopper fitted into a front sleeve, a second rubber stopper fitted into a rear end portion of a cartridge, a third rubber stopper for hermetically dividing the interior of the cartridge into front and rear compartments and a bypass formed by radially outwardly bulging a portion of a peripheral wall of the cartridge. In an axial direction of the cartridge, a length of the third rubber stopper is slightly smaller than an inner length of the bypass. When the third rubber stopper has been displaced into the bypass, the sealing property of the rear compartment with the front compartment is cancelled such that the dissolving agent, suspension or the like in the rear compartment is carried, via the bypass, into the front compartment containing dry medicament or the like.

Abstract: A novel microparticle preparation comprising microparticles of a polymer which contain a drug and are at least partially or wholly coated with a water-soluble inorganic salt, a water-soluble organic acid or a water-soluble salt of an organic acid, which acts as an agent for preventing aggregation of the microparticle preparation is disclosed. The preparation is produced by spraying a polymer solution containing a drug and a solution or dispersion of a water-soluble inorganic salt, a water-soluble organic acid or a water-soluble salt of an organic acid from different nozzles and contacting them with each other in a spray dryer. In this procedure, if desired, a non-ionic surfactant may be added to the solution of the water-soluble inorganic salt, the water-soluble organic acid or the water-soluble salt of organic acid, or a solution of non-ionic surfactant may be sprayed from the other nozzle simultaneously.

Abstract: When a transdermal therapeutic composition which contains a pharmaceutically effective ingredient, a water-soluble absorption enhancer, a fat-soluble absorption enhancer and a super water-absorbent resin is applied to the skin of mammals, release of the pharmaceutically effective ingredient and the absorption enhancers is controlled and the pharmacological action lasts for a long period of time.

Abstract: The present invention concerns a sustained-release microcapsule preparation comprising an ion exchange resin with 6 to 16% crosslinking, containing a drug adsorbed in an amount not less than 80% of its theoretical ion adsorption amount and coated with a water-permeable polymer.