摘要:
The present invention provides a particulate pharmaceutical composition which has improved drug encapsulation stability and is suitable for a drug delivery system. The particulate pharmaceutical composition 1 contains: a plurality of block copolymer unit 2 arranged radially, each of which has a hydrophobic polymer-chain segment 2b, which is arranged radially inside, and a hydrophilic polymer-chain segment 2a, which is arranged radially outside; a drug 4, which includes a biomacromolecule; and a charged lipid 3, which has an electrical charge opposite to that of the drug 4; wherein the charged lipid 3 is being attracted to the hydrophobic polymer-chain segment 2b, and the drug 3 is positioned radially inside the hydrophobic polymer-chain segment 2b. The pharmaceutical composition 1 can effectively prevent the drug 4 from disengaging from the particle.
摘要:
The present invention provides a cationic polyamino acid suitable for a carrier that can form a stable complex with a nucleic acid under a physiological condition and release the nucleic acid in cells suitably. The cationic polyamino acid can associate with a nucleic acid and includes a cationic amino acid residue having a cationic group in a side chain and a hydrophobic amino acid residue having a hydrophobic group in a side chain. The cationic polyamino acid includes 1 to 20 units of the cationic amino acid residue and is represented by the following formula (1). The meaning of each symbol in the formula is as shown in the description.
摘要:
An object of the present invention is to provide a composition improved in the solubility or oral absorbability.The present invention provides a composition which comprises three components of a slightly water-soluble component, a surfactant and a hydrophilic polymer, and is obtainable by wet granulation in the presence of water.
摘要:
The present invention provides a method of producing coated fine particles in which core fine particles is coated with a coating layer, which comprises the steps of preparing a liquid (liquid A) containing a polar organic solvent in which core fine particles are dispersed and a component constituting a coating layer is dissolved; preparing a liquid (liquid B) which is miscible with the liquid A and does not contain a polar organic solvent or contains a polar organic solvent in a ratio lower than that in the liquid A; and letting the liquid A flow from at least one inlet of a device for producing coated fine particles equipped with an in-line mixing means having two or more inlets and one or more outlet(s) and letting the liquid B flow from at least one remaining inlet to mix the liquids thereby coating the core fine particles with the coating layer.
摘要:
An object of the present invention is to provide a method for easily producing coated fine particles in which core fine particles are coated with a coating layer component, etc. There are provided a method of producing coated fine particles comprising core fine particles coated with a coating layer component, comprising the steps of dispersing the core fine particles and the coating layer component(s) in a liquid and the process of coating the core fine particles with the coating layer component, wherein the liquid contains a polar organic solvent in which the coating layer component(s) is soluble, and the concentration of the polar organic solvent is such that the core fine particles is not dissolved and the coating layer component(s) can be in the dispersed state in the liquid, and the like.
摘要:
A composition of matter for use in encapsulating a drug is expressed by formula (1) or formula (2): wherein R1 and R2 are each independently a hydrogen atom or a substituted or unsubstituted, linear or branched alkyl group having 1 to 12 carbon atoms; A is a hydrophilic polymer chain; L1 and L3 are each a linking group; B is a cation-containing group; R3 is a side chain of an amino acid; z is an integer of 5 to 500; x is an integer of 40% or more of z; y is 0 or a positive integer; z-x-y is 0 or a positive integer; p is an integer of 1 to 10; and q is an integer of 1 to 10.
摘要:
A pharmaceutical composition containing a drug encapsulated in a polymer micelle composition containing a first block copolymer having affinity with HDL and a second block copolymer having affinity with a lipoprotein excluding HDL, each block copolymer having a hydrophobic polymer chain segment and a hydrophilic polymer chain segment such that a plurality of block copolymers arrange radially with the hydrophobic segments directed inward and the hydrophilic segments directed outward. In the composition, a detachment of the first block copolymer is induced by HDL adhesion which forms a gap and promotes the release of a drug encapsulated, while the second block copolymer excluding an affinity with HDL controls a release speed of the drug encapsulated.
摘要:
Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R—X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.
摘要:
An object of the present invention is to provide a safe, convenient and efficient method for coating fine particles with lipid membrane.There is provided a method for coating fine particles with lipid membrane, characterized in that, the rate of a polar organic solvent in an aqueous solution containing the polar organic solvent where the fine particles are dispersed and lipid is dissolved, is decreased.
摘要:
Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like. The present invention provides a compound in which a substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, is modified with a glycerol derivative represented by the following formula (1): wherein R represents a residue comprising a reactive group for the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance or for a spacer capable of binding the substance to be modified, which is selected from the group consisting of an amphiphilic substance and a hydrophobic substance, to R-X, or a group capable of being transformed into the reactive group; n represents an integer of 3 or more; and X represents a residue capable of having the following structure by n in number: directly or via the spacer, or a salt thereof; a fine particle comprising the same; and the like.