Kyowa Hakko Kirin Co., Limited

Eli Lilly and Company

Kyowa Hakko Kogyo Co., Ltd.

Techno Network Shikoku Co., Ltd.

Hiroko Kusano

Yasuki Kato

Masahiro Yamauchi

Shiro Akinaga

Takeshi Iwata

Takaaki Uochi

Motoo Yamasaki

Yosuke Watanabe

Toshiyuki Suzawa

Kunio Ito

Hisao Nemoto

Dinesh Shyamdeo Mishra

Masashi Nakakura

Yoshikazu Tashiro

Yuji Kawaguchi

Nobuhiro Yagi

Hiroko Sugishita

Hong Zhuang

An object of the present invention is to provide a method of easily producing fine particles comprising a lipid, a fatty acid, or a derivative thereof, surface-modified with a water-soluble substance, etc. There are provided a method of producing a fine particles, surface-modified with a water-soluble substance, which contains the process of dispersing fine particles comprising a lipid, a fatty acid, or a derivative thereof, and dissolving or dispersing a surface modifier which is a lipid derivative, a fatty acid derivative, or an aliphatic hydrocarbon derivative of a water-soluble substance, in a liquid containing a polar organic solvent, and the like.

Method of producing fine particles surface-modified with water-soluble substance

A coated fine particle comprisisng: (i) a complex of a drug and a cationic lipid, wherein (a) the drug is a nucleic acid and the complex is obtained by mixing the drug and the cationic lipid in water, wherein the complex has a diameter of 10 nm to 1,000 nm, and (ii) a lipid layer formed of lipid(s), wherein the lipid(s) is selected from phospholipid, glyceroglycolipid, sphingoglycolipid, cholesterol and synthetic lipid, wherein the complex is coated with the lipid layer.

Fine particles coated with lipid membrane

The present invention provides formulation parameters and manufacturing conditions for stable pharmaceutical compositions comprising N-{4-(2,2-dimethyl-propionyl)-(5R)-5-[(2-ethylamino-ethanesulfonylamino)-methyl]-5-phenyl-4,5-dihydro-[1,3,4]thiadiazol-2-yl}-2,2-dimethyl-propionamide that minimize undesirable chiral conversion to the less active S enantiomeric form.

Stable formulations of thiadiazole derivative

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.

Compound modified with glycerol derivative

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.

Method of coating fine particles with lipid film

The present invention provides a pharmaceutical preparation comprising a compound which can be obtained by reacting a compound having a free amino group with a sugar having the reducing power. The preparation is capable of improving the in vivo durability of various compounds and releasing the compounds in response to changes in pH, and thus is useful for causing the compounds to act specifically on target parts.

Medicinal preparations

Growing community of inventors

Sunto-gun, Japan

Hiroko Kusano