Daiichi Seiyaku Co., Ltd.

Daiichi Pharmaceutical Co., Ltd.

Meito Sangyo Co., Ltd.

Sadao Hirota

Hiroshi Kikuchi

Hitoshi Yamauchi

Munehiro Tomikawa

Kiyoto Yachi

Shusaburo Hokukoku

Hiromi Morita

Hideki Miyaji

Yasuyoshi Kawato

A liposomal aqueous dispersion and method of making the liposomal aqueous dispersion is useful for encapsulation of drugs. The liposomal aqueous dispersion comprises: an aqueous suspension medium; multilamellar liposomes comprising an anionic phospholipid and cholesterol as essential components; neutral phospholipid in a mole ratio of 0 to 40% based on the total amount of said multilamellar liposomes; and a cation moiety-containing water-soluble drug, wherein the electrolyte concentration of said aqueous suspension medium is not more than 40 mM.

Liposomal products

A method of producing liposomal products which comprises treating a positively or negatively charged, freeze- or spray-dried liposomal preparation with an aqueous solution of a drug charged oppositely to the charge of the liposomes.

Method of producing liposomal products from freeze or spray-dried

Lipid membrane structures containing, in the lipid membrane thereof, a compound represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a fatty acid residue; R.sub.2 represents a hydrogen atom or an acyclic hydrocarbon residue; R.sub.3 represents an amino group, a guanidino group or an amidino group; and n represents an integer of from 1 to 6; provided that R.sub.1 and R.sub.2 do not represent hydrogen atoms at the same time, or a salt thereof. The lipid membrane structures exhibit excellent specific affinity for tumor cells and can be delivered preferentially to tumor cells.

Lipid membrane structures

An ointment comprising an adenosine 3',5'-cyclic phosphate derivative as an active ingrediment, an ointment base having water-absorbing and drying properties, a saccharide and/or inorganic high polymer is disclosed. The ointment exhibits improved stability of the adenosine 3',5'-cyclic phosphate derivative.

Cyclic amp derivative ointments

Novel mannobiose derivative represented by the general formula [I]: ##STR1## wherein groups of R.sub.1 to R.sub.5 each represents --OH, --OR.sub.6, --NHR.sub.6, (R.sub.6 represents an acyl group) or a group represented by the following formula (a), (b), (c), (d) or (e), provided that one of R.sub.1 to R.sub.5 represents --OR.sub.6 or --NHR.sub.6, one of the other 4 groups of R.sub.1 to R.sub.5 represents one of the groups represented by the formulae (a) to (e), and the remaining 3 groups of R.sub.1 to R.sub.5 represent --OH: ##STR2## wherein   represents .alpha. or .beta. bond are provided by the invention. These compounds give liposomes a specific affinity for Kupffer cells of liver, and can be produced industrially.

Mannobiose derivatives

Lipid membrane structures containing a lactose monofatty acid ester or amide are disclosed. The lipid membrane structures are delivered preferentially to the liver parenchymal cells and are useful as carriers of drugs.

A topical preparation containing, as an active ingredient, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[ 1,2,3][1,4]-benzoxazine-6-carboxylic acid or a salt thereof.

Growing community of inventors

Tokyo, Japan

Sadao Hirota