Nof Corporation

Daiichi Pharmaceutical Co., Ltd.

Miho Takahashi

Norio Suzuki

Hiroshi Kikuchi

Tohru Yasukohchi

Chika Itoh

Kazuhiro Kubo

Hitoshi Yamauchi

Syunsuke Ohhashi

Yusuke Ohkawa

A phospholipid derivative represented by the following formula (1): wherein [PG]k represents a residue of polyglycerin having a polymerization degree of k, wherein k is 2 to 50, RCO and RCO independently represent an acyl group having 8 to 22 carbon atoms, symbol 'a' independently represents an integer of 0 to 5, symbol 'b' independently represents 0 or 1, M represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium, and k1, k2, and k3 represent numbers satisfying the following conditions: 1&#x2266;k1&#x2266;(k+2)/2, 0&#x2266;k2, and k1+k2+k3=k+2. The phospholipid derivative is highly safe for living bodies and can be suitably utilized in drug delivery systems such as liposome, and the like.

Phospholipid derivatives and process for the production there

A phospholipid derivative represented by the formula (1) (Z represents a residue of a compound having 3 to 10 hydroxyl groups; AO represents an oxyalkylene group having 2 to 4 carbon atoms; RCO and RCO represent an acyl group having 8 to 22 carbon atoms; X represents hydrogen atom, an alkali metal atom, ammonium or an organic ammonium; 'a' represents an integer of 0 to 4; 'b' represents 0 or 1; Q represents hydrogen atom or methyl group; m represents an average number of moles of the oxyalkylene group added; and m, k1, k2, and k3 are numbers satisfying the following conditions: 3&#x2266;m&#x2266;200, 9&#x2266;m&#xd7;(k1+k2+k3)&#x2266;1000, 1&#x2266;k1&#x2266;2, 0&#x2266;k2&#x2266;9 and 0&#x2266;k3&#x2266;9, and 3&#x2266;k1+k2+k3&#x2266;10), which is highly safe for living bodies, and is suitably used for solubilization and dispersion of physiologically active substances and the like, or in the fields of drug delivery systems such as liposomes and cosmetics. 

Phospholipid derivative

A phospholipid derivative represented by the following formula (I) wherein RCO and RCO independently represent an acyl group; Rrepresents hydrogen atom, or a hydrocarbon group; symbol 'a' represents an integer of 0 to 4; symbol 'b' represents 0 or 1, provided that when a is 0, b is 0; X represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium; AO and AO represent an oxyalkylene group containing oxyethylene group, wherein the ratio of the oxyethylene group to the oxyalkylene group in AO and AO is 0.5 or larger in terms of a weight ratio; AO represents an oxyalkylene group; symbols &#x201c;m&#x201d; and &#x201c;q&#x201d; represent an average molar number of added oxyalkylene groups; and symbol &#x201c;n&#x201d; represent an average molar number of added oxyalkylene groups; provided that m, n and q satisfy the following conditions: 5&#x2266;m&#x2266;600, 1&#x2266;n&#x2266;45, 0&#x2266;q&#x2266;200, 10&#x2266;m+n+q&#x2266;600, 0.04&#x2266;n/(m+n+q), and q/(m+n+q)&#x2266;0.8, which can thicken the water shell of liposome surface by suppressing the spreading of the polyalkylene oxide structure on the surface and thus increase stability of the liposome 

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Shizuoka, Japan

Miho Takahashi