PHOSPHOLIPID LIPOSOME CONTAINING THE COMBINATION OF NEGATIVELY IONIC POLYMER AND PHOSPHOLIPID AND PREPARATION PROCESS THEREOF

摘要

PURPOSE: A phospholipid liposome containing the combination of negatively ionic polymer and phospholipid and a preparation process thereof are provided, thereby preparing the phospholipid liposome having improved tolerance to hydrogen concentration(pH), bile acid, and pancreatic juice, and prolonged retention time. Therefore, absorption of drugs through oral administration can be improved. CONSTITUTION: The phospholipid liposome contains the combination of negatively ionic polymer and phospholipid represented by formula(I), wherein n is 1 to 10,000; R1 and R2 are (-CH2-)m; m is 1 to 30; and R3 is COOH, OH or SO3H, the combination of negatively ionic polymer and phospholipid is contained in an amount of 0.1 to 100%; the negatively ionic polymer is selected from polyvinyl sulfonic acid, polyacrylic acid and copolymer thereof, polymer synthesized by attaching carboxyl or sulfo to the terminal group or side chain of the polymer, and copolymer of polyaspartic acid and polyglutamic acid wherein the main chain is formed by amide bond; and the phospholipid is selected from disteroyl-sn-phosphatidylethanol amine, dipalmitoyl phosphatidylethanol amine, phosphatidylethanol amine, phosphatidyl serine, phosphatidyl glycerol, phosphatidyl choline, dipalmitoyl phosphatidyl serine, palmitoyl phosphatidyl glycerol and dipalmitoyl phosphatidyl choline.