Anthracycline antibiotic coupled nonlinear multi-block copolymer and its preparation method and application
A technology of multi-block copolymers and anthracyclines, applied in the direction of drug combinations, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of low solubility, limited application, short half-life, etc., and achieve the effect of easy dissolution and good therapeutic effect
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Embodiment 1
[0039] 1) A mixture of 25 g of 1,6-bis(p-carboxyphenoxy)hexane in 500 ml of acetic anhydride is refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0040]2) 3.5 g of methoxypolyethylene glycol amine, 55 mg of hydroxyglutaric acid, 165 mg of dicyclohexylcarbodiimide and 8 mg of pyridine were mixed, stirred overnight at room temperature; then washed with ether and dried under vacuum to obtain polymer;
[0041] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 180°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0042] 4) Put doxorubicin and the polymer of step 3 into 20ml dimethyl sulfoxide solution for 48 hours; then put it in an oven for 3 hours; at minus 10-20 degrees, ultrasonic for 15 minutes; homogenizer at high speed Stir for 1 minute, then put into 5% cholic acid solution and stir at 400 rpm for 2 hours; collect by centrifugation and fr...
Embodiment 2
[0044] 1) A mixture of 30 g of 1,6-bis(p-carboxyphenoxy)hexane in 300 ml of acetic anhydride was refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0045] 2) Mix 3 g of methoxypolyethylene glycol amine, 30 mg of hydroxyglutaric acid, 130 mg of dicyclohexylcarbodiimide and 5 mg of pyridine, stir overnight at room temperature; then wash with ether and dry under vacuum to obtain a polymer thing;
[0046] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 150°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0047] 4) Put pirarubicin and the polymer into a solution mixed with 5ml of ethanol and 5ml of dichloromethane; then put it in an oven for 24 hours; at minus 10-20 degrees, ultrasonic for 2 minutes; then homogenizer Stir at high speed for 2 minutes, put the product in 3% cholic acid solution and stir at 400 rpm for 2 hours; collect by centrifu...
Embodiment 3
[0049] 1) A mixture of 1,6-bis(p-carboxyphenoxy)hexane 17 g in 500 ml acetic anhydride is refluxed to form acetylated 1,6-bis(p-carboxyphenoxy)hexane;
[0050] 2) Mix 2 g of methoxypolyethylene glycol amine, 28 mg of hydroxyglutaric acid, 90 mg of dicyclohexylcarbodiimide and 4 mg of pyridine, add 10 ml of chloroform, stir overnight at room temperature; then wash with ether and dry under vacuum , to obtain the polymer;
[0051] 3) Mix the products of step 1) and step 2) into a flask, melt and polymerize under reduced pressure at 170°C for 1 hour; dissolve the polymer in chloroform after cooling to room temperature, wash with petroleum ether and dry;
[0052] 4) Put arubicin and the polymer of step 3 into a solution mixed with 10ml of dichloromethane and 6ml of dimethyl sulfoxide; then put it in an oven to dry for 1 hour; at minus 20-30 degrees, ultrasonic 1 minute, then high-speed stirring with a homogenizer for 5 minutes, the product was put into 2% cholic acid solution and ...
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