Multifunctional polyethylene glycol-dual vitamin E succinate derivative and application thereof in drug delivery
A technology of polyethylene glycol and succinate, applied in drug delivery, medical preparations of non-active ingredients, pharmaceutical formulations, etc., can solve the problems of high toxicity and low efficiency, and achieve easy operation and high encapsulation rate , the effect of easy preparation
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[0041] Example 1 Preparation of monomethoxy polyethylene glycol 2000-lysine-bis-vitamin E succinate block copolymer
[0042] (a) Dissolve 2.1 g of vitamin E succinate in dichloromethane, add 1 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.6 g of 1-Hydroxybenzotriazole was magnetically stirred for 1 h in an ice bath at 0 °C. 1.3 g of benzyloxylysine ester hydrochloride sulfonate was mixed with 3 mL of triethylamine, then added to the above activation solution, N 2 Magnetic stirring at 30 °C for 24 h under the protection. After the reaction was completed, it was washed and dried. After purification, benzyloxylysine divitamin E succinate (structural formula as formula I) was obtained.
[0043]
[0044] (b) Dissolve the product of step (a) in ethyl acetate, in palladium carbon (Pd / C) and H 2 Under the action of magnetic stirring at 30 °C for 6 h. Filtration, collecting the filtrate, and rotary evaporation to obtain lysine divitamin E succinate (...
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[0049] Example 2 Preparation of polyethylene glycol 5000-lysine-bis-vitamin E succinate block copolymer
[0050] (a) Dissolve 2.1 g of vitamin E succinate in dichloromethane, add 1 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.6 g of 1-Hydroxybenzotriazole was magnetically stirred for 1 h in an ice bath at 0 °C. 1.3 g of benzyloxylysine ester hydrochloride sulfonate was mixed with 3 mL of triethylamine, then added to the above activation solution, N 2 Magnetic stirring at 30 °C for 24 h under the protection. After the reaction was completed, it was washed and dried. After purification, benzyloxylysine divitamin E succinate (structural formula as formula I) was obtained.
[0051]
[0052] (b) The product of step (a) was dissolved in ethyl acetate, and magnetically stirred at 30 °C for 6 h under the action of palladium carbon and hydrogen. Filtration, collecting the filtrate, and rotary evaporation to obtain lysine divitamin E succinate (struc...
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[0057] Example 3 Preparation of monomethoxy polyethylene glycol amidation-lysine-bis-vitamin E succinate block copolymer
[0058] (a) Dissolve 2.1 g of vitamin E succinate in dichloromethane, add 1 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) and 0.6 g of 1-hydroxybenzotriazole (HOBT) was magnetically stirred in an ice bath at 0 °C for 1 h. 1.3 g of benzyloxylysine ester hydrochloride sulfonate was mixed with 3 mL of triethylamine, then added to the above activation solution, N 2 Magnetic stirring at 30 °C for 24 h under the protection. After the reaction was completed, it was washed and dried. After purification, benzyloxylysine divitamin E succinate (structural formula as formula I) was obtained.
[0059]
[0060] (b) Dissolve the product of step (a) in ethyl acetate in palladium on carbon (Pd / C) and H 2 Under the action of magnetic stirring at 30 °C for 6 h. Filtration, collecting the filtrate, and rotary evaporation to obtain lysine d...
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