Medicinal composition and preparation method and application thereof
A composition and drug technology, applied in the field of pharmaceutical composition and its preparation and application, can solve the problems of limiting the dosage and frequency of use of chemotherapy drugs, achieve strong lethality, facilitate stable existence, and reduce systemic toxicity
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[0036] The invention provides a preparation method of a pharmaceutical composition, the method comprising loading the drug on a carrier, characterized in that the carrier is poly(aspartic acid-co-lactic acid) having a structure shown in formula (1) - phosphatidylethanolamine graft polymer, the drug is a water-soluble drug,
[0037] Formula 1),
[0038] Formula (2),
[0039] Wherein, the value ranges of n, x, y and z, and the ranges of R and R' are the same as above, and will not be repeated here.
[0040] According to the present invention, before the drug and the carrier are loaded, the carrier, i.e. poly(aspartic acid-co-lactic acid)-phosphatidylethanolamine graft polymer, will be synthesized at first, and the synthesis method of the carrier comprises the following steps,
[0041] (1) Under the protection of an inert gas, under stirring conditions, aspartic acid is contacted with lactide to obtain poly(aspartic acid-co-lactic acid) graft polymerization containing a str...
preparation Embodiment 1
[0087] Synthesis of poly(aspartic acid-co-lactic acid)-dipalmitoylphosphatidylethanolamine copolymer.
[0088](1) L-aspartic acid (3.33g, 0.025mol) (Alfar Aesar company, 98% by weight, analytically pure), L-lactide (7.2g, 0.05mol) (Alfar Aesar company, 97% by weight , analytically pure) was added to a 50mL single-necked round-bottomed flask, vacuumed for 1 hour to remove oxygen, fed with nitrogen, and stirred and reacted in an oil bath at 180°C under nitrogen protection, the solution turned into a yellow transparent liquid. After 2.5 hours of reaction, the temperature was lowered to 160° C. for 21 hours of reaction, and the reaction liquid was a viscous light brown liquid. It was taken out from the oil bath and cooled to produce a tan solid, which was dissolved in 15 mL of N,N-dimethylformamide (Beijing Chemical Plant, analytically pure), and filtered to remove unreacted lactide. The filtrate was precipitated in 250 mL of deionized water and washed three times with 100 mL of ...
Embodiment 1
[0103] Preparation of pharmaceutical composition by double emulsification method.
[0104](1) Dissolve 5 mg of poly(aspartic acid-co-lactic acid)-dipalmitoylphosphatidylethanolamine copolymer in 1.5 mL of dichloromethane, and dissolve 2 mg of doxorubicin (Beijing Huafeng Lianbo Technology Co., Ltd.) Mix the two in 0.5ml of water, and use an ultrasonic breaker (Ningbo Xinzhi Biotechnology Co., Ltd.) to ultrasonically break for 3min to make the primary emulsion; (2) mix the primary emulsion with 3mL of 3% polyethylene The alcohol PVA aqueous solution was mixed, and ultrasonically crushed with an ultrasonic cell breaker for 3 minutes to form a double emulsion; (3) the double emulsion was mixed with 10 mL of a 0.6% by weight PVA aqueous solution, and vortexed for 5 minutes; (4) used at room temperature Rotary evaporator removes dichloromethane in the mixed solution in the previous step; (5) centrifuge the mixed solution from which dichloromethane has been removed at room temperatu...
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