Gel drug sustained-release preparation and preparation method and application thereof
A slow-release preparation and gel technology, applied in the field of medicine, to achieve the effect of reducing systemic side effects, long-term anti-inflammation and anti-fibrosis
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Embodiment 1
[0047] Weigh 15g of dihydroxypolyethylene glycol (PEG1500) in a 250mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3h under mechanical stirring. Then cool down to 80°C with argon gas, add 37g of D,L-lactide and glycolide with a molar ratio of 1:1 in total, stir well; add toluene solution containing 50mg of stannous octoate, and repeatedly vacuumize 3 times After removing the toluene, the temperature was raised to 150°C and reacted for 12h under the protection of argon. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the BAB type triblock polymer PLGA - PEG-PLGA (copolymer-1), about 85% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned BAB type triblock polymer by gel permeation chromatog...
Embodiment 2
[0049] Weigh 10 g of dihydroxypolyethylene glycol (PEG1000) in a 250 mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3 hours under mechanical stirring. Then cool down to 80°C with argon, add 25g of D,L-lactide, stir well; add toluene solution containing 50mg of stannous octoate, repeat vacuuming 3 times to remove toluene, then heat up to 150°C under the protection of argon Reaction 12h. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the BAB type triblock polymer PLA - PEG-PLA (copolymer-2), about 80% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned BAB type triblock polymer by gel permeation chromatography (GPC, polystyrene is a standard sample) n ,M w ) are 4750 and 6120 respectivel...
Embodiment 3
[0051] Weigh 15 g of monomethoxypolyethylene glycol (mPEG750) in a 250 mL three-necked bottle, seal each port with vacuum ester, and remove water under vacuum at 130° C. for 3 h under mechanical stirring. Then cool down to 80°C with argon gas, add 30g of D,L-lactide and 10g of glycolide, stir well; add toluene solution containing 40mg of stannous octoate, repeat vacuuming 3 times to remove toluene, then heat up to 150°C The reaction was carried out under the protection of argon for 12h. Then lower the temperature to 120°C and vacuumize for 3 hours to remove unreacted monomers, pour it out while it is hot, wash the crude product with 80°C deionized water three times, and obtain the final product after freeze-drying to obtain the AB type block polymer mPEG- PLGA (copolymer-3), about 79% yield. Measure the number average and weight average molecular weight (M) of the above-mentioned AB type block polymer by gel permeation chromatography (GPC, polystyrene is a standard sample) n...
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