Scutellarin prodrug using poly-aspartate derivant as the carrier and method for preparing the same
A technology of polyaspartic acid and scutellarin, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Availability, simple effect of preparation method
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Embodiment 1
[0034] Weigh 200 grams of aspartic acid, add 10 grams of concentrated phosphoric acid as a catalyst, carry out polycondensation reaction at 180 ° C, and gradually reduce the pressure to 1 × 10 4 Pa, after 10 hours of reaction, succinimide PSI can be prepared with a yield of 95%.
[0035] Dissolve 5.0 g of PSI in 25 ml of DMF, cool to 0°C, add 13.0 g of diethanolamine dropwise at this temperature, and react at room temperature for 2 h. The mixture was added dropwise to 150ml of n-butanol with constant stirring, and after standing for 1 h, it was filtered and washed with a large amount of acetone until the pH value of the filtrate was neutral. Vacuum drying at room temperature for 24 hours yielded 8.7 g of poly(α,β-N-dihydroxyethyl-DL-asparagine) PDHEA white powder with a yield of 85% and a molecular weight of 2000.
[0036] Dissolve 0.70 g of scutellarin in 20 ml of DMF, and then add the solution dropwise to a solution of 0.30 g of PDHEA in 10 ml of DMF. The above mixture was...
Embodiment 2
[0038] Same as the preparation method of PDHEA in Example 1, the difference is that the reaction time of PSI and diethanolamine is 2.5 hours to obtain PDHEA with a molecular weight of 5000.
[0039]Dissolve 0.47 g of scutellarin in 15 ml of DMF, and then add the solution dropwise to a solution of 0.21 g of PDHEA in 8 ml of DMF. The above mixed solution was stirred well, 0.47 g of DMAP was added, and the reaction was stirred. Dissolve 0.8 g of DCC in an appropriate amount of 20 ml of DMF to form a colorless solution, which is added dropwise to the above mixture. The reaction was stirred at 50°C. After 72 hours, filter with slow filter paper, take the clear part and place it in a pear-shaped bottle, and evaporate to dryness. Wash the light green solid on the wall of the pear-shaped bottle with n-propanol, filter, wash the solid with n-propanol until the filtrate is colorless, and dry the precipitate under vacuum at 40°C to obtain 0.35 g of light green solid scutellarin prodrug...
Embodiment 3
[0041] Same as the preparation method of PDHEA in Example 1, the difference is that the reaction time of PSI and diethanolamine is 4 hours to obtain PDHEA with a molecular weight of 20,000.
[0042] 1.41 g of scutellarin was dissolved in 60 ml of DMF, and then the solution was added dropwise to a solution of 0.92 g of PDHEA in 30 ml of DMF. The above mixed solution was stirred well, 2.8 g of DMAP was added, and the reaction was stirred. 0.50 g of DCC was dissolved in 25 ml of DMF to form a colorless solution, which was added dropwise to the above mixture. After stirring and reacting at 20°C for 12 hours, filter with slow filter paper, take the clear liquid, place it in a pear-shaped bottle, and evaporate to dryness. Wash the light green solid on the wall of the pear-shaped bottle with n-propanol, filter, wash the solid with n-propanol until the filtrate is colorless, and vacuum-dry the precipitate at 60°C to obtain 1.39 g of light green solid scutellarin prodrug PDHEAS, The ...
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