Manufacture of polyglutamate-therapeutic agent conjugates
A technology of polyglutamic acid and conjugates, which is applied in the field of large-scale production of polyglutamic acid therapeutic agent conjugates, and can solve problems such as the influence of dust pollution, polluted operation rooms, and difficult packaging
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Embodiment 1
[0100] Example 1 Preparation of poly-L-glutamic acid
[0101] Poly-L-glutamic acid sodium salt (85.9 g) (Sigma Chemicals, MW 37 kd determined by viscometry) was dissolved in USP purified water (534 ml; 6.2 ml / g), and the solution was cooled to 0° C. ~5°C. Dilute hydrochloric acid solution (1M) was added dropwise with vigorous stirring and maintaining the temperature TM Freeze dry wet solids in a lyophilization system until constant weight is obtained. The weight percent sodium does not exceed 7000 ppm as determined by ICP.
Embodiment 2
[0102] Example 2 Preparation of poly-L-glutamic acid-2'-paclitaxel conjugate
[0103]Poly-L-glutamic acid (16.82 g) prepared as described in Example 1 above was suspended in anhydrous N, N-dimethylformamide (180 ml), paclitaxel (9.923 g, 11.6 mmol) and N, N- In dimethylaminopyridine (283mg, 2.32mmol). The reaction mixture was stirred for 30 minutes. A solution of N,N-diisopropylcarbodiimide (1.903 g, 15.08 mmol) in N,N-dimethylformamide (50 mL) was added over 3 hours using a syringe pump. After the addition, stir until the reaction is complete (approximately 4 hours at room temperature). The reaction was cooled to 5° C. to 10° C., and 10% sodium chloride solution (345 ml) was slowly added to precipitate the poly-L-glutamic acid-paclitaxel conjugate by transferring the mixture into a centrifuge tube and centrifuging it at 1500 g. Separate the precipitate. The wet solid was resuspended in water (150ml), and 1M sodium bicarbonate solution (120ml) was added slowly under vigoro...
Embodiment 3
[0106] Example 3 Preparation of poly-L-glutamic acid-2'-paclitaxel conjugate (production process)
[0107] Poly-L-glutamic acid (42 g), prepared as described in Example 1 above, was charged to a three-necked three-liter round bottom flask equipped with a mechanical stirrer, feeding funnel, and temperature probe. N,N-dimethylformamide (350ml) was added and stirred for 10 minutes, paclitaxel (24.66g) and N,N-dimethylaminopyridine (0.70g) were added and stirred for 10 minutes. A solution of N,N-diisopropylcarbodiimide (4.73 g) in N,N-dimethylformamide (143 ml) was added with a feeding funnel at room temperature over 1 hour and stirred for 4 hours. The reaction mixture was cooled to 5°C-10°C, then a cold 10% sodium chloride solution (1.2 L) was added dropwise using a feed funnel, and the temperature was maintained at 5°C-10°C by cooling the flask in an ice-salt mixture. After adding the sodium chloride solution, 1N hydrochloric acid solution (35 ml) was added dropwise until the p...
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