Polyester-polyether temperature-sensitive gel with slow release of batimastat and preparation method thereof
A sustained-release preparation, batimastat technology, applied in pharmaceutical formulations, aerosol delivery, liquid delivery, etc., can solve problems such as poor oral bioavailability and inconvenient treatment
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Embodiment 1
[0035]30g of polyethylene glycol (Mn 1500) was dewatered under vacuum at 120°C for 4 hours in an oil bath, and after the temperature dropped to 80°C, under the protection of argon, according to the designed polylactide-glycolide (PLGA) terminal molecular weight and LA / GA ratio, add the calculated amount of glycolide (GA) and lactide (LA), and continue vacuuming to remove water for 15 minutes. Add stannous octoate (w / w, 30 mg / mL anhydrous toluene solution) with 0.15% monomer weight, and remove toluene by vacuuming at 80°C. The temperature of the oil bath was raised to 150°C for 12 hours. After the reaction was completed, the temperature was lowered to 120° C., and vacuum was applied for 2 hours. Pour the reaction product into hot water at 80°C while it is hot, stir and wash it thoroughly, let it stand for 10 minutes, discard the upper liquid, and freeze-dry the solid viscous precipitate at the bottom to obtain the product.
Embodiment 2
[0037] Using the preparation method in Example 1, controlling the feeding amount of the monomers glycolide (GA) and lactide (LA), to obtain polyester-polyether block copolymers with different molecular weight compositions and gelation temperatures.
[0038] Table 1 Molecular weight and gelation temperature of different polymers
[0039]
[0040] a) Gelling temperature: measured by inverted tube method, polymer concentration 20wt%
Embodiment 3
[0042] Utilizing the preparation method in Example 1, controlling the feed ratio of the monomers glycolide (GA) and lactide (LA), to obtain polyester-polyether block copolymers with different LA / GA ratios and degradation times.
[0043] Table 2 Different polymer monomer ratios and degradation time
[0044]
[0045] a) Degradation time: pH7.4 phosphate buffer solution is the degradation simulation solution, and the polymer concentration is 20wt%
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