Ophthalmic temperature-sensitive in-situ gel preparation containing Remdesivir as well as preparation method and application of ophthalmic temperature-sensitive in-situ gel preparation
A technology of in-situ gel and temperature-sensitive gel matrix, which is applied in the field of temperature-sensitive in-situ gel, can solve the problems of short ocular residence time and achieve improved drug bioavailability, good tissue compatibility, and good ocular surface tolerance Effect
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Embodiment 1
[0044] 10.0 g of PEG and PPG mixture (feeding ratio 2:1) were mixed in a flask, and dried overnight at 40° C. under vacuum. Then add 200mL of anhydrous toluene to remove water by azeotropic distillation. The reactant was heated in an oil bath at 75° C. under argon, and 0.913 g of hexamethylene diisocyanate (HMDI) and two drops of dibenzothiophene (DBT) were added to the reaction system during the heating process. After the mixture continued to react for 48 hours, the product was collected, precipitated in ether and freeze-dried to finally obtain a PEG-PPG-PEG block copolymer.
Embodiment 2
[0046] Weigh 50 mg of the PEG-PPG-PEG block copolymer prepared in Example 1 and dissolve it in 1 mL of methanol, and then weigh 100 mg of remdesivir and dissolve it in 1 mL of ethanol, then mix the two solutions, and mix them uniformly by ultrasonication for 50 minutes to obtain solution 1 . Slowly add Solution 1 to 8 mL of deionized water under ultrasonication, mix well, place in a fume hood overnight, volatilize the organic solvent, add deionized water to 10 mL, and prepare remdesivir micelles (solution 2). In addition, 300 mg of PEG-PPG-PEG block copolymer was weighed and directly dissolved in 5 mL of physiological saline to prepare a hydrogel material (solution 3). Measure 5mL of solution 2 and 5mL of solution 3, stir and mix at low temperature, vortex, and sonicate to mix evenly, and then add a small amount of sorbic acid and trehalose in sequence to obtain an ophthalmic thermosensitive in-situ gel containing 0.25% remdesivir.
Embodiment 3
[0048]10.0 g of PEG, PPG mixture and 0.05 g of DHSe were mixed in a flask and placed at 40° C. under vacuum to dry overnight. Then add 200mL of anhydrous toluene to remove water by azeotropic distillation. The reactant was heated in an oil bath at 75° C. under argon, and 0.913 g of HMDI and two drops of DBT were added to the reaction system during the heating process. After the mixture continued to react for 48 h, the product was collected, precipitated in ether and freeze-dried to finally obtain a DHSe-PEG-PPG block copolymer.
[0049] Determination of DHSe-PEG-PPG block copolymer by using American JEOL 500MHz NMR 1 H NMR spectrum. Gel Permeation Chromatography (GPC) using two Phenogels connected in series TM Chromatographic column (10 3 and 300 x 7.80 mm) were performed under a Vistek GPCmax module (Malvern Panalytical, Malvern, U.K.). The eluent of GPC is tetrahydrofuran, and the flow rate is 1.0ml / min.
[0050] The DHSe-PEG-PPG block copolymer that present embodime...
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