Sustained-release pasireotide microspheres and preparation method thereof
A pasireotide and microsphere technology, applied in microcapsules, cyclic peptide components, pharmaceutical formulations, etc., can solve the problems of long action, short action time, slow release of microspheres, etc., and achieve high encapsulation efficiency and uniform particle size. , the effect of simple preparation process
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Embodiment 1
[0056] Preparation of the inner water phase: Weigh 100 mg of pasireotide and water, vortex and shake to dissolve, weigh 100 mg of mannitol in the prescribed amount, add it to the pasireotide aqueous solution to disperse, and dissolve in a water bath to obtain the inner water phase;
[0057] Preparation of the external water phase: Measure an appropriate amount of purified water, add 50 mg of polyvinyl alcohol, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;
[0058] Preparation of the oil phase: take 0.8g PLGA and dissolve it in 30g of dichloromethane as the oil phase;
[0059] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (2000rpm) for 20 seconds to obtain colostrum;
[0060] Preparation of double emulsion: Add colostrum to polyvinyl alcohol solution under stirring to obtain double emulsion, continue to stir the double emulsion to remove organic solvent, centrifuge...
Embodiment 2
[0062]Preparation of the inner water phase: Weigh 120 mg of pasireotide and water, vortex shake to dissolve, weigh 180 mg of hypromellose in the prescribed amount, add it to the aqueous solution of pasireotide to disperse, and dissolve in a water bath to obtain the inner water phase ;
[0063] Preparation of the external water phase: Measure an appropriate amount of purified water, add 200 mg of Tween, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;
[0064] Preparation of the oil phase: Weigh 1.0g PLGA and dissolve it in 30g of ethyl acetate as the oil phase;
[0065] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (16000rpm) for 30 seconds to obtain colostrum;
[0066] Preparation of double emulsion: Add colostrum to 200 mg Tween solution under stirring to obtain double emulsion, continue to stir the double emulsion to remove organic solvent, centrifuge, wash and c...
Embodiment 3
[0068] Preparation of the inner aqueous phase: Weigh 120 mg of pasireotide and water, vortex shake to dissolve, weigh 180 mg of mannitol in the prescribed amount, add it to the aqueous solution of pasireotide to disperse, dissolve in a water bath, and then add 100 mg of human serum white albumen, add suspending agent gum arabic 100mg simultaneously, obtain inner aqueous phase;
[0069] Preparation of the external water phase: Measure an appropriate amount of purified water, add polyvinyl alcohol with a prescribed amount of 120 mg, heat and stir to dissolve, pass through the gauze to obtain the external water phase solution;
[0070] Preparation of the oil phase: Weigh 1.1g PLGA and dissolve it in 30g of dichloromethane as the oil phase;
[0071] Preparation of colostrum: transfer the dissolved oil phase to the inner water phase and use high-speed stirring (16000rpm) for 30 seconds to obtain colostrum;
[0072] Preparation of double emulsion: Add colostrum to polyvinyl alcohol...
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