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