Benserazide sustained-release microspherical composition and preparation method thereof
A technology for slow-release microspheres and benserazide, which is applied in the directions of drug combinations, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the inconvenience, and there is no relevant literature report on the preparation of microspheres of benserazide, actions and methods. Memory problems and other problems, to avoid the effect of the effect, good re-dispersion, and improve the effect of treatment
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Embodiment 1
[0029] ①Use a microscope to observe whether 100mg benserazide is 0.4-10μm, if not, use a pulverizer to crush it into 0.4-5μm;
[0030] ②Preparation of benserazide sustained-release microsphere composition
[0031] (a) Mix 37.5 mg of polylactic acid (PLA, molecular weight 90,000-140,000) into an organic solution of 15% dichloromethane by weight and 12.5 mg of benserazide microparticles obtained in ① and mix and stir , vortex or ultrasonic for 1-5 minutes to form a uniform suspension, that is, solid-in-oil (S / O) emulsion; the theoretical percentage of benserazide prepared into sustained-release microspheres is 25%.
[0032] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) with a weight percent concentration and Stir, vortex or sonicate for 0.1-5 minutes to form double emulsion;
[0033] (c) adding the double emulsion of step (...
Embodiment 2
[0040] ①Preparation of benserazide microparticles
[0041] 100mg of benserazide, first use a microscope to observe whether it is 0.4-10μm, if not, you can use a pulverizer to crush it into 0.4-5μm;
[0042] ②Preparation of benserazide sustained-release microsphere composition
[0043] (a) 495mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide 48-54% Mole; molecular weight 5000-6000) was weighed to prepare a concentration of 30% by weight The organic solution of dichloromethane and 5 mg of benserazide microparticles obtained in ① were mixed and stirred, vortexed or sonicated for 1-5 minutes to form a uniform suspension, that is, solid-in-oil (S / O) emulsion; The theoretical percentage of benserazide is 1% sustained-release microspheres.
[0044] (b) adding the emulsion obtained in step (a) to 10 mL of aqueous solution of 1% sodium chloride and 2% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholysis degree 98-99%) w...
Embodiment 3
[0052] ①Preparation of benserazide microparticles
[0053] 100mg of benserazide, first use a microscope to observe whether it is 0.4-10μm, if not, you can use a pulverizer to crush it into 0.4-5μm;
[0054] ②Preparation of benserazide sustained-release microsphere composition
[0055] (a) 37.5 mg of polyglycolic acid-polylactic acid (PLGA, d, l-lactide: 46-52% Mole and glycolide 48-54% Mole; molecular weight 5000-6000) was formulated to have a weight percent concentration of 15 % organic solution of dichloromethane and 12.5 mg of benserazide microparticles obtained in ① were mixed and stirred, vortexed or sonicated for 1-5 minutes to form a uniform suspension, that is, solid-in-oil (S / O) emulsion; The theoretical percentage of benserazide prepared is 25% sustained-release microspheres.
[0056] (b) adding the emulsion obtained in step (a) to 10 mL of an aqueous solution of 5% sodium chloride and 1% polyethylene glycol (the molecular weight of PVA is 146,000-186,000, alcoholy...
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