Oral slow release preparation, entrapment material and preparation method
A technology for encapsulating materials and slow-release drugs, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. It can solve problems such as short duration of action, improve compliance, prolong Action time, high biocompatibility effect
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[0041] Example one
[0042] Weigh exenatide 5mg, sodium alginate: sodium hyaluronate = 2:3, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three-distilled water with a concentration of 25 mg / ml, stir and dissolve Obtain the water phase, add 2% Span-80 to 20ml of liquid paraffin to obtain the oil phase, add the water phase dropwise to the oil phase, magnetically stir at 500rpm / min to make the water phase uniformly dispersed in the oil phase; add to the oil phase 2ml 25% glutaraldehyde solution and 10ml 1M dilute hydrochloric acid, react at 20℃; after the reaction, add 20ml ethanol, stir at room temperature for 15 minutes, let stand for layering, discard the upper layer, filter the lower layer and wash it several times with ethanol. Preparation is complete after freeze-drying. Weigh 100mg of the drug-loaded Exenatide microspheres and 100mg of the blank microspheres prepared under the same conditions, and place them in a 20ml system to determine the en...
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[0043] Example two
[0044] Weigh exenatide 10mg, sodium alginate: sodium hyaluronate=1:1, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three-distilled water to a concentration of 20mg / ml, stir and dissolve Obtain the water phase, add 1% Span-80 to 50ml of liquid paraffin to obtain the oil phase, add the water phase dropwise to the oil phase, magnetically stir at 700rpm / min to make the water phase uniformly dispersed in the oil phase; add to the oil phase 20ml 25% glutaraldehyde solution and 10ml 1M dilute hydrochloric acid, react at 50℃; after the reaction, add 20ml absolute ethanol, stir at room temperature for 15 minutes, let stand for layering, discard the upper layer, filter the lower layer and wash with ethanol. The preparation is complete after freeze-drying. The encapsulation rate of Exenatide microspheres determined by BCA method is 78%, and the particle size <200μm.
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[0045] Example three
[0046] Weigh exenatide 10mg, sodium alginate: sodium hyaluronate=1:3, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three-distilled water, the concentration is 40mg / ml, stir to dissolve Obtain the water phase, add 1% Span-80 to 20ml of liquid paraffin to obtain the oil phase, add the water phase dropwise to the oil phase, magnetically stir at 500rpm / min to make the water phase uniformly dispersed in the oil phase; add to the oil phase 5ml 25% glutaraldehyde solution and 5ml 1M dilute hydrochloric acid, react at 25℃, add 20ml ethanol after the reaction, stir at room temperature for 15 minutes, let stand for layering, discard the upper layer, filter the lower layer and wash it several times with ethanol, freeze After drying, the preparation is complete. The encapsulation rate of Exenatide microspheres determined by BCA method is 86%, and the particle size is <220μm.
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