Method for preparing composite drug-loaded microsphere by emulsion chemical crosslinking process and application
A technology of chemical cross-linking and drug-loaded microspheres, which is applied in the drug slow-release preparations for embolization treatment of benign prostatic hyperplasia, and the improved S/W/O emulsification chemical cross-linking method to prepare composite drug-loaded microspheres, which can solve related problems. Dissolution, low drug loading rate and encapsulation rate, difficulty in crystallization of hydrophobic drugs, etc., to achieve dispersion without adhesion, good drug sustained release effect, and high uniformity
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[0052] (1) Preparation of the inner water phase: Dissolve PVA124 at 80°C-90°C to prepare a PVA aqueous solution, and at the same time dissolve a certain amount of CS with 1% dilute acetic acid, and mix the two solutions according to a certain ratio to prepare a PVA / CS mixture ;
[0053] (2) High-pressure homogenization: Weigh a certain amount of FNS and add it to the PVA1788 aqueous solution, and then homogenize in the high-pressure homogenization for 3min-6min;
[0054] (3) Add the high-pressure homogeneous FNS suspension in S2 to the PVA / CS solution in S1, stir and ultrasonically disperse to form a S / W mixed phase;
[0055] (4) Add the S / W mixed phase obtained in S3 to the pre-emulsified oil phase of Span80, stir to form a S / W / O emulsion, add ether-saturated glutaraldehyde (w / w, 25%), and stir for several Minutes later, add 1M hydrochloric acid solution, raise the temperature of the reaction system to 50°C-65°C for chemical crosslinking for 3h-6h;
[0056] (5) Collect and ...
Embodiment 1
[0064] Weigh 1.71g of PVA 124 solid particles and heat it in a water bath to dissolve in 12.5mL of hot water at 85°C. At the same time, weigh 0.117g of CS powder and dissolve it in 15mL of 1% acetic acid solution. Mix the two in a certain volume ratio to obtain 7.2% ( w / v) PVA / CS mixed solution, wherein the mass percentage of CS is 5%. 200 mg of FNS was added to 3 mL of 0.5% (w / v) PVA1788 solution, and homogenized at 10,000 rpm for 4 min under a high-pressure homogenizer to obtain a white FNS suspension. Add FNS to the PVA / CS solution prepared above for mechanical stirring and ultrasonication for 30 min to obtain a S / W mixed phase, in which the mass percentage of FNS and PVA / CS is 20:80. Add the S / W mixed phase into Span80 pre-emulsified n-heptane (O), where the volume ratio of S / W phase to O phase is 1:6.5. After mechanical stirring at 500rpm for 30min, S / W / O emulsion was obtained, 2.6mL of glutaraldehyde solution (w / w, 25%) was added, and after stirring for 5min, 1.8mL of 1...
Embodiment 2
[0069]Weigh 1.12g of PVA124 solid particles, heat and dissolve them in 10.4mL of hot water at 80°C, and simultaneously weigh 0.2g of CS powder and dissolve them in 10mL of 1% acetic acid solution, and mix the two in a certain volume ratio to obtain 5.6% ( w / v) PVA / CS mixed solution, wherein the mass percentage of CS is 3%. Add 150 mg of dutasteride to 4 mL of 1% (w / v) PVA1750±50 solution, and homogenize for 5 min at 15,000 rpm under a high-pressure homogenizer to obtain a white dutasteride suspension. Dutasteride was added to the PVA / CS solution prepared above, mechanically stirred and ultrasonicated for 20 min to obtain a S / W mixed phase, in which the mass percentage of dutasteride and PVA / CS was 15:85. Add the S / W mixed phase to the Span80 pre-emulsified petroleum ether (O), wherein the volume ratio of the S / W phase to the O phase is 1:5.2. After stirring mechanically at 600rpm for 30min, an S / W / O emulsion was obtained, 3.0mL of glutaraldehyde solution (w / w, 25%) was added,...
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