Injection paclitaxel nanocrystal and preparation method thereof
A technology of nanocrystals and paclitaxel, which is applied in the field of medicine, can solve problems such as the inability to improve solubility and bioavailability, difficulty in obtaining nanocrystal suspensions, and difficulty in redissolving particle sizes, so as to reduce adverse drug reactions and have good application prospects , good stability
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Embodiment 1
[0057] Example 1: Preparation of paclitaxel nanocrystal suspension (1)
[0058] Prescription composition:
[0059]
[0060] Preparation:
[0061] According to the above ratio, at room temperature, the two stabilizers, poloxamer and docusate sodium, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 1200 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 50 mg / ml. Then, under the condition of high-speed stirring at 1200 rpm, 1 ml of the organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 1200 rpm for 20 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 100 W for 20 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 200.9nm.
Embodiment 2
[0062] Example 2: Preparation of paclitaxel nanocrystal suspension (2)
[0063] Prescription composition:
[0064]
[0065] Preparation:
[0066] According to the above ratio, at room temperature, the two stabilizers, poloxamer and docusate sodium, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 1000 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 100 mg / ml. Then, under the condition of high-speed stirring at 1000 rpm, 0.5 ml of organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 1000 rpm for 30 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 100 W for 30 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 217.5nm.
Embodiment 3
[0067] Example 3: Preparation of paclitaxel nanocrystal suspension (3)
[0068] Prescription composition:
[0069]
[0070] Preparation:
[0071] According to the above proportions, at room temperature, two stabilizers, hypromellose and sodium lauryl sulfate, were dissolved in 10 ml of water, and the resulting aqueous mixture was stirred and mixed at a high speed at 800 rpm as the water phase. An appropriate amount of paclitaxel was dissolved in ethanol as the organic phase, with a concentration of 100 mg / ml. Then, under the condition of high-speed stirring at 800 rpm, 1 ml of organic phase was added to the above-mentioned aqueous phase, and then the high-speed stirring was continued at 800 rpm for 60 min, and most of the ethanol was removed. Then the paclitaxel nanocrystal suspension obtained was sonicated at 120 W for 10 min to fully stabilize it. The particle size of paclitaxel nano crystal suspension can reach 264.5nm.
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