Docetaxel liposome containing chitosan derivative, lyophiled preparation and preparation method thereof
A technology of chitosan derivatives and docetaxel, applied in liposome delivery, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc. The method is not suitable for industrialized large-scale production, poor liposome stability and other problems, and achieves the effects of reducing unsafe factors, reducing dosage and high stability
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Embodiment 1
[0046] Weigh 15mg of docetaxel, 375mg of lecithin and 45mg of cholesterol and dissolve them in 10ml of ethanol solution, mix well after passing through nitrogen gas, drain the ethanol with a rotary evaporator in a water bath at a temperature of 45°C, and form a uniform phospholipid film, use Phosphate buffer solution of pH7.4 was used to elute 10ml of phospholipid membrane. The obtained liposome suspension was poured into an APV2000 homogenizer, homogenized 5 times under the pressure of the primary valve 1760bar and the secondary valve 270bar, and then extruded through the extruder with a 200nm filter membrane. After the liposome suspension is prepared, 50 mg of palmitic acid acylated chitosan is dissolved and dispersed uniformly with an acetic acid solution of pH 6.5. The liposome suspension was flushed with nitrogen gas and stirred slowly at room temperature, then dropped into the liposome suspension at a constant speed, and incubated at room temperature for 1 hour after the...
Embodiment 2
[0048] Weigh 10mg of docetaxel, 200mg of soy lecithin, 50mg of PEG-DSPE and 30mg of cholesterol and dissolve in 10ml of ether solution, slowly lower the solution into 10ml of pH7.4 phosphate buffer, and evaporate the ether at room temperature. The obtained liposome suspension was poured into an APV2000 homogenizer, homogenized 5 times under the pressure of the primary valve 1760bar and the secondary valve 270bar, and then extruded through the extruder with a 200nm filter membrane. After the liposome suspension is prepared, 40 mg of the stearic acid acylated chitosan is dissolved and dispersed uniformly with an acetic acid solution of pH 6.5. The liposome suspension was flushed with nitrogen gas and stirred slowly at room temperature, then dropped into the liposome suspension at a constant speed, and incubated at room temperature for 1 hour after the dropwise addition to obtain a suspension for use. The phosphate buffer solution with pH 7.5 is added to the suspension and mixed,...
Embodiment 3
[0050] Weigh 10mg of docetaxel, 500mg of lecithin and 40mg of cholesterol and dissolve in 15ml of ethanol solution, drop the solution into 8ml of phosphate buffer solution with pH 7.4 slowly at a uniform speed, and evaporate the ethanol at room temperature. The obtained liposome suspension was poured into an APV2000 homogenizer, homogenized 5 times under the pressure of the primary valve 1760bar and the secondary valve 270bar, and then extruded through the extruder with a 200nm filter membrane. After the liposome suspension is prepared, 40 mg of lauric acid acylated chitosan is dissolved and dispersed evenly with 5 ml of acetic acid solution of pH 6.8. The liposome suspension was flushed with nitrogen gas and stirred slowly at room temperature, dropped into the liposome suspension at a constant speed, and incubated at room temperature for 2 hours after the dropwise addition to obtain a suspension for use. The phosphate buffer solution with pH 7.5 is added to the suspension and...
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