A kind of paclitaxel self-emulsifying preparation and its preparation method and application
A technology of self-emulsification and paclitaxel, which is applied in the direction of making drugs into special physical or ingestible devices, anti-inflammatory agents, pharmaceutical formulas, etc., which can solve the problems of device incompatibility and poor stability, and achieve a concentrated particle size distribution , high drug loading and simple preparation process
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Embodiment 1
[0038] 1) At 20°C, add 3 g of polyethylene glycol caprylic / capric glyceride (Labrasol Gattefosse), 1 gram of polyethylene glycol 1000 vitamin E succinate (water-soluble VE, Beijing Bai Lilaisi Biochemical Co., Ltd.), and 0.4 gram of caprylic / capric glycerides (GTCC, DuPont, Malaysia), in Stir the mixture for 5-15 minutes at 200r / min until it becomes transparent and clear;
[0039] 2) Add 1.5ml paclitaxel ethanol solution with a concentration of 17.6mg / ml to the product of step 1) at 20°C and 200r / min, and increase the rotation speed to 800r / min, and continue stirring for 5-30 minutes until transparent Clear;
[0040] 3) Ethanol in the product of step 2) was removed by vacuum distillation to finally obtain a self-emulsifying preparation with a paclitaxel concentration of 6 mg / ml (relative to the total mass of the paclitaxel self-emulsifying preparation, the content of paclitaxel being 0.6%).
Embodiment 2
[0042] 1) At 70°C, add 2 grams of polyethylene glycol stearate (Gelucire 50 / 13 Gattefosse), 0.4 gram of glyceryl stearate (glyceryl stearate, Wako), at 500r / min rotating speed, the mixture was stirred for 5~15 minutes until transparent and clear;
[0043] 2) at 70 ℃, under the condition of 500r / min, 2ml concentration is 22mg / ml paclitaxel ethanol solution, 0.4 gram phospholipid (Epikuron 170, Degussa) and 1.2 gram polyglycerol-6-dioleate (Plurol Oleique 497, Gattefosse ) into the product of step 1), increase the rotating speed to 800r / min, and continue stirring for 2 to 3 hours until transparent and clear;
[0044] 3) At 70°C, under the condition of stirring at 300r / min, volatilize the ethanol in the product of step 2), and finally obtain a paclitaxel concentration of 11 mg / ml (relative to the total mass of the paclitaxel self-emulsifying preparation, the paclitaxel content is 1.1%) self-emulsifying formulations.
Embodiment 3
[0046] 1) At 30°C, add 2 g of polyethylene glycol caprylic / capric glyceride (Labrasol Gattefosse), 1 gram of polyethylene glycol 1000 tocopheryl succinate (water-soluble VE, Beijing Belliles Biochemical Co., Ltd.), 0.2 gram of caprylic / capric glycerides (GTCC, DuPont Malaysia), and 0.3 gram of vitamin E (Ve, Beijing Bei Lilaisi Biochemical Co., Ltd.), the mixture was stirred for 5 to 15 minutes at a rotating speed of 350r / min until it was transparent and clear;
[0047] 2) Add 2.5ml of paclitaxel ethanol solution with a concentration of 21mg / ml and 0.2g of polyethylene glycol (Pluracare E400, BASF) 400 to the product of step 1) at 30°C and 350r / min, maintaining 350r / min Continue to stir for 5 to 30 minutes until it is transparent and clear;
[0048] 3) Ethanol in the product of step 2) was removed by vacuum distillation to finally obtain a self-emulsifying preparation with a paclitaxel concentration of 15 mg / ml (relative to the total mass of the paclitaxel self-emulsifying p...
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