A kind of cyclosporine liposome and preparation method thereof
A technology of cyclosporine lipid and cyclosporine, which is applied in the field of cyclosporine liposome and its preparation, can solve the problems of complex preparation process, low encapsulation efficiency, poor stability and the like, and achieves good repeatability and encapsulation efficiency. High, avoid irritation effect
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Embodiment 1
[0030] 1. Preparation method
[0031] 1. Weigh 300mg of dipalmitoyl lecithin (DPPC) and 150mg of cholesterol (CHO)-HP, put them in a stoppered test tube, heat in a circulating water bath until the temperature is 70°C and maintain this temperature, add 4ml of ethanol to dissolve all the lipid materials;
[0032] 2. Dissolve 50 mg of cyclosporine in the container in step 1. Heat 100ml of normal saline to the same temperature as the liposome material, pour the ethanol phase into the water phase, and then use a homogenizer to homogenize at 10,000 rpm for 5 minutes to obtain colostrum, and wait until the colostrum is cooled.
[0033] Adopt HPLC method to measure cyclosporine total amount in cyclosporine liposome (see figure 1 ).
[0034] Two, the determination of cyclosporine liposome encapsulation efficiency
[0035] 1. Method summary
[0036] Determination by centrifugation, that is, according to the different centrifugal forces received by the liposome and free drug, so that...
Embodiment 2
[0057] 1. Weigh 200mg of dipalmitoyl lecithin (DPPC) and 40mg of cholesterol (CHO)-HP into a stoppered test tube, heat in a circulating water bath until the temperature is 70°C and maintain this temperature, add 14ml of ethanol to dissolve the lipid material completely ;
[0058] 2. Dissolve 50 mg of cyclosporine in the container in step 1. Heat 100ml of normal saline to the same temperature as the liposome material, pour the ethanol phase into the water phase, and then use a homogenizer to homogenize at 10,000 rpm for 5 minutes to obtain colostrum, and wait until the colostrum is cooled.
[0059] 3. Determination of the total amount of cyclosporine in cyclosporine liposomes by HPLC (injection volume: 30 μl, see figure 2 ), according to encapsulation rate (%)=(1-W 游 / W 总 )×100%, the results are shown in Table 2.
[0060] The encapsulation efficiency content determination result of cyclosporin liposome in the finished product of table 2
[0061]
Embodiment 3
[0063] 1. Weigh 300mg of distearoylphosphatidylglycerol (DSPC) and 150mg of CHO-HP into a stoppered test tube, heat in a circulating water bath until the temperature is 70°C and maintain this temperature, add 14ml of ethanol to dissolve all the lipid materials;
[0064] 2. Dissolve 50 mg of cyclosporine in the container in step 1. Heat 100ml of normal saline to the same temperature as the liposome material, pour the ethanol phase into the water phase, and then use a homogenizer to homogenize at 10,000 rpm for 5 minutes to obtain colostrum, and wait until the colostrum is cooled.
[0065] 3. Adopt HPLC method to measure cyclosporine total amount in cyclosporine liposome (injection volume: 30 μ l, see image 3 ), according to encapsulation rate=(1-W 游 / W 总 )×100%, the results are shown in Table 3.
[0066] Encapsulation efficiency content determination of cyclosporin liposome in the finished product of table 3
[0067]
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