Etoposide self-microemulsion preparation as well as preparation method and application thereof
A technology of poside self-microemulsion and etoposide, applied in the field of etoposide self-microemulsion preparations and its preparation, can solve the problems of only 50% bioavailability and large individual differences
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Embodiment 1
[0021] Use Capryol 90 as the oil phase, RH40 (Cremophor RH40) as the emulsifier, and HP (Transcutol HP) as the co-emulsifier. Mix the emulsifier and co-emulsifier evenly in the weight ratio of 2:1, 1:1, 1:2, and then mix it with the oil phase in the weight ratio of 1:9, 2:8, 3:7, 4:6, 5:5 , 6:4, 7:3, 8:2, 9:1 mixed at 50r·min -1 Drop into water preheated to 37°C while stirring, and observe the state of microemulsion. Record the changes and status of the mixing system in different proportions, and limit the proportion of emulsifier to ≤40%, the proportion of co-emulsifier to more than 40%, and the proportion of oil phase to between 10% and 30%, and draw these proportion data Ternary phase diagram, select the effective area of the blank self-microemulsion and the effective area of etoposide self-microemulsion, see figure 1 Middle shaded part.
[0022] from figure 1 It can be seen from Figure B in the figure that the ratio range of the etoposide self-microemulsion prescri...
Embodiment 2
[0024] Etoposide self-microemulsion prescription with etoposide concentration of 20mg / ml (100ml)
[0025]
[0026] Preparation method: dissolve the prescribed amount of etoposide in the prescribed amount of Transcutol HP, add the prescribed amount of Cremophor RH40 and Capryol 90, mix well, and obtain.
[0027] The prepared etoposide self-microemulsion is a colorless uniform transparent liquid. Take the prepared etoposide self-microemulsion, dilute 100 times with water, measure the particle size, and the average particle size is 18.3nm. Take 5ml of etoposide self-microemulsion, at 50r·min -1 Add 10 times the amount of water at 37°C under stirring, and the self-microemulsion stock solution can be completely emulsified within 1 minute, forming a transparent O / W type microemulsion with slightly bluish light, and at 50r·min -1 It remained stable for 8 hours under stirring, and no crystals were precipitated.
Embodiment 3
[0029] Etoposide self-microemulsion prescription with etoposide concentration of 25mg / ml (100ml)
[0030]
[0031] Preparation method: dissolve the prescribed amount of etoposide in the prescribed amount of Transcutol HP, add the prescribed amount of Cremophor RH40 and Capryol 90, mix well, and obtain.
[0032] The prepared etoposide self-microemulsion is a colorless uniform transparent liquid. Take the prepared etoposide self-microemulsion, dilute 100 times with water, measure the particle size, and the average particle size is 18.1nm. Take 5ml of etoposide self-microemulsion, at 50r·min -1 Add 10 times the amount of water at 37°C under stirring, and the self-microemulsion stock solution can be completely emulsified within 1 minute, forming a transparent O / W type microemulsion with slightly bluish light, and at 50r·min -1 It remained stable for 8 hours under stirring, and no crystals were precipitated.
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