Fipronil and methoprene dihydric alcohol plastid, and preparation method and application thereof
A technology of methoprene and fiprenil, which is applied in the field of diol plastids and preparations of fiprenyl and methoprene, can solve the problems of insignificant transdermal effect and insignificant therapeutic effect, etc. To achieve the effects of promoting drug transdermal penetration, increasing drug percutaneous penetration, and prolonging the action time
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[0031] Another aspect of the present invention, proposes the preparation method of fiprenil and methoprene glycol plastosome, comprises the following steps:
[0032] (1) Take feprenil, methoprene, dipalmitophosphatidylcholine, glycol (ethanol: propylene glycol = 6.5: 3.5) and sodium lauryl sulfate according to the formula described in any of the above , sealed and stirred until dissolved;
[0033] (2) Stir while adding phosphate buffer solution dropwise, and cool to room temperature;
[0034] (3) Ultrasound to obtain nano-alcoholsomes;
[0035] (4) Fiprenil and methoprene diol plastom was obtained by filtration.
[0036] Preferably, the stirring temperature in step (1) is 29.5-30.5°C, the stirring speed is 600-800rpm; the dropping speed in step (2) is 3-6mL / min; the pH of the phosphate buffer is 6.5-7.0; the stirring time is 20-30min .
[0037] Preferably, step (3) ultrasonic power 100~120W, frequency 45~50kHz; ultrasonic 3~4s, interval 3~4s, 30~40 cycles; Step (4) 50~100nm
Embodiment 1
[0043] A kind of fiprenil and methoprene glycol plastosome, comprising following parts by weight: 5.0 parts of fiprenil; 4.0 parts of methoprene; 2.0 parts of dipalmitone phosphatidylcholine; glycol ( Ethanol:propylene glycol=6.5:3.5) 30.0 parts; sodium lauryl sulfate, 0.5 parts and 55 parts of phosphate buffer (pH=6.5). (take the total amount of 100ml as an example)
[0044] A kind of preparation method of fiprenyl and methoprene glycol plastid:
[0045] (1) Take by weighing fiprenil, methoprene, dipalmitophosphatidylcholine, glycol (ethanol: propylene glycol=6.5:3.5), sodium lauryl sulfate and add reaction tank by proportioning, stirring temperature is 30°C, stir at 700rpm, stir until dissolved;
[0046](2) Then add phosphate buffer (pH=6.5) at a drop rate of 3mL / min, stir in an airtight container for 20 minutes until completely dissolved, and cool to room temperature;
[0047] (3) Under ultrasonic power 100W and ultrasonic frequency 45kHz, ultrasonic 3s, interval 3s, carr
Embodiment 2
[0051] A kind of fiprenil and methoprene glycol plastosome, comprising following components by weight: 6.0 parts of fiprenil; 5.0 parts of methoprene; 2.5 parts of dipalmitone phosphatidylcholine; glycol ( Ethanol: propylene glycol=6.5:3.5) 35.0 parts; sodium lauryl sulfate 0.5 part and 70 parts of phosphate buffer (pH=6.5). (take the total amount of 100ml as an example)
[0052] A kind of preparation method of fiprenyl and methoprene glycol plastid:
[0053] (1) Take by weighing fiprenil, methoprene, dipalmitophosphatidylcholine, glycol (ethanol: propylene glycol=6.5:3.5), sodium lauryl sulfate and add reaction tank by proportioning, stirring temperature is 30°C, stir at 700rpm, stir until dissolved;
[0054] (2) Then add phosphate buffer (pH=6.5) at a drop rate of 3mL / min, stir in an airtight container for 20 minutes until completely dissolved, and cool to room temperature;
[0055] (3) Under ultrasonic power 100W and ultrasonic frequency 45kHz, ultrasonic 3s, interval 3s,
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