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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

Active Publication Date: 2020-01-10
INST OF ANIMAL HEALTH GUANGDONG ACADEMY OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The combined transdermal agent of feprenil and methoprene is currently the main way of external administration, but the transdermal effect is not obvious, and the therapeutic effect is not significant

Method used

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  • Fipronil and methoprene dihydric alcohol plastid, and preparation method and application thereof
  • Fipronil and methoprene dihydric alcohol plastid, and preparation method and application thereof
  • Fipronil and methoprene dihydric alcohol plastid, and preparation method and application thereof

Examples

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preparation example Construction

[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) 50~100n...

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, car...

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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Abstract

The invention discloses a fipronil and methoprene dihydric alcohol plastid, and a preparation method and application thereof. An insect repellent preparation is prepared from the following components:fipronil, methoprene, dipalmitoyl phosphatidyl choline, dihydric alcohol (including ethyl alcohol and propylene glycol), lauryl sodium sulfate and a phosphate buffer solution with the pH being 6.5. Through animal experiments, it is confirmed that the fipronil and methoprene dihydric alcohol plastid preparation has the effect of resisting dog and cat ectoparasitic infection. Relative to a fiproniland methoprene compound transdermal agent, the prepared new fipronil and methoprene dihydric alcohol plastid preparation significantly reduces toxicity and has good skin permeability, drugs reach thelong effective effect time, the insect repellent effect of the preparation is enhanced, and the action time of the preparation is prolonged.

Description

technical field [0001] The invention belongs to the field of insect control, and in particular relates to a diol plastid of fiprenyl and methoprene, a preparation method and application thereof. Background technique [0002] With the increase in the number of pets and the increase in outdoor activities of pets, the chances of pets being exposed to various pathogens have increased. Parasitic diseases are one of the common diseases of pets. For example, the bites of fleas and ticks, which are ectoparasites of pets, can cause skin inflammation and itching in dogs and cats. Biting the affected area can lead to hair loss and aggravate skin damage. Flea eggs and larvae can not only carry pathogens, but also cause symptoms such as skin redness, inflammation, itching, and systemic allergies of humans, dogs, and cats, which are harmful to the health of humans, dogs, and cats. Regular use of drugs for deworming, scientific feeding, and improvement of resistance are of great significa...

Claims

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Application Information

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IPC IPC(8): A61K31/415A61K9/127A61P33/14A61K31/231
CPCA61K31/415A61K31/231A61K9/1272A61K9/0014A61P33/14A61K2300/00Y02A50/30
Inventor 孙铭飞廖申权戚南山吕敏娜吴彩艳李娟林栩慧胡俊菁蔡海明于林增肖文婉
Owner INST OF ANIMAL HEALTH GUANGDONG ACADEMY OF AGRI SCI