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Doramectin microemulsion transdermal agent and preparation method thereof

A technology of doramectin and transdermal agent, applied in the field of doramectin microemulsion transdermal agent and preparation thereof, can solve the factors that do not comprehensively consider transdermal absorption, do not conduct drug transdermal absorption test, and are not suitable for veterinary drugs. Field application and other issues, to achieve good transdermal absorption, prolonged absorption and action time, and stable efficacy

Active Publication Date: 2010-12-29
ACAD OF NAT FOOD & STRATEGIC RESERVES ADMINISTRATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Invention patent ZL200610010055.6 "Doramectin, Selamectin Emulsion in Water and Its Preparation Method" has developed a preparation method of doramectin, selamectin microemulsion, emulsion in water, and suspension, which is a new pesticide In the field of dosage forms, the solvents used (such as xylene, toluene, etc.) are highly irritating, and have obvious acute and chronic toxicity to the whole body of animals, so they are not suitable for application in the field of veterinary medicine.
The use of microemulsions for transdermal drug delivery is a hot spot in current pharmacy research. Invention patent ZL200610010055.6 makes microemulsions, water emulsions, and suspensions and is mostly used for spraying. Factors that affect animal skin transdermal absorption are not comprehensively considered in the formula, so No drug percutaneous absorption test, nor animal clinical treatment test

Method used

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  • Doramectin microemulsion transdermal agent and preparation method thereof
  • Doramectin microemulsion transdermal agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The doramectin microemulsion of the present invention consists of:

[0031] Doramectin 0.1g

[0032] Ethyl butyrate 1.08ml

[0033] Oleic acid 0.42ml

[0034] Triphenylethylphenol polyoxypropylene polyoxyethylene block polymer PEP type 1602 # 1.35ml

[0035] Calcium dodecylbenzenesulfonate 500 # 0.45ml

[0036] Propylene glycol 2.7ml

[0037] Azone 0.2ml

[0038] Glycerin 0.2ml

[0039] Distilled water 3.5ml

[0040] Preparation includes the following steps:

[0041] a Mix ethyl butyrate and oleic acid until completely mixed.

[0042] b will be 1602 # 、500 # Mix until completely combined.

[0043] c Dissolve the doramectin in the oil phase of (a) until the mixed phase is uniform and transparent.

[0044] d Add the mixed phase containing doramectin to the mixed emulsifier obtained in (b), add an appropriate amount of distilled water, stir until uniform, then add the corresponding amount of emulsifier, antifreeze, penetration enhancer, mix until clea...

Embodiment 2

[0046] The doramectin microemulsion of the present invention consists of:

[0047] Doramectin 0.1g

[0048] n-Butyl acetate 0.72ml

[0049] Lauric acid 0.28ml

[0050] Castor oil polyoxyethylene ether BY-140 1.32ml

[0051] Calcium dodecylbenzenesulfonate 500 # 0.48ml

[0052] Propylene glycol 2.66ml

[0053] Dimethyl sulfoxide 0.2ml

[0054] Ethanol 0.2ml

[0055] Distilled water 4.04ml

Embodiment 3

[0057] The doramectin microemulsion of the present invention consists of:

[0058] Doramectin 0.1g

[0059] Ethyl propionate 1.02ml

[0060] Oleic acid 0.48ml

[0061] Triphenylethylphenol polyoxypropylene polyoxyethylene block polymer PEP type 1602 # 1.32ml

[0062] Alkylphenol ether sulfosuccinate sodium salt MS-1 0.58ml

[0063] Ethylene glycol 2.66ml

[0064] Azone 0.1ml

[0065] Glycerin 0.1ml

[0066] Distilled water 3.64ml

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Abstract

The invention discloses a doramectin microemulsion transdermal agent and a preparation method thereof. The doramectin microemulsion transdermal agent comprises the following components in percentage by weight: 0.2-2.0 percent of doramectin, 7-22 percent of oil phase, 10-22 percent of emulsifier, 5-50 percent of co-emulsifier, 1-5 percent of antifreezer, 1-10 percent of penetration enhancer and the balance of water. The doramectin microemulsion transdermal agent has the advantages of stable quality, good drug efficacy, low cost, little environmental pollution, high safety, little irritation, simple operation in application, convenient use, good clinical application effect and long sustained release period, can efficiently reduce the drug administration time, can be used for treatment and also prevention and overcome the defects of trouble and cost increase to animal husbandry production due to repeated drug administration.

Description

technical field [0001] The invention relates to a doramectin microemulsion transdermal agent and a preparation method thereof, belonging to the field of new dosage forms of veterinary drugs. Background technique [0002] Doramectin is a new generation of macrolide antiparasitic drug developed in the 1990s. It uses cyclohexanecarboxylic acid (cyclohexanecarboxylic acid) as a precursor and is produced by A A kind of avermectin antibiotic fermented by Streptomyces avermitilis mutant strain, it is considered to be one of the best antiparasitic drugs in the avermectin family at present. , arthropods have a good killing effect. It was first discovered that its ability to drive and kill parasites was in the animal models of Trichostrongylus serpentineum and Rabbit-killing itch mite, compared with other commercially available ivermectin products, its anti-parasite range is wider Broader, more effective, and more effective in preventing parasitic reinfection for a longer period of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/7048A61P33/00
Inventor 张晓琳肖兵南李爱科王会明汪洋李思长郭伟群陈茜
Owner ACAD OF NAT FOOD & STRATEGIC RESERVES ADMINISTRATION
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