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Nanoemulsion of N-[4-(2,4 dimethoxy phenyl)-5-oxygroup-4,5-dihydro-[1,2] disulfide group-[4,3-b]-6-pyrryl]-3,5-di-trifluoromethyl benzamide and preparation method thereof

A technology of trifluoromethylbenzamide and dimethoxyphenyl, which is applied in the field of pharmaceutical preparations, can solve problems such as difficult absorption, poor water solubility, and difficult metabolism, and achieve the effects of promoting absorption, low toxicity, and low preparation cost

Inactive Publication Date: 2010-10-06
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4,3-b]-6-pyrrole Base]-3,5-bis-trifluoromethylbenzamide is an orange solid with low solubility in most organic solvents and poor water solubility. It is difficult to absorb and metabolize in humans and animals.

Method used

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  • Nanoemulsion of N-[4-(2,4 dimethoxy phenyl)-5-oxygroup-4,5-dihydro-[1,2] disulfide group-[4,3-b]-6-pyrryl]-3,5-di-trifluoromethyl benzamide and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment

[0026] Embodiments 1-6 are each a kind of N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4 , 3-b]-6-pyrrolyl]-3,5-bis-trifluoromethylbenzamide nanoemulsion, the respective ingredients include the components shown in the table above, wherein the "drug" is N-[4- (2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4,3-b]-6-pyrrolyl]-3, 5-Bis-trifluoromethylbenzamide.

[0027] The preparation method of each nanoemulsion among the embodiment 1-6 is carried out according to the following step order:

[0028] (1) Get medicine and co-emulsifier to mix, heat in water bath, make medicine fully dissolve in co-emulsifier, obtain solution A,

[0029] (2) Add solution A to the emulsifier while it is hot, and keep stirring to make it evenly mixed to obtain system B,

[0030] (3) Drop the oil phase into system B, stir evenly, add deionized water dropwise, and stir while adding, as the amount of deionized water increases, the system suddenly becomes viscous and appears liquid cr...

Embodiment 3

[0032] Taking Example 3 as an example, the preparation method of its nanoemulsion is carried out in the following steps:

[0033] (1 3 ) Take 3g N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4,3-b]- 6-pyrrolyl]-3,5-bis-trifluoromethylbenzamide drug is mixed with 100g n-butanol, and dissolved in a water bath until the drug is dissolved to obtain solution A 3 ;

[0034] (2 3 ) to solution A 3 Add it to 450g Tween-80 while it is hot, and mix well to get System B 3 ,

[0035] (3 3 ) to the system B 3 Add 50g of olive oil to the solution and stir evenly; add deionized water to the system dropwise, and stir while adding, as the amount of deionized water increases, the system gradually becomes viscous, and the system appears in a liquid crystal state at this time, continue to add deionized water Water, when the system becomes dilute, O / W type stable N-[4-(2,4-dimethoxyphenyl)-5-oxyl-4,5-dihydro-[1, 2] Nanoemulsion of dithio-[4,3-b]-6-pyrrolyl]-3,5-bis-trifluorome...

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Abstract

The invention discloses a nanoemulsion of N-[4-(2,4 dimethoxy phenyl)-5-oxygroup-4,5-dihydro-[1,2] disulfide group-[4,3-b]-6-pyrryl]-3,5-di-trifluoromethyl benzamide and a preparation method thereof. The nanoemulsion is prepared from medicines, a water phase, an oil phase, an emulsifier, an assistant emulsifier, and the like and can enhance the dispersity of the medicines and promote the absorption of the medicines so as to further enhance the bioavailability of the medicines. The nanoemulsion has low toxicity, no hemolysis, and the like, is beneficial to the absorption of the medicines and has the advantages of simple and easy preparation method, safe and non-toxic operation, low preparation cost, high medicine content and no medicine loss. The invention is used for preparing the nanoemulsion of the N-[4-(2,4 dimethoxy phenyl)-5-oxygroup-4,5-dihydro-[1,2] disulfide group-[4,3-b]-6-pyrryl]-3,5-di-trifluoromethyl benzamide.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio- Nanoemulsion of [4,3-b]-6-pyrrolyl]-3,5-bis-trifluoromethylbenzamide and its preparation method. Background technique [0002] Compound N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4,3-b]-6- Pyrrolyl]-3,5-bistrifluoromethylbenzamide, as a drug, can promote the production of leukocytes in the body, has an anti-tumor effect, and can also be used for the prevention and treatment of bacterial infections (such as HIV), blood disorders (such as neutral Leukopenia) and other related diseases. [0003] N-[4-(2,4-dimethoxyphenyl)-5-oxo-4,5-dihydro-[1,2]dithio-[4,3-b]-6-pyrrole Base]-3,5-bis-trifluoromethylbenzamide is an orange solid with low solubility in most organic solvents and poor water solubility. It is difficult to absorb and metabolize in humans and animals. [0004] Nanoemulsion is a new drug do...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/407A61P7/00A61P35/00A61P31/04A61P31/18
Inventor 张越韩玉翠高春辉赵树春刘惠娴
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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