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Antihypertensive drug of enalapril and safflower oil nanoemulsion

A technology of safflower seed oil and enalapril, applied in the field of medicine, can solve the problems such as the inability to fully utilize the medicinal effects of enalapril and safflower seed oil, slow action of enalapril, slow drug dissolution rate, and the like, Achieve the effect of maintaining blood drug concentration and pharmacological effect, improving bioavailability and promoting gastrointestinal absorption

Inactive Publication Date: 2012-10-03
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are antihypertensive drugs such as enalapril tablets on the market now, and safflower oil is also used. Although it can be absorbed from the gastrointestinal tract after oral administration, the absorption is not complete. In addition, the dissolution rate of the drug is slow and the bioavailability is poor. , coupled with the slow action of enalapril, the efficacy of enalapril and safflower seed oil cannot be fully utilized

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Accurately weigh 9.1g of safflower seed oil, 28g of EL40 and 4g of ethanol and stir evenly at room temperature (25°C), then slowly drop distilled water in which enalapril is dissolved. As the amount of distilled water increases, the viscosity of the system increases. When the amount of distilled water is added to make the system change from water-in-oil to oil-in-water nanoemulsion, the viscosity of the system becomes thinner from the most viscous state. What is colorless and transparent enalapril, safflower seed oil nanoemulsion, the amount that adds distilled water at this moment is 51.3g, and enalapril is 7.6g. This ratio is the optimal ratio of enalapril and safflower seed oil antihypertensive nanoemulsion.

[0054] Following embodiment steps are with embodiment 1:

Embodiment 2

[0056] Safflower seed oil 8.5g, EL40 27g, 1,2-propanediol 3g, distilled water 53.6g, enalapril 7.9g.

Embodiment 3

[0058] Safflower seed oil 8.5g, RH40 28g, glycerol 7g, distilled water 50g, enalapril 6.5g.

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PUM

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Abstract

The invention discloses an oil-in-water type antihypertensive drug of enalapril and safflower oil nanoemulsion. The materials and the weight percentages of the materials are as follows: 1-20% of the enalapril, 15-35% of surfactant, 0-20% of cosurfactant, 1-25% of the safflower oil, and the balance of distilled water. The sum of the weight percentages of the materials is 100%. The nanoemulsion has the advantages of small emulsion droplet particles, uniform distribution, small viscosity and good flowability. With the adoption of the dosage form of the nanoemulsion, water-soluble enalapril and fat-soluble safflower oil are organically combined, so that the dissolving and penetrating abilities of the safflower oil are improved, and the stability and the pesticide effect of the enalapril are increased. The advantages of the enalapril and the safflower oil are combined after the enalapril and the safflower oil are prepared into nanoemulsion formulation, so that the antihypertensive effect is obviously increased, the half-life period of the drug is prolonged and the administration times are also reduced.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of antihypertensive drug enalapril and safflower seed oil, in particular to a nanoemulsion antihypertensive drug of enalapril and safflower seed oil. Background technique [0002] Molecular formula of Enalapril: C 20 h 28 N 2 o 5 . This product is an angiotensin converting enzyme inhibitor (ACEI). This product is hydrolyzed into enalaprilat in the liver and becomes a competitive angiotensin-converting enzyme inhibitor, so that angiotensin Ⅰ cannot be converted into angiotensin Ⅱ, resulting in increased plasma renin activity and decreased aldosterone secretion. Vascular resistance decreased. Enalaprilat also interferes with the degradation of bradykinin, which also reduces vascular resistance. Although this product is considered to lower blood pressure mainly by inhibiting the renin-angiotensin-aldosterone system, it is also effective for hypertension with low renin a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K36/286A61K9/107A61P9/12
Inventor 欧阳五庆孙江宏杜娟
Owner NORTHWEST A & F UNIV
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