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Oil-in-water type sotalol and eucommia seed oil nanoemulsion antihypertensive drug

A technology of Eucommia ulmoides seed oil and anti-hypertension, applied in the field of medicine, can solve the problems such as the inability to fully utilize the efficacy of sotalol and eucommia seed oil, slow action of sotalol, slow drug dissolution rate, etc. Blood concentration and pharmacological effects, reducing first-pass effect and improving bioavailability

Inactive Publication Date: 2012-12-19
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There are antihypertensive drugs such as sotalol tablets on the market now, and the use of eucommia seed oil is also available. 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 sotalol, the efficacy of sotalol and eucommia seed oil cannot be fully utilized

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Accurately weigh 8.2g of Eucommia ulmoides seed oil, 28g of EL40 and 4g of ethanol and stir evenly at room temperature (25°C), then slowly drop distilled water in which sotalol 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 sotalol, eucommia seed oil nanoemulsion, the amount of adding water at this moment is 53.7g, and sotalol is 6.1g. This ratio is the optimal ratio of sotalol and eucommia seed oil antihypertensive nanoemulsion.

[0056] Following embodiment steps are with embodiment 1:

Embodiment 2

[0058] Eucommia ulmoides seed oil 7.5g, EL40 26g, 1,2-propanediol 12g, water 48.5g, sotalol 6g.

Embodiment 3

[0060] Eucommia ulmoides seed oil 9.5g, RH40 25g, glycerol 18g, water 44g, sotalol 3.5g.

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Abstract

The invention discloses an oil-in-water type sotalol and eucommia seed oil nanoemulsion antihypertensive drug which comprises raw materials, in mass percent, of 1%-18% of sotalol, 15%-40% of surface active agent, 0-25% of assisted surface active agent, 1%-25% of eucommia seed oil and the balance of distilled water, wherein a sum of mass percents of the raw materials is 100%. According to the invention, the nanoemulsion is small in emulsion droplet, even in distribution, small in viscosity and good in mobility. The nanoemulsion formulation organically combines the water-soluble drug sotalol and the fat-soluble eucommia seed oil, dissolving and infiltration capacities of the eucommia seed oil are improved, and stability and pesticide effects of the sotalol are increased. After the sotalol and the eucommia seed oil are prepared into the nanoemulsion formulation, the nanoemulsion formulation combines the advantages of the sotalol and the eucommia seed oil, antihypertensive effects are obviously increased, a half-life period of the drug is prolonged, and drug taking times are reduced.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of antihypertensive drug sotalol and eucommia seed oil, in particular to an oil-in-water type sotalol and eucommia seed oil nanoemulsion antihypertensive drug. Background technique [0002] Sotalol is the most representative beta receptor blocker. It is non-selective to β1 and β2 receptors, has no intrinsic activity, has membrane stabilizing effect, and exerts pharmacological effects mainly by blocking β receptors. The blocking effect on cardiac β1 receptor is manifested as slowing heart rate, inhibiting myocardial contractility, reducing cardiac output, and lowering blood pressure. When the sympathetic tension increases, the effect is more obvious. The effect of blocking smooth muscle β2 receptors manifests itself as bronchoconstriction and vasoconstriction. It can reduce the maximum expiratory volume in the first second. Can reduce plasma renin activity. Total periphe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/46A61K9/107A61P9/12A61K31/18
Inventor 欧阳五庆孙江宏杜娟
Owner NORTHWEST A & F UNIV
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