Oil-in-water type sotalol nanoemulsion antihypertensive drug

A lorol nanometer and anti-hypertensive technology, applied in the field of medicine, can solve the problems such as insufficient utilization of the efficacy of sotalol, slow action of sotalol, slow drug dissolution rate, etc. Pharmacological effects, effects of enhancing bioavailability, enhancing therapeutic capacity

Inactive Publication Date: 2016-10-12
张鸿利
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are antihypertensive drugs such as sotalol tablets on the market now, although they can be absorbed from the gastrointestinal tract after oral administration, the absorption is not complete, and the dissolution rate of the drug is slow in addition, and the bioavailability is poor. Slow-acting, making sotalol underutilized

Method used

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  • Oil-in-water type sotalol nanoemulsion antihypertensive drug
  • Oil-in-water type sotalol nanoemulsion antihypertensive drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050]Accurately weigh 28 g of EL40 and 4 g of ethanol and stir evenly at room temperature (25° C.), and 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 nanoemulsion, the amount of adding water at this moment is 61.9g, and sotalol is 6.1g. This ratio is the optimal ratio of sotalol antihypertensive nanoemulsion.

[0051] Following embodiment step is with embodiment 1:

Embodiment 2

[0053] 26 g of EL40, 12 g of 1,2-propanediol, 56 g of water, and 6 g of sotalol.

Embodiment 3

[0055] RH40 25g, glycerol 18g, water 53.5g, sotalol 3.5g.

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Abstract

The invention discloses an oil-in-water type sotalol nanoemulsion antihypertensive drug, the raw materials and the mass percentages of each raw material are: 1%-18% of sotalol, 15%-40% of surfactant, Co-surfactant is 0-25%, the rest is distilled water, and the sum of the mass percentages of the above-mentioned raw materials is 100%. The nano-emulsion emulsion has small particles, uniform distribution, low viscosity and good fluidity. After the water-soluble drug sotalol is prepared into nanoemulsion form, the stability and drug efficacy of sotalol are increased, the antihypertensive effect is obviously increased, the half-life of the drug is prolonged, and the number of administrations is reduced.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of antihypertensive drug sotalol, in particular to an oil-in-water type sotalol nanoemulsion antihypertensive drug. technical background [0002] Sotalol is the most representative β-blocker drug. 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 peripheral resistance increases, but autoregulatory mechan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/18A61K47/26A61K47/10A61P9/12
CPCA61K9/1075A61K31/18A61K47/10A61K47/26
Inventor 张鸿利
Owner 张鸿利
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