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Compound atenolol nanoemulsion antihypertensive medicine

An antihypertensive and drug technology, applied in the field of medicine, can solve the problems such as the inability to quickly utilize the efficacy of atenolol, the slow action of atenolol, and the slow dissolution rate of the drug, so as to maintain the blood drug concentration and the pharmacological effect. , the effect of improving solubility and improving bioavailability

Inactive Publication Date: 2016-12-07
张鸿利
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Existing antihypertensive drugs such as atenolol tablets are available on the market now. Although they can be absorbed from the gastrointestinal tract after oral administration, the absorption rate is slow and incomplete. In addition, the dissolution rate of the drug in the tablet is slow and the bioavailability is poor. Coupled with the slow action of atenolol itself, the drug effect of atenolol cannot be utilized quickly

Method used

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  • Compound atenolol nanoemulsion antihypertensive medicine
  • Compound atenolol nanoemulsion antihypertensive medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Accurately weigh 18g of EL40, 10g of ethyl acetate, 8.1g of atenolol, 15g of 1,2-propanediol and stir evenly at room temperature (25°C), then slowly drop into it the dissolved Eucommia water extract and Cortex Moutan Distilled water for aqueous extract. As the amount of distilled water increases, the viscosity of the system increases. When the amount of distilled water changes the system from water-in-oil to oil-in-water nanoemulsion, the viscosity of the system becomes thinner from the most viscous state, and what is produced at this time is Colorless and transparent compound atenolol nanoemulsion, 6.1g of Eucommia water extract, 4.8g of Moutan cortex water extract, and the balance is water. This embodiment is the optimal proportioning of compound recipe atenolol nanoemulsion.

[0050] Following embodiment step is with embodiment 1:

Embodiment 2

[0052] Atenolol 7g, Tween 80 28g, isopropyl myristate 12g, ethanol 12g, Eucommia ulmoides water extract 5g, Moutan cortex water extract 4g, and the balance is 32g water.

Embodiment 3

[0054] RH40 28g, oleic acid 10g, atenolol 8g, PEG400 3g, Eucommia ulmoides water extract 5g, Moutan bark water extract 7g, distilled water 39g.

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Abstract

The invention discloses a compound atenolol nano-emulsion antihypertensive drug. The raw materials and the mass percentages thereof are: atenolol 1%-15%, surfactant 5%-35%, cosurfactant 1% %~20%, oil 1%~20%, Eucommia ulmoides water extract 0.5%~10%, Moutan bark water extract 0.5%~10%, the rest components are distilled water, and the sum of the mass percentages of the above raw materials is 100%. The nano-emulsion droplet has small particles, uniform distribution, low viscosity and good fluidity. After atenolol is prepared into a nanoemulsion, the ability to pass through the blood-brain barrier is significantly increased, the bioavailability of the original drug is significantly improved, the half-life of the drug is prolonged, and the number of administrations is reduced; nanoemulsion improves atenolol Atenolol's drug dissolving and penetrating ability increases the stability of atenolol; and after compounding with the water extracts of Eucommia ulmoides and Paeonia suffruticosa, it has obvious synergistic effect, and the drug efficacy is more fully exerted.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of an antihypertensive drug atenolol, in particular to a compound atenolol nanoemulsion antihypertensive drug. technical background [0002] Atenolol (Atenolol), molecular formula: C 14 h 22 N 2 o 3 , molecular weight: 266.34. This product is a cardioselective β-receptor blocker with no membrane stabilizing effect and no endogenous sympathomimetic activity. Generally used for sinus tachycardia and premature beats, etc., can also be used for hypertension, angina pectoris and glaucoma. [0003] Atenolol has the effect of competitively inhibiting catecholamines at the adrenoceptor β receptor site, but mainly inhibits the activity of β1 receptors. By weakening or preventing the excitation of β receptors, the contraction force and contraction velocity of the heart are reduced, and the conduction velocity through the conduction system is slowed down, so that the heart's res...

Claims

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Application Information

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IPC IPC(8): A61K36/71A61K36/65A61K9/107A61K47/10A61K47/34A61P9/12A61K31/138
CPCA61K36/46A61K9/1075A61K31/138A61K36/65A61K36/71A61K47/10
Inventor 张鸿利
Owner 张鸿利
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