Compound alprenolol nano-emulsion antihypertensive drug

An alprenolol anti-hypertensive technology, applied in the field of medicine, can solve the problems that the drug effect of alprenolol cannot be quickly utilized, the drug dissolution rate is slow, and the bioavailability is poor, so as to maintain the blood drug concentration and pharmacological effect, enhanced bioavailability, effect of low surface tension

Inactive Publication Date: 2012-08-15
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing antihypertensive drugs such as Alprenol tablets on the market, although they can be absorbed from the gastrointestinal tract after oral administration, the absorption is not complete. In addition, the dissolution rate of the drug in the tablet is slow, and the bioavailability is extremely poor, making the drug The efficacy of Lol cannot be utilized quickly; on the other hand, there are no suitable dosage forms of traditional Chinese medicines such as Gastrodia elata and Uncaria, which have significant effects.

Method used

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  • Compound alprenolol nano-emulsion antihypertensive drug
  • Compound alprenolol nano-emulsion antihypertensive drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Accurately weigh 12g co-solvent ethanol, dissolve in Alprenolol as much as possible, obtain its dissolution amount as 6.3g, and then dissolve with 7gIPM; accurately weigh surfactant EL40 28g and co-surfactant ethanol 4g, and The alprenolol-dissolved oil was stirred evenly at room temperature (25°C), and then the distilled water in which the water extract of Uncaria uncaria and the water extract of Gastrodia elata was dissolved was slowly dropped into it. 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 clear and transparent compound Alprenolol nanoemulsion, the amount of distilled water added at this time is 32.5g, the water extract of Uncaria uncaria is 4.8g, and the water extract of Gastrodia elata is 5.4g. This ratio is the optimal ratio ...

Embodiment 2

[0064] Co-solvent ethanol 10g, Alprenolol 5.7g, IPM 6.5g, EL40 24g, 1,2-propanediol 8g, Uncaria water extract 5.2g, Gastrodia elata water extract 6g, distilled water 34.6 g.

Embodiment 3

[0066] Co-solvent ethanol 14g, alprenolol 8.1g, ethyl acetate 9.5g, poloxamer 188 24g, glycerol 12g, Uncaria water extract 1.8g, Gastrodia elata water extract 2.7g, distilled water 27.9 g .

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Abstract

The invention discloses a compound alprenolol nano-emulsion antihypertensive drug. The drug comprises the following raw materials by weight: 0.1%-13% of alprenolol, 5%-45% of surfactant, 1%-25% of cosurfactant, 5%-35% of oil, 0-30% of cosolvent, 0.5%-15% of uncaria rhynchophylla water extract, 0.5%-15% of gastrodia elata water extract and the balance of distilled water, and the sum of the weight percents of the raw materials is 100%. The nano-emulsion drops are small in size, low in viscosity and good in flowability and can be distributed uniformly. Due to the nano emulsion, the drug dissolving and penetrating capability of the alprenolol is improved, the stability of the alprenolol is improved, and the capability of the alprenolol for passing through the blood brain barrier is improved. After the alprenolol is prepared to be nano emulsion, the antihypertensive effect is improved obviously, the half-life period of the drug is prolonged, and the times of administration are reduced. The compound alprenolol nano-emulsion antihypertensive drug has very broad market prospect.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of an antihypertensive drug alprenol, in particular to a compound alprenolol nanoemulsion antihypertensive drug. Background technique [0002] Alprenolol is 1-(isopropylamino)-3-(2-allylphenoxy)-2-propanol [1-(Isopropylamino)-3-(2-allylphenoxy)-2 -propanol]. Molecular formula C 15 h 23 NO 2 . Molecular weight 249.35. CAS number 13655-52-2. This product has the effect of competitively inhibiting catecholamines at the site of adrenergic β 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 response to exercise or stress is weakened. This product lowers blood pressure through central, adrenergic neuron blockade, anti-renin activity, and reduced cardiac output, and is suitable for the trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/8988A61K9/107A61P9/12A61K31/138
Inventor 欧阳五庆孙江宏杜娟
Owner NORTHWEST A & F UNIV
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