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Compound spirolactone nanoemulsion drug

A nano-drug, spironolactone technology, applied in the field of medicine, can solve the problems that spironolactone cannot be used quickly, the effect of spironolactone is slow, and the drug dissolution rate is slow, so as to maintain blood drug concentration and pharmacological effects, low surface tension, and improve biological The effect of utilization

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

[0003] Existing antihypertensive drugs such as spironolactone 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. Spironolactone itself acts slowly, so that the drug effect of spironolactone cannot be utilized quickly

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Accurately weigh 15g of EL40, 10g of ethyl acetate, 1g of spironolactone, 20g of 1,2-propanediol and stir evenly at room temperature (25°C), then slowly drop into it the distilled water in which hawthorn extract and Asarum extract have been dissolved. 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 For the colorless and transparent compound spironolactone nanoemulsion, 34 g of distilled water, 10 g of hawthorn water extract, and 10 g of asarum water extract were added.

Embodiment 2

[0056] Tween 80 28g, isopropyl myristate 15g, spironolactone 8g, ethanol 12g, distilled water 29g, hawthorn water extract 4g, asarum water extract 4g.

Embodiment 3

[0058] RH40 20g, oleic acid 20g, spironolactone 10g, PEG400 10g, distilled water 28g, hawthorn water extract 5g, asarum water extract 7g.

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Abstract

The invention discloses a compound spirolactone nanoemulsion drug. The nano drug is prepared from the following materials in mass percentage: 1%-15% of spirolactone, 15%-35% of surfactant, 5%-20% of cosurfactant, 5%-20% of oil, 0.5%-10% of hawthorn extract, 0.5%-10% of asarum extract and the balance of distilled water, wherein the sum of the mass percentages of the ingredients is 100%. According to the invention, after the spirolactone is prepared into nanoemulsion dosage form, the ability of penetrating blood brain barrier is obviously increased, the bioavailability of active compound is obviously improved, the half-life period of the drug is prolonged, and the administration times are reduced. The dissolving and penetrating abilities of the drug of the spirolactone are improved by the nanoemulsion, and the stability of the spirolactone is increased. The spirolactone nanoemulsion drug has obvious synergistic effect after being combined with aqueous extract of the hawthorn and asarum, and the curative effect of the drug is brought into full play.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of an antihypertensive drug spironolactone, in particular to a compound spironolactone nanoemulsion drug. Background technique [0002] Spironolactone (spironolactone, Antisterone, Aldactine, Aldonar, Verospiron, spirolang) chemical name 17β-hydroxy-3-oxo-7α-(acetylthio)-17α-pregn-4-ene-21-carboxylic acid gamma-lactone , the molecular formula is C 24 h 32 o 4 S, molecular weight 416.57, CAS No. 52-01-7. [0003] Existing antihypertensive drugs such as spironolactone 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. Spironolactone itself acts slowly, so that the drug effect of spironolactone cannot be utilized quickly. [0004] Contents of the i...

Claims

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Application Information

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IPC IPC(8): A61K36/734A61K9/107A61P9/12A61K31/585
Inventor 欧阳五庆孙江宏曹统
Owner NORTHWEST A & F UNIV
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