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Oil-in-water compound spironolactone nano emulsion medicine

An oil-in-water type, nano-medicine technology, applied in the field of medicine, can solve the problems of spironolactone that cannot be quickly utilized, slow drug dissolution rate, slow action of spironolactone, etc., to maintain blood drug concentration and pharmacological effects, and improve bioavailability The effect of high degree and low surface tension

Inactive Publication Date: 2012-10-10
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

[0053] 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

[0055] Tween 80 28g, isopropyl myristate 15g, spironolactone 8g, ethanol 12g, distilled water 29g, hawthorn water extract 4g, asarum water extract 4g.

Embodiment 3

[0057] 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 an oil-in-water compound spironolactone nano emulsion medicine. The nano medicine is prepared from the following raw materials in percentage by mass: 1 to 5 percent of spironolactone, 15 to 30 percent of surfactant, 5 to 20 percent of cosurfactant, 5 to 20 percent of oil, 0.5 to 10 percent of hawthorn extract, 0.5 to 1.0 percent of wild ginger extract and the balance of distilled water, and the sum of the mass percentages of the components is 100 percent. After spironolactone is prepared into the nano emulsion preparation, so that the blood brain barrier penetrating capacity is improved obviously, the bioavailability of raw medicines is improved obviously, the half-life period of the medicine is prolonged, and the administration times are reduced; the nano emulsion improves the medicine dissolution and infiltration capacity of spironolactone and the stability of spironolactone; and after the hawthorn water extract and the wild ginger water extract are compounded, the nano emulsion medicine is obvious in synergistic effect, and is full in curative effect.

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 an oil-in-water type compound spironolactone nanoemulsion drug. . Background technique [0002] Oil-in-water spironolactone (spironolactone, Antisterone, Aldactine, Aldonar, Verospiron, spirolang) chemical name 17β-hydroxy-3-oxo-7α-(acetylthio)-17α-pregna-4-ene-21-carboxylic acid γ-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....

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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