Trimetaphan camsilate and linseed oil nanoemulsion antihypertensive drug

A technology of anisodime and linseed oil, applied in the field of medicine, can solve the problems such as the inability to fully utilize the efficacy of the anisodime and the linseed oil, the slow action of the anisodime, the slow drug dissolution rate, and the like. The effect of maintaining blood concentration and pharmacological effect, improving bioavailability and promoting gastrointestinal absorption

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

[0008] Existing antihypertensive drugs such as camphorsulfaphene tablets on the market now also have the use of linseed oil, although they can be absorbed from the gastrointestinal tract after oral administration, the absorption is not complete, and the dissolution rate of the medicine is slow in addition, and the bioavailability is poor. Coupled with the slow action of tamophen, the efficacy of tamophen and linseed oil cannot be fully utilized

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Accurately weigh 11.2g of linseed oil, 25g of EL40 and 5g of ethanol and stir evenly at room temperature (25°C), then slowly drop into it distilled water dissolved in camphor. 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 campyphene, linseed oil nanoemulsion, the amount that adds water this moment is 52.5g, campyline is 6.3g. This ratio is the optimal ratio of camphorsulfaphene and linseed oil antihypertensive nanoemulsion.

[0054] Following embodiment step is with embodiment 1:

Embodiment 2

[0056] Linseed oil 10.5g, EL40 20g, 1,2-propanediol 15g, distilled water 48.7g, campebutazone 5.8g.

Embodiment 3

[0058] Flaxseed oil 9.7g, RH40 20g, glycerol 15g, distilled water 49.4g, sampephene 5.9g.

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Abstract

The invention discloses an oil-in-water type trimetaphan camsilate and linseed oil nanoemulsion antihypertensive drug which comprises the following raw materials in percentage by weight: 1%-15% of trimetaphan camsilate, 15%-35% of surfactant, 0-20% of cosurfactant, 1%-25% of linseed oil and the balance of distilled water, wherein the sum of the mass percent of the raw materials is 100%. The nanoemulsion has the advantages of small emulsion drop granule, uniform distribution, small viscosity and good flowability. In the nanoemulsion dosage form, the hydralazine which is a water-soluble medicine and the fat soluble linseed oil are organically combined, so the dissolving and infiltration capacities of the linseed oil are improved, and the stability and the pesticide effect of the trimetaphan camsilate are improved; and after the trimetaphan camsilate and the linseed oil are prepared into the nano dosage form, the advantages of the trimetaphan camsilate and the linseed oil are combined, so the antihypertensive effect is obviously increased, the half-life period of the drug is prolonged, and the drug administration times is reduced.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of antihypertensive drug camphoramiphene and linseed oil, in particular to a kind of antihypertensive drug camphoramiphene and linseed oil nanoemulsion. [0002] Background technique [0003] Trimetaphan camsilate is also known as trimetaphan camphorsulfonate, mithiaphene. White crystalline powder with a melting point of about 245°C. This drug is a controlled antihypertensive drug, which can inhibit the conduction of sympathetic ganglion nerve impulses, dilate peripheral blood vessels, and lower blood pressure. It is mainly used for controlled hypotension and reduces vascular tension. [0004] This product competes with acetylcholine for the nicotinic (N1) receptor on the ganglion cell membrane, thereby blocking the nerve impulse transmission of the sympathetic and parasympathetic ganglion, causing peripheral blood vessel expansion, blood pressure drop and other effects...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/55A61K31/4188A61K9/107A61P9/12
Inventor 欧阳五庆孙江宏向高青
Owner NORTHWEST A & F UNIV
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