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Oil-in-water type terazosin nanoemulsion antihypertensive drug

A terazosin and antihypertensive technology, applied in the field of medicine, can solve the problems such as the inability to fully utilize the efficacy of terazosin, slow action of terazosin, slow drug dissolution rate, etc., and achieve the maintenance of blood drug concentration. and pharmacological effects, enhancing drug efficacy and improving bioavailability

Inactive Publication Date: 2016-10-12
张鸿利
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing antihypertensive drugs such as terazosin tablets are now on the market, 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. Slow action, so that the efficacy of terazosin can not be fully utilized

Method used

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  • Oil-in-water type terazosin nanoemulsion antihypertensive drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Accurately weigh 28 g of EL40 and 4 g of ethanol and stir evenly at room temperature (25° C.), then slowly drop into it the distilled water in which terazosin is dissolved. 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. That is colorless and transparent terazosin nanoemulsion, the amount of adding water this moment is 62.9g, and terazosin is 5.1g. This ratio is the optimum proportioning ratio of terazosin antihypertensive nanoemulsion.

[0050] Following embodiment steps are with embodiment 1:

Embodiment 2

[0052] 32 g of EL40, 4 g of 1,2-propanediol, 60 g of water, and 4 g of terazosin.

Embodiment 3

[0054] RH40 24g, glycerol 4g, water 65.3g, terazosin 6.7g.

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Abstract

The invention discloses an oil-in-water type terazosin nanoemulsion antihypertensive drug, the particle diameter of the nanoemulsion antihypertensive drug is between 45.3 and 92.4 nm, and the raw materials and the mass percentage of each raw material are: 1%-15% of lazosin, 15%-40% of surfactant, 0-20% of co-surfactant, the rest of the ingredients are distilled water, and the sum of the mass percentages of the above raw materials is 100%. The nano-emulsion emulsion has small particles, uniform distribution, low viscosity and good fluidity. After the water-soluble drug terazosin is prepared into a nanoemulsion type, the stability and drug efficacy of the terazosin are increased, the antihypertensive effect is obviously increased, the half-life of its drug is prolonged, and the number of administrations is reduced.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of an antihypertensive drug terazosin, in particular to an oil-in-water type terazosin nanoemulsion antihypertensive drug. technical background [0002] Terazosin (Terazosin) molecular formula: C 19 h 25 N 5 o 4 . Molecular weight: 387.44. CAS number: 63590-64-7. This product is a selective α1-receptor blocker, which can reduce peripheral vascular resistance and have a lowering effect on systolic and diastolic blood pressure. Hypertension In animals, terazosin lowers blood pressure by reducing total peripheral vascular resistance. The vasodilation and blood pressure lowering effects of terazosin seem to be mainly caused by blockade of α1-adrenergic receptors. Within 15 minutes after administration, terazosin gradually lowered blood pressure. Patients with mild (about 77%, diastolic blood pressure 95-105mmHg) or moderate (about 23%, diastolic blood pressure 105-115m...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/517A61K47/26A61K47/10A61P9/12
CPCA61K9/1075A61K31/517A61K47/10A61K47/26
Inventor 张鸿利
Owner 张鸿利
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