Compound ramipril nano-emulsion for antihypertension

Abstract

The invention discloses an oil-in-water type compound ramipril nano-emulsion, which is prepared from 1%-25% of ramipril, 0.1%-25% of hydralazine, 0.1%-25% of lisinopril, 10%-55% of surfactant, 5%-30% of oil and the balance distilled water, wherein the sum of the mass percent of the ingredients is 100%. The nano-emulsion is small in emulsion droplet granule, even in distribution, low in viscosity, and good in liquidity and has antihypertensive capacity, the dissolubility of the ramipril is enhanced, the bioavailability and the drug stability of the ramipril are improved, the metabolic time of the nano-emulsion in vivo is delayed, and the problem of hypertension can be synthetically solved because the hydralazine and the lisinopril are synthesized. With the adoption of the compound ramipril nano-emulsion, the dosage of the adjuvants of the antihypertension is reduced, the toxicity of the antihypertension to body is lowered, and the production cost is lowered; and furthermore, the preparation method of the compound ramipril nano-emulsion is simple and is low in energy consumption.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of antihypertensive drug compound ramipril, in particular to a compound ramipril nanoemulsion antihypertensive drug. Background technique [0002] Ramipril, chemical name: (S)-2-[N-(1-ethoxycarbonyl-3-phenyl-propyl)alanyl]-2-azabicyclo[3.3.0 ] Octane-3-carboxylic acid, molecular formula: C 23 h 32 N 2 o 5 , molecular weight: 416.50. CAS number: 87333-19-5. Chemical properties: white or off-white crystalline powder. Melting point 107.0-110.0°C. Ramipril is a prodrug that is hydrolyzed in the liver after absorption from the gastrointestinal tract to generate an active angiotensin-converting enzyme (ACE) inhibitor, ramiprilat, which is a potent and long-acting ACE Inhibitors. Taking ramipril can lead to an increase in plasma renin activity and a decrease in plasma concentrations of angiotensin II and aldosterone. Because of the reduction of angiotensin II, ACE inhi...

AI Technical Summary

Problems solved by technology

Existing antihypertensive drugs such as ramipril tablets are available on the market now, although they can be quickly 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 poor. Ramipril itself acts slowly, making it impossible to utilize the effects of ramipril quickly

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