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Metal salt of quinaprilat

A technology of quinapril and metal salt, applied in the field of medicine, can solve the problems of poor water solubility and poor stability of quinapril

Active Publication Date: 2011-02-02
NANJING YOKO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem of poor water solubility and stability of quinaprilat, the inventors, through a large amount of screening work, found that the metal salt of quinaprilat and its hydrate can greatly improve its water solubility and stability, including its combination with Lithium, sodium, potassium, barium, calcium, magnesium, zinc ions or salts formed by combining any two ions and their hydrates, especially their sodium salts, potassium salts, sodium potassium salts and their hydrates

Method used

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  • Metal salt of quinaprilat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Preparation of quinaprilat metal salt

[0042] 1) preparation of quinaprilat sodium:

[0043] Reaction formula:

[0044]

[0045] Take 5.0 g of refined quinapril hydrochloride, dissolve it in 100 ml of dioxane:water (9:1), stir for 5 min, adjust the pH of the solution to 12 with 1N NaOH, and react at 60°C. After 20 minutes, add 1N NaOH to adjust the pH of the solution to 12, and continue to stir for 30 minutes to complete the reaction (can be monitored by spotting the plate). Add 1.0 g of activated carbon, filter while hot after 15 minutes, the filtrate is rotary steamed at 50°C for 1 hour and becomes an oily substance, add 100ml of acetone that has been preheated to boiling, shake vigorously, the oily substance dissolves, and the insoluble substance is NaCl, filter while hot. Put the filtrate in an environment of 0-5°C for about 3 hours, a large amount of white solid appeared, filter it, dry the solid in vacuum at 40°C for 20 hours, weigh about 4.0g,...

Embodiment 2

[0061] Embodiment 2 Preparation of aseptic powder of the present invention

[0062] 1. Prescription

[0063] Prescription 1:

[0064]

[0065] Prescription 2:

[0066]

[0067] Prescription 3

[0068]

[0069] 2. Preparation process:

[0070] In the aseptic batching room, the aseptic compound of the present invention is weighed according to the prescription, subpackaged and sealed to obtain the product.

Embodiment 3

[0071] Example 3 Preparation of the aqueous injection of the present invention

[0072] 1. Prescription

[0073] Prescription 1:

[0074]

[0075] Prescription 2:

[0076]

[0077] Prescription 3:

[0078]

[0079] 2. Preparation process:

[0080] 1) Pre-treat the containers, ampoules, production equipment, instruments, etc. used for liquid preparation.

[0081] 2) Weigh the raw materials and auxiliary materials according to the prescription quantity.

[0082] 3) Add the raw materials into water for injection with a dosing volume of 80%, stir and dissolve, add 0.1% activated carbon for needles, stir at 50°C for 10 minutes, and filter for decarbonization.

[0083] 4) Measure the pH value of the solution, add water to make up to the total volume.

[0084] 5) Filter with a 0.45 μm microporous membrane.

[0085] 6) Check the clarity of the solution.

[0086] 7) Inspection of semi-finished products.

[0087] 8) The semi-finished product is melted and sealed in t...

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Abstract

The invention belonging to the field of medical technique relates to a metal salt of S-2-[S-N-[(S)-1-carboxyl-3-phenpropyl]-L-alanyl]-1, 2, 3, 4-tetrahydro-3-isoquinoline acid (quinaprilat) and a hydrate of the metal salt, a preparation method and applications in preparing medicines of curing high blood pressure. As proved by experiments, compared with the quinaprilat, the water solubility and stability of the metal salt of quinaprilat of the invention including salt and hydrate synthesized by the the metal salt of quinaprilat and one or two of ions of lithium, natrium, kalium, barium, calcium, magnesium and zinc, particularly the sodium salt, kalium salt, sodium potassium salt of the metal salt and the hydrate of the metal salt, is notably increased, and various clinically acceptable dosage forms can be easily produced.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, in particular to S-2-[S-N-[(S)-1-carboxy-3-phenylpropyl]-L-alanyl]-1,2,3,4-tetrahydro- The metal salt of 3-isoquinolinic acid, that is, quinaprilat, and its hydrate, its preparation method and its use in the preparation of medicines for treating hypertension. 2. Background technology [0002] Hypertension is a disease that seriously endangers human health and affects the quality of life. The clinical manifestations include headache, dizziness, dizziness, neck tension, tinnitus, vertigo, forgetfulness, insomnia, boredom, fatigue, numbness of limbs, palpitations, etc. It is also an important cause of limb paralysis, heart failure, cerebral infarction, cerebral hemorrhage, and renal failure. Clinically, cases of disability and death due to hypertension are not uncommon, and they are called "invisible killers". The prevalence of hypertension in my country is about 12%, and there are more than 1...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D217/26A61K31/472A61K9/08A61P9/12
Inventor 晁阳高建兴梁静黄振华
Owner NANJING YOKO PHARMA
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