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Brand new levamlodipine and hydrochlorothiazide medicinal composition and preparation method thereof

A technology of levamlodipine hydrogen and levamlodipine, which is applied in the field of new levamlodipine hydrochlorothiazide pharmaceutical composition and its preparation, can solve the problems of slow dissolution rate of hydrochlorothiazide, unsatisfactory curative effect of pharmaceutical preparations and unsatisfactory preparation stability Significant improvement and other issues

Active Publication Date: 2012-01-25
HAINAN JINRUI PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Patent application CN101659643A discloses a crystal form of hydrochlorothiazide and its use. Aiming at the problems of slow dissolution and poor bioavailability of hydrochlorothiazide commonly found in the prior art, a new hydrochlorothiazide crystal form III (such as figure 2 shown), the results show that the dissolution rate of the preparation product made of hydrochlorothiazide crystal form III or the composition of hydrochlorothiazide III and other types of antihypertensive drugs can reach a level similar to that of similar foreign products, and solve the problem of hydrochlorothiazide dissolution to a certain extent. slow speed problem
However, the stability of the preparation has not been significantly improved, and the curative effect of the pharmaceutical preparation is not ideal. In view of this, the present invention is proposed

Method used

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  • Brand new levamlodipine and hydrochlorothiazide medicinal composition and preparation method thereof
  • Brand new levamlodipine and hydrochlorothiazide medicinal composition and preparation method thereof
  • Brand new levamlodipine and hydrochlorothiazide medicinal composition and preparation method thereof

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Effect test

Embodiment 1

[0064] The preparation of embodiment 1 hydrochlorothiazide crystal

[0065] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.1g / ml hydrochlorothiazide;

[0066] (2) Add distilled water dropwise to the acetone solution under stirring at 160r / min until the solution becomes turbid;

[0067] (3) under the ultrasonic field that power is 0.5KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 25r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 5: 6, The volume ratio of described mixed solution and acetone is 1: 1;

[0068] (4) Continue ultrasonication for 2 minutes, let stand, grow crystals at 16° C. for 2 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0069] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by measuring...

Embodiment 2

[0070] The preparation of embodiment 2 hydrochlorothiazide crystals

[0071] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.2g / ml hydrochlorothiazide;

[0072] (2) Add distilled water dropwise to the acetone solution under stirring at 120r / min until the solution becomes turbid;

[0073] (3) under the ultrasonic field that power is 0.4KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 20r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 2: 3, The volume ratio of described mixed solution and acetone is 4: 5;

[0074] (4) Continue ultrasonication for 2 minutes, let stand, grow crystals at 12° C. for 1.5 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0075] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by measur...

Embodiment 3

[0076]The preparation of embodiment 3 hydrochlorothiazide crystals

[0077] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain a solution of acetone with a concentration of 0.08g / ml hydrochlorothiazide;

[0078] (2) Add distilled water dropwise to the acetone solution under stirring at 180r / min until the solution becomes turbid;

[0079] (3) under the ultrasonic field that power is 0.6KW, flow the organic mixed solution of ethanol and ether in the solution gained in step 2, continue the stirring of 30r / min; Wherein the volume ratio of ethanol and ether in the organic mixed solution is 7: 6, The volume ratio of described mixed solution and acetone is 8:5;

[0080] (4) Continue ultrasonication for 3 minutes, let stand, grow crystals at 18° C. for 2.5 hours, filter, wash the filter cake with ether, and vacuum-dry to obtain hydrochlorothiazide crystals.

[0081] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by m...

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Abstract

The invention discloses a brand new levamlodipine and hydrochlorothiazide medicinal composition and a preparation method thereof. The medicinal composition is an oral preparation which is prepared by adding pharmaceutically acceptable auxiliary materials into hydrochlorothiazide crystals and levamlodipine; and the oral preparation comprises but is not limited to tablets or capsules. The composition comprises the following components in part by weight: 2.5 to 5 parts of levamlodipine, 6.25 to 12.5 parts of hydrochlorothiazide crystal, 10 to 45 parts of pregelatinized starch, 20 to 25 parts of carboxymethyl starch, 15 to 35 parts of microcrystalline cellulose PH102, 10 to 45 parts of hydroxy propyl cellulose, and 0.5 to 1 part of magnesium stearate. The medicinal composition is reasonable in a prescription, stable and reliable in quality and good in disintegration time and high in dissolution rate; and a process for directly tabletting by using powder is adopted, the process is simple, the production cycle is short, production cost is low, and industrial production is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a novel levoamlodipine-hydrochlorothiazide medicinal composition and a preparation method thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases that endanger human health and is a major public health problem worldwide. At present, the control rate of hypertension in major countries in the world is not high. The National Nutrition and Health Status Survey released by the Ministry of Health of China in 2002 showed that there were nearly 160 million hypertensive patients in China, and the control rate of blood pressure was only 6.16%. A large number of evidence-based medical studies have confirmed that with the increase of blood pressure, the risk of cardiovascular events will increase significantly, especially in today's aging society, and the research and development of major and multiple diseases that meet the spectrum...

Claims

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Application Information

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IPC IPC(8): A61K31/549A61K31/4422A61K9/20A61K9/48A61P9/12C07D285/28
Inventor 马鹰军
Owner HAINAN JINRUI PHARMA
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