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Fosinopril sodium and hydrochlorothiazide pharmaceutical composition and preparation method thereof

A technology of sodium hydrochlorothiazide and hydrochlorothiazide, which is applied in the field of medicine, and can solve the problems of slow dissolution of hydrochlorothiazide, slow dissolution speed of hydrochlorothiazide, and influence of preparation efficacy

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

AI Technical Summary

Problems solved by technology

However, the stability of hydrochlorothiazide in the above preparations is poor, thus affecting the curative effect of the preparations
[0010] 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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  • Fosinopril sodium and hydrochlorothiazide pharmaceutical composition and preparation method thereof
  • Fosinopril sodium and hydrochlorothiazide pharmaceutical composition and preparation method thereof
  • Fosinopril sodium and hydrochlorothiazide pharmaceutical composition and preparation method thereof

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Effect test

Embodiment 1

[0066] The preparation of embodiment 1 hydrochlorothiazide crystal

[0067] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.1g / ml hydrochlorothiazide;

[0068] (2) Add distilled water dropwise to the acetone solution under stirring at 160r / min until the solution becomes turbid;

[0069] (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;

[0070] (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.

[0071] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by measuring...

Embodiment 2

[0072] The preparation of embodiment 2 hydrochlorothiazide crystals

[0073] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain acetone solution whose concentration is 0.2g / ml hydrochlorothiazide;

[0074] (2) Add distilled water dropwise to the acetone solution under stirring at 120r / min until the solution becomes turbid;

[0075] (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;

[0076] (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 dry in vacuum to obtain hydrochlorothiazide crystals.

[0077] Such as figure 1As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by meas...

Embodiment 3

[0078] The preparation of embodiment 3 hydrochlorothiazide crystals

[0079] (1) 1kg hydrochlorothiazide is dissolved in acetone to obtain a solution of acetone with a concentration of 0.08g / ml hydrochlorothiazide;

[0080] (2) Add distilled water dropwise to the acetone solution under stirring at 180r / min until the solution becomes turbid;

[0081] (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;

[0082] (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.

[0083] Such as figure 1 As shown, the characteristic peaks in the X-ray powder diffraction pattern obtained by ...

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Abstract

The invention discloses a fosinopril sodium and hydrochlorothiazide pharmaceutical composition and a preparation method thereof. The pharmaceutical composition is a tablet or capsule prepared from hydrochlorothiazide crystal, fosinopril sodium and pharmaceutically acceptable auxiliary materials. The composition comprises the following components in parts by weight: 5-45 parts of fosinopril sodium, 5-30 parts of hydrochlorothiazide crystal, 10-50 parts of pregelatinized starch, 20-25 parts of sodium carboxymethyl starch, 15-35 parts of microcrystalline cellulose PH102, 10-45 parts of hydroxypropyl cellulose and 0.5-1 part of magnesium stearate. The pharmaceutical composition has the advantages of reasonable prescription, stable and reliable quality, and better disintegration time limit and dissolution rate. In the invention, a powder direct tabletting process is adopted, thus the preparation method has the advantages of simple process, short production period and low production cost and can easily realize industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a fosinopril sodium hydrochlorothiazide tablet 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 of cardiovascular ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/549A61K9/48A61K9/28C07D285/28A61K31/675A61P9/12
Inventor 马鹰军钟正明罗韬王小树
Owner HAINAN JINRUI PHARMA
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