Enalapril drops

A technology of enalapril and matrix, applied in pill delivery, cardiovascular system diseases, organic active ingredients, etc., can solve the problems of allergic reactions or adverse reactions of injections, hepatic and intestinal first-pass effect bioavailability, manufacturing and medical treatment High cost and other issues, to achieve flexible and accurate dosage, improve bioavailability, reduce manufacturing and medical costs

Inactive Publication Date: 2010-05-05
JIAMUSI LULING PHARMA CO LTD SUNFLOWER PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0032] However, due to the inherent characteristics of the preparation technology, the conventional oral preparations have problems such as long dissolution time, low dissolution rate, poor absorption, hepatic first-pass effect and low bioavailability after taking, which affect the efficacy of the drug. Play, also directly affect the effect of treatment
Both hypertension and cardiovascular patients need to take the effect quickly after taking it. Due to the disadvantage of long dissolution time, the use of conventional oral preparations such as tablets and capsules is limited for acute attack diseases.
[0033] Although enalapril injection has the advantage of fast onset of action, because the injection is often prone to allergic reactions or adverse reactions, etc., it also has the disadvantages of difficult operation, great pain for patients, high manufacturing and medical costs, and low cost for patients. The shortcomings of heavy burden and inconvenient use make its application also limited, so it is still necessary to find an oral formulation of enalapril that is both convenient to use and effective as soon as possible

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] 1. Example 1 Experiments of different ratios of enalapril and matrix

[0064] Experimental design: In order to observe the influence of the different ratios of the active ingredients of the medicine and the matrix on the product obtained in the present invention, enalapril maleate was used as the active ingredient of the medicine, and polyethylene glycol was used as the active ingredient. 4000 , polyethylene glycol 10000 , carboxymethyl starch sodium and other three materials are mixed according to the ratio of 4:2:1 as the matrix, and the enalapril maleate and the above mixed matrix are respectively mixed in a ratio of 1:1 to 12 (step size is 1). The ratio is mixed evenly, liquid paraffin is selected as the condensing agent, and the preparation is carried out according to the steps given in the preparation method, 12 experiments with different ratios can be obtained, and 12 groups of corresponding experimental results are shown in Table 1.

Embodiment 2

[0065] 2. Example 2 Experiment of mixing enalapril with different substrates

[0066] Experimental Design: In order to observe the influence of the drug active ingredient mixed with different bases on the product of the present invention, polyethylene glycol was first 4000 and polyethylene glycol 10000 Mix evenly in a ratio of 2:1, and then mix the resulting mixture with sodium carboxymethyl starch, glycerol monostearate and polyoxyethylene monostearate in a ratio of 6:1 to obtain three kinds of mixed matrix. Enalapril maleate is used as the active ingredient of the drug, mixed with the above three different combination bases at a ratio of 1:7, and liquid paraffin is selected as the condensing agent, and the preparation is carried out according to the steps given in the preparation method to obtain Experiments with three different matrix combinations, and three sets of corresponding experimental results are shown in Table 2.

Embodiment 3

[0067] 3. Example 3 Experiments of selecting different dripper temperatures

[0068] Experimental design: In order to observe the influence of selecting different dripper temperatures on the product obtained in the present invention during the preparation process, the matrix combination given in Example 1 was selected, and the pharmaceutical active ingredient and matrix content and proportioning ratio given in Example 2 were selected. The DW-35 dripping pill machine produced by Taixing No. 2 Pharmaceutical Machinery Factory or a self-made special pilling machine, adjust its temperature control system to keep the temperature of the dripper at (60, 70, 80, 90, 100) ± 2°C, Select liquid paraffin as the condensing agent, and prepare according to the steps given in the preparation method. Five different experiments can be obtained, and the corresponding experimental data of the five groups are shown in Table 3.

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PUM

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Abstract

A dripping pill of enalaprol for preventing and treating hypertension is prepared from enalaprol and its salts through proportionally mixing surfactant (polyethanediol), heating until the mixture is fused, stirring and dripping in condensing liquid.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating and preventing various hypertension and cardiovascular diseases, especially an oral preparation with enalapril as the active ingredient. The enalapril also includes its medically acceptable salts. Background technique [0002] In the past 30 years, with the in-depth study of the pathogenesis of hypertension, it has been confirmed that the renin-angiotensin-aldosterone system is one of the important pressurization mechanisms. The general process of its function is that when the body’s renal blood flow is insufficient or the blood sodium is reduced, the kidney’s juxta-glomerular cells secrete a proteolytic enzyme called renin, which converts α in the blood 2 Globulin (i.e., angiotensinogen) is decomposed into angiotensin I, which is converted into angiotensin II under the action of angiotensin-converting enzyme (ACE), and angiotensin II is a powerful vasoconstrictor substance. If the a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/401A61K9/20A61P9/12
Inventor 曲韵智
Owner JIAMUSI LULING PHARMA CO LTD SUNFLOWER PHARMA GRP
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