Novel isosorbide mononitrate injection

A technology of isosorbide dinitrate and injection, which is applied in the field of medicine, can solve the problems that the pH range of the injection is not the optimal choice, no pH regulator is given, and the pH regulator is single, so as to reduce adverse reactions and achieve accurate dosage , to expand the effect of the application

Active Publication Date: 2008-04-30
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, after the oral preparation is taken orally, the blood drug concentration rises rapidly to 400ng / ml, which greatly exceeds the minimum effective dose (100ng / ml), causing the patient to have severe side effects such as headache, nausea, vomiting, and circulatory collapse. About 14%, and in long-term use, tolerance often occurs, reducing the curative effect
[0005] In addition, in the existing injection product prescriptions on the market, the pH regulators used all use a single acid or alkali, which cannot maintain the pH in a relatively constant range for a long time, and has the disadvantage of instability
[0006] "Chinese Journal of New Drugs" 2000 Volume 9 No. 8 "Development of 5-Isosorbide Mononitrate Injection" discloses the preparation method of Isosorbide Mononitrate Injection, but this technical process does not provide optimal pH adjustment It only mentions that the most commonly used 0.5mol / L NaOH and 0.5mol / L HCl are used to adjust the pH to 6.0-8.0, and the given injection pH range is not the optimal choice

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 water injection preparation process

[0016] Isosorbide Mononitrate 15g

[0017] 1,2-propanediol 1000ml

[0018] NaH 2 PO 4 -Na 2 HPO 4 Buffer (PH5.0) appropriate amount

[0019] Add water for injection to 5000ml

[0020] NaH 2 PO 4 -Na 2 HPO 4 Buffer (pH5.0) preparation method: take 0.2mol / L NaH 2 PO 4 A certain amount of solution is adjusted to pH 5.0 with sodium hydroxide test solution.

[0021] Dissolve the prescribed amount of isosorbide mononitrate in 70% of the total water for injection, then add the prescribed amount of 1,2-propanediol, appropriate amount of NaH 2 PO 4 -Na 2 HPO 4 Mix the buffer solution with the above-mentioned isosorbide mononitrate solution, add water for injection to an appropriate amount, mix evenly, add 0.1% activated carbon for needles, stir and adsorb for 10-20 minutes, decarbonize and filter. Add water for injection to the full amount, mix well, circulate and filter, and control the pH within the range of 6...

Embodiment 2

[0022] Embodiment 2 water needle preparation process

[0023] Isosorbide Mononitrate 15g

[0024] 1,2-propanediol 1000ml

[0025] NaH 2 PO 4 -Na 2 HPO 4 Buffer (PH5.6) appropriate amount

[0026] Add water for injection to 5000ml

[0027] NaH 2 PO 4 -Na 2 HPO 4 Buffer solution (PH5.6) configuration method: precision weigh anhydrous NaH dried at 115°C±5°C for 2-3 hours 2 PO 4 3.8g with Na 2 HPO 4 0.5g, add water to dissolve and dilute to 100ml.

[0028] The preparation process is the same as in Example 1.

Embodiment 3

[0029] Embodiment 3 water injection preparation process

[0030] Isosorbide Mononitrate 15g

[0031] 1,2-propanediol 1000ml

[0032] NaH 2 PO 4 -Na 2 HPO 4 Buffer (PH5.7) appropriate amount

[0033] Add water for injection to 5000ml

[0034] NaH 2 PO 4 -Na 2 HPO 4 Buffer (PH5.7) configuration method: 6.5ml of 0.2mol / L Na 2 HPO 4 With 93.5ml of 0.2mol / L NaH 2 PO 4 Just mix well.

[0035] The preparation process is the same as in Example 1.

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PUM

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Abstract

The invention provides a novel isosorbide mononitrate injection composition containing 1,2-propylene glycol and phosphate buffer and a preparation method thereof. Phosphate buffer is used to adjust the pH of the injection to 6.8-7.9. The injection prepared by the application of the invention improves the purity of the effective components of the medicine, reduces the content of related substances, and reduces the toxicity at the same time.

Description

Technical field [0001] The invention belongs to the field of medicine, and in particular relates to an isosorbide mononitrate injection composition containing phosphate buffer solution and a preparation method thereof. Background technique [0002] Isosorbide mononitrate is a commonly used drug for treating coronary heart disease and angina pectoris. It was first developed by Behringer Mannheim GmbH in Germany and launched in the market in 1981. It has been clinically used for many years and has a definite curative effect. Its main mechanism of action is to expand venous volume vessels and peripheral resistance vessels, reduce cardiac preload and postload, and reduce myocardial oxygen consumption. The drug has the characteristics of high bioavailability, small individual differences, long half-life, and remarkable curative effect, and is better than indigestion and nitroglycerin in the prevention of coronary heart disease and angina pectoris. [0003] Recent studies have sh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61K47/02A61P9/10
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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