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Arginine-ketoprofen with antalgic and inflammation relieving actions and its preparing process

An arginine ketone, arginine technology, applied in the direction of anti-inflammatory agents, organic chemistry, non-central analgesics, etc., can solve the problem of increasing the route of administration, reducing the irritation of the gastrointestinal tract, and limiting the clinical application of ketoprofen Scope and other issues to achieve the effect of improving safety and eliminating stomach pain

Inactive Publication Date: 2002-10-30
CHENGDU SHENGNUO BIOTEC CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the above reasons, the scope of clinical application of ketoprofen is limited, domestic and foreign pharmacists have been looking for new drug combinations of ketoprofen, reducing the irritation to the gastrointestinal tract, increasing the route of administration, and expanding the clinical application of ketoprofen scope

Method used

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  • Arginine-ketoprofen with antalgic and inflammation relieving actions and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach ： Embodiment 1

[0013] DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS Example 1: Preparation of Arginine Ketoprofen

[0014] Add 101.6 g (0.4 mol) of ketoprofen, 69.6 g (0.4 mol) of L-arginine and 1000 ml of distilled water in sequence to the reaction flask, stir to react to a clear liquid, freeze-dry, and the specific conditions are shown in the following table.

[0015] Freeze drying conditions

[0016] Temperature (℃) Time (hours) Remarks

[0017] -40 8 Pre-freeze

[0018] -40 2 vacuum

[0019] -30 2 vacuum

[0020] -20 2 vacuum

[0021] -10 4 Vacuum

[0022] -5 6 Vacuum

[0023] 0 6 Vacuum

[0024] 10 6 Vacuum

[0025] 20 3 Vacuum

[0026] 30 3 was evacuated to obtain 168.8 g of white solid with a yield of 98.6%.

[0027] Using ketoprofen as the reference substance for content determination, the content of the product was 99.8%.

Embodiment 2

[0028] Example 2 Hot plate analgesia test

[0029] 60 female mice weighing 19-21 grams were selected and randomly divided into 6 groups with 10 mice in each group. After measuring the pain threshold before administration by the hot plate method, groups 1-5 were given arginine ketoprofen by gavage. Arabic gum liquid, the dose calculated by ketoprofen is 40.82, 28.41, 20.14, 10mg / kg; the administration concentration is 1.63, 1.14, 0.80, 0.56, 0.39mg / ml, and the administration volume is 0.5ml / 20g; Group 6 In the same way, 0.5ml / 20g of 10% gum arabic was given. Pain thresholds were measured again at 1.5 hours, 3 hours, and 4.5 hours after administration. Calculate the mean value and standard deviation of pain threshold in each group, and do t test to compare whether there is a significant difference between each administration group and the blank control group. The results are shown in the following table.

[0030] Influence of arginine ketoprofen on pain induc...

Embodiment 3

[0035] Effect of Example 3 on the Bacterial Endotoxin Pyrogenic Model in Rabbits

[0036] 30 rabbits with a body weight of 1.85-2.25Kg were selected for the pre-selected pyrogen test, their normal body temperature was measured, and 1ml / kg of bacterial endotoxin solution was injected. , 6 in each group. The first, second and third groups were given 1 dose of ketoprofen arginine ketoprofen calculated as 10, 5, 2.5 mg / kg, and the concentrations were 1 mg / ml, 0.5 mg / ml and 0.25 mg / ml, respectively. The gavage volume was 10ml / kg, and the fourth group was gavaged with 10% gum arabic, 10ml / kg, for the negative control. After gavage, the body temperature of rabbits was measured every 30 minutes, a total of 8 times, and the average body temperature before the bacterial endotoxin was subtracted to obtain the temperature increase value. t-test was used to compare whether there was a significant difference between each administration group and the gum arabic negative control group. The ...

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Abstract

The present invention relates to the arginine-ketoprofen with antalgic and inflammation-relieving functions, relative isomers and its preparing process. Its solubility in water is solved to reduce its by-effect and it can provide a new application approach.

Description

Technical field: [0001] The present invention relates to a kind of arginine ketoprofen suitable for analgesia and anti-inflammatory and corresponding isomeric isomers and a preparation method. technical background: [0002] Ketoprofen is a non-steroidal anti-inflammatory drug. Because its efficacy is better than that of ibuprofen, it has attracted widespread attention from pharmacologists and clinicians around the world. Rheumatoid arthritis, ankylosing spondylitis, gout, osteoarthritis, hemophilic arthritis, cervical and lumbar spondylosis and migraine, trauma and post-operative pain. Because ketoprofen is an organic acid drug, insoluble in water, it is mainly distributed in the stomach, small intestine and kidney after gastrointestinal administration, so it has a great stimulating effect on the gastrointestinal tract, and the main clinical side effects are stomach pain and heartburn. Symptoms, nausea, vomiting, diarrhea, constipation, loss of appetite, weakness, etc., and...

Claims

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Application Information

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IPC IPC(8): A61P29/00C07C279/14
Inventor 文永均谢期林韩五成
Owner CHENGDU SHENGNUO BIOTEC CO LTD
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