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Pharmaceutical composition containing aryl propionic acid compound

A technology of compounds and compositions, applied in the field of medicinal chemistry, can solve problems such as inability to meet

Active Publication Date: 2020-10-27
NANJING HERON PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is also difficult to meet the therapeutic purposes of rapid analgesia, antipyretic and anti-inflammatory in clinical hope

Method used

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  • Pharmaceutical composition containing aryl propionic acid compound
  • Pharmaceutical composition containing aryl propionic acid compound
  • Pharmaceutical composition containing aryl propionic acid compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of embodiment 1 formula I compound

[0041] The preparation method of the compound of formula I is obtained from the reference "Tetrahedron Asymmetry, 2011, 22: 1125-1132". Those of ordinary skill in the art can obtain this compound through conventional synthesis methods, and the structure has been confirmed, see the attached Figure 1-3 ,No longer.

[0042] It is worth noting that, in the prescriptions of the following preparation examples, the selection and dosage of each component of the main drug and auxiliary materials are only for illustration. Those skilled in the art can make conventional adjustments, replacements and changes based on information such as therapeutic doses, specifications, and administration characteristics. degree. These should also belong to the scope of the design idea of ​​the present invention. In addition, in the preparation examples of the present invention, the dosage of the main drug is based on the weight of the acti...

Embodiment 2

[0043] Example 2 Preparation of Formula I Compound Injection

[0044] Main drug 10g

[0045] Sodium hydroxide 1.6g

[0046] Sodium chloride 8g

[0047] Water for injection to 1000mL;

[0048] Preparation method: Add water for injection with 80% of the prescription amount in the preparation container, weigh the main drug, sodium hydroxide and sodium chloride, dissolve and stir evenly, adjust the pH to 6.9 with sodium hydroxide and / or hydrochloric acid solution, and dilute to Final volume; filter with a 0.22 μm pore size sterile filter, divide the filtered solution into ampoules, seal, and sterilize at 121°C for 20 minutes to obtain the final product.

Embodiment 3

[0049] Example 3 Preparation of Formula I Compound Injection

[0050] Main ingredient 10g

[0051] L-Arginine 7g

[0052] Sodium chloride 8g

[0053] Water for injection to 1000mL

[0054] Preparation method: Add water for injection with 80% of the prescription amount in the preparation container, weigh the main drug, L-arginine and sodium chloride to dissolve, stir evenly, adjust the pH to 7.2 with arginine solution, and dilute to the final volume ; Use a 0.22 μm pore size sterile filter to filter, the filtered solution is divided into ampoules, sealed, and sterilized at 121 ° C for 20 minutes to obtain the product.

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Abstract

The invention provides a pharmaceutical composition containing (S)-2-(4-(((1R,2S)-2-hydroxycyclopentyl)methyl)phenyl)propionic acid represented by a formula I, wherein the pharmaceutical composition can be in various preparation forms including injections, oral solid preparations, external semisolid preparations and the like. The invention also provides a preparation method of the pharmaceutical composition, and application of the pharmaceutical composition in preparation of antipyretic, analgesic and anti-inflammatory drugs. The pharmaceutical composition disclosed by the invention has the advantages of relatively small dosage, relatively fast drug effect and relatively small toxic and side effects, and has a wide prospect in the clinical treatment fields of analgesia, antipyretic treatment and inflammation diminishing.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to a pharmaceutical composition containing aryl propionic acid compounds, the aryl propionic acid compounds are (S)-2-(4-(((1R,2S)- 2-hydroxycyclopentyl) methyl) phenyl) propionic acid, and the application of the pharmaceutical composition in the preparation of antipyretic, analgesic and anti-inflammatory drugs. Background technique [0002] Loxoprofen sodium, chemical name 2-[4-(2-oxocyclopentane-1-ylmethyl) phenyl] sodium propionate dihydrate, English name Loxoprofen Sodium, molecular formula is C 15 h 17 o 3 Na·2H 2 O, the molecular weight is 304.32, and the CAS number is 80382-23-6. Loxoprofen sodium belongs to arylpropionic acid non-steroidal anti-inflammatory drugs, and its mechanism of action is to inhibit the synthesis of prostaglandins by inhibiting cyclooxygenase. When loxoprofen sodium is taken orally, it is absorbed through the digestive tract in a precurs...

Claims

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Application Information

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IPC IPC(8): C07C59/54A61K31/192A61P29/00A61P17/02A61P19/02A61P19/08A61P27/02A61P1/02A61P15/00
CPCC07C59/54A61P29/00A61P17/02A61P19/02A61P19/08A61P27/02A61P1/02A61P15/00C07C2601/08C07B2200/07
Inventor 闵涛徐烨胡情姣宿连征陈晨曹卫李瑜
Owner NANJING HERON PHARMA SCI & TECH CO LTD
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