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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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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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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 "TetrahedronAsymmetry, 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
[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
[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] Loxoprofensodium, chemical name 2-[4-(2-oxocyclopentane-1-ylmethyl) phenyl] sodiumpropionate dihydrate, English name LoxoprofenSodium, 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. Loxoprofensodium 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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