Novel pharmaceutical composition of 2-(4-isobutyl phenyl) propionic acid

A composition and drug technology, applied in the field of medicine, can solve the problems of content change, purity reduction, influence on preparation safety, etc.

Active Publication Date: 2015-06-03
广州新创翼有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the methods described in the above-mentioned patents all have disadvantages: either the prepared salt, such as sodium salt, is highly irritating; or the salt needs to be prepared into a raw material drug first, which is cumbersome and costly, and is not conducive to environmental protection.
However, our research found that when the proportion of arginine in the composition was greater than that of ibuprofen, after terminal sterilization of the injection prepared, although the purity and content of ibuprofen did not decrease, the content of arginine changed, due to The content of arginine is difficult to be detected by conventional ultraviolet detectors. Our HPLC analysis of pre-column derivatization found that the content and purity of arginine decreased. We speculated that arginine was degraded. As a comparison, it was confirmed that degraded small molecule urea appeared in the system, which was caused by the decomposition of arginine in the preparation at high temperature, and the higher the molar ratio of arginine in the injection: ibuprofen, the higher the urea and other urea in the system. The higher the content of a degradation product α, ω-diaminovaleric acid, it far exceeds ICH’s requirements for impurity limits and seriously affects the safety of the preparation

Method used

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  • Novel pharmaceutical composition of 2-(4-isobutyl phenyl) propionic acid
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  • Novel pharmaceutical composition of 2-(4-isobutyl phenyl) propionic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of powder injection with arginine: ibuprofen molar ratio of 1.2:1

[0051] prescription

[0052]

[0053] Arginine and ibuprofen were both treated with activated carbon for needles according to the powder injection workshop's requirements for material entry and exit, equipment and utensils, and standard operating procedures for use. Add about 1.8 liters of water for injection in the arginine of 209g, stir at room temperature until dissolving, then add the ibuprofen of 206g in the arginine solution of gained, mix at room temperature until dissolving, add water to 2.06 liters in the gained solution, obtain Molar ratio (arginine: ibuprofen) is the 100mg / ml ibuprofen solution of 1: 1.2, then the medicinal liquid filling after the inspection is qualified in the aseptic antibiotic glass bottle, then the glass bottle is placed in lyophilization After pre-freezing in the machine for 4 hours, sublimation at low temperature for 16 hours, and then drying under redu...

Embodiment 2-4

[0055] The same method as in Example 1 was used to prepare arginine: ibuprofen lyophilized powders with molar ratios of 1.1:1, 1.5:1 and 1.8:1 respectively.

Embodiment 5

[0057] Preparation of Injection with Ibuprofen Arginine Salt:Arginine Hydrochloride Molar Ratio of 1:0.2

[0058] prescription

[0059]

[0060]The arginine of 209g, the ibuprofen of 206g are added in 1.4 liters of water for injection, after heating and stirring until dissolving, be cooled to 0 ℃, slowly add hydrochloric acid and then be settled to 2.06 liters with water for injection again, obtain molar ratio (arginine Acid: ibuprofen) is 1: 1.2 100mg / ml solution (i.e. ibuprofen arginine salt: arginine hydrochloride molar ratio is 1: 0.2), adds the carbon for needle by 0.15% of total water, Stir at 60°C for 10 to 15 minutes, then filter the resulting solution through a G6 sand rod and a 0.2 μm microporous membrane, and then pack it into a receiving bottle. After passing the clarity inspection, it is filled and sealed. Terminal sterilization, the sterilized product is packaged after vacuum leak detection, uniform dispersion by shaking, cooling and light inspection.

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PUM

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Abstract

The invention provides a novel pharmaceutical composition of a 2-(4-isobutyl phenyl) propionic acid (ibuprofen). The molar ratio of arginine to ibuprofen is (1.1:1) to (2:1); and the arginine is protonized by acid or exists in a form of a solution for forming a salt together with the acid. The invention further provides a method for preparing the composition. The composition provided by the invention is capable of reducing the incidence rate of the adverse reaction on a gastrointestinal tract and a cardiovascular system caused by the ibuprofen at a certain degree. In addition, the composition is relatively stable, and visible foreign matters and the phenomenon that total impurities exceed the standard are not easily generated in sterilization or degerming and long-term storage processes.

Description

[0001] The present invention is a divisional application of a Chinese patent application with the application number 201110192251.0, the application date being July 8, 2011, and the invention name being "a novel pharmaceutical composition of 2-(4-isobutylphenyl)propionic acid". technical field [0002] The invention belongs to the field of medicine, and relates to lyophilized or solution form preparations of 2-(4-isobutylphenyl) propionic acid, more specifically, the present invention relates to basic amino acid arginine and 2-(4-isobutylphenyl) ) A pharmaceutical composition in the form of lyophilization or solution in which the molar ratio of propionic acid is greater than or equal to 1, and a preparation method thereof. Background of the invention [0003] 2-(4-isobutylphenyl) propionic acid is the chemical name of the well-known non-steroidal anti-inflammatory analgesic drug ibuprofen, and has become the largest non-steroidal anti-inflammatory antipyretic analgesic (NSAID...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K47/18A61P29/00A61P9/14A61P1/16A61P25/00
Inventor 王海勇孙天宇
Owner 广州新创翼有限公司
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