Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Fenofibric acid crystal form and preparation method thereof

A fenofibric acid and crystal form technology, applied in the field of medicine, achieves the effects of low impurity content, good reproducibility, and mild reaction conditions

Inactive Publication Date: 2015-05-20
XUZHOU UNIV OF TECH
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no relevant report on the crystalline form of fenofibric acid

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Fenofibric acid crystal form and preparation method thereof
  • Fenofibric acid crystal form and preparation method thereof
  • Fenofibric acid crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Get the fenofibric acid crude product (Wuhan Hongxinkang Fine Co., Ltd.) 10.0g of light yellow powder, and the isopropanol of 100mL is placed in the round bottom flask of 250mL, heats in oil bath, the setting of oil bath The temperature is 95°C, after heating to reflux, add 1.0 g of activated carbon, and continue to reflux for 10 minutes. Use a Buchner funnel to vacuum filter while it is hot. The filtrate is cooled to crystallize at room temperature, and the Buchner funnel is vacuum filtered. The filter cake is washed once with 10 mL of isopropanol. After washing, the product is vacuum-dried at 80 ° C for 12 hours to obtain a white The powdered crystals are 8.6 g of fenofibric acid, and the fenofibric acid obtained in this example was detected by X-ray powder diffraction.

[0021] Test instrument: Swiss x’TRA X-ray diffractometer;

[0022] Test conditions: 40kv 40mA;

[0023] slit:2 / 4 / 0.5 / 0.2;

[0024] step: 0.02DEG;

[0025] Target type: Cu;

[0026] Range: 7.00-4...

Embodiment 2

[0035] Get fenofibric acid crude product (Wuhan Hongxinkang Fine Co., Ltd.) 10.0g, and 100mL of isopropanol (analytical pure) is placed in a 250mL round bottom flask, heated in an oil bath, and the temperature set by the oil bath is After heating to reflux, add 1.0g of activated carbon, continue to reflux for 10min, and vacuum filter with a Buchner funnel while it is hot. Once, after washing, the product was vacuum-dried at 80°C for 12 hours to obtain a white powdery crystal, which was fenofibric acid, weighing 8.6g, and the crystal was detected by X-ray powder diffraction method, and the detection parameters and implementation Example 1 is the same, and the gained XRD pattern is as follows Image 6 As shown, in terms of 2θ angle and interplanar spacing (d value), it is expressed at 15.920 (5.562), 18.440 (4.807), 19.240 (4.609), 20.220 (4.388), 21.440 (4.141), 23.100 (3.847), 23.760 (3.742) , 25.060 (3.550), 26.480 (3.363), 28.420 (3.138), 30.180 (2.959), 32.120 (2.784), wit...

Embodiment 3

[0038] Example 3 Stability detection of fenofibric acid crystal form

[0039] The fenofibric acid obtained in Example 1 is placed in the following environment, and the light intensity is 4500lx ± 500lx, and the obtained results are shown in Table 1-3:

[0040] Table 1 Investigation results of stability test under strong light irradiation

[0041]

[0042] Table 2 High temperature test stability test results (60±2°C)

[0043]

[0044] Table 3 High humidity test stability test results (RH90±5%)

[0045]

[0046] It can be seen from Table 1-3 that the fenofibrate acid crystal form of the present invention has no change in related substances, the appearance and color of the fenofibrate acid crystal form of the present invention under the conditions of strong light, high temperature and high humidity, and the content of fenofibric acid does not change. Changes occur, indicating that the crystal form obtained by the method of the present invention has good stability and i...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a fenofibric acid crystal form and a preparation method thereof. The fenofibric acid crystal form has characteristic absorption peaks on the powder diffractogram when the 2theta angle is 18.44+ / -0.1 degrees, 19.24+ / -0.1 degrees, 21.44+ / -0.1 degrees and 23.08+ / -0.1 degrees. The preparation method comprises the following steps: mixing a fenofibric acid crude product with isopropanol, heating under reflux, cooling the filtrate to crystallize, and drying the precipitated crystal, thereby obtaining the fenofibric acid crystal form.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a crystal form of fenofibric acid and a preparation method thereof. Background technique [0002] Fenofibric acid, English name: fenofibric acid, chemical name: 2-[4-4-chlorobenzoyl)phenoxy]-2-methyl-propionic acid, molecular formula is C 17 h 15 ClO 4 , is a clofibrate derivative-like blood lipid regulator, which is a metabolite of the lipid regulator fenofibrate in the human body, which inhibits the formation of very low-density lipoprotein and triglyceride and simultaneously catabolizes it Increase, lower blood low-density lipoprotein, cholesterol and triglycerides. Fenofibrate is insoluble in water, and its preparations have a tendency to recrystallize during release in the human body, thereby reducing the bioavailability of the drug; in contrast, fenofibric acid has a higher concentration in the small intestine The solubility of fenofibrate can better overcome the insol...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07C59/68C07C51/43
CPCC07C51/43C07B2200/13C07C59/90
Inventor 周俊董黎明
Owner XUZHOU UNIV OF TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com