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

Crystal form I of olaparib and preparation method thereof

A technology of crystal form and powder diffraction pattern, applied in the directions of medical preparations, pharmaceutical formulations, organic active ingredients, etc. containing active ingredients, which can solve the differences in clinical efficacy, solubility and stability, and affect drug absorption and bioavailability. and other problems, to achieve the effect of simple process, non-toxic solvent and environmental protection

Inactive Publication Date: 2020-12-01
CRYSTAL PHARMA CO LTD
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Different crystal forms of solid chemical drugs can cause different solubility and stability, which will affect the absorption and bioavailability of drugs, and will lead to differences in clinical efficacy

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
  • Crystal form I of olaparib and preparation method thereof
  • Crystal form I of olaparib and preparation method thereof
  • Crystal form I of olaparib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation method of olaparib crystal form I:

[0048] Dissolve 10.0 mg of olaparib free base in 1.0 mL of pure water, stir at room temperature for 7 days, filter with suction, dry, and collect the solid. After testing, the crystal form prepared in this example is Form I.

[0049] Table 1 shows the X-ray powder diffraction data of the crystal forms obtained in this example. Its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in image 3 .

[0050] Table 1

[0051]

[0052]

Embodiment 2

[0054] The preparation method of olaparib crystal form I:

[0055] Add 10.0 mg of olaparib crystal form A in patent CN101528714B to 0.5 mL of pure water, then add 1.0 mg of crystal form I seed crystals, stir at room temperature for 72 hours, filter with suction, wash with pure water, and dry. The solid was collected, and it was detected that the crystalline form prepared in this example was crystalline form I.

[0056] Table 2 shows the X-ray powder diffraction data of Form I obtained in this example.

[0057] Table 2

[0058]

[0059]

Embodiment 3

[0061] Stability comparative test of olaparib crystal form I and crystal form A in patent CN101528714B:

[0062] Take 10.0 mg of the crystal form A in patent CN101528714B and 1.0 mg of the crystal form I prepared in Example 1 in a vial, add 0.5 mL of pure water to make a suspension. After stirring at room temperature for 72 hours, the XRPD of the test sample showed that the crystal form A in the patent CN101528714B had been completely transformed into the crystal form I in the present invention, and the results are shown in Table 3.

[0063] table 3

[0064]

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 relates to a crystal form I of olaparib and a preparation method thereof. Specifically, the crystal form I is characterized in that an X-ray powder diffraction pattern of the crystal form I has characteristic peaks when 2theta values are 6.4 + / -0.2 degrees, 12.7 + / -0.2 degrees and 15.1 + / -0.2 degrees. The crystal form I is better in stability and has important value for optimizing and developing the medicine in the future.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, in particular to the crystal form I of olaparib and a preparation method thereof. Background technique [0002] Olapani was first developed by the British biotechnology company KuDOS (Kudos) Pharmaceutical Co., Ltd. After being acquired by AstraZeneca, it continued to develop a drug for the treatment of ovarian cancer. On December 19, 2014, Olaparib was approved by the FDA for marketing in the United States. It is the first targeted drug approved by the FDA for ovarian cancer patients with BRCA mutations, and is suitable for patients who have previously undergone chemotherapy. It has been demonstrated in preclinical models that olaparib is a first-in-class oral poly ADP ribose polymerase (PARP) inhibitor that exploits defects in the DNA repair pathway to preferentially kill cancer cells. [0003] The chemical name of olaparib is 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-b...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/32A61K31/502A61P35/00
CPCC07D237/32
Inventor 陈敏华张炎锋刘凯邹坡张晓宇
Owner CRYSTAL PHARMA CO LTD
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