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Pharmaceutical co-crystal of elagolix and palmoxiric acid and preparation method of pharmaceutical co-crystal

A technology of pamoic acid and co-crystal, which is applied in the field of drug co-crystal of elagolix and pamoic acid and its preparation, and can solve the problems of low bioavailability and low solubility, etc.

Pending Publication Date: 2021-01-08
国家卫生健康委科学技术研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to make up for the deficiencies in the prior art, the object of the present invention is to provide a new crystal form of ethinyl estradiol to improve the low solubility and low bioavailability of ethinyl estradiol raw materials.

Method used

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  • Pharmaceutical co-crystal of elagolix and palmoxiric acid and preparation method of pharmaceutical co-crystal
  • Pharmaceutical co-crystal of elagolix and palmoxiric acid and preparation method of pharmaceutical co-crystal
  • Pharmaceutical co-crystal of elagolix and palmoxiric acid and preparation method of pharmaceutical co-crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1 Preparation of elagolix drug cocrystal

[0050] In a common 50ml three-neck flask, add 50mg of elagoli (free acid) and 24.5mg of pamoic acid, then add 2ml of methanol, heat up and reflux for 30min, then slowly cool down, and the mixed solution slowly volatilizes at room temperature for about 1 week, and obtain White powdery solid, HPLC purity test is 99.3%.

Embodiment 2

[0051] Example 2 PXRD detection of elagolix drug cocrystal

[0052] 1. Sample

[0053] The solid obtained by the method of Example 1 was ground and sieved and accurately weighed, and a sample of 50 mg was detected.

[0054] 2. PXRD detection

[0055] The D8 X-ray powder diffractometer of German Bruker Company was used for PXRD detection of drug cocrystals.

[0056] Experimental conditions:

[0057]

[0058] Pipe pressure 40kV;

[0059] Pipe flow 40mA;

[0060] Time constant 0.1S;

[0061] The test range is 5°~90°.

[0062] 3. Results

[0063] The results of X-ray powder diffraction of elagoli drug cocrystal are shown in Table 1 and figure 1 shown.

[0064] Table 1 PXRD peak list of elagolix drug cocrystal

[0065] 2θ d BG Height ％ area ％ wxya 4.135 21.352 372 776 100 5111 100 0.112 7.529 11.7325 353 210 27.1 2884 56.4 0.234 8.351 10.5787 359 235 30.3 1543 30.2 0.112 9.08 9.7311 346 75 9.7 531 10.4 0...

Embodiment 3

[0066] The thermogravimetric analysis of embodiment 3 elagolix drug cocrystals

[0067] 1. Sample

[0068] Weigh 5-10 mg of the solid obtained by the method of Example 1 of the sample for detection.

[0069] 2. Thermogravimetric analysis

[0070] Mettler Thermogravimetric Analyzer (TGA-1) was used to detect the out-of-order of the drug.

[0071] Experimental conditions:

[0072] Alumina crucible;

[0073] The temperature detection range is 30~400℃;

[0074] Heating rate 10K / min;

[0075] The nitrogen flow rate was 50ml / min.

[0076] 3. Results

[0077] The result is as figure 2 As shown, the drug eutectic has no obvious out-of-order phenomenon in the heating stage.

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Abstract

The invention discloses a pharmaceutical co-crystal of elagolix and palmoxiric acid and a preparation method of the pharmaceutical co-crystal, wherein the crystal form has high stability under the conditions of high temperature, high humidity and illumination, and compared with a raw material medicine, the crystal form has higher purity.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a drug co-crystal of elagolix and pamoic acid and a preparation method thereof. Background technique [0002] Elagolix (1) was approved by the U.S. Food and Drug Administration through Priority Review for ORILISSA™ (Elagolix), the only oral stimulant currently available, for the treatment of women with moderate to severe endometriosis pain. Gonadal hormone-releasing hormone (GnRH) antagonists. [0003] The structure of elagolil is shown in (1). Since the structure contains a n-butyric acid and a secondary amine structure, elagolil is unstable and easily forms a lactam structure (2). [0004] [0005] At present, oxaraguride is marketed as the salt form of oxaraguride sodium, and its sodium salt is in the form of an amorphous solid, which cannot be purified by recrystallization in solution. In addition, the sodium salt of elagolix has low solubility and can form a lactam ring during sta...

Claims

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Application Information

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IPC IPC(8): C07D239/22C07D301/00C07D303/38A61P15/00A61P29/00A61K31/513A61K31/336
CPCC07D239/22C07D301/00C07D303/38A61P15/00A61P29/00C07B2200/13
Inventor 陈晓锋宁丽锋徐娟王慧萍
Owner 国家卫生健康委科学技术研究所
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