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Gemfibrozil co-crystal and preparation method thereof

A technology of gemfibrozil and hexamethylenetetramine, applied in the field of drug development, can solve the problems of complex preparation process, poor stability, low drug loading and the like

Inactive Publication Date: 2020-02-07
BEIJING INSTITUTE OF TECHNOLOGYGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although preparation technology can improve the absorption properties of drugs to a certain extent, there are still some problems, such as: poor stability, low drug loading, and complicated preparation process

Method used

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  • Gemfibrozil co-crystal and preparation method thereof
  • Gemfibrozil co-crystal and preparation method thereof
  • Gemfibrozil co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～12

[0035] Examples 1-12 Preparation experiment and solubility test of gemfibrozil-isonicotine co-crystal

[0036] Take gemfibrozil and the corresponding isonicotine synthon in a molar ratio of 1:0.5 to 1:2 and place them in a ball mill jar, add 0.1 to 0.3ml of different auxiliary solvents and a stainless steel grinding ball with a diameter of 12mm, 1300 to 1800r The ball milled for 20-30 minutes under the vibration condition of / min. After the ball milling, the sample was dried naturally to obtain the gemfibrozil-isonicotine eutectic, and then the dissolution test was done in the in vitro buffer solution.

[0037] Table 1. Experimental parameters of gemfibrozil-isonicotine cocrystal, wherein the solubility of the original drug gemfibrozil is 0.22mmol / L.

[0038]

Embodiment 13～24

[0039] Example 13-24 Preparation of Gemfibrozil Hexamethylenetetramine Cocrystal

[0040] Take gemfibrozil and the corresponding hexamethylenetetramine synthon at a molar ratio of 1:0.5 to 1:2 and place them in a ball mill jar, add 0.1 to 0.3ml of different auxiliary solvents and a stainless steel grinding ball with a diameter of 12mm, Under the vibration condition of 1300~1800r / min, ball mill for 20~30min. After the ball milling, the sample was dried naturally to obtain Gemfibrozil hexamethylenetetramine eutectic, and then the dissolution test was done in the in vitro buffer solution.

[0041] Table 2. Experimental parameters of gemfibrozil hexamethylenetetramine cocrystal, wherein the solubility of the original drug gemfibrozil is 0.22mmol / L.

[0042]

[0043]

[0044] Gemfibrozil isonicotine and gemfibrozil hexamethylenetetramine cocrystals were analyzed by X-ray powder diffraction (PXRD), infrared (IR), thermogravimetric (DSC) 1 H NMR) for characterization, the stru...

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Abstract

The invention relates to gemfibrozil eutectic crystals prepared by a solvent-assisted ball milling method, belonging to the field of drug development. The method comprises the following steps: putting gemfibrozil and a corresponding eutectic crystal synthon in a mole ratio of 1:0.5-1:2 into a ball mill, adding 0.1-0.3 mL of different secondary solvents and a stainless steel milling ball with the diameter of 12mm, and carrying out ball milling under the vibration condition of 1300-1800 r / min for 20-30 minutes; and after finishing the ball milling, naturally drying the test sample in the air, thereby obtaining the gemfibrozil eutectic crystals. The structure of the gemfibrozil eutectic crystals is characterized by powder X-ray diffraction (PXRD), infrared spectrometry (IR), 1H nuclear magnetic resonance (1H NMR), differential scanning calorimetry (DSC), thermogravimetry (TG) and other means. The in-vitro dissolution rate experiment indicates that the solubility of the gemfibrozil eutectic crystals is obviously enhanced by 10.7 times and 132.48 times as compared with the original drug.

Description

technical field [0001] The gemfibrozil co-crystal and its preparation method involved in the present invention belong to the field of drug development. Background technique [0002] Gemfibrozil, Gemfibrozil is white powder, insoluble in water, easily soluble in organic solvents. The structural formula is as follows: [0003] [0004] Gemfibrozil was first screened by Dr. Crege's research group as a blood lipid-lowering drug, and then it was launched in the United States in 1982. Gemfibrozil is a derivative of clofibrate, which is very effective in the treatment of patients with severe type IV or V hyperlipoproteinemia, high risk of coronary heart disease and ineffective diet control and weight loss. The latest research shows: Clinical studies have shown that gemfibrozil can also prevent cardiovascular diseases by increasing high-density lipoprotein cholesterol (Engl.J.Med.1999,341,410). [0005] Gemfibrozil belongs to the class II drug, which has poor solubility and hi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C59/68C07C51/43C07D213/81C07D487/18
CPCC07B2200/13C07C51/43C07C59/68C07D213/81C07D487/18
Inventor 迟瑛楠杨秋红胡长文尧思
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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