Gemfibrozil polycrystalline type and preparation thereof
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A technology of rozil crystal form and gemfibrozil, which is applied in the field of medicinal chemistry, can solve the problems of difficulty in storage and poor stability of gemfibrozil in amorphous form, and achieve the effects of no reduction in drug content, good stability, and easy production
Inactive Publication Date: 2009-05-27
ZHEJIANG UNIV
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Problems solved by technology
[0007] The present invention aims at the problems of poor amorphous stability and difficult preservation of gemfibrozil existing in the prior art, and provides a polymorphic preparation method of gemfibrozil, and obtains gemfibrozil crystal form II, which has good stability and no static electricity. , easy to produce, transport and store
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Embodiment 1
[0016] Embodiment 1: Preparation of gemfibrozil crystal form II
[0017] Add 10 g of gemfibrozil to 5 mL of toluene, heat (about 50° C.) to reflux, stir until completely dissolved, cool to crystallize, filter, and vacuum-dry at 40° C. for 8 hours to obtain Gemfibrozil Form II.
Embodiment 2
[0018] Embodiment 2: Preparation of gemfibrozil crystal form II
[0019] Add 10 g of gemfibrozil to 10 mL of toluene, heat (about 50° C.) to reflux, stir until completely dissolved, cool to crystallize, filter, and vacuum-dry at 40° C. for 8 hours to obtain Gemfibrozil Form II.
Embodiment 3
[0020] Embodiment 3: Preparation of gemfibrozil crystal form II
[0021] Add 10 g of gemfibrozil to 20 mL of toluene, heat (about 50° C.) to reflux, stir until completely dissolved, cool to crystallize, filter, and vacuum-dry at 40° C. for 8 hours to obtain Gemfibrozil Form II.
[0022] Gemfibrozil crystal form IX-ray powder diffraction pattern (XRD) of above-mentioned embodiment 1-3, see figure 1 , X-ray diffraction pattern of crystal form at 2θ (°, ±0.2) 5.85°, 8.06°, 8.51°, 11.49°, 11.79°, 12.66°, 12.86°, 13.43°, 13.78°, 16.24°, 16.59°, 17.12 °, 19.00°, 20.86°, 21.88°, 23.23°, 24.14°, showing characteristic diffraction peaks. At 59.3°C in the differential thermal analysis curve, an endothermic peak is shown. See figure 2 .
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Abstract
The invention relates to a Gemfibrozil crystal form II and a preparation method thereof. Gemfibrozil is dissolved through with certain amount of toluene and is crystallized, filtered and dried to form a new Gemfibrozil crystal form. The X-ray diffraction pattern of the crystal form shows character diffraction peaks at 2theta(degree,+/-0.2)5.85 degrees, 8.06 degrees, 8.51 degrees, 11.49 degrees, 11.79 degrees, 12.66 degrees, 12.86 degrees, 13.43 degrees, 13.78 degrees, 16.24 degrees, 16.59 degrees, 17.12 degrees, 19.00 degrees, 20.86 degrees, 21.88 degrees, 23.23 degrees, and 24.14 degrees and has the advantages that the crystal form has good stability and no static electricity, is convenient to produce, transport and store, and can meet all requirements as a preparation material and the like. The Gemfibrozil crystal form II can be kept unchanged for two years under the condition of normal temperature, does not reduce the content of medicine and fully meets the requirement of the medicine.
Description
technical field [0001] The invention belongs to the technical field of medicinal chemistry. The invention relates to a preparation method of polymorphic forms of gemfibrozil, in particular to crystal form II of gemfibrozil and a preparation method thereof. Background technique [0002] The chemical name of Gemfibrozil is 2,2-dimethyl-5-(2,5-dimethylphenyloxy)-pentanoic acid, and the English name is 5-(2,5-dimethylphenoxy)-2. 2-dimethylpentanoic acid, the structural formula is as follows: [0003] [0004] Gemfibrozil is a new blood lipid-lowering drug that was launched in the United States in 1982. It overcomes the severe toxic and side effects of the previous blood lipid-lowering drug clofibrate on the liver, retains its effective effect, and is used to prevent arteriosclerosis and help reduce the risk of myocardial infarction. Incidence rate, after oral administration, the gastrointestinal tract absorbs well and can be taken for a long time, so it is welcomed by patie...
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