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Loratadine crystal form and its preparation method and use

A technology of loratadine and crystal form, which is applied in the field of preparation of anti-allergic compounds and loratadine crystal form, which can solve the differences in clinical drug efficacy, solubility and stability, and affect drug absorption and bioavailability, etc. problem, to achieve the effect of simple preparation method and high solubility

Inactive Publication Date: 2019-05-21
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Different crystal forms of drugs can cause differences in solubility and stability, affect drug absorption and bioavailability, and lead to differences in clinical efficacy

Method used

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  • Loratadine crystal form and its preparation method and use
  • Loratadine crystal form and its preparation method and use
  • Loratadine crystal form and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0025] The present invention will be further illustrated by the following examples, but it is not intended to limit the protection scope of the present invention.

[0026] (1) Crystal form identification method

[0027] The X-ray powder diffraction pattern in the present invention is collected on Shimadzu XRD-6100 X-ray powder diffractometer. The method parameters of X-ray powder diffraction are as follows:

[0028] X-ray diffractometer parameters: Cu-Kα target, tube voltage: 40kV, tube current: 30mA, scanning range 2θ: 5°~45°, scanning speed: 2° / min;

[0029] In the present invention, the differential scanning calorimetry chart is collected on TA Q2000. The method parameters for the differential scanning calorimetry analysis are as follows:

[0030] Scan rate: 0.5°C / min

[0031] Protective gas: nitrogen

[0032] In the present invention, the thermogravimetric analysis chart is collected on TA Q5000. The method parameters for thermogravimetric analysis are as follows:

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Abstract

The invention discloses a loratadine crystal as well as a preparation method and application thereof. The preparation method of the crystal comprises the following steps: adding amorphous solid of loratadine into a methanol aqueous solution, then stirring for at least two hours, then carrying out suction filtration, and drying filtration residue obtained by suction filtration. Values of positions of three intensive characteristic peaks in an X-ray powder diffraction pattern of the prepared crystal at 2theta are 19.5 degrees plus or minus 0.2 degree, 21.2 degrees plus or minus 0.2 degree and 23.9 degrees plus or minus 0.2 degree. The loratadine crystal has higher solubility and has an important value on optimization and development of loratadine.

Description

technical field [0001] The invention relates to the field of chemistry and medicine, and relates to an antiallergic compound, in particular to the preparation of loratadine crystal form. Background technique [0002] Anaphylaxis is a kind of allergic disease, which is an abnormal reaction that occurs when the human body contacts some special allergens (such as heterogeneous serum, virus, bacteria, plant pollen and dust, etc.). When an allergic reaction occurs, the histamine released from the cells will bind to the specific receptors on the target cells, resulting in redness and swelling of the skin, itching, symptoms of allergic rhinitis, bronchial asthma, accompanied by a drop in blood pressure, increased heart rate and Clinical manifestations such as edema, severe cases may also lead to shock or even death. Since histamine plays an important role in the pathophysiology of allergic diseases, the study of antihistamine pathways has become an effective method for the study o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04A61K31/4545A61P37/08
CPCC07B2200/13C07D401/04
Inventor 傅强畅瑞苗曾爱国余佩杜玮常春
Owner XI AN JIAOTONG UNIV