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New chlorpheniramine maleate crystal and preparation method thereof

A technology of chlorpheniramine maleate and crystals, which is applied in the field of chlorpheniramine maleate crystals and its preparation, can solve the problems that affect the stability and bioavailability of original drugs and preparations, and the solubility and stability of crystal forms need to be further improved. Improve the problems of unfavorable preparation development and industrial production, and achieve the effect of improving bioavailability, good chemical stability and simple preparation method

Pending Publication Date: 2020-04-07
HARVEST PHARMA HUNAN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation of its crystals requires a variety of solvents, including more toxic chloroform and more dangerous ether, and the amount of solvent used is relatively large, so it is not conducive to formulation development and industrial production
[0005] Different crystal forms of chlorpheniramine maleate have different physical properties, such as stability and solubility, etc. These properties can directly affect the stability and bioavailability of original drugs and preparations, while the solubility and bioavailability of existing crystal forms Stability needs to be further improved

Method used

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  • New chlorpheniramine maleate crystal and preparation method thereof
  • New chlorpheniramine maleate crystal and preparation method thereof
  • New chlorpheniramine maleate crystal and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0027] Maleic acid (9.0 g, 0.078 mol) and isopropanol (22.5 g) were dissolved at 55°C, and then chlorpheniramine (22.5 g, 0.082 mol) was added to the maleic acid isopropanol solution. Subsequently, 67.5 g of methyl tert-butyl ether was added to the system for clarification. The system was lowered to 6° C. for crystallization, filtered, and the filter cake was washed with 5 g of methyl tert-butyl ether. The filter cake was dried at 35° C. to obtain chlorpheniramine maleate crystals (29 g).

Embodiment 2

[0029] Maleic acid (9 g, 0.078 mol) and isopropanol (36.0 g) were dissolved at 55° C., and then chlorpheniramine (22.5 g, 0.082 mol) was added to the maleic acid isopropanol solution. Subsequently, 150 g of methyl tert-butyl ether was added to the system for clarification, the system was lowered to 15° C. for crystallization, filtered, and the filter cake was washed with 5 g of methyl tert-butyl ether. The filter cake was dried at 45° C. to obtain chlorpheniramine maleate crystals (26 g).

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Abstract

The invention belongs to the technical field of medicines, and specifically provides a new chlorpheniramine maleate crystal and a preparation method thereof, wherein the chlorpheniramine maleate crystal has characteristic peaks at 2[theta] of 12.4+ / -0.2 DEG, 13.1+ / -0.2 DEG, 18.8+ / -0.2 DEG, 19.3+ / -0.2 DEG, 20.2+ / -0.2 DEG, 24.9+ / -0.2 DEG and 26.5+ / -0.2 DEG in an X-ray diffraction spectrogram. The preparation method of the chlorpheniramine maleate crystal is simple, and the prepared chlorpheniramine maleate crystal has high dissolution rate, high solubility and good chemical stability, is beneficial to rapidly exerting the drug effect and improving the bioavailability, and can also be well stored.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a chlorpheniramine maleate crystal and a preparation method thereof. Background technique [0002] Histamine is a self-active substance widely present in human tissues, with the highest content in mast cells in connective tissue and basophils in blood. Since the discovery of histamine receptors in the 1960s, H1 receptor antagonists have been used to treat allergic diseases. Chlorpheniramine Maleate is a first-generation antihistamine, also known as chlorpheniramine, commonly used in tablet and injection forms, suitable for skin allergies such as urticaria, eczema, dermatitis, drug eruption, skin Pruritus, neurodermatitis, insect bites, eye dermatitis, allergic rhinitis, vasomotor rhinitis, drug and food allergies. Chlorpheniramine has a weak anticholinergic effect and can relieve runny nose symptoms. Therefore, the compound preparation composed of chlorpheniramine, acetaminop...

Claims

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Application Information

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IPC IPC(8): C07D213/38C07C57/145C07C51/41C07C51/43
CPCC07D213/38C07C57/145C07B2200/13
Inventor 袁金桥秦敏禹曾达刘虎
Owner HARVEST PHARMA HUNAN CO LTD
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