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Econazole nitrate compound crystal and preparation method and drug composition thereof

A technology of econazole nitrate and compound, applied in the directions of drug combination, drug delivery, organic chemistry, etc., can solve problems such as polymorphism, and achieve the effect of improving solubility and good stability

Active Publication Date: 2013-01-16
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Econazole nitrate may also have polymorphism

Method used

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  • Econazole nitrate compound crystal and preparation method and drug composition thereof
  • Econazole nitrate compound crystal and preparation method and drug composition thereof
  • Econazole nitrate compound crystal and preparation method and drug composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] [Example 1] Preparation of Econazole Nitrate Compound Crystal

[0050] 1) Take 50g of crude econazole nitrate, add N,N-dimethylformamide / methanol mixed solvent, and dissolve to obtain a solution. The ratio of the crude econazole nitrate to the mixed solvent is 1g:12ml, The volume ratio of N,N-dimethylformamide to methanol is 1:3.5;

[0051] 2) Adjust the pH value of the solution to 3 with hydrochloric acid, then add 0.10 g of activated carbon, stir for adsorption, filter for decarbonization and sterilization to obtain a clear solution, and reflux at 72°C for 3 hours;

[0052] 3) Then lower the temperature to 65°C, keep the temperature and add distilled water at 65°C dropwise under stirring, wherein the volume ratio of the distilled water to the mixed solvent is 5:1, and the stirring rate is 28r / min;

[0053] 4) Continue to keep stirring at 65°C for 25 minutes after dropping, let stand and cool down to room temperature naturally, filter, wash with methanol 3 times, and ...

Embodiment 2-9

[0055] [Example 2-9] Preparation of econazole nitrate compound crystals according to the parameters shown in Table 1

[0056] The following are embodiments 2-9 of the present invention, and the operation steps are the same as in embodiment 1, and the concrete process parameters are shown in Table 1:

[0057] Table 1, Embodiment 2-9

[0058]

[0059] The X-ray powder diffraction patterns obtained by measuring the econazole nitrate compound crystals obtained in Examples 2-9 using Cu-Kα rays are similar to those in Example 1.

preparation Embodiment 1

[0060] [Preparation Example 1] Econazole Nitrate Vaginal Effervescent Tablets

[0061] 1. Prescription (according to 1000 tablets):

[0062] Specification: 50mg

[0063]

[0064] 2. Preparation process:

[0065] 1) The econazole nitrate and other auxiliary materials prepared in Example 1 were pulverized through a 120-mesh sieve;

[0066] 2) Weigh half of the parts by weight of econazole nitrate, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, sodium carboxymethyl starch, lactose and sodium bicarbonate of the parts by weight, and add an appropriate amount of 95% Ethanol granulation, drying at 65°C for 18 minutes to obtain dry granules A;

[0067] Weigh half of the econazole nitrate, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, sodium carboxymethyl starch, lactose and the tartaric acid of the weight part, add an appropriate amount of 95% ethanol to granulate, Dry at a temperature of 65°C for 18 minutes to obtain dry granules B;...

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Abstract

The invention relates to an econazole nitrate compound crystal. After the compound crystal is determined by using a powder X-ray diffraction determination method, an X-ray powder diffraction pattern which is expressed by a diffraction angle of 2theta plus or minus 0.2 degrees shows characteristic diffraction peaks at 10.1 degrees, 10.6 degrees, 14.8 degrees, 15.4 degrees, 16.9 degrees, 19.8 degrees, 20.4 degrees, 26.7 degrees, 29.8 degrees, 30.3 degrees and 33.4 degrees. The compound crystal is a novel crystal which is different from the econazole nitrate crystal in the prior art. According to a solubility test, the compound crystal has higher water solubility. Besides, the invention additionally provides a preparation method of the econazole nitrate compound crystal, drug composition containing the compound crystal and a preparation method of the drug composition.

Description

technical field [0001] The invention belongs to the improvement of pharmaceutical dosage forms, and in particular relates to a crystal of econazole nitrate compound, its preparation method and its pharmaceutical composition. Background technique [0002] At present, women's vaginitis, cervicitis and cervical erosion and other gynecological reproductive tract infection diseases have become the main diseases that endanger the health of modern women. Faced with many problems that need to be solved in the field of reproductive health, people regard the prevention and treatment of reproductive tract infection as an important part of reproductive health. social and economic burden, and a major threat to human health. With the excessive and uncontrolled use of antibiotics, some antibiotics that were originally extremely lethal to bacteria are due to the emergence of bacterial resistance, resulting in an increasing dose of their treatment and a continuous extension of the treatment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/60A61K31/4174A61K9/46A61P31/10A61P15/02
Inventor 李明杰阮朝滨杨丽娟李华
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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