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Clarithromycin spherical crystal as well as preparation method and application thereof

A technology of spherical crystals and clarithromycin, which is applied in the field of medicine, can solve the problems of uneven crystal particle size distribution, poor fragmentation and friability, and increased production costs, and achieve simple operation, improved fluidity and compressibility, and spherical The effect of compact and round crystal particles

Active Publication Date: 2021-12-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Clarithromycin has a variety of crystal forms, wherein the crystal form II is a stable crystal form, and it is also the main crystal form of commercially available raw materials and preparations, but its crystal size distribution is uneven (such as figure 1 As shown), low fluidity and extremely poor compressibility lead to problems such as low hardness, cracks and poor friability in the production process of tablets, which makes a large number of excipients added to the formulation and the process is cumbersome, and the production cost increases

Method used

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  • Clarithromycin spherical crystal as well as preparation method and application thereof
  • Clarithromycin spherical crystal as well as preparation method and application thereof
  • Clarithromycin spherical crystal as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Preparation of clarithromycin spherical crystals

[0046] Take about 0.2 g of clarithromycin raw material, weigh it accurately, put it in a beaker, add 20 mL of good solvent methanol, and dissolve it by ultrasonic; take about 0.03 g of hydroxypropyl cellulose, and slowly add it to the container under stirring conditions. In a beaker with 100 mL of water, stir continuously to dissolve it completely, and place it in a crystallization container; add the drug solution and place it immediately for 25 o Shake fully at 250 rpm in a constant temperature shaking incubator. After 40 min, the resulting suspension was suction-filtered, and the solid product was o C. Dry under reduced pressure in a vacuum oven for 24 h, and the resulting dried solid particles are the product.

[0047] The appearance of the product is spherical, the Carr index is 15.44%, the angle of repose is 30.38°, d 90 is 55 μm.

Embodiment 2

[0049] Preparation of clarithromycin spherical crystals

[0050] Take about 0.1 g of clarithromycin raw material, weigh it accurately, put it in a beaker, add 20 mL of good solvent ethanol, and dissolve it by ultrasonic; take about 2 g of hydroxypropyl methylcellulose, and slowly add it under the condition of stirring into a beaker filled with 40 mL of water, stir continuously to dissolve it completely, and place it in a crystallization vessel; add the drug solution and place it immediately for 30 o Shake thoroughly at 100 rpm in a constant temperature shaking incubator. After 90 min, the resulting suspension was suction-filtered, and the solid product was o C. Dry under reduced pressure in a vacuum oven for 48 h, and the resulting dried solid particles are the product.

[0051] The appearance of the product is spherical, the Carr index is 20.35%, the angle of repose is 39.68°, d 90 is 60 μm.

Embodiment 3

[0053] Preparation of clarithromycin spherical crystals

[0054] Take about 1 g of clarithromycin raw material, accurately weigh it, put it in a beaker, add 20 mL of good solvent ethyl acetate, and ultrasonically dissolve it; take about 6 g of methylcellulose, and slowly add it to In a beaker with 200 mL of water, stir continuously to dissolve it completely, and place it in a crystallization container; add the drug solution and place it immediately for 20 o Shake fully at 300 rpm in a constant temperature shaking incubator. After 50 min, the resulting suspension was suction-filtered, and the solid product was o C. Dry under reduced pressure in a vacuum oven for 24 h, and the resulting dried solid particles are the product.

[0055] The appearance of the product is spherical, the Carr index is 19.76%, the angle of repose is 37.65°, d 90 is 58 μm.

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Abstract

The invention discloses a clarithromycin spherical crystal as well as a preparation method and application thereof, and belongs to the technical field of medicines. The spherical crystal is prepared through an anti-solvent method of adding a polymer, the crystallization process is simple, convenient and rapid, the obtained product is spherical or sphere-like, the carr index is about 10-20%, and the angle of repose is about 25-40 degrees. Compared with an original commercially available clarithromycin raw material medicine, the powder X-ray diffraction spectrogram, the differential scanning calorimetry analysis spectrogram and the infrared spectrogram of the spherical crystal are kept consistent; and the flowability and compressibility are obviously improved, and good application value is achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to clarithromycin spherical crystals and a preparation method and application thereof. Background technique [0002] Clarithromycin is a derivative of erythromycin, its chemical name is 6-O-methylerythromycin, its molecular formula and relative molecular weight are C 38 h 69 NO 13 and 747.95, the chemical structure is shown in the following formula: [0003] . [0004] Clarithromycin is a 14-membered ring macrolide antibiotic with broad antibacterial spectrum and strong antibacterial activity, and has strong inhibitory effect on Gram-positive bacteria, Chlamydia pneumoniae and Legionella pneumophila. Clarithromycin is widely used clinically and can be used to treat respiratory tract infection, reproductive system infection, skin and soft tissue infection, etc. At present, clinical preparations of clarithromycin include tablets (immediate-release tablets, dispersi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C30B29/54C30B29/60C30B7/14C30B28/04C07H1/06C07H17/08
CPCC30B29/54C30B29/60C30B7/14C30B28/04C07H17/08C07H1/06C07B2200/13Y02A50/30
Inventor 高缘赵继云孟文卉钱帅张建军魏元锋
Owner CHINA PHARM UNIV
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