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Preparation method of rebamipide aqueous suspension

A technology of rebamipide and water suspension, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, liquid delivery, etc., which can solve the problem of sandy feeling, irritation, and discomfort of patients and other problems, to achieve the effect that the particle size will not increase

Active Publication Date: 2016-08-24
ZHUHAI ESSEX BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the average particle size of the rebamipide aqueous suspension prepared in this way is greater than 10 μm, and the average particle size becomes larger and layered after high-temperature sterilization; in addition, during the preservation process, the fine particles of rebamipide will aggregate into particles or crystals. The particles are enlarged, and the precipitated suspended particles are not easy to disperse into fine particles. When dripped into the eyes, there will be a feeling of sand and irritation, and the patient will feel uncomfortable.

Method used

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Embodiment 1

[0044] The preparation method of the rebamipide aqueous suspension provided in this embodiment comprises the following steps:

[0045] (1) According to the prescription requirements, weigh all the excipients with an electronic balance, and dissolve all the excipients in purified water through the liquid mixing tank to obtain an aqueous solution of the excipients;

[0046] (2) Insert the cutting head of the high-speed shearing machine into the auxiliary material aqueous solution, turn on the shearing machine, adjust the rotation speed to 12000-16000rmp, add rebamipide while cutting, and then cut 5 -10 minutes to obtain the initial liquid of rebamipide aqueous suspension;

[0047] (3) After the initial solution of rebamipide aqueous suspension is constant in volume and pH is adjusted, add a high-pressure homogenizer, homogenize 2-3 times at a low pressure of 8-12MPa, and homogenize at a high pressure of 50-55MPa for 10-15 times to obtain Rebamipide Pat water suspension; ...

Embodiment 2

[0051] The preparation method of the rebamipide aqueous suspension provided in this embodiment comprises the following steps:

[0052] (1) According to the prescription requirements, weigh all the excipients with an electronic balance, and dissolve all the excipients in purified water through the liquid mixing tank to obtain an aqueous solution of the excipients;

[0053] (2) Insert the cutting head of the high-speed shearing machine into the auxiliary material aqueous solution, turn on the shearing machine, adjust the rotation speed to 12000-16000rmp, add rebamipide while cutting, and then cut 5 -10 minutes to obtain the initial liquid of rebamipide aqueous suspension;

[0054] (3) After the initial solution of rebamipide aqueous suspension is constant to volume and pH is adjusted, add a high-pressure homogenizer, homogenize 2-3 times at a low pressure of 8-12MPa, and homogenize at a high pressure of 56-60MPa for 10-15 times to obtain Rebamipide Pat water suspension; ...

Embodiment 3

[0057] Rebamipex

[0058] Sodium citrate

[0059] Prepare with reference to the method of Example 1.

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Abstract

The invention discloses a preparation method of a rebamipide aqueous suspension. The preparation method comprises the following steps: (1) dissolving all adjuvant materials in injection water, so that an adjuvant material aqueous solution is obtained; (2) adding rebamipide to the adjuvant material aqueous solution obtained in the step (1), performing crushing and dispersing, so that primary liquid of the rebamipide aqueous suspension is obtained; (3) homogenizing the primary liquid of the rebamipide aqueous suspension under high pressure, so that the aqueous suspension containing the rebamipide is finally obtained; and (4) sterilizing the rebamipide aqueous suspension obtained in the step (3), and sub-packaging the rebamipide aqueous suspension in a sterile environment in containers for clinical use. Compared with the prior art, the preparation method has the advantages that the average grain size of the rebamipide in the rebamipide aqueous suspension prepared by the rebamipide aqueous suspension preparation method disclosed by the invention is less than 1[micron]m; and the grain size cannot change much after high-temperature sterilization and cannot increase after long-term storage.

Description

technical field [0001] The invention relates to the field of eye drops, in particular to a preparation method of rebamipide aqueous suspension. Background technique [0002] Rebamipide: a quinolone compound, an odorless and bitter white crystalline powder, very slightly soluble in methanol and ethanol, almost insoluble in water, CAS registration number: 90098-04-7. Rebamipide can improve gastric motility and has a significant effect on gastric mucosal damage caused by gastric ulcer, acute gastritis or acute exacerbation of chronic gastritis. It also has the effect of increasing the density of goblet cells in the eye, the effect of increasing the mucus in the eye, and the effect of increasing the fluid of the lacrimal gland. [0003] Dry eye is a common chronic eye disease that can lead to corneal and conjunctival epithelial damage due to the lack of natural tears and ocular mucous fluid. If left untreated, dry eye can cause corneal ulcers or loss of vision. [0004] Rebam...

Claims

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Application Information

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IPC IPC(8): A61K31/4704A61K9/10A61K47/32A61P1/04A61P27/02
Inventor 曲伟王振恒田元黄伟静冯汝鹏
Owner ZHUHAI ESSEX BIO PHARMA
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