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Epinastine hydrochloride granule, and preparation method thereof

A technology of epinastine hydrochloride and granules, which is applied in the field of epinastine hydrochloride granules and its preparation, can solve the problems of difficulty in obtaining uniform mixing, narrow particle size distribution, difficulty in masking bitterness, etc., and achieve improved compliance, Easy to prepare, solve the effect of extremely bitter taste

Active Publication Date: 2016-06-29
重庆瑞泊莱医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Epinastine hydrochloride tastes extremely bitter after being dissolved in water, and it is difficult for a single flavoring agent to cover up its bitter taste, and after a large amount of flavoring agent is used, it increases the difficulty of granulation, and it is difficult to obtain uniform mixing and narrow particle size distribution. particle

Method used

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  • Epinastine hydrochloride granule, and preparation method thereof
  • Epinastine hydrochloride granule, and preparation method thereof
  • Epinastine hydrochloride granule, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The composition prescription of granule described in the present embodiment is as follows:

[0029]

[0030]

[0031] Firstly, the described epinastine hydrochloride, sucrose, aspartame, sucralose, and monoamine glycyrrhizinate S are respectively passed through a 120 mesh sieve, and are set aside; then the prescribed amount of epinastine hydrochloride and sucrose aspartame Add tannin, sucralose, and monoamine glycyrrhizinate S into the wet granulator, start stirring for 5 minutes until all materials are fully mixed and evenly distributed. Then add 5% (w / w) povidone aqueous solution 600g as binder granulation. Fluidized bed drying until the moisture content is less than 3%, sizing with a sieve with a sieve aperture of 0.5 mm. Spray 600 g of 2% (w / w) povidone aqueous solution into the fluidized bed as a binder to granulate, granulate after drying, add strawberry essence, mix evenly, and pack into corresponding specifications to obtain final product.

Embodiment 2

[0033] The composition prescription of granule described in the present embodiment is as follows:

[0034]

[0035] First described epinastine hydrochloride, erythritol, aspartame, sucralose, glycyrrhizic acid monoamine S are respectively passed through 120 mesh sieves, for subsequent use; then the epinastine hydrochloride and sucrose Put aspartame, sucralose, and monoamine glycyrrhizinate S into the wet granulator, and start stirring for 5 minutes until all materials are fully mixed and uniform. Then add 20% (w / w) povidone aqueous solution 600g as binder granulation. Fluidized bed drying until the water content is less than 3%, sizing with a sieve with a sieve aperture of 1.0mm. Spray 600 g of 3% (w / w) povidone aqueous solution into the fluidized bed as a binder to granulate, granulate after drying, add milk essence, mix evenly, and pack into corresponding specifications to obtain final product.

Embodiment 3

[0037] The composition prescription of granule described in the present embodiment is as follows:

[0038]

[0039]

[0040] First described epinastine hydrochloride, erythritol, sucrose, aspartame, sucralose, glycyrrhizic acid monoamine S are passed through 120 mesh sieves respectively, for subsequent use; Then the epinastine hydrochloride of prescription quantity Put it into the wet granulator with sucrose aspartame, sucralose, and monoamine glycyrrhizinate S, and start stirring for 5 minutes until all materials are fully mixed evenly. Then add 15% (w / w) povidone aqueous solution 600g as binder granulation. Fluidized bed drying until the moisture content is less than 3%, sizing with a sieve with a sieve aperture of 0.5mm. Then spray 600g of 1% (w / w) povidone aqueous solution into the fluidized bed as a binder to granulate, granulate after drying, add pineapple essence, mix evenly, pack into corresponding specifications, and obtain less than 30 mesh Granules.

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Abstract

The invention discloses an epinastine hydrochloride granule, and a preparation method thereof. 1000 weight parts of the epinastine hydrochloride granule comprise 10 parts of epinastine hydrochloride, 945 parts of a filler, 40 parts of a composite flavoring agent, 3 parts of polyvinylpyrrolidone, and 2 parts of an essence. The preparation method comprises two times of granulation. According to the preparation method, epinastine hydrochloride, the filler, and the composite flavoring agent are uniformly mixed; an appropriate amount of a polyvinylpyrrolidone solution is added for wet granulation; drying is carried out; and an appropriate amount of polyvinylpyrrolidone is added for fluidized bed granulation; granule shaping is carried out; and an obtain product is uniformly mixed with the essence so as to obtain a finished product. The preparation method is capable of solving problems that epinastine hydrochloride granule particle size distribution range is wide, and much particle fine powder is generated; stable and uniform granules are obtained via the preparation method; and the preparation method is suitable for industrialized production.

Description

technical field [0001] The invention relates to epinastine, in particular to an epinastine hydrochloride granule and a preparation method thereof. Background technique [0002] Epinastine hydrochloride, whose chemical name is 3-amino-9,13b-dihydro-1H-diphenyl[c,f]imidazo[1,5-a]azepine hydrochloride, is a highly selective H 1 receptor inhibitors. European patent EP-B0035749 discloses its use for treating allergic bronchitis, allergic rhinitis and allergic conjunctivitis. Chinese patent CN1104242A discloses its use in treating pain. Since epinastine tablet was launched in Japan in 1994, it has been the leading oral antiallergic drug in Japan due to its good effect, high safety, wide range of indications, few drug interactions and low cardiotoxicity. Products, capsules, eye drops and other dosage forms have been developed and launched one after another. [0003] Epinastine hydrochloride tastes extremely bitter, so it is mostly coated tablets or capsules clinically. Because ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/55A61K47/26A61P11/06A61P11/02A61P17/00A61P17/04A61P37/08
Inventor 陈向李锋鲁定国梁玉勤
Owner 重庆瑞泊莱医药科技有限公司
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