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Preparation method of epinastine hydrochloride fine granule

A kind of Epinastine hydrochloride fine granules and Epinastine hydrochloride technology, applied in the field of Epinastine, can solve the problems of difficult to obtain uniform mixing, difficult to mask bitterness, narrow particle size distribution, etc., and achieve low cost, preparation Easy, compliance-improving effect

Active Publication Date: 2016-06-29
重庆瑞泊莱制药有限公司
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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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  • Preparation method of epinastine hydrochloride fine granule
  • Preparation method of epinastine hydrochloride fine granule
  • Preparation method of epinastine hydrochloride fine granule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The composition prescription of fine granule described in the present embodiment is as follows:

[0028]

[0029]

[0030] 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 600 g of 5% (w / w) hydroxypropyl cellulose aqueous solution as binder to granulate. 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) hydroxypropyl cellulose aqueous solution into the fluidized bed as a binder to granulate, granulate after drying, add strawberry essence, mix evenly, and pack into corresponding specifications ...

Embodiment 2

[0032] The composition prescription of fine granule described in the present embodiment is as follows:

[0033]

[0034] 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 600 g of 5% (w / w) hydroxypropyl cellulose aqueous solution as binder to granulate. 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) hydroxypropyl cellulose 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

[0036] The composition prescription of fine granule described in the present embodiment is as follows:

[0037]

[0038]

[0039] First described epinastine hydrochloride, erythritol, sucrose, aspartame, sucralose, glycyrrhizic acid monoamine S are passed through 120 mesh sieves respectively, standby; Then the epinastine hydrochloride of recipe 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 600 g of 5% (w / w) hydroxypropyl cellulose aqueous solution as binder to granulate. Fluidized bed drying until the moisture content is less than 3%, sizing with a sieve with a sieve aperture of 0.5 mm. Spray 600g of 2% (w / w) hydroxypropyl cellulose aqueous solution into the fluidized bed again to make binder granulation, granulate after drying, add pineapple essence, mix uniformly, pack into corresponding specification, obtain less than 30...

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Abstract

The invention discloses a preparation method of an epinastine hydrochloride fine granule. According to the preparation method, a composite flavoring agent is prepared from aspartame, sucralose, and glycyrrhizic acid monoammonium S at a mass ratio of 8:1:1, a sweet filler is taken as an assistant agent, and synergistic effect is achieved via adding an appropriate amount of an essence, so that the bitter taste of epinastine hydrochloride is covered effectively, and patient drug compliance is improved. According to the preparation method, problems that epinastine hydrochloride fine granule particle size distribution range is relatively wide, and much particle fine powder is generated are solved effectively via controlling on parameters such as adhesive aqueous solution concentration, fluidized bed temperature, and drying time, and stable and uniform granules are obtained. The auxiliary materials of the preparation method are cheap and easily available; preparation is simple; no special equipment is needed; production cycle is short; cost is low; and the preparation method is suitable for industrialized production.

Description

technical field [0001] The invention relates to epinastine, in particular to a preparation method of epinastine hydrochloride fine particles. Background technique [0002] Epinastine hydrochloride has inhibitory effects on histamine, leukotriene C4, PAF, serotonin, and can inhibit the release of histamine and slow-reacting substance A (SRS-A) chemical mediators. Its tablets have been released since 1994 Since it was launched in the Japanese market, due to its good effect, high safety, wide range of indications, few drug interactions and low cardiotoxicity, it has been the leading product in Japanese oral anti-allergic drugs, capsules, eye drops, etc. Various dosage forms have been developed and marketed one after another. [0003] Epinastine hydrochloride tastes extremely bitter, so it is mostly coated tablets or capsules clinically. Because this product has few side effects, low toxicity, and good patient tolerance, 1% hydrochloric acid was developed in Japan for pediatric...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/55A61K47/18A61K47/26A61K47/12A61P11/06A61P11/02A61P17/00A61P17/04A61P37/08
Inventor 陈向李锋鲁定国梁玉勤
Owner 重庆瑞泊莱制药有限公司
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