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Ebastine salt tablet and preparation method thereof

A technology for ebastine and tablet is applied in the field of ebastine salt tablet and its preparation, which can solve the problems of low solubility, slow dissolution, low bioavailability, etc. The effect of improving water solubility

Pending Publication Date: 2022-07-08
南京联智医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the defects of the prior art. The present invention proposes a tablet of ebastine salt and its preparation method, which improves the solubility of the drug by forming a water-soluble salt with an organic acid. , to overcome the low in vitro solubility of ebastine tablets and the low in vivo bioavailability caused by slow dissolution

Method used

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  • Ebastine salt tablet and preparation method thereof
  • Ebastine salt tablet and preparation method thereof
  • Ebastine salt tablet and preparation method thereof

Examples

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preparation example Construction

[0023] The preparation method of the tablet of the salt of above-mentioned ebastine is as follows:

[0024] Weigh a class of ebastine salt, lactose, starch, and microcrystalline cellulose into a wet granulator, stir, chop, add purified water to make soft materials, wet and granulate by a granulator, and use a fluidized granulator. The bed is dried. The dry granules are mixed with magnesium stearate and croscarmellose sodium to obtain intermediate granules. The intermediate particles are taken for testing, and after passing the inspection, the intermediate particles are compressed to obtain intermediate voxel tablets. The intermediate voxel tablets were taken for testing, and after passing the inspection, the intermediate voxel tablets were coated to obtain intermediate-coated tablets. Take the intermediate-coated tablets for testing, and after passing the inspection, aluminum-plastic and outsourcing the intermediate-coated tablets.

[0025] The above-mentioned inspection pr...

Embodiment 1

[0043] Table 3. Ebastine Hydrochloride Tablet Formulation

[0044]

[0045] Preparation:

[0046] Weigh ebastine hydrochloride, lactose, starch, and microcrystalline cellulose into a wet granulator, stir, chop, add purified water to make soft materials, wet and granulate by a granulator, and use a fluidized bed for drying . The dry granules are mixed with magnesium stearate and croscarmellose sodium to obtain intermediate granules. The intermediate particles are taken for testing, and after passing the inspection, the intermediate particles are compressed to obtain intermediate voxel tablets. The intermediate voxel tablets were taken for testing, and after passing the inspection, the intermediate voxel tablets were coated to obtain intermediate-coated tablets. Take the intermediate-coated tablets for testing, and after passing the inspection, aluminum-plastic and outsourcing the intermediate-coated tablets.

Embodiment 2

[0048] Table 4 Ebastine sulfate tablet prescription

[0049]

[0050]

[0051] Preparation:

[0052] Weigh ebastine sulfate, lactose, starch, and microcrystalline cellulose into a wet granulator, stir, chop, add purified water to make soft materials, wet and granulate by a granulator, and use a fluidized bed for drying . The dry granules are mixed with magnesium stearate and croscarmellose sodium to obtain intermediate granules. The intermediate particles are taken for testing, and after passing the inspection, the intermediate particles are compressed to obtain intermediate voxel tablets. The intermediate voxel tablets were taken for testing, and after passing the inspection, the intermediate voxel tablets were coated to obtain intermediate-coated tablets. Take the intermediate-coated tablets for testing, and after passing the inspection, aluminum-plastic and outsourcing the intermediate-coated tablets.

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Abstract

The invention provides a preparation method of an ebastine salt tablet. The preparation method comprises the following steps: S1, placing ebastine salt, lactose, starch and microcrystalline cellulose in a wet granulator to complete a granulation process, and then drying to obtain dry granules; s2, mixing the dry particles obtained in the S1 with magnesium stearate and croscarmellose sodium to prepare intermediate particles, and tabletting the intermediate particles to prepare intermediate tablets; s3, coating the intermediate tablet obtained in the step S2 to prepare an intermediate coated tablet, namely the tablet of the ebastine salt; in the step S1, the ebastine tablet comprises the following components in parts by mass: 5-10 parts of ebastine salt, 65-70 parts of lactose, 3-8 parts of microcrystalline cellulose and 10-20 parts of starch; in the step S2, the composition comprises the following components in parts by mass: 1-3 parts of croscarmellose sodium and 0.5-2.0 parts of magnesium stearate. According to the invention, ebastine and organic acid generate water-soluble salt, so that the solubility of the medicine is improved.

Description

technical field [0001] The present invention relates to a tablet of a salt of ebastine and a preparation method thereof. Background technique [0002] Ebastine (chemical name is 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl] -1-butanone), is a long-acting, potent and highly selective histamine H1 receptor blocker, which is clinically used for the treatment of allergic diseases, including seasonal, allergic rhinitis and chronic Idiopathic urticaria, eczema, itchy skin and other diseases. [0003] Because the molecular structure of ebastine contains multiple hydrophobic groups, it is insoluble in water, the tablet has slow dissolution in vitro, low bioavailability, and is difficult to absorb in vivo, which limits the therapeutic effect of ebastine. SUMMARY OF THE INVENTION [0004] The technical problem to be solved by the present invention is to overcome the defects existing in the prior art. The present invention proposes a tablet of ebastine salt ...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/445A61P37/08A61P11/02A61P29/00A61P17/04A61P17/00
CPCA61K9/2866A61K31/445A61P37/08A61P11/02A61P29/00A61P17/04A61P17/00
Inventor 陈梦牛犇杭夏清郭励梁
Owner 南京联智医药科技有限公司
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