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Bepotastine besilate

A technology for bepotastine besylate and bepotastine besylate tablets, which are applied in the field of bepotastine besylate tablets and their preparation, can solve the problems of low dissolution rate, low bioavailability and the like, Achieve the effect of improving dissolution, simple preparation process and no solvent residue

Inactive Publication Date: 2019-10-25
浙江天顺药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to solve the problems of low drug dissolution rate and low bioavailability, and provide a bepotastine besylate tablet and a preparation method thereof, so that the drug can be dissolved in aqueous solution, acetate buffer solution and phosphate The in vitro dissolution rate in the buffer solution medium has been greatly improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1, bepotastine besylate tablet components and preparation method thereof, bepotastine besylate tablet components are as follows by weight percentage,

[0018]

[0019]

[0020] Preparation method: ① Grind bepotastine besylate, crospovidone, povidone k30, mannitol, polyethylene glycol and poloxamer respectively, and pass through a 40-80 mesh sieve to carry out Mix and stir evenly; ②Set the extrusion temperature of the screw extruder at 90°C. After reaching the preset temperature, add the above-mentioned mixture into the extruder for extrusion molding, and then crush it with crushing equipment. Pass 24 mesh screening to obtain solids with uniform particle size; ③ mix the pulverized solids with microcrystalline cellulose, starch, croscarmellose sodium and magnesium stearate, and stir evenly; ④ press the mixture in step ③ Tablets are made into tablets.

Embodiment 2

[0021] Embodiment 2, bepotastine besylate tablet components and preparation method thereof, bepotastine besylate tablet components are as follows by weight percentage,

[0022]

[0023] Preparation method: ① Grind bepotastine besylate, hydroxypropylmethylcellulose, polyethylene glycol, poloxamer and sodium lauryl sulfate respectively, and then pass through a 40-80 mesh sieve, and carry out Mix and stir evenly; ②Set the extrusion temperature of the screw extruder at 110°C. After reaching the preset temperature, add the above-mentioned mixture into the extruder for extrusion molding, and then use crushing equipment for crushing. Screening through 32 meshes to obtain a solid with uniform particle size; ③ mixing the pulverized solid with microcrystalline cellulose, lactose, croscarmellose sodium, low-substituted hydroxypropyl cellulose and magnesium stearate, and stirring evenly; ④ compress the mixture in step ③ to make tablets.

Embodiment 3

[0024] Embodiment 3, bepotastine besylate tablet components and preparation method thereof, bepotastine besylate tablet components are as follows by weight percentage,

[0025]

[0026] Preparation method: ① respectively pulverize bepotastine besilate, povidone k30, xylitol, poloxamer and glyceryl monostearate, pass through a 40-80 mesh sieve, mix, and Stir evenly; ②Set the extrusion temperature of the screw extruder at 120°C. After reaching the preset temperature, add the above-mentioned mixture into the extruder for extrusion molding, and then crush it with crushing equipment, pass through 40 mesh Screen to obtain a solid with uniform particle size; ③Mix the pulverized solid with sorbitol, sucrose, ethyl cellulose, low-substituted hydroxypropyl cellulose and magnesium stearate, and stir evenly; ④Compress the mixture in step ③ into tablets Made into tablets.

[0027] Dissolution investigation, assay method: get sample 40mg among the embodiment 1-3, according to dissolutio...

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Abstract

The invention discloses bepotastine besilate, and belongs to the field of organic chemistry and medicinal chemistry. The technical scheme mainly includes that the bepotastine besilate, polymers, plasticizers, lubricating agents a, surface active agents, diluting agents, binding agents, disintegrating agents and lubricating agents b are combined to prepare bepotastine besilate tablets by a hot-meltextrusion technique. The tablets have stability and further have the advantages of high drug dissolution and bioavailability.

Description

technical field [0001] The invention belongs to the field of organic chemistry and medicinal chemistry, and in particular relates to a bepotastine besylate tablet and a preparation method thereof. Background technique [0002] Bepotastine, chemical name (+)-4-[[(S)-p-chloro-α-2-pyridylbenzyl]oxy]-1-piperidine butanoic acid, English name Bepotastine, clinical Bepotastine Bepotastine is marketed with bepotastine besylate as the active ingredient. Bepotastine besylate is the besylate salt of bepotastine, a drug with antihistamine activity that can be used to treat Allergic diseases such as rhinitis, and skin diseases such as eczema, dermatitis, prurigo, itchy skin, and urticaria. [0003] Some currently disclosed bepotastine bepotastine tablets and their preparation methods are as follows: Publication No. CN201711025980.0 discloses a preparation method of bepotastine besilate pharmaceutical composition, the process adopts wet granulation, although simple , but the dissolution...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/32A61K31/4545A61P11/02A61P37/08A61P17/00A61P17/04
CPCA61K9/2027A61K9/2054A61K9/2095A61K31/4545A61P11/02A61P17/00A61P17/04A61P37/08
Inventor 张胜
Owner 浙江天顺药业有限公司
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