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Bepotastine besilate composition and preparation prepared thereby

A technology of bepotastine bepotastine and bepotastine besilate tablets, which is applied in the field of bepotastine bepotastine tablets, can solve problems such as industrialization difficulties, large fluctuations in tablet content, and unqualified content uniformity , to achieve the effect of simple and feasible method, uniform content of main components and convenient operation

Inactive Publication Date: 2017-01-11
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor referred to Example 13 of JP3909998 to trial-produce 10mg bepotastine bepotastine tablets (plain tablets), and the results showed that the content of the tablets fluctuated greatly (95-120%), and A+2.2S was greater than 30, far exceeding the 2015 edition of the Pharmacopoeia A+ 2.2S should be less than 15, and the content uniformity is unqualified
And the process of JP3909998 requires special equipment, that is, a high-speed stirring granulator that can be heated by an external bath. This kind of production equipment is currently rarely used in China and has not been sold, so there are difficulties in industrialization

Method used

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  • Bepotastine besilate composition and preparation prepared thereby
  • Bepotastine besilate composition and preparation prepared thereby
  • Bepotastine besilate composition and preparation prepared thereby

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Bepotastine bepotastine tablet of the present embodiment, its composition is as follows:

[0043]

[0044]

[0045] The preparation steps are as follows:

[0046] (1) Bepotastine bepotastine (particle size D90 is 250 μm), mannitol 200SD (particle size D90 is 260 μm) and polyethylene glycol 8000 (particle size D90 is 280 μm) are sequentially put into the granulator at room temperature and high speed Stir and mix for 3 minutes to obtain mixed powder;

[0047] (2) Heat the mixed powder in an oven at 80°C for 1.5 hours, then take it out and pass it through a 20-mesh sieve, let it cool, and then sieve it again to obtain the granules of bepotastine besilate composition;

[0048] (3) Put the granules of bepotastine bepotastine composition, microcrystalline cellulose PH102 and magnesium stearate into a granulator, stir and mix at room temperature at low speed for 2 minutes to obtain uniformly mixed granules;

[0049] (4) Compress the mixed granules into tablets, the the...

Embodiment 2

[0051] Bepotastine bepotastine tablet of the present embodiment, its composition is as follows:

[0052] 1000 pieces Composition (g) Bepotastine besilate (D90=250μm) 10 Mannitol 100SD (D90=200μm) 64 Polyethylene glycol 8000 (D90=280μm) 12 Microcrystalline Cellulose PH102 13 Magnesium stearate 1

[0053] The preparation steps are as follows:

[0054] (1) Bepotastine bepotastine (particle size D90 is 250 μm), mannitol 100SD (particle size D90 is 200 μm) and polyethylene glycol 8000 (particle size D90 is 280 μm) are sequentially put into the granulator at room temperature and high speed Stir and mix for 3 minutes to obtain mixed powder;

[0055] (2) Heat the mixed powder in an oven at 80°C for 1.5 hours, then take it out and pass it through a 20-mesh sieve, let it cool, and then sieve it again to obtain the granules of bepotastine besilate composition;

[0056] (3) Put the granules of bepotastine bepotastine composition, microcrystal...

Embodiment 3

[0059] Bepotastine bepotastine tablet of the present embodiment, its composition is as follows:

[0060] 1000 pieces Composition (g) Bepotastine besilate (D90=250μm) 10 Mannitol 200SD (D90=260μm) 60 Polyethylene glycol 6000 (D90=220μm) 18 Microcrystalline Cellulose PH102 11 Magnesium stearate 1

[0061] The preparation steps are as follows:

[0062] (1) Bepotastine bepotastine (particle size D90 is 250 μm), mannitol 200SD (particle size D90 is 260 μm) and polyethylene glycol 6000 (particle size D90 is 220 μm) are sequentially put into the granulator at room temperature and high speed Stir and mix for 3 minutes to obtain mixed powder;

[0063] (2) Heat the mixed powder in an oven at 80°C for 1 hour, take it out and pass it through a 20-mesh sieve, let it cool, and then sieve it again for granulation to obtain bepotastine besilate composition granules;

[0064] (3) Put the granules of bepotastine bepotastine composition, microcrysta...

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Abstract

The invention belongs to the technical field of medicines, and relates to a bepotastine besilate composition and a preparation prepared thereby, and the preparation particularly relates to a bepotastine besilate tablet. The composition is prepared from bepotastine besilate, mannitol and solid-state polyethylene glycol polymer, and the partical sizes of bepotastine besilate, mannitol and solid-state polyethylene glycol polymer are all controlled at D90 of 200 micrometers to 300 micrometers. The preparation is a bepotastine besilate preparation containing the bepotastine besilate composition. In particular, the bepotastine besilate tablet is prepared from the bepotastine besilate composition and a pharmaceutically acceptable carrier. The composition has good flowability and pressing ability, and is used for preparing the bepotastine besilate tablet and other preparations which are easy to mix evenly and shape by tablet compressing, thus a finished product with uniform content and stable quality is obtained. The preparation method is easy, operation is convenient, requirements for production equipment are low, and it is easy to realize industrialization.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a bepotastine besilate composition and a preparation thereof, and the preparation particularly relates to a bepotastine besilate tablet. Background technique [0002] Bepotastine bepotastine is a non-sedating highly selective histamine H1 receptor antagonist, which has no affinity for 5-HT2, α1, α2, muscarinic receptors, etc. It has a stabilizing effect on mast cells and can inhibit the The accumulation and infiltration of eosinophils can inhibit IL-5, LTB4 and blood PAF, so it has anti-allergic and antipruritic effects. The chemical name of bepotastine bepotastine is (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridine)methoxy]piperidine]butyric acid benzenesulfonate, CAS No.: 190786-44-8, molecular formula is C 21 h 25 ClN 2 o 3 ·C 6 h 6 o 3 S. The chemical structural formula is as follows: [0003] [0004] As a second-generation non-sedating antihistamine drug, Bepotastine ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4545A61K47/26A61K47/10A61P37/08A61P17/04
CPCA61K31/4545A61K9/2018A61K9/2031
Inventor 兰洁
Owner CHONGQING HUAPONT PHARMA
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