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Bepotastine besilate nasal spray and preparation method thereof

A technology of bepotastine besylate and nasal spray, which is applied in the preparation field of bepotastine besylate and its preparation field, and can solve the problems of rapid absorption of unfavorable drugs, easy precipitation of crystallization, easy blockage of spray pump ports, etc.

Active Publication Date: 2014-05-28
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the solubility of bepotastine besilate in water is slightly soluble (1g of solute dissolves in 30-100ml of solvent), bepotastine besilate may exist in the form of solid particles in the composition of this patent, and it may exist in the form of solid particles during long-term storage It is easy to precipitate crystals during the process, which is not conducive to the rapid absorption of drugs, and it is easy to block the spray pump port

Method used

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  • Bepotastine besilate nasal spray and preparation method thereof
  • Bepotastine besilate nasal spray and preparation method thereof
  • Bepotastine besilate nasal spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]

[0037]

[0038] Preparation:

[0039] Dissolve bepotastine benzenesulfonate, disodium edetate, disodium hydrogen phosphate, anhydrous glucose, propylene glycol, caprylic capric macrogol glyceride, and benzalkonium chloride in 80ml of pure water, mix, Add 1mol / L sodium hydroxide to adjust the pH to 6.5, add 20ml of pure water, mix well, filter, fill, and add a spray pump to obtain a solution-type nasal spray.

[0040] The above-mentioned nasal spray was subjected to three cycles of low temperature test, each cycle was at 2°C for 2 days, and then at 40°C for 2 days under accelerated conditions, sampling and testing showed that the solution was clear and no crystallization was observed.

[0041] The above-mentioned nasal spray was subjected to three cycles of freeze-thaw test, each cycle was subjected to -10°C for 2 days, and then inspected under accelerated conditions of 40°C for 2 days, and samples were taken for testing. As a result, the solution was clear and ...

Embodiment 2

[0043]

[0044]

[0045] The preparation method is the same as in Example 1. Get a solution nasal spray.

[0046] The above-mentioned nasal spray was subjected to three cycles of low temperature test, each cycle was at 8°C for 2 days, and then at 40°C for 2 days under accelerated conditions, sampling and testing showed that the solution was clear and no crystallization was observed.

[0047] The above-mentioned nasal spray was subjected to three cycles of freeze-thaw test, each cycle was at -20°C for 2 days, and then inspected at 40°C for 2 days under accelerated conditions, and samples were taken for testing. As a result, the solution was clear and no crystals were precipitated.

Embodiment 3

[0049]

[0050] The preparation process is the same as in Example 1. Get a solution nasal spray.

[0051] The above-mentioned nasal spray was placed in three cycles of low temperature and freeze-thaw as in Example 1, and the solution was clear without crystallization.

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PUM

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Abstract

The invention discloses a bepotastine besilate nasal spray and a preparation method thereof. For the nasal spray, 1-10 g of bepotastine besilate and 3-15 g of solubilizing composition are added in 100 mL of water; the solubilizing composition comprises components in percentage by weight as follows: 80%-95% of propylene glycol, polyethylene glycol 300 or polyethylene glycol 400 and the balance of caprylocaproyl macrogolglycerides; and pH of a nasal spray solution ranges from 6 to 8. In the composition, bepotastine besilate does not exist in a solid particle mode and cannot be crystallized during a long-term storage process, so that not only is rapid medicine absorption facilitated, but also a spray pump port is not blocked easily, and anaphylactic rhinitis and mucous membrane inflammation related to rhinitis can be cured effectively.

Description

technical field [0001] The invention relates to a preparation of bepotastine besilate and a preparation method thereof. Background technique [0002] Bepotastine bepotastine is a histamine H1 receptor antagonist jointly developed by Tanabe Seiyaku and UBE Industries of Japan. It was approved in Japan in 2000 for the treatment of allergic rhinitis and approved in 2002. For urticaria / itching, it is sold in Japan by Mitsubishi Tanabe Pharma under the trade name Talion (Tan Liang), which is a 10 mg white film-coated tablet. Bepotastine bepotastine tablets have been imported into my country for the treatment of itching caused by allergic rhinitis, urticaria, and skin diseases (eczema·dermatitis, prurigo, pruritus). Its chemical name is (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid monobenzenesulfonate, chemical The structural formula is as follows: [0003] [0004] Bepotastine is a non-sedating, highly selective histamine (H1) receptor inhibitor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K31/4545A61K47/34A61K47/10A61P11/02A61P37/08A61K47/14
Inventor 吴闻哲侯惠民罗世华姚孝林徐晓寒
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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