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Ramatroban glue pill and its preparation method

A technology for rematroban and capsules, applied in the field of rematroban capsules and its preparation, capable of solving problems such as caking, changes in bioavailability, unfavorable practical applications and industrial production

Inactive Publication Date: 2005-01-19
杭州容立医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, if it is directly made into capsules, tablets or used in suspensions and ointments, accompanying phenomena such as caking and changes in bioavailability will be found, which is very unfavorable for practical application and industrial production.

Method used

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  • Ramatroban glue pill and its preparation method
  • Ramatroban glue pill and its preparation method
  • Ramatroban glue pill and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: Preparation of ramatroban aqueous capsules

[0033] Dissolve 100 parts by weight of ramatroban in 300 parts by weight of acetone, add 25 parts by weight of sodium lauryl sulfate and 300 parts by weight of polyethylene glycol, stir at a temperature of 40°C to make it mix uniformly Capsules can be made.

Embodiment 2

[0034] Embodiment 2: Preparation of ramatroban aqueous capsules

[0035] Dissolving 100 parts by weight of ramatroban in 500 parts by weight of ethanol, adding 15 parts by weight of Tween-20 and 500 parts by weight of polyethylene glycol, stirring at a temperature of 55°C to make it evenly mixed can be prepared Capsules.

Embodiment 3

[0036] Embodiment 3: Preparation of ramatroban aqueous capsules

[0037] Dissolve 100 parts by weight of ramatroban in 150 parts by weight of acetone, add 5 parts by weight of sodium lauryl sulfate and 250 parts by weight of stearyl alcohol, stir at 25°C to make it evenly mixed Make capsules.

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Abstract

The invention discloses a Ramatroban gelatin-coated capsule pill comprising liquid solution with active constituent and outer wrapping material, wherein the liquid solution with active constituent is Ramatroban solution prepared from Ramatroban and findings, the invention also discloses the process for preparing the Ramatroban capsule and pill.

Description

technical field [0001] The invention relates to capsules containing ramatroban pharmacologically active components and a preparation method thereof. Background technique [0002] (R)-3-{[(4-fluorophenyl)sulfonyl]amino}-1,2,3,4-tetrahydro-9H-carbazole-9-propionic acid (ramatroban) is a thromboxane A 2 Receptor antagonist that inhibits the permeability of capillaries and the infiltration of eosinophils in the nasal mucosa. [0003] Thromboxane A 2 The preparation and use of the receptor antagonist ramatroban has been disclosed in EP242518. [0004] In the preparation process described therein, ramatroban was obtained in crystalline form, having a melting point of 137°C, this crystalline form had an X-ray diffraction pattern, but during the experiments we could find that this crystalline form was metastable . Therefore, if it is directly made into capsules, tablets or used in suspensions and ointments, accompanying phenomena such as caking and changes in bioavailability wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/403A61K47/42A61P11/02A61P11/06A61P37/08
Inventor 陆峰
Owner 杭州容立医药科技有限公司
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