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Ramatroban cyclodextrin inclusion

A technology of ramatroban and cyclodextrin, which is applied in the field of ramatroban pharmaceutical preparations, can solve problems such as unfavorable practical application, industrial production, changes in bioavailability, etc., and achieves improved bioavailability, simple method, and increased stability. sexual effect

Inactive Publication Date: 2006-10-04
EAST CHINA NORMAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystalline form of ramatroban obtained by the preparation method described in this patent has a melting point of 137 ° C. This crystalline form has an X-ray diffraction pattern, but in the course of the test, we can find that this crystalline form is metastable. When used in solid and semi-solid preparations such as capsules, tablets, suspensions and ointments, accompanying phenomena such as caking and changes in bioavailability will be found, which is not conducive to practical application and industrial production

Method used

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  • Ramatroban cyclodextrin inclusion
  • Ramatroban cyclodextrin inclusion

Examples

Experimental program
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Effect test

Embodiment 1

[0018] 5 g of β-cyclodextrin and 1 gram of ramatroban were reacted in 25 ml of water-ethanol (1:2) mixture for 12 hours at room temperature. The solvent was removed by spray-drying or freeze-drying to obtain a white microcrystalline solid, which was shown to be a new crystalline inclusion by X-ray powder diffraction. The inclusions are suitable for direct compression or filled capsules.

Embodiment 2

[0020] Add 5 grams of ramatroban, add appropriate amount of ethanol to dissolve it, weigh another 5 grams of hydroxypropyl cyclodextrin, add water, and make a saturated solution in a constant temperature water bath at 40°C. Under electric stirring, slowly add the ramatroban ethanol solution into the hydroxypropyl cyclodextrin solution, stir at constant temperature for 1 hour, stop heating, and continue stirring to room temperature to obtain a white suspension, put it in the refrigerator for 12 hours, pump Filter, and vacuum-dry the precipitate at 40°C, pass through an 80-mesh sieve, and dry it for later use. X-ray powder diffraction showed that it was an inclusion of a new crystalline state (see figure 1 ). The inclusions can be directly compressed into tablets or filled into capsules.

Embodiment 3

[0022] Add 5 grams of β-cyclodextrin and 25ml of water, grind it evenly with a high-energy grinder, add 5 grams of Rematroban, and grind it fully until it becomes a paste, about 1 hour, after drying in a freeze dryer for 4 hours, use 10ml Rinse the dry matter with ethanol, and then freeze-dry it.

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Abstract

The invention discloses an inclusion complex of ramatroban and beta-cyclodextrin and its preparing process, with the use of cyclodextrin inclusion method, the dissolvability and bioavailability of the medicament is improved. The cyclodextrin inclusion complex can be further used for the preparation of oral medicinal compositions.

Description

technical field [0001] The invention relates to a ramatroban pharmaceutical preparation, in particular to a ramatroban cyclodextrin inclusion and a pharmaceutical composition thereof. Background technique [0002] Ramatroban, chemical name: (R)-3{[(4-fluorophenyl)sulfonyl]amino}-1,2,3,4-tetrahydro-9H-carbazole-9-propionic acid is a thrombus Alkane A2 receptor antagonist, can inhibit the permeability of capillaries and the infiltration of eosinophils in the nasal mucosa. [0003] The preparation and use of ramatroban as a thromboxane A2 receptor antagonist has been disclosed in EP242518. The crystalline form of ramatroban obtained by the preparation method described in this patent has a melting point of 137 ° C. This crystalline form has an X-ray diffraction pattern, but in the course of the test, we can find that this crystalline form is metastable. When used in solid and semisolid preparations such as capsules, tablets, suspensions and ointments, accompanying phenomena su...

Claims

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Application Information

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IPC IPC(8): A61K31/403A61K47/40A61K9/20A61K9/48A61P11/02
Inventor 杨琍苹肖元晶张磊曾振亚
Owner EAST CHINA NORMAL UNIV
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