Rivaroxaban oral microsphere preparation

A technology of rivaroxaban and microspheres, applied in the field of rivaroxaban oral microsphere preparations, can solve the problems of restricted use, great differences in solubility and the like

Inactive Publication Date: 2014-02-05
JIANGSU ALPHA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the great difference in the solubility of different crystal forms of rivaroxaban, crystal form 2 is selected as the pharmaceutical crystal form under the existing technology, which limits the use of other crystal forms

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Mix and stir 50g of hydroxypropylmethylcellulose and 450g of water to obtain a complete solubility solution. Weigh 10 g of rivaroxaban and 50 g of THF, mix and stir to dissolve. The two solutions were mixed and stirred.

[0013] A nozzle-type spray dryer was selected for spraying at a spray temperature of 90°C and a spray speed of 8ml / min to obtain rivaroxaban microspheres with an average particle size of 76 μm.

Embodiment 2

[0015] Mix and stir 10 g of polyvinylpyrrolidone with 90 g of water to obtain a complete solubility solution. Weigh 10 g of rivaroxaban and 50 g of THF, mix and stir to dissolve. The two solutions were mixed and stirred.

[0016] A nozzle-type spray dryer was selected to spray at a spray temperature of 115°C and a spray speed of 3ml / min to obtain rivaroxaban microspheres with an average particle size of 38 μm.

Embodiment 3

[0018] Mix and stir 100 g of polyethylene glycol with 900 g of water to obtain a complete solubility solution. Weigh 10 g of rivaroxaban and 50 g of THF, mix and stir to dissolve. The two solutions were mixed and stirred.

[0019] An atomization-type spray dryer was selected for spray drying at 100° C., a spray speed of 4500 rpm, and a spray speed of 5 ml / min to obtain rivaroxaban microspheres with an average particle size of 53 μm.

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Abstract

The invention provides a rivaroxaban oral microsphere preparation. The rivaroxaban oral microsphere preparation comprises rivaroxaban and a water-soluble polymer carrier, wherein the water-soluble polymer carrier comprises one or a few of hydroxypropyl methyl cellulose, polyethylene glycol, polyvinylpyrrolidone and cellulose polymer, the weight ratio of the rivaroxaban and water-soluble polymer carrier is 1:(1-10), and the average grain diameter of the microsphere is 38-79 m um. According to the microsphere preparation, the solubility and bioavailability of indissolvable medicines are improved, and the preparation of rivaroxaban medicinal preparation is no longer restricted by crystal form.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to a rivaroxaban oral microsphere preparation. Background technique [0002] Rivaroxaban is a new type of anticoagulant drug developed by Bayer after 10 years. It is the world's first direct factor Xa inhibitor. It is a chemically synthesized small molecule compound with a molecular weight of 435.89 and its general name is Rivaroxaban Tablets. Since September 2008, rivaroxaban has been listed in more than 50 countries around the world, and was officially launched in China in June 2009, and in the United States on July 1, 2011. Rivaroxaban has high selectivity and directly inhibits the activity of factor Xa, thereby inhibiting the generation of thrombin and the formation of thrombus. Factor Xa is the junction of the intrinsic coagulation pathway and the extrinsic coagulation pathway, and plays a key role in the coagulation process, so it is considered to be a very important target in the dev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/5377A61K47/38A61K47/34A61K47/32A61P7/02
Inventor 蔡进吉民徐春涛尹晓龙
Owner JIANGSU ALPHA PHARM CO LTD
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