Rivaroxaban pharmaceutical composition and preparation method thereof

A technology of rivaroxaban and composition, applied in the field of medicinal chemistry, can solve the problems of long time, large energy consumption and high cost of wet granulation process

Inactive Publication Date: 2015-11-25
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the wet granulation process consumes a lot of energy, takes a long time and is expensive

Method used

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  • Rivaroxaban pharmaceutical composition and preparation method thereof
  • Rivaroxaban pharmaceutical composition and preparation method thereof
  • Rivaroxaban pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
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preparation example Construction

[0026] In the second aspect, the composition described in the first aspect of the present invention is prepared by the following method, and the preparation method includes the following steps:

[0027] a) dissolving the solubilizer in the binder solution;

[0028] b) adding rivaroxaban active substance, filler and disintegrant to the granulation equipment, and using a) to obtain the binder solvent to granulate, and dry;

[0029] c) passing the rivaroxaban granules obtained in b) through a comil sieve for granulation, and then placing them in a mixing tank;

[0030] d) Manually mix the lubricant with an appropriate amount of rivaroxaban granules obtained in b), pass through a 30-mesh sieve (0.600mm), add to the mixing tank, and mix to obtain the prepared granules;

[0031] In some embodiments, the preparation method of the present invention further includes the steps of compressing the prepared granules by using a tablet machine and coating the plain tablet after tableting. ...

specific Embodiment approach

[0039] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0040] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0041] Unless otherwise stated, all content percentages given below are mass percentages.

Embodiment 1

[0043] prescription

[0044] name

Content per tablet (mg)

Ratio (%, w / w)

Rivaroxaban, micronized

10.00

10.00

microcrystalline cellulose

37.80

37.80

[0045] lactose monohydrate

32.50

32.50

Croscarmellose Sodium

7.00

7.00

hypromellose

5.50

5.50

Sodium dodecyl sulfate (SDS)

1.50

1.50

Magnesium stearate

3.00

3.00

Opadry II

2.70

2.70

Total

100.00

100.00

[0046] Preparation:

[0047] Weigh an appropriate amount of sodium dodecyl sulfate (SDS), dissolve it in a hypromellose solution to prepare a binder solution, and set aside. Put rivaroxaban, microcrystalline cellulose, lactose monohydrate and croscarmellose sodium in a fluidized bed, and granulate in the fluidized bed with the previously prepared binder solution, and the fluidized bed The hole diameter of the cloth bag used in the step is less than 20mm, and the...

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Abstract

The invention relates to the field of pharmaceutical chemicals, and in particular relates to a rivaroxaban pharmaceutical composition and a preparation method thereof; the pharmaceutical composition consists of a rivaroxaban active substance, a solubilizer, a binding agent, a lubricant, a filling agent and a disintegrating agent, wherein the rivaroxaban active substance is not subject to hydrophilic treatment; and the solubilizer accounts for about 1.5%-3.5% in the entire composition in percentage by mass. The rivaroxaban pharmaceutical composition is stable and good in dissolution; and the preparation method is simple and convenient and is energy-saving, and the preparation method is applicable to industrial production.

Description

technical field [0001] The invention relates to a rivaroxaban pharmaceutical composition suitable for oral application and a preparation method thereof, belonging to the field of medicinal chemistry. Background technique [0002] Rivaroxaban, whose chemical name is 5-chloro-N-(((5S)-2-oxo-3-(4-(3-oxomorpholin-4-yl)phenyl)-1,3 -Oxazolin-5-yl)methyl)thiophene-2-carboxamide, the chemical structural formula is as follows: [0003] [0004] It is a low molecular weight and oral coagulation factor Xa inhibitor, which is used to prevent or / and treat various thromboembolic diseases (see WO01 / 47919). JANSSENPHARMS has developed and launched oral tablets of rivaroxaban. Said rivaroxaban is a publicly known compound. [0005] Rivaroxaban has poor solubility in water, about 7 mg / L, thus resulting in poor dissolution in the composition. A low dissolution rate in the pharmaceutical composition may lead to low bioavailability, so it can be seen that the bioavailability of rivaroxaba...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K47/20A61P7/02
Inventor 朱文涛余义义胡相靖谭晓峰
Owner SUNSHINE LAKE PHARM CO LTD
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