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Composition containing rivaroxaban and preparation method thereof

A technology for rivaroxaban and a composition is applied in the field of compositions containing rivaroxaban, which can solve the problems of cumbersome process, high energy consumption, degradation reaction of drugs, etc., and achieves the effect of wide application and increased dissolution.

Active Publication Date: 2018-04-24
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the dry granulation and direct compression process, this method has cumbersome process and high energy consumption, and it may also cause some drugs to degrade due to the heat treatment.

Method used

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  • Composition containing rivaroxaban and preparation method thereof
  • Composition containing rivaroxaban and preparation method thereof
  • Composition containing rivaroxaban and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Measurement comparison implementation 1 disintegration: about 6.5 minutes;

[0029] Dissolution: Dissolution conditions: USP paddle method, 900ml sodium acetate buffer solution with pH 4.5 containing 0.5% sodium lauryl sulfate, rotating speed 75 rpm). Samples were taken at 15, 30, 45 and 60 minutes respectively, filtered, and the filtrate was taken for HPLC determination, and the cumulative dissolution percentage was calculated.

[0030] Dissolution results

[0031]

Embodiment 1

[0051] Composition of rivaroxaban / per tablet:

[0052]

[0053] Among them, rivaroxaban uses micronized crystal form I, and the particle size distribution is X 50 =3.5μm, X 90 =7.6μm

[0054] Preparation Process:

[0055] Using methods known in the pharmaceutical industry, mix rivaroxaban with β-cyclodextrin, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate and micronized silica gel into the hopper of a dry granulator In the process, the medicine-containing flakes are rolled and pressed at a pressure of 5-7 Mpa, and then pulverized with a 30-mesh screen to prepare granules. The obtained granules are mixed with magnesium stearate and compressed into tablets, the diameter of the tablet is 6mm, and the hardness is 60-90N. The obtained tablet is coated with a coating material comprising iron oxide, hydroxypropylmethylcellulose and polyethylene glycol.

Embodiment 2

[0057] Composition of rivaroxaban / per capsule:

[0058]

[0059] Among them, rivaroxaban uses micronized crystal form I, and the particle size distribution is X 50 =4.8μm, X 90 =9.2μm

[0060] Preparation Process:

[0061] Using methods known in the pharmaceutical industry, mix rivaroxaban with α-cyclodextrin, micronized silica gel and sodium lauryl sulfate, and put them into No. 1 capsules with a capsule filling machine.

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Abstract

The invention discloses a rivaroxaban-containing composition and a preparation method thereof. The composition contains rivaroxaban and cyclodextrin with a weight ratio of (1: 1) to (1: 20). The composition disclosed by the invention is wide in process application range, and capable of improving rivaroxaban dissolution and guaranteeing no influences of a preparation process on the bioavailability.

Description

technical field [0001] The invention relates to a composition containing rivaroxaban and a preparation method thereof. Background technique [0002] Rivaroxaban (Rivaroxaban), the chemical name is 5-chloro-nitrogen-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1, 3-oxazolidin-5-yl}-2-thiophene-carboxamide, its structural formula is as shown in formula (I): [0003] [0004] Rivaroxaban is the world's first oral direct factor Xa inhibitor, which can highly selectively and competitively inhibit free and bound Xa coagulation factor, interrupt the intrinsic and extrinsic pathways of blood coagulation, thereby inhibiting the thrombin generation and thrombosis. [0005] Rivaroxaban is a highly hydrophobic and poorly soluble drug with a low solubility in water (about 7 mg / L). Appropriate solubilization techniques must be used to achieve the desired therapeutic effect. Bayer applied for protection of a wet granulation process of rivaroxaban and its composition (method for pre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/5377A61P7/02A61P9/10A61P9/14
Inventor 陶涛柴旭煜谢双赵雁陈中亚印玺璟
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT