Solid composition containing rivaroxaban and preparation method thereof

Abstract

The invention discloses a solid composition containing rivaroxaban. The solid composition is prepared from the following components in percentage by weight: 20 percent to 80 percent of a micronized rivaroxaban lactose monohydrate mixture, wherein in the micronized rivaroxaban lactose monohydrate mixture, the weight percent ratio of rivaroxaban to lactose monohydrate ranges from (1 to 2) to (1 to 10); the solid composition is prepared from the following components: 20 percent to 80 percent of a diluting agent, 1 percent to 10 percent of a bonding agent, 2 percent to 8 percent of a disintegrating agent, 0.5 percent to 8 percent of a surfactant and 0.5 percent to 5 percent of a lubricant. Furthermore, the invention further provides a preparation method of the solid composition containing therivaroxaban; the preparation method comprises the following steps: crushing crude drugs, mixing, granulating, drying, totally blending, tabletting and coating. Compared with the prior art, a crushingmethod of the crude drugs has high yield and the crude drugs have small granularity and are uniformly micronized; rivaroxaban tablets disclosed by the invention have a high dissolution rate, the content of a single impurity and total impurities is lower and the stability is high; the production quality is ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid composition containing rivaroxaban and a preparation method thereof. Background technique [0002] Rivaroxaban is a highly selective drug that interrupts the intrinsic and extrinsic pathways of the coagulation cascade by directly inhibiting factor Xa, inhibiting the generation of thrombin and the formation of thrombus. [0003] Rivaroxaban, developed by Bayer, is a chemically synthesized small molecule compound, English name: Rivaroxaban, chemical name: 5-chloro-N-({(5S)-2-oxo-3-[-4-(3- Oxygen-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl})-2-thiophene-carboxamide, the structural formula is: [0004] Rivaroxaban is a poorly soluble drug with a solubility in water of about 10 mg / mL at room temperature. In the biopharmaceutical classification system (BCS), it belongs to class II, that is, low solubility and high permeability. The solubility of the drug has a grea...

AI Technical Summary

Problems solved by technology

[0007] The rivaroxaban is pulverized by airflow. During the pulverization process, the adhesion of rivaroxaban is enhanced, and it is easy to adhere to the inside of the equipment, prolonging the pulverization time and reducing the yield; the particle size of rivaroxaban is large and uneven

[0008] In addition, the imported commercially available product (trade name: Xarelto, specification: 10mg) has relatively large individual impurities and total impurities, which may exceed the limit during storage

Images