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Toluenesulfonic acid edoxaban tablet and preparation method thereof

A technology of edoxaban tosylate and tablets, which is applied in the field of medicine and can solve problems such as poor dissolution, affecting drug absorption, and unfavorable clinical treatment.

Active Publication Date: 2018-11-06
安徽佳和药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Edoxaban is a basic compound with good solubility in acidic aqueous solution, but decreased solubility in neutral solution (such as neutral pH6.8 buffer)
The poor dissolution rate of edoxaban in the medium under neutral conditions may also affect the absorption of the drug in the intestine, which will lead to a decrease in bioavailability, which is not conducive to clinical treatment

Method used

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  • Toluenesulfonic acid edoxaban tablet and preparation method thereof
  • Toluenesulfonic acid edoxaban tablet and preparation method thereof
  • Toluenesulfonic acid edoxaban tablet and preparation method thereof

Examples

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Effect test

Embodiment 1

[0039] Embodiment 1, preparation edoxaban tosylate sheet

[0040] The present embodiment provides the prescription and preparation method for preparing 1000 Edoxaban Tosylate Tablets (the specification is 15 mg / tablet, calculated as Edoxaban), as follows:

[0041] Prescription composition:

[0042]

[0043]

[0044] Crushing the raw material edoxaban toluenesulfonate (D90≤25 μm) through a 100-mesh sieve, mannitol and pregelatinized starch as auxiliary materials, respectively, through a 80-mesh sieve, and magnesium stearate through a 100-mesh sieve;

[0045] The preparation method is as follows:

[0046] 1) Weigh the prescription amount of edoxaban tosylate, hydrophilic polymer carrier (HPMCAS, PVP-K30), surfactant (poloxamer 188) and dissolve in 2.5L solvent (dimethyl sulfoxide In the mixed solvent that is 1:4 with water volume ratio), adopt ultrasonic-assisted dissolving to obtain homogeneous solution; Then remove described solvent with spray drying, obtain edoxaban tos...

Embodiment 2

[0049] Embodiment 2, preparation Edoxaban tosylate sheet

[0050] The present embodiment provides the prescription and preparation method for preparing 1000 Edoxaban Tosylate Tablets (the specification is 30 mg / tablet, calculated as Edoxaban), as follows:

[0051] Prescription composition:

[0052]

[0053]

[0054] The preparation method is basically the same as in Example 1.

Embodiment 3

[0055] Embodiment 3, preparation Edoxaban tosylate sheet

[0056] The present embodiment provides the prescription and preparation method for preparing 1000 Edoxaban Tosylate Tablets (the specification is 15 mg / tablet, calculated as Edoxaban), as follows:

[0057] Prescription composition:

[0058]

[0059] The preparation method is basically the same as in Example 1.

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Abstract

The invention discloses a toluenesulfonic acid edoxaban tablet and a preparation method thereof. Raw materials of the toluenesulfonic acid edoxaban tablet include the following substances by mass: 20.2 parts of toluenesulfonic acid edoxaban, 10.1-101 parts of polymeric carrier, 2.02-10.1 parts of surfactant, 30-45 parts of filler and 0.4-0.8 part of lubricant. The polymeric carrier is preferably amixture of PVP K-30 and HPMCAS with the mass ratio of (2-4):1. The preparation method includes dissolving the toluenesulfonic acid edoxaban, the polymeric carrier and the surfactant in a solvent; spraying and drying to obtain a solid dispersion of the toluenesulfonic acid edoxaban; 2) mixing the solid dispersion of the toluenesulfonic acid edoxaban with other accessories and conducting tabletting. The tablet can significantly improve the dissolution rate and the solubility of a drug, increase the drug absorption and improve the bioavailability. In particular, the tablet significantly improvesthe dissolution behavior in a buffer solution of neutral pH 6.8 compared with the existing preparations.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an edoxaban tosylate tablet and a preparation method thereof. Background technique [0002] Edoxaban, English name Edoxaban, chemical name: N1-(5-chloropyridine-2- [0003] Base)-N2-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)]-2-[(5-methyl-4,5,6,7-tetrahydro- 1,3-Thiazolo [0004] [5,4-c]-pyridine-2-carboxamido)cyclohexyl]oxalamide, American Chemical Abstracts registration number CAS: 912273-65-5, its structural formula is shown in the following formula: [0005] [0006] Its tosylate, edoxaban tosylate, English name: Edoxaban Tosilate Hydrate, chemical name: N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4 -(Dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamido) Cyclohexyl] oxamide mono(4-methylbenzenesulfonate) monohydrate, American Chemical Abstracts registration number CAS: 480449-71-6, the structural formula is as follows: [0007] [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K47/32A61K47/38A61K31/444A61P7/02
CPCA61K9/2027A61K9/2054A61K9/282A61K31/444A61P7/02
Inventor 罗桓刘宇晶利虔袁伟锋孙跃军张文腾谌宗永
Owner 安徽佳和药业有限公司
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