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Edoxaban sustained release tablet and preparation method thereof

A technology for edoxaban and sustained-release tablets, which is applied in the field of sustained-release matrix tablets containing active ingredient edoxaban and its preparation, and can solve the problems of reduced therapeutic effect, increased adverse drug reactions, and excessive fluctuations in blood drug concentration And other issues

Inactive Publication Date: 2014-07-16
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It will be very difficult to prepare a drug with a short half-life for 24-hour administration
[0018] Attached by the above Form 1, Form 2 and instructions figure 1 According to the data, C of the active metabolite of edoxaban max About only Edoxaban C max The half-life of edoxaban and its active metabolites is about 5 hours. Although its use is once a day, that is to say, its therapeutic index is very wide, but this will cause fluctuations in blood drug concentration Too large, the blood concentration is not stable enough
Although the therapeutic index of edoxaban is relatively wide, the huge gap in the "peak-to-valley ratio" when taken once a day still increases the potential adverse reactions of the drug. Therefore, edoxaban is made into sustained-release tablets in order to make The fluctuation range of edoxaban plasma concentration is significantly reduced, so that edoxaban will not only reduce the therapeutic effect, but also greatly reduce adverse reactions

Method used

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  • Edoxaban sustained release tablet and preparation method thereof
  • Edoxaban sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Prescription %

[0048] Edoxaban p-toluenesulfonate hydrate 20.2g 20.2%

[0049] HPMC K100M 20g 20.0%

[0050] Carbomer 974P 10g 10.0%

[0051] Lactose 17g 17.0%

[0052] Starch 30g 30.0%

[0053] Talc 2g 2.0%

[0054] Magnesium Stearate 1g 1.0%.

[0055]Preparation method: 1. Pass the raw material through a 120-mesh sieve; 2. Mix the raw material, HPMC K100M, and Carbomer 974P evenly, granulate with about 90% ethanol, and then dry; 3. Sieve and granulate, add the prescribed amount of Talc and magnesium stearate, mix well and compress.

[0056] In the release test, the release rate of the sample was measured according to the second appendix XC of the 2010 edition of the Chinese Pharmacopoeia, and the first method of the second appendix XD of the Chinese Pharmacopoeia of the 2010 edition was used. Take 900ml of buffer salt with pH 6.8 as the solvent, rotate at 50 rpm, take samples at 1, 4 and 8 hours, and measure the release degree of ...

Embodiment 2

[0062] Prescription %

[0063] Edoxaban p-toluenesulfonate hydrate 40.4g 20.2%

[0064] HPMC K100M 36g 18.0%

[0065] Carbomer 974P 12g 6.0%

[0066] Lactose 34g 17.0%

[0067] Starch 72g 36.0%

[0068] Talc 4g 2.0%

[0069] Magnesium Stearate 2g 1.0%

[0070] Preparation method: 1. Pass the raw material through a 120-mesh sieve; 2. Mix the raw material, HPMC K100M, and Carbomer 974P evenly, granulate with about 90% ethanol, and then dry; 3. Sieve and granulate, add the prescribed amount of Talc and magnesium stearate, mix well and compress.

[0071] In the release test, the release rate of the sample was measured according to the second appendix XC of the 2010 edition of the Chinese Pharmacopoeia, and the first method of the second appendix XD of the Chinese Pharmacopoeia of the 2010 edition was used. Take 900ml of buffer salt with pH 6.8 as the solvent, rotate at 50 rpm, take samples at 1, 4 and 8 hours, and measure the release degree of the sample. The results are as...

Embodiment 3

[0077] Prescription %

[0078] Edoxaban p-toluenesulfonate hydrate 20.2g 20.2%

[0079] HPMC K100M 35g 35.0%

[0080] Lactose 11g 11.0%

[0081] Starch 30g 30.0%

[0082] PVP K30 3g 3.0%

[0083] Magnesium Stearate 1g 1.0%

[0084] Preparation method: 1. Pass the raw material through a 120-mesh sieve; 2. Mix the raw material and HPMC K100M uniformly, granulate with about 90% ethanol solution of PVP K30, and then dry; 3. Sieve and granulate, and add the prescribed amount of stearic acid. Magnesium, mix well and tablet.

[0085] In the release test, the release rate of the sample was measured according to the second appendix XC of the 2010 edition of the Chinese Pharmacopoeia, and the first method of the second appendix XD of the Chinese Pharmacopoeia of the 2010 edition was used. Take 900ml of buffer salt with pH 6.8 as the solvent, rotate at 50 rpm, take samples at 1, 4 and 8 hours, and measure the release degree of the sample. The results are as follows:

[0086] Time ...

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Abstract

The invention provides a preparation method of an edoxaban sustained release matrix tablet. The specific prescription of the edoxaban sustained release tablet consists of the following components in percentage by weight: 14-21 percent of edoxaban p-toluene sulfonate hydrate, 0-36 percent of hydroxypropyl methylcellulose, 0-28 percent of carbomer, 10-28 percent of lactose, 29-38 percent of diluent, 0-3 percent of povidone and 0.6-4 percent of lubricant.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and specifically relates to a sustained-release matrix tablet containing active ingredient edoxaban and a preparation method thereof. Background technique [0002] The chemical name of Edoxaban is N-(5-chloro-2-pyridyl)-N ’ -[(1S,2R,4S)-4-[(Dimethylamino)formyl]-2-[[4,5,6,7-tetrahydro-5-methylthiazolo[5,4-C] Pyridin-2-yl) formyl] amino] cyclohexyl] oxalamide p-benzene mesylate monohydrate, the structural formula is as follows: [0003] . [0004] The solubility of this product in the Japanese manual: easily soluble in dimethyl sulfoxide, N,N-dimethylformamide, slightly soluble in methanol, water, acetonitrile, slightly soluble in ethanol (99.5), very slightly soluble in acetone, Ethyl acetate, practically insoluble in isopropanol. [0005] Healthy adult males take Edoxaban 30mg orally on an empty stomach once, the pharmacokinetic parameters of Edoxaban and its ac...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K47/38A61K47/32A61K31/44
Inventor 孙晋瑞陈修毅颜东刘宜辉
Owner SHANDONG INST OF PHARMA IND
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