Preparation method of oral preparation containing rivaroxaban

A rivaroxaban and content technology, applied in the field of oral tablets containing rivaroxaban, can solve problems such as sticky punching, complicated preparation process, and loose tablets

Active Publication Date: 2014-09-24
JILIN BODA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Chinese patent 201310504757.X discloses a fast-release oral solid pharmaceutical composition containing rivaroxaban and its preparation method, which processes suitable pharmaceutical excipients through a wet granulation process, and then reacts with rivaroxaban active The ingredients are mixed to obtain a pharmaceutical composition with significantly improved dissolution. The preparation method of the present invention has the characteristics of simple process and is suitable for industrial production, and solves the problem that the preparation process of the prior art is relatively complicated.
[0013] The preparation process of the above-mentioned rivaroxaban mostly adopts wet granulation. The inventors found in the process of studying rivaroxaban tablets that rivaroxaban has certain hygroscopicity, and wet granulation is used to compress the tablet. It brings difficulties, such as tablet pitting, sticky punching, loose tablets, disintegration, etc., and affects dissolution rate and stability at the same time

Method used

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  • Preparation method of oral preparation containing rivaroxaban
  • Preparation method of oral preparation containing rivaroxaban
  • Preparation method of oral preparation containing rivaroxaban

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] 10mg tablet

[0054]

[0055] The preparation method is as follows:

[0056] 1. Mix the raw materials with sodium lauryl sulfate evenly - mix for not less than 30 minutes to obtain mixture I;

[0057] 2. Mix mixture Ⅰ and lactose in equal amounts and mix evenly—each time mixing for no less than 20 minutes to obtain mixture Ⅱ;

[0058] 3. Mix the mixture II and the remaining materials evenly, and press into tablets;

Embodiment 2

[0060] 5mg tablet

[0061]

[0062]

[0063] The preparation method is as follows:

[0064] 1. Mix the raw materials with sodium lauryl sulfate evenly - mix for not less than 30 minutes to obtain mixture I;

[0065] 2. Mix mixture Ⅰ and lactose in equal amounts and mix evenly—each time mixing for no less than 20 minutes to obtain mixture Ⅱ;

[0066] 3. Mix the mixture II and the remaining materials evenly, and press into tablets;

Embodiment 3

[0068] 20mg tablet

[0069]

[0070] The preparation method is as follows:

[0071] 1. Mix the raw materials with sodium lauryl sulfate evenly - mix for not less than 30 minutes to obtain mixture I;

[0072] 2. Mix mixture Ⅰ and lactose in equal amounts and mix evenly—each time mixing for no less than 20 minutes to obtain mixture Ⅱ;

[0073] 3. Mix the mixture II and the remaining materials evenly, and press into tablets;

[0074] In the above embodiments, if 100,000 pieces are prepared in industrial scale-up production, the weight of the raw and auxiliary materials will increase by 100,000 times accordingly.

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Abstract

The invention relates to an oral tablet containing rivaroxaban. The tablet is prepared by adopting a powder direct mixing and tabletting method. an inventor solves partial problems and solves the problems of pitted surface, sticking, loosening tablet and disintegration and dissolution rate and stability problems through addition and replacement of a proper additives and a screening experiment, so as to obtain a novel formula of rivaroxaban tablets and a preparation method of the rivaroxaban tablets by adopting the powder direct mixing and tabletting method. Each rivaroxaban tablet comprises the following components by weight: 5-20mg of rivaroxaban, 60-80mg of lactose, 4-6mg of mannitol, 2-4mg of croscarmellose sodium, 1-3mg of citric acid, 0.5-2mg of lauryl sodium sulfate, 3-5mg of carbomer, 3-5mg of povidone K90, 3-5mg of hydroxyl propyl cellulose, 0.5-2mg of magnesium stearate and 0.5-2mg of silicon dioxide.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an oral tablet containing rivaroxaban, which is prepared by a preparation method of directly mixing and pressing powders. Background technique [0002] Rivaroxaban is an anticoagulant drug, a factor Xa inhibitor, English name: rivaroxaban, structural formula: [0003] [0004] Factor Xa is the intersection of extrinsic and intrinsic coagulation pathways, and is a key point in the coagulation process. Rivaroxaban can selectively and directly inhibit the activity of factor Xa, thereby inhibiting the generation of thrombin and the formation of thrombus. The pharmacokinetic study of rivaroxaban shows that it has a rapid onset of action and can quickly reach the peak plasma concentration within 2-4 hours after administration. The absolute bioavailability is as high as 80-100%. Moreover, the maximum inhibitory effect on factor Xa can be obtained 1-4 hours af...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/5377A61K47/38A61K47/32A61K47/26A61K47/10A61P7/02
Inventor 李帅胡伟利殷晓华路兴海李昊张文清
Owner JILIN BODA PHARMA
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