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ORAL PHARMACEUTICAL COMPOSITIONS OF RIVAROXABAN

IP.com Disclosure Number: IPCOM000245143D
Publication Date: 2016-Feb-12
Document File: 4 page(s) / 191K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure provides a process for the preparation of rivaroxaban tablets.

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ORAL PHARMACEUTICAL COMPOSITIONS OF RIVAROXABAN

Abstract


The present disclosure provides a process for the preparation of rivaroxaban tablets.

Reported herein is a process for the preparation of rivaroxaban tablets using mixer granulation, wherein rivaroxaban has a d90 value of not more than 30 µm, preferably not more than 15 µm, and most preferably not more than 10 µm.

The term “rivaroxaban,” as used herein, refers to a racemic form or enantiomerically pure form of rivaroxaban.  Rivaroxaban may be present in crystalline form, amorphous form, anhydrous form, hydrate form, solvate form, or as mixtures thereof.

The term “mixer granulation,” as used herein, refers to wet granulating rivaroxaban and one or more pharmaceutically acceptable excipients in a rapid mixer granulator using a suitable binder solution.

The term “d90,” as used herein, means that 90% of the particles are less than the specified particle size value based on volume.

The rivaroxaban tablets prepared according to the above process comprise one or more pharmaceutically acceptable excipients.

The term “pharmaceutically acceptable excipients,” as used herein, includes disintegrating agents, diluents, surfactants, glidants, lubricants, binders, plasticizers, opacifiers, coloring agents, solvents, and mixtures thereof.

Suitable diluents are selected from the group comprising starch, lactose, sucrose, glucose, sorbitol, calcium carbonate, calcium phosphate dibasic, calcium phosphate tribasic, calcium sulfate, microcrystalline cellulose, silicified microcrystalline cellulose, dextrates, dextrins, dextrose, fructose, lactitol, mannitol, sorbitol, pregelatinized starch, and mixtures thereof.

Suitable binders are selected from the group comprising methyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, polyvinyl pyrrolidone, poloxamer, gelatin, ethyl cellulose, polyvinyl alcohol, pullunan, pregelatinized starch, agar, tragacanth, sodium alginate, propylene glycol, gum arabic, and mixtures thereof.

Suitable disintegrating agents are selected from the group comprising cross-linked polyvinyl pyrrolidone, sodium starch glycolate, cross-linked sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, alginic acid, alginates, pregelatinized starch, starch and its derivatives, low-substituted hydroxypropyl cellulose, and mixtures thereof.

Suitable surfactants are selected from the group comprising anionic surfactants such as sodium lauryl sulfate, sodium dodecane sulfonate, sodium oleyl sulfate, and sodium laurate mixed with stearates and talc; cationic surfactants such as benzalkonium chlorides and alkyltrimethylammonium bromides; neutral surfactants such as glyceryl monooleate, polyoxyethylene sorbitan fatty acid esters, polyvinyl alcohol, and sorbitan esters; wetting agents such as poloxamers and polyoxyethylene castor oil derivatives; and mixtures thereof.

The rivaroxaban tablets as reported herein release more than 85% of rivaroxaban in 30 minut...