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PHARMACEUTICAL FORMULATION OF REGORAFENIB

IP.com Disclosure Number: IPCOM000244858D
Publication Date: 2016-Jan-22
Document File: 6 page(s) / 54K

Publishing Venue

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Abstract

The present disclosure provides a pharmaceutical formulation comprising regorafenib, vitamin E TPGS, and optionally one or more pharmaceutically acceptable excipients. It further provides processes for the preparation of said pharmaceutical formulation.

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PHARMACEUTICAL FORMULATION OF REGORAFENIB

Abstract

The present disclosure provides a pharmaceutical formulation comprising regorafenib, vitamin E TPGS, and optionally one or more pharmaceutically acceptable excipients.  It further provides processes for the preparation of said pharmaceutical formulation.

Reported herein is a pharmaceutical formulation comprising:

(i)   regorafenib;

(ii)  vitamin E TPGS; and

(iii) optionally, one or more pharmaceutically acceptable excipients.

The weight ratio of regorafenib to vitamin E TPGS ranges from about 1:1 to about 1:20, preferably from about 1:1 to about 1:10, and most preferably 1:6.

The term “about,” as used herein, refers to any value which lies within the range defined by a variation of up to ±10% of the value.

The term “regorafenib,” as used herein, refers to regorafenib as well its pharmaceutically acceptable salts, polymorphs, prodrugs, solvates, or hydrates.

The term “vitamin E TPGS,” as used herein, refers to d-α-tocopheryl polyethylene glycol 1000 succinate, also known as TPGS. 

The term “pharmaceutically acceptable excipients,” as used herein, includes any physiologically inert additives that are routinely used in pharmaceutical formulations.  The pharmaceutically acceptable excipients may include, but are not limited to, diluents, disintegrants, surfactants, lubricants/glidants, sorbents, binders, and mixtures thereof.

Suitable diluents are selected from the group comprising microcrystalline cellulose, powdered cellulose, dibasic or tribasic calcium phosphate, calcium sulfate, calcium carbonate, lactose monohydrate, lactose anhydrous, sucrose, sorbitol, xylitol, erythritol, kaolin, calcium silicate, maltodextrin, starch, modified starch, e.g., pregelatinized starch, maize starch, corn starch, and mixtures thereof.

Suitable disintegrants are selected from the group comprising croscarmellose sodium, carboxymethyl cellulose sodium, carboxymethyl cellulose calcium, low-substituted hydroxypropyl cellulose (L-HPC), crospovidone, sodium starch glycolate, gums, alginic acid or alginates, starch, corn starch, modified starch, carboxymethyl starch, polyacrylates, and mixtures thereof.

Suitable surfactants are selected from the group comprising sodium lauryl sulfate, sodium dodecyl sulfate, ammonium lauryl sulfate, benzalkonium chloride, alkyl poly(ethylene oxide), copolymers of poly(ethylene oxide) and poly(propylene oxide) commercially known as poloxamers or poloxamines, sorbitol monolaurate (e.g., Span® 20 or Span® 80), polyvinyl alcohol, fatty alcohols, polyoxyethylene alkyl ether, polyoxyethylene alkylaryl ether, alkylene glycol fatty acid ester, polyethylene glycol fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid mono ester, polyoxyethylene sorbitan fatty acid ester (polysorbates), soy lecithin, and mixtures thereof.

Suitable lubricants/glidants are selected from the group comprising magnesium stearate, colloidal silicon dioxide, hydrogenated vegetable o...