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STABILITY-IMPROVED FORM OF AMORPHOUS SOFOSBUVIR

IP.com Disclosure Number: IPCOM000250038D
Publication Date: 2017-May-19
Document File: 7 page(s) / 113K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure relates to a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium selected from the group consisting of croscarmellose, mannitol, microcrystalline cellulose, and mixtures thereof. The present disclosure further relates to a stable pharmaceutical composition comprising said stability-improved form of amorphous sofosbuvir and one or more pharmaceutically acceptable excipients.

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STABILITY-IMPROVED FORM OF AMORPHOUS SOFOSBUVIR

Abstract

The present disclosure relates to a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium selected from the group consisting of croscarmellose, mannitol, microcrystalline cellulose, and mixtures thereof.  The present disclosure further relates to a stable pharmaceutical composition comprising said stability-improved form of amorphous sofosbuvir and one or more pharmaceutically acceptable excipients.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium selected from the group consisting of croscarmellose, mannitol, microcrystalline cellulose, and mixtures thereof.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium, wherein the sofosbuvir and the carrier medium are present in the ratio of from 1:99 to 99:1.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium, wherein the amorphous sofosbuvir may be substantially amorphous.

“Substantially amorphous,” as used herein, refers to at least about 90% amorphous, preferably about 95% amorphous, and more preferably about 100% amorphous.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium, wherein the amorphous sofosbuvir may be present in an amount of from 10% to 99% by total weight of the intimate mixture.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium, wherein the carrier medium may be present in an amount of from 1% to 90% by total weight of the intimate mixture.

Reported herein is a stability-improved form of amorphous sofosbuvir comprising an intimate mixture of sofosbuvir and a carrier medium, wherein the intimate mixture is a solid dispersion.

“Stability-improved form of amorphous sofosbuvir,” as used herein, includes an amorphous form that does not deliquesce at 40°C and 75% relative humidity (“RH”) for a period of 3 months.

“Intimate mixture” as used herein, includes a solid dispersion or solution, a co-precipitate, and the like of the mixture of sofosbuvir and a carrier medium.  Intimate mixtures are not obtained by merely blending solid forms of the components.

“Solid dispersion,” as used herein, includes a solidified form of a drug obtained by dispersing or dissolving the drug in a carrier medium.

Croscarmellose is a cross-linked polymer of carboxymethylcellulose sodium.  It appears as a white, fibrous, water insoluble, free-flowing powder, and is used commonly as a disintegrant in pharmaceutical manufacturing.  Mannitol is a polyol (sugar alcohol) and an isomer of sorbitol, used in pharmaceutical products as a sweetening agent, tablet and c...