Browse Prior Art Database

PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

IP.com Disclosure Number: IPCOM000240185D
Publication Date: 2015-Jan-09
Document File: 9 page(s) / 61K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure relates to solid oral pharmaceutical compositions consisting essentially of linaclotide and a cation, and processes for their preparation. The pharmaceutical compositions of the present invention do not comprise amines.

This text was extracted from a Microsoft Word document.
At least one non-text object (such as an image or picture) has been suppressed.
This is the abbreviated version, containing approximately 16% of the total text.

PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

Abstract

The present disclosure relates to solid oral pharmaceutical compositions consisting essentially of linaclotide and a cation, and processes for their preparation.  The pharmaceutical compositions of the present invention do not comprise amines.

Reported herein are solid oral pharmaceutical compositions consisting essentially of linaclotide and a cation.

“Linaclotide,” as used herein, refers to a polypeptide having the chemical name L-cysteinyl-L-cysteinyl-L-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonyl-glycyl-L-cysteinyl-L-tyrosine, cyclic (1-6), (2-10), (5-13)-tris (disulphide).

“Cation,” as used herein, is selected from the group comprising NH4+, K+, Na+, Li+, Fe2+, Mn2+, Ni2+, Ba2+, Zn2+, Mg2+, Cu2+, Fe3+, Sn2 +, Co2+, Co3+, Cr3+, Al3+, Cu3+, and choline.  The cation may be in the form of a salt with an appropriate counter ion, for example, ammonium chloride, ammonium lactate, ammonium sulphate, ammonium acetate, ammonium phosphate, ammonium carbonate, ferrous sulphate, ferrous chloride, ferrous oxide, ferric sulphate, ferric chloride, ferric oxide, lithium hydroxide, barium chloride, barium sulphate, copper sulphate, copper chloride, or 1,2-dimyristoyl-SN-glycero-3-phosphocholine.  These salts may be formed during the manufacturing of the pharmaceutical composition, for example, ammonium chloride may be formed by the reaction of hydrochloric acid and ammonia.  The amount of cation used in the pharmaceutical compositions of the present invention ranges from about 0.01% w/w to about 20% w/w of the pharmaceutical composition, in particular from 0.05% w/w to 5% w/w of the pharmaceutical composition.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and a cation, wherein the cation is selected from the group consisting of NH4+, K+, Na+, Li+, Fe2+, Mn2+, Ni2+, Ba2+, Zn2+, Mg2+, Cu2+, Fe3+, Sn2 +, Co2+, Co3+, Cr3+, Al3+, Cu3+, choline, and mixtures thereof.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and a cation, wherein the cation is NH4+.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and a cation, wherein the composition does not comprise an amine.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and a cation, wherein the pharmaceutical composition further comprises pharmaceutically acceptable excipients selected from the group comprising fillers, binders, surfactants, anti-oxidants, pH-adjusting agents, disintegrants, lubricants, and mixtures thereof.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and a cation, wherein the pharmaceutical composition may be in the form of pellets, granules, capsules, tablets, or mini-tablets.  In particular, the pharmaceutical composition is in the fo...