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PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

IP.com Disclosure Number: IPCOM000240184D
Publication Date: 2015-Jan-09

Publishing Venue

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Abstract

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

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PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

Abstract

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

Reported herein are solid oral pharmaceutical compositions consisting essentially of linaclotide and an amine.

“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).

“Amine,” as used herein, includes amino acids, trimethylamine, and cyclohexylamine.  In particular, the amine is an amino acid.  The amino acid may be a naturally-occurring amino acid selected from the group consisting of histidine, phenylalanine, alanine, glutamic acid, aspartic acid, glutamine, leucine, methionine, asparagine, tyrosine, threonine, isoleucine, tryptophan, valine, sarcosine, lysine, serine, arginine, cysteine, glycine, proline, and mixtures thereof.  Alternatively, the amino acid may be a non-naturally occurring amino acid or amino acid derivative, such as 1-aminocyclohexane carboxylic acid, lanthionine, or theanine.  The amount of amine used ranges from 0.01% w/w to 20% w/w of the pharmaceutical composition; preferably 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 an amine, wherein the amine is selected from the group consisting of histidine, phenylalanine, alanine, glutamic acid, aspartic acid, glutamine, leucine, methionine, asparagine, tyrosine, threonine, isoleucine, tryptophan, valine, sarcosine, lysine, serine, arginine, cysteine, glycine, proline, 1-aminocyclohexane carboxylic acid, lanthionine, theanine, trimethylamine, cyclohexylamine, and mixtures thereof.

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and an amine, wherein the amine is trimethylamine.

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

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide and an amine, wherein the pharmaceutical composition further comprises pharmaceutically acceptable excipients.

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

Reported herein is a solid oral pharmaceutical composition consisting essentially of linaclotide...