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PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

IP.com Disclosure Number: IPCOM000240186D
Publication Date: 2015-Jan-09
Document File: 9 page(s) / 55K

Publishing Venue

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Abstract

The present disclosure relates to solid oral pharmaceutical compositions of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of leucine to linaclotide is above 100:1 and the molar ratio of calcium chloride to linaclotide is above 100:1, and processes for their preparation.

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PHARMACEUTICAL COMPOSITIONS OF LINACLOTIDE

Abstract

The present disclosure relates to solid oral pharmaceutical compositions of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of leucine to linaclotide is above 100:1 and the molar ratio of calcium chloride to linaclotide is above 100:1, and processes for their preparation.

Reported herein are solid oral pharmaceutical compositions of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of leucine to linaclotide is above 100:1 and the molar ratio of calcium chloride to linaclotide is above 100:1.

“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).

“Calcium chloride,” as used herein, includes anhydrous or hydrate forms of calcium chloride.  Hydrate forms may further be a monohydrate, dihydrate, or trihydrate form.  The amount of calcium chloride used in the pharmaceutical composition of the present invention ranges from about 6% w/w to about 50% w/w of the pharmaceutical composition, in particular from more than about 6% w/w to about 30% w/w of the pharmaceutical composition.

“Leucine,” as used herein, includes L-leucine, D-leucine, or a racemic mixture thereof.  The amount of leucine used in the pharmaceutical composition of the present invention ranges from about 10% w/w to about 50% w/w of the pharmaceutical composition, in particular from more than about 10% w/w to about 30% w/w of the pharmaceutical composition.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of leucine to linaclotide is between 105:1 and 600:1 and the molar ratio of calcium chloride to linaclotide is between 105:1 and 600:1.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of leucine to linaclotide is between 105:1 and 550:1.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein the molar ratio of calcium chloride to linaclotide is between 105:1 and 300:1.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein calcium chloride is present in an amount from about 6% w/w to about 30% w/w of the pharmaceutical composition.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein leucine is present in an amount from about 10% w/w to about 30% w/w of the pharmaceutical composition.

Reported herein is a solid oral pharmaceutical composition of linaclotide comprising leucine and calcium chloride, wherein the pharmaceutical composition further comprises pharma...