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PHARMACEUTICAL COMPOSITION COMPRISING SEVELAMER

IP.com Disclosure Number: IPCOM000179472D
Publication Date: 2009-Feb-13
Document File: 6 page(s) / 75K

Publishing Venue

The IP.com Prior Art Database

Abstract

A pharmaceutical composition comprising sevelamer or pharmaceutically acceptable salt thereof has been prepared by using a melt granulation technique.

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PHARMACEUTICAL COMPOSITION COMPRISING SEVELAMER

Abstract

A pharmaceutical composition comprising sevelamer or pharmaceutically acceptable salt thereof has been prepared by using a melt granulation technique.

Sevelamer is an aliphatic amine polymer indicated for the control of serum level of phosphate in chronic kidney disease.  It decreases serum level of phosphate by binding phosphate in the gastrointestinal tract, without concomitantly increasing the absorption of any clinically undesirable material, particularly calcium or aluminium.  Sevelamer is known chemically as poly (allylamine-co-N, N’-diallyl-1, 3-diamino-2-hydroxypropane).

Sevelamer is known to be very hygroscopic and swells when in contact with water.  Such swelling of the sevelamer complicates formulating the active pharmaceutical ingredient in a pharmaceutical composition.  Moreover, compressibility is apparently dependent on the degree of hydration, adding water to sevelamer results in a swollen material and this swollen material is impossible to compress into the tablets.

A pharmaceutical composition comprising sevelamer or pharmaceutically acceptable salt thereof has been prepared by using melt granulation technique. This technique overcomes the problem of swelling of active ingredient by avoiding the use of aqueous solvents.  Processing time required for melt granulation is shorter, as it does not require solvent removal or drying phase.  This technique is beneficial for high-dose active ingredients such as sevelamer as it requires low quantities of excipients enabling smaller dosage forms, which could lead to improved patient compliance.

An example a pharmaceutical composition mentioned above comprises:

i.       less than 80% w/w of sevelamer;

ii.       about 2 to 15% w/w of meltable binder;

iii.            about 1 to 10% w/w of disintegrant; and

iv.           about 5 to 25% w/w of binder;

Another example of a pharmaceutical composition mentioned above comprise:

i.       about 50 to 75% w/w of sevelamer;

ii.       about 2 to 15% w/w of polyethylene glycol;

iii.      about 1 to 10% w/w of disintegrant; and

iv.      about 5 to 25% w/w of binder;

The pharmaceutical compositions disclosed above can be used for the control of serum level of phosphate in chronic kidney disease.

The term “sevelamer”, as used herein, includes hydrated or anhydrate form of sevelamer.  The pharmaceutically acceptable salts thereof include hydrochloride, carbonate, hydrobromide, phosphate, sulfate, and the like.

The term “pharmaceutical composition”, as used herein, includes solid dosage forms such as tablet, capsule, pill and the like.  The pharmaceutical composition comprises sevelamer less than 80% by weight of composition.  In particular, the composition comprises sevelamer about 40 to 75% by weight of composition, more particularl...