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Process for the preparation of sevelamer

a technology of sevelamer and process, which is applied in the field of process for the preparation of sevelamer, can solve the problems of laborious and laborious further reaction steps, entail substantial costs at industrial level, and produce a highly congealed and viscous reaction mass

Inactive Publication Date: 2012-04-26
LAB CHIM INTERNAZ
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]It has now been found that it is possible to avoid the use of reactors to process high viscosity materials and also the use of organic solvents, starting from polyallylamine aqueous solutions, at specific concentrations.
[0031]Therefore, with the process of the invention, which involves the use of specific concentrations of initial polyallylamine, it is possible to obtain a final reaction mixture that is easy to work and filter. On the contrary, as will be shown by the comparative tests in the experimental section of the present description, greater concentrations lead to an extremely dense and congealed reaction mixture, which can only be processed in special equipment, such as the LIST reactor, or by adding organic solvents.
[0035]This last experimental solution is not necessary but can be used to facilitate obtaining a sevelamer that is easier to filter, or which can even be separated by decantation of the liquid part of the mixture.

Problems solved by technology

One of the major problems encountered during the synthesis of sevelamer is the production of a highly congealed and viscous reaction mass, which must be adequately stirred and crumbled in order to obtain a final product in solid form.
It is easily understood that this reactor is not commonly used and that its use requires specific and economically important investments, unjustified for the preparation of a single active ingredient.
It is evident that these further reaction steps are laborious and entail substantial costs at industrial level.

Method used

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  • Process for the preparation of sevelamer

Examples

Experimental program
Comparison scheme
Effect test

example 1

Sevelamer Preparation

Loads

[0041]

PAASolutionPAAPAA (molHClwashing14.0%100%allylamineepichlorohydrinepichlorohydrinHCl38.2%isopropanol(g)(g)units)(mol)(g)(mol)(g)(g)16650234441.14.6426.511.9113714630

[0042]A conventional reactor, with blade stirrer, is used. HCl is added to the polyallylamine loaded into the reactor in two batches dosed at a distance of 15 minutes. When the temperature reaches around 25° C., dosing of epichlorohydrin begins and continues for around 10 minutes. After 45 minutes, heating to 78° C.-83° C. begins and continues for 3 hours, at the end of which the product, after cooling to room temperature, is washed with isopropanol. Washing is performed by maintaining the product under stirring with isopropanol for 1 hour, then the product is centrifuged and vacuum dried at 60° C. for 3 hours, finally obtaining 2.94 kg of product in the form of a whitish solid.

example 2

Sevelamer Preparation

[0043]The same procedure as described in example 1 is followed, but isopropanol is not added and the reaction mixture is instead maintained at 20-25° C. for three hours. The final product is isolated by filtration.

Properties of the Sevelamer Obtained

[0044]

Swell index12.5   Phosphate binding capacity (mmol / g) 5.8   Chloride content (weight / weight)18.5%Epichlorohydrinnot detectable (

[0045]The analytical evaluations are performed according to methods known in the art and conventionally used for sevelamer.

example 3

Sevelamer Carbonate / Bicarbonate Preparation

[0049]1.4 kg of water is loaded into a 2 litre glass reactor. The temperature is set to 35° C. and 100 g of sevelamer hydrochloride is added in portions, stirring the mixture. A solution of 30% sodium hydroxide is then added until pH 12 is reached (around 71 g) and gaseous carbon dioxide is bubbled through. The temperature is maintained at 35-37° C. until pH 7.2 is reached. The mixture is maintained at 35° C. under stirring for 2 hours and if necessary further carbon dioxide is bubbled through until the pH is stabilized at 7.2. The suspension is filtered, the solid washed repeatedly with water to eliminate as much of the residual chlorine as possible. The solid thus obtained is dried and ground.

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Abstract

The present invention relates to a process for the preparation of sevelamer, in particular sevelamer hydrochloride and sevelamer carbonate / bicarbonate, by means of a process that allows sevelamer to be obtained with good yields and using conventional reactors, without requiring to use specific and expensive equipment.

Description

TECHNICAL BACKGROUND [0001]Sevelamer, or poly(allylamine-co-N,N′-diallyl-1,3-diamino-2-hydroxypropane), is a polymer compound having the formulawherein a+b=9; c=1; and m is variable,[0002]Sevelamer is marketed as the hydrochloride salt under the trade name Renagel® for controlling hyperphosphatemia (increase in the level of phosphates in the blood) in adult patients undergoing dialysis or hemodialysis. Recently, the sevelamer carbonate / bicarbonate salt, under the trade name Renvela®, has also been placed on the market.[0003]Different types of the synthesis of sevelamer are known, all substantially deriving from cross-linking with high molecular weight polyallylamine epichlorohydrin.[0004]Polyallylamine is a polymer compound known in the art with the CAS RN 71550-12-4 and is obtained by allylamine polymerization.[0005]One of the major problems encountered during the synthesis of sevelamer is the production of a highly congealed and viscous reaction mass, which must be adequately stir...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C08F8/30C08F8/00
CPCC08J3/24C08J2339/00C08F26/02C08F8/00C08F8/18C08F126/02C08F8/44
Inventor VILLANI, FLAVIODE ANGELIS, BRUNONARDI, ANTONIOPATERNOSTER, MARIA
Owner LAB CHIM INTERNAZ
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