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Crosslinked polyallylamine or acid addition salt thereof, and use thereof for medical purposes

An acid addition salt, polyallylamine technology, applied in the field of cross-linked polyallylamine or its acid addition salt and its medicinal uses, can solve the problems of low swelling degree, no disclosure of phosphoric acid adsorption capacity, etc., and achieves alleviation of constipation , the effect of high phosphoric acid selectivity

Inactive Publication Date: 2010-03-31
TORAY IND INC
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the method described in Patent Document 5 discloses a water-absorbing polymer, and does not disclose a polymer having a low swelling degree while exhibiting phosphoric acid adsorption capacity in a living body.

Method used

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  • Crosslinked polyallylamine or acid addition salt thereof, and use thereof for medical purposes
  • Crosslinked polyallylamine or acid addition salt thereof, and use thereof for medical purposes
  • Crosslinked polyallylamine or acid addition salt thereof, and use thereof for medical purposes

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Embodiment

[0092] The present invention will be described in more detail based on the following examples, but the present invention is not limited to these examples.

reference example 1

[0093] (Reference Example 1) Synthesis of Allyl Ammonium Dihydrogen Phosphate

[0094] In a three-neck round bottom flask equipped with a mechanical stirrer and a thermometer, 46.1 g (0.40 mol) of phosphoric acid (85%) and 500 mL of ethanol were added, and 30.0 mL (0.40 mol) of allylamine was added under ice cooling. After stirring at room temperature for 30 minutes, the precipitated white crystals were filtered and washed well with ethanol. By drying under reduced pressure at 60°C, 59.6 g of allyl ammonium dihydrogenphosphate was obtained.

reference example 2

[0095] (Reference Example 2) Synthesis of N, N'-diallyl-1,3-diaminopropane and its diphosphate

[0096] 38.0 mL (0.40 mol) of 1,3-dichloropropane and 300 mL (4.00 mol) of allylamine were added to the flask, and heated and stirred at an internal temperature of 50-52° C. for 16 hours under an argon atmosphere. Approximately half of the excess allylamine was distilled off under reduced pressure, and an aqueous potassium hydroxide solution (prepared by dissolving 48 g of potassium hydroxide in 144 g of water) was added. The precipitated salt was removed by filtration, and the filtrate was further concentrated under pressure to about half the volume. Extraction was carried out with diethyl ether, and the organic layer was dried over sodium sulfate and concentrated under reduced pressure to obtain an oily crude product. The crude product was distilled under reduced pressure (42 to 44°C / 0.3 kPa) to obtain 38.4 g of N,N'-diallyl-1,3-diaminopropane. Add 15.0 g (130 mmol) of phosphori...

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Abstract

Disclosed is a crosslinked polyallylamine or an acid addition salt thereof which has both of high phosphoric acid adsorption ability and a low degree of swelling. Also disclosed is use of the crosslinked polyallylamine or the acid addition salt thereof for medical purposes. Specifically disclosed is a crosslinked polyallylamine or an acid addition salt thereof which is produced by copolymerizing allylammonium dihydrogen phosphate and an acid addition salt of N,N'-diallyl-1,3-diaminopropane in an amount of 5 to 25 mol% relative to the amount of allylammonium dihydrogen phosphate, and which hasa phosphoric acid adsorption amount of 2.7 to 5.0 mmol / g and a degree of swelling of 2.0 to 5.0. The crosslinked polyallylamine or the acid addition salt thereof is useful as a therapeutic or prophylactic agent for hyperphosphatemia or the like.

Description

technical field [0001] The present invention relates to cross-linked polyallylamine or its acid addition salt and its medical application. Background technique [0002] Patients with renal impairment often suffer from hyperphosphatemia due to decreased phosphorus excretion. Hyperphosphatemia leads to severe disturbance of calcium and phosphorus metabolism, resulting in renal osteodystrophy caused by decrease of serum calcium, promotion of PTH production and secretion, ectopic calcification and inhibition of vitamin D activation. Even if the patient is transferred to dialysis therapy due to renal failure, as long as the normality of phosphorus cannot be maintained, the above-mentioned condition will continue. Therefore, the treatment of hyperphosphatemia is essential for patients with renal failure on dialysis or not. Currently, hyperphosphatemia is treated by diet therapy or drug therapy using oral phosphorus adsorbents. However, it is generally accepted that dietary ther...

Claims

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Application Information

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IPC IPC(8): C08F230/02A61K31/785A61P3/12
CPCA61K31/785C08F226/02A61P3/12A61P7/00
Inventor 井上淳须山和晴皆神贤宫本美津子板场翔一
Owner TORAY IND INC
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