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Sevelamer niacin, preparation method and application

The technology of sevelamer hydrochloride and sevelamer, which is applied in the field of biomedicine, can solve the problems of vitamin deficiency and large dosage, and achieve the effects of less dosage, less reaction impurities and simple preparation method.

Inactive Publication Date: 2013-03-27
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These sevelamer salts have a common shortcoming: the dosage is large, and the daily dosage will reach 2-3g. Due to the large dosage, it will often cause symptoms such as constipation and vitamin deficiency in the user.

Method used

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  • Sevelamer niacin, preparation method and application
  • Sevelamer niacin, preparation method and application
  • Sevelamer niacin, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of basic sevelamer

[0051] First 80mg of Sevelamer hydrochloride is dispersed in 500ml pure water, then the aqueous solution 0.04mg / ml of preparation sodium hydroxide, in the aqueous solution of Sevelamer hydrochloride, add the sodium hydroxide solution of 500ml, mixed solution is warmed up to Stir at 35°C for 30 minutes, filter, collect the filter cake, wash the filter cake 3 times with pure water, and then dry the wet cake obtained after washing at 80°C for 5 hours to obtain basic sevelamer. Sevelamer was analyzed and identified.

Embodiment 2

[0053] Analysis of Basic Sevelamer

[0054] Part of the sample obtained in the basic sevelamer obtained in Example 1 was dissolved in water, stirred, and silver nitrate solution was added to the solution, and no precipitation occurred. It shows that the chloride ions in the basic sevelamer have been completely removed.

Embodiment 3

[0056] Analysis of Basic Sevelamer

[0057] The basic sevelamer prepared in Example 1 was subjected to infrared spectroscopic analysis, and the infrared spectrometer was a Varian640 Fourier transform infrared spectrometer produced by Varian Corporation of the United States. Characterization of results: at 3380.6cm -1 At 2920.4cm -1 and 2851.4cm -1 at the peak, which is considered to be -CH 2- peak; at 1580.1cm -1 The peak at 1310.1cm is considered to be the stretching vibration peak of NH; -1 The peak is at the peak, which is considered to be the bending vibration peak of C-N; 1461.2cm -1 , 1380cm -1 at the peak, which is considered to be -CH 3 and -CH 2 - peak; 1310.1cm -1 It is considered to be the stretching vibration peak of C-O. The combination of this embodiment and the detection method of Example 2 proves that basic sevelamer has been obtained.

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Abstract

The invention provides sevelamer niacin, a preparation method and an application. The sevelamer has a structural formula I shown as follows; wherein in the structural formula I, the ratio of (a+b): c is 45: 1 to 2: 1, m represents an integer which is not the zero or negative number, each x independently represents 0 or 1, and each x can not be 0 at the same time; and the proportion of the sevelamer niacin is 2.00-2.50. The sevelamer niacin has similar therapeutic effect with sevelamer hydrochloride under the condition that the usage amount of sevelamer niacin is 50% of that of sevelamer hydrochloride.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a preparation method of nicotinic acid sevelamer and nicotinic acid sevelamer, the use of nicotinic acid sevelamer in preparing medicines for treating hyperphosphatemia, and nicotinic acid sevelamer Use of Vilamer in the preparation of medicines for lowering blood lipids. Background technique [0002] Niacin and its derivatives, such as nicotinic acid esters, can not only reduce the levels of triglycerides, very low-density lipoprotein cholesterol, low-density lipoprotein cholesterol, and lipoproteins in plasma, but also effectively increase the level of high-density lipoprotein cholesterol. Recent studies It was found that niacin and its derivatives can effectively reduce the blood phosphorus level of hemodialysis patients with hyperphosphatemia. [0003] Sevelamer salt is a new generation drug approved by the U.S. Food and Drug Administration. It is mainly used as a phosphorus binde...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F126/02C08F8/30A61K31/785A61K31/455A61P3/12A61P3/06
Inventor 王振国易崇勤任爱国托娅张峰王玉莉
Owner NEW FOUNDER HLDG DEV LLC
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