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A kind of sevelamer carbonate analogue and its preparation method and application

A technology of sevelamer carbonate and its analogs, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of high waste rate and many wastes, and achieve low carcinogen residues and excellent preparation process The effect of simplicity and environmental protection, process safety and environmental protection

Active Publication Date: 2021-08-31
江苏中天药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] In view of the above-mentioned shortcoming of the prior art, the object of the present invention is to provide a kind of sevelamer carbonate analog, for solving the problem that three wastes are many, waste product rate is higher in the synthetic process of sevelamer carbonate in the prior art , meanwhile, the present invention will also provide the preparation method of sevelamer carbonate analogue; In addition, the present invention will also provide the new application of sevelamer carbonate analogue

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  • A kind of sevelamer carbonate analogue and its preparation method and application
  • A kind of sevelamer carbonate analogue and its preparation method and application
  • A kind of sevelamer carbonate analogue and its preparation method and application

Examples

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Embodiment 1

[0051] The preparation route of sevelamer carbonate analogue is as follows:

[0052]

[0053] The preparation method of carbonic acid sevelamer analogue is: allylamine hydrochloride is prepared into allylamine carbonate earlier; Polymerization occurs under the condition of sevelamer carbonate analogues. The specific process is as follows:

[0054] Preparation of allylamine carbonate:

[0055] Dissolve 50kg of allylamine hydrochloride in 50L of water, add sodium hydroxide to adjust the pH to 10-11, then pass through the carbon dioxide system to control the pressure of 0.5-0.6kg, react at 40°C, monitor the density of the reaction solution in the middle, when the density When controlled within the range of 2.15 to 2.20 g / ml, stop the reaction to obtain an allylamine carbonate solution, observe the properties of the allylamine carbonate solution, and measure its pH and density. The specific results are shown in Table 1. Then use high-performance liquid chromatography to dete...

Embodiment 2

[0088] The preparation route of the sevelamer carbonate analog is the same as in Example 1.

[0089] The preparation method of carbonic acid sevelamer analogue is: allylamine hydrochloride is prepared into allylamine carbonate earlier; Polymerization occurs under the condition of sevelamer carbonate analogues. The specific process is as follows:

[0090] Preparation of allylamine carbonate:

[0091] Dissolve 50kg of allylamine hydrochloride in 55L of water, add sodium hydroxide to adjust the pH to 10-11, then pass through the carbon dioxide system to control the pressure of 0.5-0.6kg, react at 40°C, monitor the density of the reaction solution in the middle, when the density When controlled within the range of 2.15-2.20g / ml, stop the reaction to obtain the allylamine carbonate solution, observe the properties of the allylamine carbonate solution, measure its pH and density, and the specific results are shown in Table 6. Then use high-performance liquid chromatography to det...

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Abstract

The present invention relates to the field of pharmaceutical technology, in particular to a sevelamer carbonate analogue and its preparation method and application, wherein the preparation method of the sevelamer carbonate analogue is: firstly prepare allylamine hydrochloride into allylamine carbonate Salt; Allylamine carbonate and diallylamine-epichlorohydrin conjugates are polymerized under the conditions of a polymerization initiator to generate carbonic acid sevelamer analogues. The prepared sevelamer carbonate analogue can be used to prepare phosphate ion adsorbent. The present invention solves the problem of many wastes and high waste rate in the synthesis process of sevelamer carbonate in the prior art, and the structure of the sevelamer carbonate analog provided is similar to that of sevelamer carbonate, retaining Vilam has the property of adsorbing phosphorus, and the preparation process is simple and environmentally friendly.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a sevelamer carbonate analogue and its preparation method and application. Background technique [0002] The name of the sevelamer carbonate compound is (allylamine-co-N,N'-diallyl-1,3-diamino-2-hydroxypropane) carbonate, which is a polymer compound that cannot be absorbed by the human body , for the treatment of hyperphosphatemia after hemodialysis in patients with end-stage renal disease. Its mechanism of action is that the structural formula of sevelamer carbonate contains primary and secondary amines, and these amines exist in the form of ionization in the human gastrointestinal tract, and can combine with phosphate through the force of hydrogen bonds and ionic bonds. It can be combined with the phosphate in the intestinal tract in time to prevent it from being absorbed by the body when the patient takes it with a meal, thereby reducing the blood phosphorus concentration of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F226/02A61K31/785A61P3/00
CPCA61K31/785A61P3/00C08F226/02
Inventor 管运才汤晓雷
Owner 江苏中天药业有限公司
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