A kind of preparation method of bishalom

Abstract

The invention discloses a preparation method of bisalom, which is simple in operation, low in chlorine content, low in swelling rate, equivalent in phosphate binding amount to the preparation on the market in Japan, avoids amplification effect, and is especially suitable for industrial production. The specific steps are: dissolve N,N,N',N'-tetrakis(3-aminopropyl)-1,4-butanediamine in purified water, add epichlorohydrin dropwise, and control the temperature not to exceed 25°C. After the dropwise addition, heat up to 80°C, react for 9 to 10 hours, then cool down to room temperature, add the reaction residue into purified water, stir, pulverize, wash, and dry; among them, N,N,N',N'‑ The substance ratio of tetrakis(3-aminopropyl)-1,4-butanediamine to epichlorohydrin is 1:2.1-2.3.

Description

technical field [0001] The invention relates to a preparation method, in particular to a preparation method of bisalom. It belongs to the field of medical technology. Background technique [0002] The incidence rate of chronic kidney disease is as high as 10%, and it has become an invisible killer threatening human health. Hyperphosphatemia is a common complication in patients with chronic kidney disease, especially end-stage renal disease, and can be found in 80% of dialysis patients. Hyperphosphatemia is an important factor in ectopic calcification, secondary hyperparathyroidism, and renal osteodystrophy. Effective control of serum phosphorus levels is key to the prognosis of patients with chronic kidney disease. Most patients cannot achieve the control standard by controlling the phosphorus intake in the diet, so they need to use phosphorus binders to achieve the control purpose. Even when dialysis treatment is initiated in the late stages of chronic kidney disease, p...

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Problems solved by technology

[0012] Method one can obtain solid product, but, it uses toluene as solvent, and toluene belongs to the second class solvent disclosed in Chinese Pharmacopoeia, has certain toxicity, and it is recommended to limit and control its use; in this method, more expensive surfactant is used, and the production High cost; and the resulting product has high chlorine content, high swelling rate, and low phosphate binding

[0013] Method two can obtain solid product, and this product swelling rate (when being in aqueous environment equilibrium, the number of grams of solvent absorbed per gram of dry cross-linked polymer) is low, about less than 2.5, but the phosphate binding capacity of product is all low In Bisalom Japan marketed preparations (trade name: キックリン カプセル 250mg, Astellas Pharma Inc.), and the chlorine content of the resulting product is relatively high, which has a more serious amplification effect

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