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A kind of preparation method of terlipressin and pharmaceutical composition thereof

A technology of terlipressin and acetic acid, which is applied in the field of biomedicine, can solve the problems of inability to purify terlipressin on a large scale, low purity and yield of terlipressin, and inability to meet industrial production, and achieve easy The effect of industrialized production, convenient storage and transportation, and low production cost

Active Publication Date: 2020-06-09
北京市新里程医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Terlipressin is a polypeptide that is easily degraded under conditions of acid, alkali, light, oxidation, and high temperature, and the purity and yield of terlipressin currently prepared are low, which cannot meet the requirements of industrial production. Demand, especially the inability to purify terlipressin on a large scale, restricts the application of terlipressin

Method used

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  • A kind of preparation method of terlipressin and pharmaceutical composition thereof
  • A kind of preparation method of terlipressin and pharmaceutical composition thereof
  • A kind of preparation method of terlipressin and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Step 1: Dissolve 1000 g of crude terlipressin acetate in 10 L of acetic acid aqueous solution with a mass concentration of 5%, collect the filtrate by filtration, and then dilute the acetic acid in the crude solution with water to a mass concentration of 0.45%;

[0032] Step 2: Using octadecylsilane as the stationary phase, after loading the crude product solution obtained in step 1, use disodium hydrogen phosphate-sodium dihydrogen phosphate buffer (pH6.9) containing 35% methanol as phase A , with the mass concentration of 60% methanol aqueous solution as the B phase, the flow rate is 105ml / min, the elution is 350min, the gradient is 40%B→70%B, the eluate with a purity of more than 95% is collected, and the eluate is washed with 0.22μm Membrane filtration, concentrated to a relative density of 1.05-1.08 at 25°C;

[0033] Step 3: Use octaalkylsilane bonded silica gel as the stationary phase. After loading the solution obtained in step 2, wash it with 80% methanol aqueou...

Embodiment 2

[0035] Step 1: Dissolve 100 g of terlipressin peak crude product in 1000 ml of acetic acid aqueous solution with a mass concentration of 3%, collect the filtrate by filtration, and then dilute the acetic acid in the crude product solution with water to a mass concentration of 0.45%;

[0036] Step 2: using octadecylsilane as the stationary phase, after loading the crude product solution obtained in step 1, use disodium hydrogen phosphate-sodium dihydrogen phosphate buffer (pH5.5) containing 40% methanol as phase A , with the mass concentration of 90% methanol aqueous solution as the B phase, the flow rate is 90ml / min, the elution is 40min, the gradient is 40%B→70%B, and the eluate with a purity of more than 95% is collected, and the eluate is washed with 0.22μm Membrane filtration, concentrated to a relative density of 1.05-1.08 at 25°C;

[0037] Step 3: Use octaalkylsilane bonded silica gel as the stationary phase. After loading the solution obtained in step 2, wash it with 80...

Embodiment 3

[0039] Step 1: Dissolve 50 g of crude terlipressin acetate in 500 ml of acetic acid aqueous solution with a mass concentration of 1%, collect the filtrate by filtration, and then dilute the acetic acid in the crude product solution to a mass concentration of 0.5% with water;

[0040] Step 2: Using octadecylsilane as the stationary phase, after loading the crude product solution obtained in step 1, use disodium hydrogen phosphate-sodium dihydrogen phosphate buffer (pH6.5) containing 45% methanol as phase A , with the mass concentration of 80% methanol aqueous solution as the B phase, the flow rate is 75ml / min, the elution is 25min, the gradient is 40%B→70%B, the eluate with a purity of more than 95% is collected, and the eluate is washed with 0.22μm Membrane filtration, concentration;

[0041]Step 3: Use octaalkylsilane bonded silica gel as the stationary phase. After loading the solution obtained in step 2, wash it with 80% methanol aqueous solution with a mass concentration o...

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Abstract

The invention belongs to the technical field of biological medicines, and in particular relates to a preparation method of terlipressin and a pharmaceutical composition containing the terlipressin. The preparation method adopts two different steps to prepare a liquid phase so as to obtain the terlipressin; the method, provided by the invention, for purifying the terlipressin is simple and easy tooperate; the purity of obtained terlipressin reaches 99.7% or above, and the yield can reach 60% or above. A lyophilized powder injection prepared from the composition provided by the invention is good in solubility, stability and resolubility; the lyophilized powder injection prepared from the composition is convenient to use, easy to storage and transport, simple in preparation method, suitablefor industrial production and low in production cost.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a preparation method of terlipressin and a pharmaceutical composition containing terlipressin. Background technique [0002] Terlipressin (Terlipressin, also known as thymosin acetate α1), the chemical name is N-α-triglycyl-8-lysine-vasopressin, the structural formula is as follows, and the molecular formula is C 52 h 74 N16O 15 S 2 , the relative molecular mass is 1227.37, it is a white powder. [0003] [0004] Terlipressin is a new type of artificially synthesized long-acting vasopressin preparation, which belongs to a prodrug and is inactive in itself. In vivo, the three glycines at its N-terminal are removed by the action of aminopeptidase After the acyl residue, the active lysine vasopressin is slowly "released". It is this "slow release" mechanism that allows it to maintain smooth muscle contraction for up to 10 hours after a single dose, while the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/16C07K1/04C07K1/34A61K38/095A61K9/19A61K47/26A61K47/12A61P13/12A61P7/04A61P1/16A61P7/10A61P17/02A61P9/00
CPCA61K9/0019A61K9/19A61K47/12A61K47/26A61P1/16A61P7/04A61P7/10A61P9/00A61P13/12A61P17/02C07K7/16
Inventor 宋雪萍
Owner 北京市新里程医药科技有限公司
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