A method for purifying terlipressin

A technology of terlipressin and pure product, applied in the field of polypeptide drugs, can solve the problem of low yield of terlipressin, ineffective separation of terlipressin, and poor purity of terlipressin. Advanced problems, to achieve the effect of low cost and high yield

Active Publication Date: 2016-10-05
ADLAI NORTYE BIOPHARMA CO LTD
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

The technical problem to be solved in the present invention is: select a kind of purification method of terlipressin, solve (1) the purity of terlipressin finished product is not high, (2) the yield of terlipressin finished product is not high, ( 3) Terlipressin and impurities [βAsp 8 ]-Terlipressin cannot be effectively separated

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  • A method for purifying terlipressin
  • A method for purifying terlipressin
  • A method for purifying terlipressin

Examples

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Embodiment 1

[0088] Solid Phase Synthesis of Terlipressin: Synthesis of Terlipressin on a 10 mmol Scale

[0089] (1) Deprotection of peptide resin: 13.89 g of Rink amide AM resin (substitution degree: 0.72 mmol / g) was added to the solid-phase reaction column, washed once with DMF, and the resin was swollen with DCM for 30 min. The deprotection solution composed of 1:4 piperidine and DMF was reacted for 5 min, washed once with DMF, and reacted with a deprotection solution composed of piperidine and DMF with a volume ratio of 1:4 for 10 min, and washed 6 times with DMF.

[0090] (2) Coupling: 8.92 g Fmoc-Gly-OH (30 mmol) and 4.05 g HOBt (30 mmol) were dissolved in the solvent DMF, the ice bath cooling temperature was 0-10 ℃, and 5 mL DIC (30 mmol) was added, After activating for 5 minutes, add it to the reaction column to react with the deprotected resin. After reacting for 2 hours at 25-35 ℃, use the ninhydrin method to detect and judge the reaction end point. If the resin is colorless and ...

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Abstract

The invention relates to a purifying method for terlipressin. The method is characterized by comprising the following steps: step 1, dissolving a crude terlipressin product with water and adjusting a pH value to 3 to 4; step 2, flushing a C18 reversed-phase filled column by using an ion pair mobile phase A containing surfactant; step 3, loading a solution obtained in the step 1 into a C18 reversed-phase filling material; step 4, carrying out gradient procedures, wherein the initial-state mobile phase B of an elution gradient is 5% which is maintained for 5 min, then the proportion of the mobile phase B is increased to 30% within 60 min, and a part of target peak elution fraction is collected; and step 5, carrying out nanofiltration membrane desalination and then freeze drying so as to obtain pure terlipressin.

Description

technical field [0001] The invention relates to a purification method of polypeptide drug-terlipressin, which is a purification method with long-acting vasopressin analogs. Background technique [0002] Terlipressin, English name: Terlipressin, is a cyclic polypeptide with the following structural formula: [0003] [0004] The chemical formula is as follows: [0005] . [0006] Terlipressin is a synthetic triglycine-lysine-vasopressin, which is a synthetic vasopressin analogue. It is a prodrug, inactive in itself, and acts on aminopeptidase in vivo. After removing the three glycyl residues at its N-terminus, the active lysine vasopressin is slowly "released", so terlipressin is equivalent to a lysine vasopressin that can release lysine at a steady rate Vegetable storage. The main function of terlipressin is to contract visceral vascular smooth muscle and reduce visceral blood flow (such as reducing the blood flow of mesentery, spleen, uterus, etc.), thereby reducin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/16C07K1/20
Inventor 路杨杨东晖周俊周亮
Owner ADLAI NORTYE BIOPHARMA CO LTD
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