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Process for producing medicament with uterine contraction effect

A technology of carbetocin and amino resin, which is applied in the direction of drug combination, bulk chemical production, cyclic peptide composition, etc., and can solve the problems of inability to freeze and poor stability

Inactive Publication Date: 2011-08-10
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has poor stability and can only be stored in the refrigerator at a temperature of 2°C to 8°C, and cannot be frozen.

Method used

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  • Process for producing medicament with uterine contraction effect
  • Process for producing medicament with uterine contraction effect
  • Process for producing medicament with uterine contraction effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1: Preparation of Fmoc-Gly-resin

[0062] Add 100.00g of Fmoc-RinkAmide MBHA resin into the reaction column, and the substitution degree of this resin is 1.0mmol / g. Add 500ml DMF for swelling, then add DCM500ml / time for washing 3 times, then add DMF500ml / time for washing 3 times. Add 500ml of the prepared 50% piperidine / DMF solution into the glass reaction column, stir and react for 30min, remove the reaction solution, add DMF500ml / time for washing 6 times. The feeding amount of protected amino acid and condensation reagent is 3 times equivalent. Weigh Fmoc-Gly-OH89.19g and TBTU96.32g, HOBt40.54g, DIEA38.77g, add DMF and stir to dissolve, stir evenly and add to the glass reaction column, The reaction was stirred for 24 hours. The KaiserTest monitors the extent of the reaction until it is complete. After the reaction was completed, the reaction solution was removed, washed 3 times with DMF500ml / time, and then washed 3 times with DCM500ml / time, drained, pour...

Embodiment 2

[0063] Embodiment 2: Preparation of Fmoc-Leu-Gly-resin

[0064] Add 104.42g of Fmoc-Gly-resin to the reaction column, add DCM500ml / time for washing 3 times, then add DMF500ml / time for washing 3 times. Add 500ml of the prepared 50% piperidine / DMF solution into the glass reaction column, stir for 30min, remove the reaction solution, add DMF500ml / time for washing 6 times. Weigh and collect Fmoc-Leu-OH 94.00g, TBTU85.4lg, HOBt35.94g, DIEA34.38g, add DMF and stir to dissolve. After complete dissolution, the prepared amino acid coupling solution was added to the reaction column, and stirred for 3 hours. Samples were taken and washed 6 times with DMF, and the reaction degree was monitored by Kaiser Test until the reaction was completed. The reaction solution was removed and washed 6 times with DMF500ml / time.

Embodiment 3

[0065] Embodiment 3: Preparation of Fmoc-Pro-Leu-Gly-resin

[0066] Add 500ml of the prepared 50% piperidine / DMF solution into the glass reaction column, stir for 30mm, remove the reaction solution, add DMF500ml / time for washing 6 times. Weigh 89.75g of Fmoc-Pro-OH, 85.41g of TBTU, 35.94g of HOBt, and 34.38g of DIEA, add DMF and stir to dissolve. After complete dissolution, the prepared amino acid coupling solution was added to the reaction column, and stirred for 3 hours. Samples were taken, washed 6 times with DMF, and KaiserTest was used to monitor the degree of reaction until the reaction was completed. The reaction solution was removed and washed 6 times with DMF500ml / time.

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Abstract

The invention relates to a process for producing a uterine contraction medicament which uses carbetocin as a main drug. The process comprises a synthesis process and a preparation process. The technical scheme of solid-phase synthesis comprises the following steps of: 1, carrying out deprotection by using amino resin as a vector; 2, connecting carboxyl of Fmoc-Gly-OH with amino of the resin to obtain Fmoc-Gly-amino resin; 3, carrying out solid-phase synthesis sequentially to form sequence residual protection amino acid; 4, removing side-chain protecting groups of cysteine; 5, connecting brombutyl acid onto sulfydryl of cysteine; 6, removing terminal amino Fmoc protection; 7, carrying out solid-phase cyclization; 8, cutting to obtain carbetocin crude peptides; and 9, refining to obtain a carbetocin pure product. The process has the characteristics of simple reaction operation, easy post treatment, high yield, low cost and the like. The invention also discloses a process for preparing a carbetocin freeze-dried powder injection which mainly comprises the following material compositions: carbetocin serving as the main drug, an excipient, a pH (potential of hydrogen) value regulator and water for injection. The powder injection has the advantages of high dispersion degree, high stability and the like.

Description

Technical field: [0001] The invention relates to a production process of a uterine contraction drug with carbetocin as the main agent, in particular to a solid-phase synthesis method of carbetocin and a freeze-dried powder injection preparation process. Background technique: [0002] Carbetocin is a synthetic long-acting nonapeptide analogue of oxytocin with agonist properties. A single dose intravenously may be administered immediately after cesarean section under epidural or spinal anesthesia to prevent uterine hypotonia and postpartum hemorrhage. [0003] The clinical and pharmacological properties of carbetocin are similar to those of naturally occurring oxytocin. Like oxytocin, carbetocin binds to the oxytocin receptors of uterine smooth muscle, causing rhythmic contractions of the uterus, increasing its frequency and increasing uterine tension on the basis of the original contractions. Oxytocin receptor levels in the uterus are low in the non-pregnant state, increase...

Claims

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Application Information

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IPC IPC(8): C07K7/56A61K38/12A61P15/04
CPCY02P20/55
Inventor 李新宇姚志勇支钦
Owner SHENZHEN JYMED TECH
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