Octreotide acetate injection pharmaceutical composition and octreotide acetate

A technology of octreotide acetate and injection, which is applied in the field of medicine and can solve problems such as long half-life

Active Publication Date: 2017-06-20
CHENGDU TIANTAISHAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] (2) Long half-life: the half-life of subcutaneous injection is 2 hours

Method used

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  • Octreotide acetate injection pharmaceutical composition and octreotide acetate
  • Octreotide acetate injection pharmaceutical composition and octreotide acetate
  • Octreotide acetate injection pharmaceutical composition and octreotide acetate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Embodiment 1: the preparation of octreotide acetate

[0100] 1. Synthetic peptide chain

[0101] (1) Preparation of Boc-Thr(tBu)-OCs

[0102] Take 30.3 g of Boc-Thr(tBu)-OH (FW: 275.3, 110 mmol), dissolve it in 250 ml of methanol and 250 ml of water, pH 2.5. Take another 24g of cesium carbonate (147mmol) and add 100ml of water to dissolve until clear, and slowly add the above-mentioned Boc-Thr(tBu)-OH solution under stirring, and carbon dioxide gas will be generated. The pH of the solution was 7.5. It was dissolved in water at 40-50°C and concentrated to dryness under reduced pressure to obtain 54.2 g of Boc-Thr(tBu)-OCs as a syrupy residue.

[0103] (2) Preparation of Boc-Thr(tBu)-O-resin

[0104] Get 100 grams of chloromethyl resin (100-200 mesh, 1.0mmol / g, 100mmol), soak in DMF for 30 minutes, make the resin fully swell, add step (1) gained syrupy residue 107g and DMF of 700ml, 50- React at 55°C for 48 hours.

[0105] After filtering, the resin was washed twice...

Embodiment 2

[0136] Embodiment 2: the preparation of octreotide acetate

[0137] 1. Synthetic peptide chain

[0138] With embodiment 1.

[0139] Two, disulfide bond ring formation

[0140] Dissolve 90g of the reduced octreotide crude product in 90L of water, slowly add 2M ammonia water dropwise to pH7.8 under stirring, and feed air into the solution at room temperature (the used air passes through saturated calcium hydroxide solution and 2.5M sulfuric acid in advance) solution), so that the disulfide bonds undergo a ring-forming reaction for about 24-36 hours, add glacial acetic acid to adjust the pH to 5.5, add activated carbon to stir for 30 minutes, and filter.

[0141] 3. Separation and purification

[0142] Gained whole filtrate is purified in batches through C18 column when disulfide bonds are formed into rings, mobile phase: 0.25mol / L potassium acetate: acetonitrile (7.2:2.8); Flow rate is: 800ml / min; Effluent, the detection wavelength is: 280nm; After the sample peaks are mer...

Embodiment 3

[0143] Embodiment 3: the preparation of octreotide acetate

[0144] 1. Synthetic peptide chain

[0145] With embodiment 1.

[0146] Two, disulfide bond ring formation

[0147] Dissolve 90g of reduced octreotide crude product in 90L of water, slowly add 2M ammonia water dropwise to pH7.8 under stirring, and feed air into the solution at room temperature (the used air passes through 2.5M sulfuric acid solution and saturated calcium hydroxide in advance solution), so that the disulfide bonds undergo a ring-forming reaction for about 24-36 hours, add glacial acetic acid to adjust the pH to 5.5, add activated carbon to stir for 30 minutes, and filter.

[0148] 3. Separation and purification

[0149] Gained whole filtrate is purified in batches through C18 column when disulfide bonds are formed into rings, mobile phase: 0.25mol / L potassium acetate: acetonitrile (7.2:2.8); Flow rate is: 800ml / min; Effluent, the detection wavelength is: 280nm; After the sample peaks are combined, ...

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Abstract

The invention relates to an octreotide acetate injection pharmaceutical composition and octreotide acetate. Specifically, the octreotide acetate injection pharmaceutical composition provided by the invention is prepared from octreotide acetate containing 0.1g of octreotide, 40g to 50g of mannitol, 3g to 4g of lactic acid, a proper amount of sodium hydrogen carbonate which is added until the pH (Potential of Hydrogen) is 3.7 to 4.7 and a proper amount of injection water which is added until the total amount is 1000ml and the like. The invention further relates to an octreotide acetate product and a preparation method thereof. The octreotide acetate injection pharmaceutical composition and the octreotide acetate, provided by the invention, have the excellent technical effects shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically, the invention discloses a pharmaceutical composition of octreotide acetate injection, octreotide acetate, and a preparation method of the pharmaceutical composition of octreotide acetate injection. The octreotide acetate injection pharmaceutical composition prepared by the invention and the octreotide acetate have excellent properties. Background technique [0002] Octreotide Acetate (Octreotide Acetate) is a synthetic polypeptide composed of eight amino acids, its chemical name is: D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophanyl-L- Lysyl-L-threonyl-N-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl]-L-cysteineamide ring (2→7)-disulfide bond Acetate, its English chemical name is: L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[2-hydroxy-1-(hydroxymethyl) Propyl]-, cyclic(2→7)-disulfide; [R-(R*, R*)] acetate salt, CAS: 83150...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/08A61K47/26A61K47/12A61P35/00A61P35/04A61P1/00A61P1/18A61P7/04A61P5/00C07K7/06C07K1/04C07K1/06C07K1/20
CPCA61K9/0019A61K38/08A61K47/12A61K47/26C07K7/06Y02P20/55
Inventor 余茹金春花王秀琼黄小石曾业浩王良红丁牡丹吴国庆
Owner CHENGDU TIANTAISHAN PHARMA
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