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Stable secukinumab injection and preparation method thereof

A technology of secukinumab and injections, which is applied in the direction of chemical instruments and methods, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of few types of drugs, poor substitutability, and lack of other stabilizers. OK, etc.

Inactive Publication Date: 2019-08-30
TONGHUA DONGBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a biological antibody drug, the stability of antibody preparations is a key item for drug quality control. The applicant found in the previous search that the original drug (CN201580076632.9) preferred trehalose as a stabilizer for preparation, and other stabilizers are not yet determined. , resulting in very few international and domestic drug varieties and poor substitutability

Method used

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  • Stable secukinumab injection and preparation method thereof
  • Stable secukinumab injection and preparation method thereof
  • Stable secukinumab injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: Buffer

[0043] The effect of buffer type (phosphate, histidine, citrate) was evaluated in prefilled syringes.

[0044] Prescription 1: secukinumab 150mg / ml, sodium dihydrogen phosphate and disodium hydrogen phosphate 20mmol / L, methionine 5mmol / L, trehalose 200mmol / L, polysorbate 80 0.02%, pH5.8;

[0045] Prescription 2: secukinumab 150mg / ml, histidine and histidine hydrochloride 20mmol / L, methionine 5mmol / L, trehalose 200mmol / L, polysorbate 80 0.02%, pH5.8;

[0046] Prescription 3: secukinumab 150mg / ml, citric acid and sodium citrate 20mmol / L, methionine 5mmol / L, trehalose 200mmol / L, polysorbate 80 0.02%, pH5.8.

[0047]The above three groups of prescription injections were filled into prefilled syringes, and stability studies were carried out under long-term (4°C), accelerated (25°C) and high temperature (40°C) conditions to evaluate physical stability (SEC-HPLC (SEC Macromolecular protein: Chinese Pharmacopoeia 2015 general rule), visible particles measu...

experiment example 2

[0061] Experimental example 2: pH

[0062] Based on the prescription secukinumab 150mg / ml, histidine and histidine hydrochloride 20mmol / L, methionine 5mmol / L, trehalose 200mmol / L, polysorbate 80 0.02%, adjust the pH respectively To 4.5, 5.0, 5.5, 5.8, 6.0, 6.5, 7.0, to investigate the effect of different pH on the stability of secukinumab. The samples were stored under high temperature conditions for 4 weeks, and the stability of secukinumab was evaluated by SEC-HPLC and CEX-HPLC. It was determined from SEC-HPLC, CEX-HPLC that protein aggregation and hydrolysis were minimal around pH 6.0.

experiment example 3

[0063] Experimental Example 3: Stabilizer

[0064] Initial formulation development for an injectable dosage form aimed to evaluate the effect of different stabilizers on the formation of secukinumab soluble and insoluble aggregates (SEC - Effect of HPLC, DLS, Visible Particles and Insoluble Particles by Light Obscuration), Chemical Stability (CEX-HPLC). Stabilizers are selected from sorbitol, xylitol and trehalose, and the prescription is as follows:

[0065] Prescription 1: secukinumab 150mg / ml, histidine and histidine hydrochloride 20mmol / L, methionine 5mmol / L, sorbitol 239mmol / L, polysorbate 80 0.02%, pH5.8;

[0066] Prescription 2: secukinumab 150mg / ml, histidine and histidine hydrochloride 20mmol / L, methionine 5mmol / L, xylitol 241mmol / L, xylitol 0.02%, pH5.8;

[0067] Prescription 3: secukinumab 150mg / ml, histidine and histidine hydrochloride 20mmol / L, methionine 5mmol / L, trehalose 200mmol / L, polysorbate 80 0.02%, pH5.8

[0068] According to the separate stability test...

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Abstract

The invention provides a stable secukinumab injection. The secukinumab injection comprises the following components: 50 mg / ml-250 mg / ml of secukinumab, 5-50 mmol / L of histidine and histidine hydrochloride, 5-40 mmol / L of methionine, 150 mmol / L-370 mmol / L of lower sugar alcohol, 0.01%-0.02% of polysorbate 80 and the balance of water for injection, wherein the pH of the secukinumab injection rangesfrom 5.0 to 7.0. Stability tests prove that the stable secukinumab injection is stable in quality, the stability is superior to that of commercial varieties on the market, and all indexes conform to relevant regulations of Chinese pharmacopoeia, so that the stable secukinumab injection has good application prospects.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals and preparations, and in particular relates to a stable secukinumab injection and a preparation method thereof. [0002] technical background [0003] Psoriasis is a chronic immune-mediated skin disease with approximately 125 million patients worldwide, and as many as 6.5 million patients with psoriasis in China. [0004] Secukinumab is a fully humanized monoclonal anti-IL-17A inflammatory cytokine IgG1 antibody that directly blocks the interaction of IL-17A with its receptor by binding to IL-17A, thus altering immunity and inflammation Response achieves therapeutic goals. [0005] (Active ingredient: Secukinumab, secukinumab) is the world's first blockbuster biological drug targeting IL-17A developed by Novartis, and it has been confirmed that its efficacy in the treatment of psoriasis surpasses that of traditional TNFα-targeting drugs such as Enbrel and Humira Biological agents are not curre...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K39/395A61K47/18A61K47/26A61P17/06
CPCA61K39/3955A61K9/08A61K9/0019A61K47/183A61K47/26A61P17/06C07K16/244A61K2039/545
Inventor 王德朋魏姗姗范馨丹张忠雨张楠冷春生常晓慧
Owner TONGHUA DONGBAO PHARMA
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