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Polyethylene glycol modified rhG-CSF injection and preparation method thereof

A polyethylene glycol and injection technology, applied in the field of medicine, can solve problems such as high cost, waste of resources, unfavorable environmental protection, etc., and achieve the effects of stable properties, improved compliance and low cost

Active Publication Date: 2014-12-17
石药集团百克(山东)生物制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Neulasta is packaged in the form of a pre-filled syringe, which is costly, poor compliance with clinical medication, and causes waste of resources, which is not conducive to environmental protection

Method used

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  • Polyethylene glycol modified rhG-CSF injection and preparation method thereof
  • Polyethylene glycol modified rhG-CSF injection and preparation method thereof
  • Polyethylene glycol modified rhG-CSF injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0034] Preparation example: mPEG 20000 -Preparation of rhG-CSF stock solution

[0035] 1. mPEG 20000 -rhG-CSF crude product preparation

[0036] Contains 0.1M NaH in 10mL 2 PO 4 (pH5.0) concentration of 5mg / mL rhG-CSF solution, at 4℃, add 20kDa mPEG 7.5 times the mole number of rhG-CSF, dissolve it, add NaCNBH 3 . The reaction solution was stirred and reacted at 4°C for 16 hours, and then the pH of the reaction solution was adjusted to 3.5 with 1M HCl. Concentrate the resulting solution to get mPEG 20000 -RhG-CSF crude product.

[0037] 2. Purification

[0038] (1) Ion exchange chromatography chromatography: the mPEG obtained in preparation 1 20000 -The crude rhG-CSF is chromatographed by Macro Cap SP (diameter 300mm, height 12cm) ion exchange chromatography:

[0039] ①Sample loading: mPEG 20000 -The crude rhG-CSF is diluted to 100~200μg / mL with buffer A (pH4.0±0.5), and the sample is loaded at a flow rate of 340mL / min±10%, and the loading amount is 3mg protein / ml filler;

[0040] ②Flu...

Embodiment 1

[0046] Example 1: mPEG 20000 -rhG-CSF injection preparation

[0047] Prescription composition (specification 3.0mg (ml / piece)):

[0048] Diluent formula:

[0049] Component Dosage per liter The actual amount Sodium acetate1.36g 1.36×Yg Tween 80 40mg 40×Yg glacial acetic acid Right amount Adjust pH 3.5~4.5 Sorbitol- 5%×(batch filling count M×standard filling quantity)g Water for Injection Finally make up the volume to Y liters

[0050] Remarks: M means batch filling count.

[0051] Suppose the volume of the required stock solution is X (mL) and the volume of the preparation diluent to be added is Y (mL), then

[0052]

[0053] Y=Batch filling number M×the specification filling quantity-original liquid volume X(mL)

[0054] Preparation Process:

[0055] ①Prepare prescription amount of sodium acetate, Tween 80, glacial acetic acid, sorbitol and water for injection into diluent;

[0056] ② Take the prescribed amount of mPEG 20000 -G-CSF stock solution, diluted to the required concen...

Embodiment 2～6

[0060] Examples 2-6: Investigation of protein concentration

[0061] Refer to the prescription and preparation process of Example 1, except that the injection specifications were changed to 1, 2, 5, 8, 10 mg / mL.

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Abstract

The invention provides a polyethylene glycol modified rhG-CSF injection and a preparation method thereof. The injection is composed of mPEG20000-rhG-CSF, a stabilizing agent, an isotonic agent, a buffer with pH value of 3.5-4.5 and injection water. Per one mL of the injection contains 1-8 mg of mPEG20000-rhG-CSF, and the stabilizing agent is Tween 80. The injection is put in glass bottles or plastic bottles, and is stable in properties during transportation and storage. Therefore, the polyethylene glycol modified rhG-CSF injection is low in cost and stable in properties, and the adaptability of the injection as a clinic medicine for patients is improved.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a polyethylene glycol modified rhG-CSF injection and a preparation method thereof. Background technique [0002] Granulocyte Colony Stimulating Factor (G-CSF) is one of the colony stimulating factors that stimulate the formation of bone marrow cell colonies. It can specifically stimulate and regulate the proliferation, differentiation, survival and activation of the granulocyte system. Neutropenia caused by various reasons has potential and great application value. However, recombinant human granulocyte colony stimulating factor (rhG-CSF) has a short circulating half-life in the body, t1 / 2 is only 1.3~4.2h, and the action time It is short-lived and requires daily injections, which limits the efficacy. [0003] In 2002, the FDA approved the American Amgen company to use PEG-rhG-CSF (generic name pegfilgrastim, trade name Neulasta) to treat neutropenia. It only needs to be in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/48A61K38/19A61P7/00A61K47/26
Inventor 盖来兵窦燕峰张雪梅王龙山
Owner 石药集团百克(山东)生物制药股份有限公司