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Asparaginase freeze-dried powder injection and preparation method thereof, as well as asparaginase solution

A technology of asparaginase and freeze-dried powder injection, which is applied in freeze-dried transportation, powder transportation, pharmaceutical formulations, etc. It can solve the problems of uncertain pH value, unfavorable operation, and injection defects, etc., and achieves convenient clinical use and high production efficiency. Low cost, less irritation effect

Active Publication Date: 2013-03-13
CHANGZHOU QIANHONG BIOPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, due to the uncertain pH value of the produced 5% glucose injection, and "add 0.19mL of 5% NaHCO to every 100ml of GS (5%) 3 , to adjust the pH value of the solvent to 7.5", the solvent configuration operation is cumbersome, which is not conducive to actual operation
At the same time, we have found through actual experiments that the above-mentioned purely relying on NaHCO 3 The method of adjusting the pH value of the infusion still cannot solve the problem of the precipitation of asparaginase in the infusion
[0007] Chinese patent document CN100502944C (application number 200510102992.X) discloses an asparaginase injection, the main components of which are: 10-80 mg of asparaginase, 2-30 mmol / L of L-cysteine, 10 -30mmol / L phosphate buffer solution, 0.5-5mmol / L disodium ethylenediaminetetraacetic acid (EDTA) and 0.5%-2% sodium chloride; but the form of injection is not convenient for storage and transportation, and the composition L-cysteine ​​is unstable in nature, and the shelf life of the injection is short, so the injection of this formula has defects

Method used

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  • Asparaginase freeze-dried powder injection and preparation method thereof, as well as asparaginase solution
  • Asparaginase freeze-dried powder injection and preparation method thereof, as well as asparaginase solution
  • Asparaginase freeze-dried powder injection and preparation method thereof, as well as asparaginase solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (Example 1, asparaginase freeze-dried powder injection)

[0023] The prescription of present embodiment asparaginase lyophilized powder injection is as follows:

[0024] Asparaginase 10 million units, poloxamer 188 (F68) 4.0g, mannitol (20%w / v) 300g, sodium dihydrogen phosphate dihydrate 6.24g, 0.1mol / L NaOH aqueous solution (appropriate amount to adjust the system The pH is 7.5±0.2), water for injection is added to 2000g, and a total of 1000 tubes are made.

[0025] The preparation method of the present embodiment asparaginase freeze-dried powder injection is as follows:

[0026] Add 300 g of sodium dihydrogen phosphate dihydrate, poloxamer 188 (F68) (CAS No.: 9003-11-6), and mannitol (20% w / v) accurately weighed according to the above prescription and pre-cool to 10 After dissolving in water for injection below ℃, use 0.1mol / L NaOH to adjust the pH value of the solution to 7.3~7.5; 0.1 mol / L HCl to adjust the pH value to 7.3±0.2 (7.5 in this example); add water to ...

Embodiment 2 to Embodiment 5

[0036] (Example 2 to Example 5, asparaginase freeze-dried powder injection)

[0037] The prescriptions of the asparaginase freeze-dried powder injections of Examples 2 to 5 are shown in Table 1 below.

[0038] Table 1

[0039]

[0040] Examples 2 to 5 were prepared according to the prescriptions in the above table, and the preparation method was the same as that of the asparaginase freeze-dried powder injection in Example 1.

[0041] The freeze-dried powder injections prepared according to the prescriptions and preparation methods of Examples 2 to 5 were sequentially designated as samples S2, S3, S4, and S5.

Embodiment 6

[0042] (Example 6, asparaginase solution)

[0043] The configuration method of the asparaginase lysate of the present embodiment is as follows:

[0044] First, accurately weigh 6.24 g of sodium dihydrogen phosphate dihydrate and 4.0 g of surfactant poloxamer 188 (F68); add 300 g of the above accurately weighed sodium dihydrogen phosphate dihydrate and poloxamer 188 (F68) After dissolving in water for injection, use 0.1mol / L NaOH solution to adjust the pH value of the solution to 7.1-7.5 (7.5 in this example); then add water for injection until the total weight of the solution is 5000g, and use 0.22 Sterilize by filtration with a microporous membrane; divide the filtrate into ampoules according to 5.0 g per bottle, stopper and cap, and label to obtain 1000 special solvents, store at room temperature, and use it as sample S6.

[0045] The buffer system of the asparaginase lysate in this embodiment is composed of disodium hydrogen phosphate and sodium dihydrogen phosphate, wher...

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Abstract

The invention discloses an asparaginase freeze-dried powder injection. The injection comprises asparaginase, a buffering agent, a surfactant, medical auxiliary materials and 5% of injection water which is used as a solvent in a preparing process and less than the addition finally, wherein the surfactant is a nonionic surfactant; and the buffering agent and the nonionic surfactant are added into the formula, so that the situation that tiny visible particles exceed standard is prevented when the asparaginase is dissolved and transferred into an injection. The invention also discloses a dedicated solution for dissolving the asparaginase, wherein the solution solvent is the injection water, and the solute comprises the buffering agent and the surfactant. On the premise of not changing the conventional formula of the freeze-dried powder injection, when the freeze-dried powder is dissolved in the solution, and is transferred into sodium chloride or a glucose injection, the situation that tiny visible particles exceed standard is prevented, so that the stimulation to human bodies is reduced in use, and the clinical administration safety is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried powder injection of asparaginase and a preparation method thereof, and a solvent used for dissolving asparaginase. Background technique [0002] Asparaginase (also known as L-asparaginase, asparaginase, asparaginase, etc.) is a drug that selectively inhibits tumor cells, especially for acute lymphoblastic leukemia (ALL) The curative effect is the best, and it also has a certain effect on acute myeloid leukemia, acute monocytic leukemia, and malignant lymphoma. [0003] Asparaginase (hereinafter referred to as L-ASP) can hydrolyze asparagine in serum into aspartic acid and ammonia, and asparagine is an amino acid necessary for cell synthesis of protein and proliferation. Normal cells have their own synthesis gate However, tumor cells such as acute leukemia do not have this function; therefore, when L-ASP is used to rapidly lack asparagine, the tumor cells...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/44A61K9/19A61K38/50A61K47/10A61K47/34A61P35/02A61P35/00A61K47/14A61K47/26
Inventor 杭长标刘军
Owner CHANGZHOU QIANHONG BIOPHARMA
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