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Fludarabine phosphate lyophilized preparation for injection and preparation method thereof

A technology of fludarabine phosphate and freeze-dried preparations, applied in the field of medicine, can solve the problems of complex freeze-drying process design, difficult to precisely control, harsh conditions, etc., and achieves convenient transportation, low water content and good stability. Effect

Active Publication Date: 2012-07-11
CISEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, the patent CN 101947208 A provides a fludarabine phosphate composition for injection and its preparation method, but the design of the freeze-drying process in this method is complicated and the conditions are harsh, especially the pre-frozen first In the first stage, the temperature is controlled at -11°C to -13°C and kept for 60 to 90 minutes. This process is not easy to control accurately, and at this stage, the phenomenon of prefreezing liquid is prone to or has already occurred, and the above effect cannot be achieved.

Method used

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  • Fludarabine phosphate lyophilized preparation for injection and preparation method thereof
  • Fludarabine phosphate lyophilized preparation for injection and preparation method thereof
  • Fludarabine phosphate lyophilized preparation for injection and preparation method thereof

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Experimental program
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Effect test

Embodiment 1～4

[0017] prescription

[0018] Preparation method: Weigh the recipe amount of lactose, add 1200ml of water for injection, stir to dissolve completely, add activated carbon according to 0.5%, 1.0%, 1.5%, 2.0% (g / L), respectively, at 20 ℃, 25 ℃, 30 ℃, Stir and adsorb at 35°C for 10min, 15min, 20min, 25min, add fludarabine phosphate, adjust the pH of the solution to 7.0, 7.5, 8.0, 8.5 with 0.1mol / L sodium hydroxide solution or 0.1mol / L phosphoric acid solution Continue stirring to dissolve and mix evenly. The obtained solution is filtered through 0.45 μm and 0.22 μm microporous membranes in turn. The obtained semi-finished filtrate is checked and then filled, and the semi-finished product filled and half-sealed is placed in a freeze-drying cabinet. Pre-freeze on the inner partition, and make the semi-finished product reach the pre-freezing temperature within 0.5, 0.7, 0.8, 1.0 hours, and the pre-freezing temperature is -35°C, -37°C, -42°C, -45°C. After the temperature is maintai...

Embodiment 5～8

[0020] prescription

[0021] Preparation method: Weigh the recipe amount of lactose, add 1200ml of water for injection, stir to dissolve completely, add activated carbon according to 0.5%, 1.0%, 1.5%, 2.0% (g / L), respectively, at 20 ℃, 25 ℃, 30 ℃, Stir and adsorb at 35°C for 10min, 15min, 20min, 25min, add fludarabine phosphate, adjust the pH of the solution to 7.0, 7.5, 8.0, 8.5 with 0.1mol / L sodium hydroxide solution or 0.1mol / L phosphoric acid solution Continue stirring to dissolve and mix evenly. The obtained solution is filtered through 0.45 μm and 0.22 μm microporous membranes in turn. The obtained semi-finished filtrate is checked and then filled, and the semi-finished product filled and half-sealed is placed in a freeze-drying cabinet. Pre-freeze on the inner partition, and make the semi-finished product reach the pre-freezing temperature within 0.5, 0.7, 0.8, 1.0 hours, and the pre-freezing temperature is -35°C, -37°C, -42°C, -45°C. After the temperature is maintai...

Embodiment 9～12

[0023] prescription

[0024] Preparation method: Weigh the recipe amount of lactose, add 1200ml of water for injection, stir to dissolve completely, add activated carbon according to 0.5%, 1.0%, 1.5%, 2.0% (g / L), respectively, at 20 ℃, 25 ℃, 30 ℃, Stir and adsorb at 35°C for 10min, 15min, 20min, 25min, add fludarabine phosphate, adjust the pH of the solution to 7.0, 7.5, 8.0, 8.5 with 0.1mol / L sodium hydroxide solution or 0.1mol / L phosphoric acid solution Continue stirring to dissolve and mix evenly. The obtained solution is filtered through 0.45 μm and 0.22 μm microporous membranes in turn. The obtained semi-finished filtrate is checked and then filled, and the semi-finished product filled and half-sealed is placed in a freeze-drying cabinet. Pre-freeze on the inner partition, and make the semi-finished product reach the pre-freezing temperature within 0.5, 0.7, 0.8, 1.0 hours, and the pre-freezing temperature is -35°C, -37°C, -42°C, -45°C. After the temperature is maintai...

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Abstract

The invention discloses a fludarabine phosphate lyophilized preparation for injection and a preparation method of the lyophilized preparation, belonging to the technical field of medicament. The fludarabine phosphate lyophilized preparation is mainly prepared by active component of fludarabine phosphate and excipients; and the mass ratio of the fludarabine phosphate and the excipients is 1:0.5-2.0. Compared with the prior art, the fludarabine phosphate lyophilized preparation for injection has loose texture, rapidly dissolves in water and has good re-dissolving property; the lyophilized preparation is subjected to sublimation drying in vacuum, the water content is low, the stability is good, and long-term storage and clinical use of the products are facilitated; and besides, the preparation method of the preparation is simple, the transportation is convenient, and the production cost is effectively reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a freeze-dried preparation of fludarabine phosphate for injection and a preparation method thereof. Background technique [0002] Fludarabine is an antimetabolite fluorinated purine nucleoside analog, which is highly selective for lymphocytes, it can inhibit the repair of DNA in quiescent cells and the synthesis of DNA in dividing cells, and has the ability to promote The apoptosis of these cells has shown good therapeutic effects, and is currently widely used in the treatment of various blood system diseases, especially chronic B lymphocytic leukemia. [0003] Fludarabine phosphate is developed in Germany. Due to its poor stability, special attention should be paid during research, clinical application, storage and transportation. Clinical application is in the form of freeze-dried powder injection. it is good. In the prior art, patent CN 101947208 A provides a fludarabine ph...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/7076A61P7/00
Inventor 李明丽于清路
Owner CISEN PHARMA