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Cladribine preparation administrated by injection and preparation method thereof

A technology for cladribine and preparations, which is applied in the field of preparations administered by injection and its preparation, and can solve problems such as compound instability

Inactive Publication Date: 2010-06-30
TIANJIN PACIFIC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, one disadvantage of cladribine is that its oral bioavailability is only 50%, because the compound is unstable in acidic environment and can be degraded by bacterial nucleotide phosphatase, so it is made into injection form

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Take 3g of cladribine, put it in a container, add 0.1g of solubilizing agent polyvinylpyrrolidone, 80ml of water for injection, add 0.2g of sodium hydroxide, stir to dissolve, add 1mol / L of citric acid to adjust the pH to 7-9.0, Add 28g of mannitol, stir to dissolve, and add water to 100ml. Add 0.5g of activated carbon, stir at 30°C for 20 minutes, decarburize, filter and sterilize with a microporous membrane, divide the filtrate into 1ml tubes, pre-freeze for 2 hours, and dry under reduced pressure for 12 hours until After the temperature of the sample reached room temperature, it was dried for another 5 hours to obtain a white loose block, which was sealed to obtain cladribine freeze-dried powder injection.

Embodiment 2

[0032] Take 50g of cladribine, put it in a container, add 2g of PEG-6000, 180ml of water for injection, stir to dissolve, adjust the pH to 5.0-9.0 with 1mol / L hydrochloric acid or sodium hydroxide, add 80g of mannitol and 20g of sorbitol , stir to dissolve, add water to 2000ml. Add 0.5g of activated carbon, stir at 30°C for 20 minutes, decarburize, filter and sterilize with a microporous membrane, divide the filtrate into 2ml tubes, pre-freeze for 2 hours, and dry under reduced pressure for 18 hours until After the temperature of the sample reached room temperature, it was dried for another 5 hours to obtain a white loose block, which was sealed to obtain cladribine freeze-dried powder injection.

Embodiment 3

[0034] Take 10g of cladribine and 0.3g of xylitol, add it to 440ml of water for injection in which 5g of sodium lauryl sulfate has been dissolved, add 2g of sodium thiosulfate and stir to dissolve, add sodium bicarbonate to adjust the pH to 5.5-8.5, add 0.5g activated carbon, stirred and adsorbed at room temperature for 30 minutes, removed carbon, added water to 500ml, finely filtered, filled with 5ml each, and sterilized to obtain cladribine injection.

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PUM

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Abstract

The invention relates to a cladribine preparation administrated by injection and a preparation method thereof. The preparation is characterized by consisting of cladribine, a water-soluble filler, a pH regulator, water for injection and an osmotic pressure regulator, wherein the preparation contains 0.01 to 50 weight percent of cladribine and the balance of pharmaceutical adjuvant or water. The cladribine preparation administrated by the injection of the invention has the advantages of good stability and high bioavailability and satisfies need for injection medicaments required by the treatment of clinical acute and chronic granulocytic leukemia.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically relates to an injection-administered preparation containing cladribine as an active ingredient and a preparation method thereof. Background technique [0002] Cladribine is an adenosine deoxygenase inhibitor developed by Ortho Biotec, a subsidiary of Johnson & Johnson, and the Scripps Research Institute of the United States. Developed for the treatment of a variety of tumors, including acute myelogenous leukemia, chronic lymphocytic leukemia, chronic myelogenous leukemia, cutaneous T-cell lymphoma, hairy cell leukemia, and non-Hodgkin's lymphoma; and first launched in February 1993 Launched in the United States, followed by Canada and Sweden in the same year, under the trade name Leustatin. In the 1960s, cladribine was first used as an intermediate in the synthesis of 2-deoxynucleosides. It was not until 1984 that its potential efficacy in treating lymphoma was re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/7076A61P35/00A61P35/02
Inventor 宋德成
Owner TIANJIN PACIFIC PHARMA
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