Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Cladribine injection and preparation method thereof

A technology of injection and phosphate solution, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the unstable state of raw materials, the growth of impurities in injections, and the increase in operating costs and other issues to achieve the effect of increasing market share, stabilizing drug efficacy, and improving stability

Inactive Publication Date: 2019-01-22
瀚晖制药有限公司
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The common drug type of cladribine is injection, which is a colorless or almost colorless clear liquid. During the storage of the injection, the state of the raw material drug is likely to be unstable, and it is prone to decomposition that affects the efficacy of the drug itself. Storage conditions with a slightly higher temperature will also cause some impurities in the injection to grow, which will also have an adverse effect on the efficacy of the drug. In view of the above problems, it is necessary to store cladribine injection under relatively harsh conditions. It also increases the operating cost of storage, which is not economical and environmentally friendly

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cladribine injection and preparation method thereof
  • Cladribine injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation process of cladribine injection follows the steps below:

[0043] 1. Prepare a 0.01mol / L disodium hydrogen phosphate solution: anhydrous disodium hydrogen phosphate is dissolved in water for injection to a constant volume, and the pH is adjusted to 7 with phosphoric acid;

[0044] 2. Sodium chloride and cladribine are mixed at a mass ratio of 9:1, dissolved in 0.01mol / L disodium hydrogen phosphate solution, and the pH value of the solution is detected, and the dissolution temperature is controlled at 20°C;

[0045] 3. Check that the pH is greater than 7, adjust the pH to 7 with phosphoric acid solution, then add 0.01mol / L disodium hydrogen phosphate solution to continue to adjust the pH to 7;

[0046] 4. Check that the pH is less than 7, add 0.01mol / L disodium hydrogen phosphate solution and continue to adjust the pH to 7;

[0047] 5. Constant volume, packaging, testing, sterilization, sealing, and storage in a cool place (not exceeding 20°C) with shadi...

Embodiment 2

[0055] The preparation process of cladribine injection follows the steps below:

[0056] 1. Prepare 0.015mol / L disodium hydrogen phosphate solution: anhydrous disodium hydrogen phosphate is dissolved in water for injection to a constant volume, and the pH is adjusted to 8 with phosphoric acid;

[0057] 2. Dissolve calcium chloride with 0.015mol / L disodium hydrogen phosphate solution and stir, then add cladribine and continue stirring. Calcium chloride and cladribine are mixed in a mass ratio of 10:1, and the pH of the solution is detected value, the temperature of dissolution is controlled at 25°C;

[0058] 3. Check that the pH is greater than 7, adjust the pH to 7 with 1.5wt% phosphoric acid solution, and then add 0.015mol / L disodium hydrogen phosphate solution to continue to adjust the pH to 8;

[0059] 4. Check that the pH is less than 7, add 0.015mol / L disodium hydrogen phosphate solution and continue to adjust the pH to 8;

[0060] 5. Constant volume, packaging, testing...

Embodiment 3

[0062] The preparation process of cladribine injection follows the steps below:

[0063] 1. Prepare a 0.005mol / L calcium hydrogen phosphate solution: anhydrous calcium hydrogen phosphate is dissolved in water for injection to a constant volume, and the pH is adjusted to 7.3 with phosphoric acid;

[0064] 2. Dissolve sodium chloride with 0.005mol / L calcium hydrogen phosphate solution and stir, then add cladribine and continue stirring. Sodium chloride and cladribine are mixed in a mass ratio of 8:1, and the pH value of the solution is detected , the dissolution temperature is controlled at 30°C;

[0065] 3. Check that the pH is greater than 7, adjust the pH to 7 with 0.5wt% phosphoric acid solution, and then add 0.005mol / L calcium hydrogen phosphate solution to continue to adjust the pH to above 7.0;

[0066] 4. Check that the pH is less than 7, add 0.005mol / L calcium hydrogen phosphate solution and continue to adjust the pH to above 7.0;

[0067] 5. Constant volume, packagin...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a cladribine injection and a preparation method thereof. The preparation method comprises the following steps of: (A) dissolving a phosphate in water, and adjusting the pH to between 7 and 8 by a pH adjuster to obtain a phosphate solution; (B) dissolving a mixed powder of cladribine and a homogenizer with stirring by the phosphate solution, and adjusting the pH to between 7and 8, so as to obtain the injection. The method improves the stability of the drug substance, the injection is not easy to hydrolyze, through detection of impurities during a storage process, the impurities do not increase, the efficacy and other quality of the injection are more guaranteed, and therefore the preparation method is worthy of widespread promotion and application.

Description

technical field [0001] The invention relates to the field of preparation of cladribine injection, in particular to a cladribine injection 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. 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 the United States in February 1993 In the same year, it was launched in Canada and Sweden under the trade name of Leustatin. [0003] 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 revealed. In May 2003, the subcutaneous formulation of Litak (cladribine, cladribine) of Lip...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/08A61K31/7076A61K47/02A61K47/12A61K47/04A61P35/00A61P35/02
CPCA61K9/0019A61K9/08A61K31/7076A61K47/02A61K47/12A61P35/00A61P35/02
Inventor 张俊赵技宇邵婷婷任倩
Owner 瀚晖制药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com