Busulfan composition and preparation method and application thereof

A technology of busulfan and its composition, which is applied in the field of busulfan composition and its preparation, can solve undiscovered problems, achieve the effects of reducing storage costs, reducing use costs, and ensuring drug effectiveness and safety

Active Publication Date: 2018-12-25
JIANGSU LINGHANG BIOLOGICAL TECH CO LTD
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, no studies and reports have been found on busulfan injections that meet the current busulfan drug standards and have drug safety and long-term storage stability

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
  • Busulfan composition and preparation method and application thereof
  • Busulfan composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of busulfan composition of the present invention

[0032] Take 60mg of Busulfan raw material and dissolve it in 10mL of acetone at a temperature not exceeding 35°C. Dissolve 4.5 g of sulfobutyl-β-cyclodextrin in 20 mL of water for injection. The two solutions were mixed, fed with nitrogen, stirred for 1 hour under nitrogen atmosphere, and the organic solvent was removed. The remaining solution was filtered through a 0.22 μm microporous membrane, freeze-dried, and packaged.

Embodiment 2

[0033] Embodiment 2: the preparation of busulfan composition of the present invention

[0034] Take 60mg of Busulfan raw material and dissolve it in 10mL of acetone at a temperature not exceeding 35°C. Dissolve 6.0 g of sulfobutyl-β-cyclodextrin in 20 mL of water for injection. The two solutions were mixed, fed with nitrogen, stirred for 1 hour under nitrogen atmosphere, and the organic solvent was removed. The remaining solution was filtered through a 0.22 μm microporous membrane, freeze-dried, and packaged.

Embodiment 3

[0035] Embodiment 3: the preparation of busulfan composition of the present invention

[0036] Take 60mg of Busulfan raw material and dissolve it in 10mL of acetone at a temperature not exceeding 35°C. Dissolve 2.0 g of sulfobutyl-β-cyclodextrin in 10 mL of water for injection. The two solutions were mixed, fed with nitrogen, stirred for 2.5 hours under nitrogen atmosphere, and the organic solvent was removed. The remaining solution was filtered through a 0.22 μm microporous membrane, freeze-dried, and packaged.

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

PropertyMeasurementUnit
concentrationaaaaaaaaaa
Login to view more

Abstract

The invention discloses a busulfan composition and a preparation method and an application thereof. The busulfan composition comprises the following substances in a weight ratio: a proportion of busulfan to cyclodextrin is 1-20:100-2000. The busulfan composition is preferably prepared by the following method: dissolving the busulfan by using an organic solvent, and preparing the busulfan solutionof which the concentration is 1-20 mg / mL; dissolving SBE-Beta-cyclodextrin by using water for injection, preparing 10-40% (w / v) of SBE-Beta-cyclodextrin water solution; in a nitrogen atmosphere, mixing two types of the solution, after stirring for 1 hour, and removing the organic solvent; and filtering, and freeze-drying. The busulfan composition can be used for a tablet and injection. It is proved from research that the busulfan composition is capable of remarkably improving stability of the busulfan. The busulfan composition is lower in injection irritation, can be used for clinic injection,and is capable of improving safety of drug use as well as guaranteeing product stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a busulfan composition, a preparation method and application thereof. Background technique [0002] Busulfan is a dimethylsulfonate bifunctional alkylating agent, which was first discovered in 1953. In terms of mechanism of action, busulfan is a cytotoxic antineoplastic drug. After entering the human body, its sulfonate group will undergo alkylation with guanine in tumor cells, interfering with the formation of tumor cell genetic material. , thereby inhibiting the growth of tumor cells. Busulfan is mainly suitable for proliferative diseases of blood and bone marrow, especially for chronic myeloid leukemia, essential thrombocythemia, polycythemia vera, primary myelofibrosis and other diseases. However, due to the poor solubility of busulfan, especially the worst in water solubility, it is difficult to absorb after oral administration, and the dose required for oral admin...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/255A61K47/40A61P7/00A61P35/00A61P35/02
CPCA61K47/40A61P7/00A61P35/00A61P35/02A61K9/0019A61K9/205A61K31/255A61K9/08A61K9/19
Inventor 王刚董祥玉
Owner JIANGSU LINGHANG BIOLOGICAL TECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap