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Method for solubilizing camptothecin compound

A technology for camptothecin and compounds, which is applied in the field of solubilization of camptothecin compounds, can solve problems such as poor water solubility, and achieve the effect of high solubility

Inactive Publication Date: 2011-04-06
JIANGSU SIMCERE PHARMACEUTICAL R & D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since most camptothecin derivatives are poorly water-soluble, it is very important to adopt suitable preparation methods to improve solubility while maintaining the closed-loop structure of the lactone ring.

Method used

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  • Method for solubilizing camptothecin compound
  • Method for solubilizing camptothecin compound
  • Method for solubilizing camptothecin compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Add 10ml of 0.4M tartaric acid solution to 1gHP-β-CD, and vortex to dissolve to obtain a 10% HP-β-CD solution; add 5ml of 0.4M NaOH solution to 20mg of 10-hydroxycamptothecin, and vortex to dissolve, the alkaline solution of the drug Add 5ml of 10% HP-β-CD solution to the solution, vortex and shake until it is clear and transparent to obtain a clathrate solution with a concentration of about 2mg / ml, and the 10-hydroxycamptothecin in the solution can be detected by HPLC The purity is 98.6%.

Embodiment 2

[0046] Add 10ml of 0.55M hydrochloric acid solution to 2g of SB-β-CD, vortex to dissolve to obtain 20% HP-β-CD solution; add 5ml of 0.5M NaOH solution to 10mg of SN38, vortex to dissolve, add 5ml of 20% SB to the alkaline solution of the drug - β-CD solution, vortex and shake until clear and transparent, if necessary, adjust the pH value to 3.5 with the corresponding acid or alkali solution to obtain an inclusion complex solution with a concentration of about 1mg / ml, and divide the solution into penicillin bottle, freeze-dried to obtain SN38 freeze-dried powder. Through HPLC detection, it can be measured that the purity of SN38 in the freeze-dried powder is 99.2%.

Embodiment 3

[0048]

[0049] Add 3g of SB-β-CD to 10ml of 0.25M citric acid solution, vortex to dissolve to obtain a 30% SB-β-CD solution; add 5ml of 0.2M NaOH solution to 40mg of compound A, vortex to dissolve, add 5ml to the alkaline solution of the drug 30% SB-β-CD solution, vortex and shake until clear and transparent, and leave it for 2 hours to obtain a clathrate solution with a concentration of about 4 mg / ml. Through HPLC detection, the purity of compound A in the solution can be measured to be 97.8%. .

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Abstract

The invention discloses a method for solubilizing a camptothecin compound, which comprises the following steps of: dissolving the camptothecin compound into alkaline aqueous solution to prepare solution of camptothecin; dissolving a water-soluble cyclodextrin derivative into acid aqueous solution to prepare solution of cyclodextrin derivative; and mixing the solution of camptothecin with the solution of cyclodextrin derivative, stirring till the solution is clarified and transparent and thus, obtaining cyclodextrin clathrate compound solution of the camptothecin compound. The method is simple and practicable without using an organic solvent or special preparation equipment, and the solubility of the compound can be successfully improved by over 100 times by using the water-soluble cyclodextrin derivative through simple acid-base neutralization.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a solubilization method of camptothecin compounds. Background technique [0002] Cyclodextrin, also known as cyclopolydextrose, is a general term for a group of oligosaccharides formed by cyclic arrangement of D-glucopyranose units. Villiers discovered cyclodextrins in 1891 by enzymatically degrading starch. Because cyclodextrin is a cyclic hollow cylindrical structure, it exhibits a series of special properties and can form inclusion complexes with some small molecule drugs. Common cyclodextrins are composed of α, β, and γ, and among the three, β-cyclodextrin is the most commonly used. Since β-cyclodextrin has a small solubility in water, in order to improve its solubility, it has a series of derivatives. compounds, including methyl, ethyl, hydroxypropyl, sulfobutyl, and glucosyl derivatives, of which the most commonly used are hydroxypropyl-β-cyclodextrin (HP-β-CD), sulfobutyl-β- Cyc...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61K31/5365A61K47/48A61P35/00A61K47/61
Inventor 张翠霞陆爱军王青松
Owner JIANGSU SIMCERE PHARMACEUTICAL R & D CO LTD
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