Preparation of Camptothecin Drug Nanocrystals by Reversible Decomposition

A technology of nanocrystals and camptothecin, applied in the field of medicine, can solve the problems of limiting the clinical application of nanocrystal preparations, rapid growth of particle size, etc., and achieve the effects of retaining antitumor activity, high drug loading, and low requirements for preparation instruments

Active Publication Date: 2022-04-01
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, due to the influence of Ostwald ripening, nanocrystals generally have the defect of rapid growth in particle size, and stabilizers need to be added to maintain a relatively stable particle size.
Many factors limit the clinical application of nanocrystal preparations (Al-Kassas R, Bansal M, Shaw J. Nanosizing techniques for improving bioavailability of drugs. Journal of controlled release: Official Journal of the Controlled Release Society. 2017; 260: 202-12.)

Method used

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  • Preparation of Camptothecin Drug Nanocrystals by Reversible Decomposition
  • Preparation of Camptothecin Drug Nanocrystals by Reversible Decomposition
  • Preparation of Camptothecin Drug Nanocrystals by Reversible Decomposition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] (1) Preparation of SN38 prototype / carboxylic acid type mixture

[0046] Take 1 mL of ammonia water, dissolve it in 5 mL of water, weigh SN38 (0.2 g) and disperse it in the aqueous ammonia water solution, and react in the dark at room temperature until the solution is clear, stop the reaction, remove the reaction solvent by rotary evaporation under reduced pressure at 60°C to obtain SN38 prototype / carboxylic acid Type mixture (light yellow flaky solid), wherein the mass percentage of prototype drug is 82.1%.

[0047] (2) Preparation of SN38 nanocrystal preparation

[0048] The mixture (20 mg) obtained in step (1) was dispersed in 20 mL of purified water, and the probe was sonicated for 10 min (100 W) to obtain a blue-green opalescent solution. Subsequently, the preparation solution is filtered through a 0.22 μm filter membrane and freeze-dried to obtain a freeze-dried powder of SN38 nanocrystals. Take 20 mL of 5% glucose solution for injection to redissolve the freeze-...

Embodiment 2

[0050] (1) Preparation of camptothecin drug prototype / carboxylic acid type mixture

[0051] Take 2 mL of ammonia water, dissolve it in 5 mL of water, weigh camptothecin drugs (0.2 g, including CPT-11, HCPT, CDK-602 or TPT) and disperse them in the aqueous ammonia water solution, and react at room temperature in the dark until the solution is clear and stop the reaction , After removing the reaction solvent by rotary evaporation under reduced pressure at 60°C, solid powder or suspension (light yellow flaky solid or light yellow solution) of camptothecin drug prototype / carboxylic acid mixture was obtained.

[0052] (2) Preparation of camptothecin drug nanocrystal preparation

[0053] Disperse the mixture (20 mg) obtained in step (1) in 20 mL of purified water (or dilute the suspension to 250 mL, measure 25 mL), and sonicate the probe for 10 min (100 W) to obtain a blue-green opalescent solution. Subsequently, the preparation solution is filtered through a 0.22 μm filter membran...

Embodiment 3

[0057] (1) Preparation of SN38 prototype / carboxylic acid type mixture

[0058] Take 4 mL of triethylamine, dissolve it in 4 mL of water, weigh SN38 (0.2 g) and disperse it in the aqueous solution of triethylamine, stir at room temperature in the dark until the solution is clear, stop the reaction, and dry in vacuum to remove most of the alkaline reagents to obtain SN38 Prototype / carboxylic acid type mixture suspension (light yellow liquid), wherein the mass percentage of the prototype drug is 18.3%.

[0059] (2) Preparation of SN38 nanocrystal preparation

[0060] Set the volume of the mixture suspension prepared in step (1) to 50 mL, take (25 mL of aqueous solution (50 mg of human serum albumin was added), and stir rapidly to obtain a blue-green opalescent preparation solution. Then the preparation solution was freeze-dried to obtain SN38 / albumin nanocrystal freeze-dried powder. Take 30mL of 0.9% normal saline to redissolve the freeze-dried powder, shake and disperse to obta...

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Abstract

The invention provides a method for preparing camptothecin drug nanocrystals by using a reversible decomposition method. The nano crystal provided by the invention is needle-shaped or rod-shaped, does not contain any auxiliary material, retains the anti-tumor activity of the drug, enhances the tumor penetration effect of the drug, and reduces toxic and side effects. The preparation process is simple, suitable for industrial production, and has broad application prospects.

Description

technical field [0001] The invention specifically relates to nanocrystals of camptothecin drugs, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Anti-tumor therapy mainly relies on small-molecule anti-tumor drugs. Usually, anti-tumor drugs have many defects and limitations in clinical application, such as: low drug solubility, difficult to dissolve in clinically available solvents; short plasma half-life of drugs, which must be administered frequently In order to maintain the effective blood concentration; antineoplastic drugs have side effects on the body, frequent administration of toxic side effects and so on. Some highly active antineoplastic drugs, such as camptothecin and paclitaxel, cannot be directly administered intravenously due to the low solubility of the drug in water, and must be improved by means of chemical modification, solubilizer or new formulation technology. [0003] Camptotheci...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D491/22A61K31/4745A61K9/19A61P35/00
CPCC07D491/22A61K9/19A61P35/00C07B2200/07
Inventor 龚涛杨琴宋旭张志荣孙逊谭田田赵娟周楚楚刘兴
Owner SICHUAN UNIV
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