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Method for encapsulating hydrophobic antitumor drug by amphiphilic medicament and preparation

An anti-tumor drug and amphiphilic technology, applied in the field of anti-tumor drug preparation, can solve the problems of poor solubility, poor water solubility, and low drug entrapment rate, and achieve the effects of rapid release, simple steps, and overcoming low drug load.

Active Publication Date: 2014-03-19
杭州磐田生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, SN-38 has poor solubility even in soluble solvents and extremely poor water solubility, so the drug entrapment rate is very low and there is a possibility of burst release

Method used

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  • Method for encapsulating hydrophobic antitumor drug by amphiphilic medicament and preparation
  • Method for encapsulating hydrophobic antitumor drug by amphiphilic medicament and preparation
  • Method for encapsulating hydrophobic antitumor drug by amphiphilic medicament and preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0048] (1) Dissolve irinotecan hydrochloride (10 mg) and SN-38 (5 mg) in organic solvent dimethyl sulfoxide (80 microliters), the amount of organic solvent added is enough to completely dissolve the drug at room temperature, and mix well.

[0049] (2) Add a certain amount of water (10.8mL) to the solution obtained in step (1), and sonicate for 5min at the same time. The equivalent dose of SN-38 in the solution (SN38equivalent) is 1mg / mL.

[0050] (3) Put the solution obtained in step (2) in a dialysis membrane (molecular weight cut-off 1000), put it in a phosphate buffer solution or pure water with pH=7.0-7.4, and quickly dialyze it for 6 hours at room temperature to remove the organic solvent. Nanoemulsion of SN-38 preparation (drug loading efficiency is basically 100%).

[0051] (4) 6%wt D-trehalose was added to the obtained SN-38 emulsion as a lyoprotectant, and then freeze-dried to prepare irinotecan hydrochloride-loaded nano drug injection powder of SN-38.

[0052] The ...

Embodiment 2

[0055] The irinotecan hydrochloride in embodiment 1 is replaced by topotecan hydrochloride or doxorubicin hydrochloride, the added molar weight is the same as irinotecan hydrochloride, and other operations are the same as in embodiment 1, and topotecan hydrochloride or doxorubicin hydrochloride are prepared. Nano drug injection powder or injection emulsion assembled by mycin and SN-38.

[0056] Correspondingly, nanomedicines with different drug loadings can be prepared according to Example 1 and Example 2 as required.

Embodiment 3

[0058] According to the molar ratio of Example 1, topotecan hydrochloride was used to replace irinotecan hydrochloride, paclitaxel was used to replace SN-38, and other operating steps were the same as in Example 1 to prepare topotecan hydrochloride and paclitaxel assembled nanomedicine injection powder or injection emulsion.

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Abstract

The invention discloses a method for encapsulating a hydrophobic antitumor drug by an amphiphilic medicament, comprising: (1) adding the amphiphilic medicament and the hydrophobic antitumor drug into an organic solvent, and uniformly mixing; (2) adding distilled water into an obtained mixture, and uniformly mixing to obtain a preparation solution; and (3) removing the organic solvent in the preparation solution, adding a freeze-drying protective agent, and carrying out freezing and drying treatment, to obtain an antitumor drug pulvis encapsulated with the hydrophobic antitumor drug. The invention further discloses a medicinal preparation prepared by the method. The amphiphilic medicament irinotecan hydrochloride or topotecan hydrochloride is used as an emulsifier to encapsulate a water insoluble anticancer medicament, which greatly increases solubility of the hydrophobic medicament in water and reserves high antineoplastic activity characteristics of the medicament itself, has advantages of simple preparation technology, strong applicability and convenience for large scale production, and develops a new approach for in vivo conveying of the hydrophobic medicament.

Description

technical field [0001] The invention relates to the technical field of preparation of antineoplastic drugs, in particular to a method of using amphiphilic drugs to carry hydrophobic antineoplastic drugs and the injection-type preparation of hydrophobic antineoplastic drugs obtained by the method. Background technique [0002] Many antineoplastic drugs usually have multiple negative characteristics, such as: low solubility in water, difficult to use directly; poor targeting, toxic side effects on the body; short plasma half-life, must be repeatedly administered one after another; tumor resistance to chemotherapy treatment sex etc. Some highly active antineoplastic drugs, such as camptothecin, paclitaxel, vinblastine and docetaxel, cannot be directly administered intravenously due to their low solubility in water, and solubilizers or dosage form technology must be used. [0003] Paclitaxel drugs inhibit depolymerization by promoting tubulin polymerization, maintain tubulin st...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61K31/704A61K47/22A61K47/26A61K9/19A61K9/107A61P35/00A61K31/337
Inventor 申有青胡诗琪刘祥瑞唐建斌隋梅花
Owner 杭州磐田生物技术有限公司
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