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Ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram as well as preparation method and application of ion-sensitive nasal in-situ gel

A temozolomide and ion-sensitive technology, applied in the field of medicine, can solve the problems of low oral bioavailability, poor fat solubility, water solubility, and less brain drug aggregation, so as to achieve good biocompatibility and safety, and overcome drug resistance Sex, the effect of improving drug stability

Active Publication Date: 2022-03-01
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The logP of temozolomide is -1.32, poorly fat-soluble, moderately water-soluble, high oral bioavailability, but highly toxic and prone to drug resistance. The logP of disulfiram is 3.62, which is a fat-soluble drug with low toxicity and multiple reversibility However, its low solubility, short half-life, less drug accumulation in the brain, and low oral bioavailability limit its further application.

Method used

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  • Ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram as well as preparation method and application of ion-sensitive nasal in-situ gel
  • Ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram as well as preparation method and application of ion-sensitive nasal in-situ gel
  • Ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram as well as preparation method and application of ion-sensitive nasal in-situ gel

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preparation example Construction

[0049] In yet another specific embodiment of the present invention, the preparation method of the above-mentioned pharmaceutical preparation is provided. Specifically, the pharmaceutical preparation is an ion-sensitive nasal in-situ gel, and its preparation method includes:

[0050] (1) Completely dissolving the clathrate material in the aqueous solution containing the gelling agent material, and obtaining the first mixed solution after ultrasonication;

[0051] (2) adding an organic solution containing disulfiram to the first mixed solution obtained in step (1) to obtain a second mixed solution;

[0052] (3) Add temozolomide to the second mixture, heat and stir until the two drugs are completely dissolved, the organic solvent is volatilized, and centrifuged to obtain an ion-sensitive in-situ nasal gel containing temozolomide and disulfiram.

[0053] It should be noted that the ion-sensitive nasal in-situ gel prepared in step (3) of the present invention can be further made in...

Embodiment 1

[0064] A preparation method for an ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram, comprising the steps of:

[0065] Add 50 mg of temozolomide TMZ to 300 mg / mL hydroxypropyl-β-cyclodextrin HP-β-CD aqueous solution containing 0.4% deacetylated gellan gum DGG, and then add 300 μL of acetonitrile solution of 30 mg disulfiram DSF. Under the condition of heating at 40°C and stirring at 600rpm, TMZ and DSF are gradually clathrated and dissolved. After 2 hours, when TMZ and DSF were completely clathrated and acetonitrile was completely volatilized, an ion-sensitive nasal in-situ gel containing temozolomide and disulfiram with excellent gelling ability was obtained.

Embodiment 2

[0067] A preparation method for an ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram, comprising the steps of:

[0068] 300 μL of an acetonitrile solution of 30 mg DSF was added to a 300 mg / mL aqueous solution of HP-β-CD containing 0.4% DGG, and then 50 mg of TMZ was added. Under the condition of heating at 40°C and stirring at 400rpm, TMZ and DSF are gradually clathrated and dissolved. After 2 hours, when TMZ and DSF were completely clathrated and acetonitrile was completely volatilized, an ion-sensitive nasal in-situ gel containing temozolomide and disulfiram with excellent gelling ability was obtained.

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Abstract

The invention provides ion-sensitive nasal in-situ gel carrying temozolomide and disulfiram as well as a preparation method and application of the ion-sensitive nasal in-situ gel, and belongs to the technical field of medicines. The water solubility of temozolomide and disulfiram is remarkably improved at the same time, the stability of the temozolomide and disulfiram is improved, absorption of the two drugs in the nasal cavity is promoted, slow release of the two drugs is achieved, high enrichment of the two drugs in brain tumors is promoted, the in-vivo stability of the two drugs is improved, and therefore the temozolomide and disulfiram compound has good practical application value.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an ion-sensitive nasal in-situ gel containing temozolomide and disulfiram, a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Glioblastoma is the most devastating primary malignancy of the adult central nervous system. Most patients die within 1 to 2 years of diagnosis. A major obstacle to effective treatment of glioblastoma is its highly aggressive, tumorigenic, and 'stem cell-like' characteristics. Temozolomide (TMZ) is the standard chemotherapy drug for glioblastoma treatment. However, it leads to hematological and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4188
CPCA61K31/4188A61K31/145A61K9/06A61K9/0043A61K47/36A61K47/6951A61P35/00A61P25/00A61K2300/00
Inventor 赵忠熙曲颖李楠
Owner SHANDONG UNIV
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