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Temozolomide nuclear magnetic resonance visual injectable hydrogel as well as preparation method and application thereof

A temozolomide and nuclear magnetic resonance technology, applied in the field of temozolomide nuclear magnetic resonance visualized injectable hydrogel preparation, can solve the problem of less gel, avoid decomposition and leakage, reduce systemic side effects, and ensure drug efficacy

Active Publication Date: 2019-12-20
武汉布润脑医学科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A lot of research work has focused on in vivo MRI monitoring of nanoparticles, nanogels, microcapsules, and liposomes, but very little has been done on gels, especially injectable gels.

Method used

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  • Temozolomide nuclear magnetic resonance visual injectable hydrogel as well as preparation method and application thereof
  • Temozolomide nuclear magnetic resonance visual injectable hydrogel as well as preparation method and application thereof
  • Temozolomide nuclear magnetic resonance visual injectable hydrogel as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] 1. Preparation of Temozolomide Solid Lipid Nanoparticles

[0046] (1) Under water-bath conditions, take by weighing 500 mg of solid lipid stearic acid and dissolve in an appropriate amount of chloroform under dark heat for subsequent use;

[0047] (2) Under water-bath conditions, weigh 100 mg of temozolomide and fully dissolve it in an appropriate amount of dimethyl sulfoxide (DMSO), and set aside;

[0048] (3) Add step (2) to step (1), mix well to form 5 mL of organic phase, set aside;

[0049] (4) Dissolve 250 mg of the emulsifier Poloxamer 188 in deionized water under water bath conditions to form 25 mL of the water phase (volume ratio of the organic phase to the water phase = 1:5), and set aside;

[0050] (5) Slowly add the organic phase prepared in step (3) dropwise to the aqueous phase obtained in step (4), stir rapidly (600r / min) during the dropwise addition to form the first emulsion, and set aside;

[0051] (6) Raise the temperature of the primary emulsion pr...

Embodiment 2

[0060] 1. Preparation of Temozolomide Solid Lipid Nanoparticles

[0061] (1) Under water bath conditions, weigh 250 mg of the solid lipid glyceryl behenate, dissolve it in an appropriate amount of chloroform and heat it away from light, and set aside;

[0062] (2) Under water-bath conditions, weigh 250 mg of temozolomide and fully dissolve it in an appropriate amount of dimethyl sulfoxide (DMSO) for subsequent use;

[0063] (3) Add step (2) to step (1), mix well to form 5 mL of organic phase, set aside;

[0064] (4) Dissolve 500 mg of Poloxamer 188 in deionized water under water bath conditions to form 25 mL of water phase (volume ratio of organic phase to water phase = 1:5) for later use;

[0065] (5) Slowly add the organic phase prepared in step (3) dropwise to the aqueous phase obtained in step (4), and stir rapidly (1200r / min) during the dropwise addition to form a primary emulsion for subsequent use;

[0066] (6) Raise the temperature of the primary emulsion prepared in...

Embodiment 3

[0072] 1. Preparation of Temozolomide Solid Lipid Nanoparticles

[0073] (1) Under water-bath conditions, weigh 650 mg of the solid lipid glyceryl monostearate, dissolve it in an appropriate amount of chloroform and heat it in the dark, and set aside;

[0074] (2) Under water-bath conditions, weigh 100 mg of temozolomide and fully dissolve it in an appropriate amount of dimethyl sulfoxide (DMSO), and set aside;

[0075] (3) Add step (2) to step (1), mix well to form 5 mL of organic phase, set aside;

[0076] (4) Dissolve 250 mg of the emulsifier Poloxamer 188 in deionized water under water bath conditions to form 25 mL of the water phase (volume ratio of the organic phase to the water phase = 1:5), and set aside;

[0077] (5) Slowly add the organic phase prepared in step (3) dropwise to the aqueous phase obtained in step (4), and stir rapidly (1200r / min) during the dropwise addition to form a primary emulsion for subsequent use;

[0078] (6) Raise the temperature of the prim...

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Abstract

The invention relates to temozolomide nuclear magnetic resonance visual injectable hydrogel as well as a preparation method and application thereof. According to the invention, temozolomide solid lipid nanoparticles are loaded into a nuclear magnetic resonance visual hydrogel matrix, such that temozolomide lipid nanoparticle-loaded hydrogel is prepared. A system combines the advantages of the temozolomide solid lipid nanoparticles, injectable hydrogel and modified hydroxypropyl chitosan, so that the slow release performance of the system is obviously higher than that of the temozolomide solidlipid nanoparticles and a temozolomide active compound; the hydrogel disclosed by the invention can be used for postoperative local treatment of brain glioma; residence time of drug-loaded nanoparticles at the focus part is prolonged, and local drug concentration is increased; compared with an existing oral administration dosage form, the in-situ gel containing a temozolomide composition providedby the invention can be administered immediately after surgery, and continuously releases in an operation residual cavity, so that real-time monitoring on a focus part is realized, the bioavailabilityof the drug is improved, and postoperation lifetime is favorably prolonged.

Description

technical field [0001] The invention belongs to the technical field of chemistry and biomedicine, and in particular relates to a temozolomide nuclear magnetic resonance visualized injectable hydrogel, a preparation method and an application thereof. Background technique [0002] Human glioma is the primary brain tumor with the highest incidence rate in the central nervous system. According to foreign clinical statistics, the incidence of glioma accounts for about 60% of brain tumors. At present, the treatment of glioma is mainly surgical resection, postoperative radiotherapy or chemotherapy, but glioma is very easy to relapse, it is difficult to cure, and the clinical treatment effect is not ideal. [0003] Temozolomide (Temozolomide, trade name Temodar, TMZ for short) is a kind of mitozolomide analogue, is the second generation of oral imidazolomide anti-tumor alkylating agent chemotherapy drugs, can pass through the blood-brain barrier, on the brain Glioma has a good cura...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/4188A61K9/51A61K49/18A61K49/12A61K49/10A61K47/36A61K47/10A61P35/00
CPCA61K9/0024A61K31/4188A61K9/06A61K47/36A61K47/10A61K9/5123A61K49/126A61K49/105A61K49/1803A61P35/00Y02A90/30
Inventor 刘芝兰俞苏寰马超纪维维李志强王泽芬
Owner 武汉布润脑医学科技有限责任公司
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