Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Temozolomide slow-release system as well as preparation method and application thereof

A technology of temozolomide and sustained-release microspheres, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. And other issues

Inactive Publication Date: 2017-03-15
马晓东
View PDF1 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the sustained-release agent has certain defects in the application process, such as weak cell adhesion, poor hydrophilicity, acidic degradation products cause aseptic inflammation, and infiltration of inflammatory cells in local brain tissue and Cerebral edema is obvious. In addition, in some experiments, it was found that the histocompatibility of such degradable materials is poor, and the surrounding scar tissue is obviously formed, which is easy to affect the diffusion of sustained-release drugs. The degraded fragments cannot be absorbed in time, and the tumor cavity Swimming, risk of occlusion of the ventricular system, these defects limit its clinical application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Temozolomide slow-release system as well as preparation method and application thereof
  • Temozolomide slow-release system as well as preparation method and application thereof
  • Temozolomide slow-release system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation and analysis of embodiment 1-temozolomide sustained-release microspheres:

[0044] (1) Temozolomide-PLGA sustained-release microspheres were prepared by ultrasonic emulsification-solvent evaporation method: the molecular weights of PLGA were 15,000, 20,000, 33,000, and 36,000, respectively. TMZ crystal is dissolved in methanol, PLGA polymer is dissolved in dichloromethane, the two solutions are mixed, the obtained organic phase is stirred and emulsified in the solution containing polyvinyl alcohol, stirred at room temperature (800r / min), and the stirring speed becomes 350r after 30min / min until dichloromethane and methanol are completely volatilized. The obtained microspheres were washed with distilled water, screened to remove large particles, freeze-dried, and randomly packaged and refrigerated at 0°C. First observe the surface morphological characteristics of the four kinds of slow-release microspheres with a microscope, and then use a TOSHIBA800S scann...

Embodiment 2

[0055] Example 2-Study on the effect of TMZ-PLGA sustained-release microspheres on C6 glioma cells.

[0056] (1) Cell culture: Use a pipette gun to move glioma C6 cells into a culture flask, add 2.5ml of EMDM medium containing 10% calf serum, and put in CO 2 Inside the cell culture incubator. Cultures were changed every 2-3 days. Observe that the cell growth area accounts for more than 90% of the bottom of the culture flask, and then subculture. Remove the residual medium in the culture bottle, add 1ml of trypsin, observe with an inverted phase-contrast microscope, and find that the C6 cells become round and bright, immediately add 2ml of fresh medium containing 10% calf serum. Use a pipette to blow the cells off the bottom of the flask. Divide 1 bottle of cell suspension into 3 culture flasks equally, then add 2ml of 10% fresh medium of calf serum respectively, and finally put them into a constant temperature incubator for cultivation.

[0057] (2) Determination of cell...

Embodiment 3

[0064] Example 3-In vivo release of TMZ-PLGA sustained-release microspheres and their effects on rat C6 glioma.

[0065] (1) In vivo release study of TMZ-PLGA sustained-release microspheres: 7.5% TMZ-PLGA sustained-release microspheres were placed under the dura mater on the surface of the rat brain, respectively, at 1, 2, 3, 5, 8, 11, After 14 and 18 days, the tablets were taken out, and the peak areas corresponding to different TMZ drug concentrations were measured by high-pressure liquid chromatography, the drug concentration and the remaining TMZ content in the microspheres were calculated, and the TMZ release amount was calculated (see Figure 10-12 ). For the detection of TMZ drug concentration, the peak time is about 5min, which is relatively stable (such as Figure 10 ,11,12). Carry out linear regression with drug release rate (P%) to drug time (t) and draw regression equation to be P=4.2932t+30.5916, r2=0.9111, draw out the rat intracranial release curve of TMZ-PL...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
encapsulation rateaaaaaaaaaa
Login to View More

Abstract

The invention discloses a temozolomide slow-release system which comprises PLGA (poly (lactide-glycolide acid)) slow-release microspheres and temozolomide wrapped inside the PLGA slow-release microspheres. A preparation method of the temozolomide slow-release system comprises the following steps: 1) dissolving temozolomide crystal in methanol, and dissolving the PLGA in dichloromethane; and 2) mixing the two solutions, and stirring and emulsifying the obtained organic phase in a polyvinyl alcohol-containing solution till the dichloromethane and the methanol are completely volatilized. The invention further discloses application of the temozolomide slow-release system in treating intracranial tumors, particularly glioma.

Description

technical field [0001] The invention relates to a drug slow-release system, in particular to a sustained-release system loaded with temozolomide, a preparation method and application thereof. Background technique [0002] Intracranial tumors (also known as brain tumors) are divided into primary intracranial tumors and secondary intracranial tumors. The incidence of intracranial tumors is relatively high, ranking fifth (6.31%) in terms of the incidence of systemic tumors, only lower than tumors of the stomach, uterus, breast, and esophagus. [0003] Glioma is the most common primary intracranial tumor, accounting for more than 40% of intracranial tumors, with an incidence rate of more than 5 per 100,000. It is one of the top ten most common tumors in China. About 70% of gliomas are glioblastoma and anaplastic astrocytoma, which are highly malignant and have not made breakthrough progress in treatment. At present, the treatment of glioma is mainly surgical treatment, supplem...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4188A61K47/34A61P35/00
CPCA61K9/0002A61K9/1647A61K31/4188
Inventor 马晓东
Owner 马晓东
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com