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

Supersaturated self-microemulsified administration system for insoluble anti-tumor drugs, and preparation method thereof

A technology of anti-tumor drug and drug delivery system, which is applied in the field of drug delivery system, supersaturated self-microemulsification drug delivery system and its preparation, and can solve the problem of inability to inhibit P-gp efflux, failure to meet clinical application requirements, and limited drug delivery. Transmembrane absorption and other issues to achieve the effect of avoiding the first pass effect, improving bioavailability, and increasing penetration

Inactive Publication Date: 2011-09-21
FUDAN UNIV
View PDF1 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies by scholars at home and abroad have shown that although the common self-microemulsifying drug delivery system can improve the oral bioavailability of poorly soluble drugs to a certain extent, it often cannot meet the clinical requirements of some highly fat-soluble drugs. The application requirements, on the one hand, are due to the spontaneous formation of emulsion droplets smaller than 100nm after the self-microemulsified drug delivery carrier is diluted with the gastrointestinal solution. During this process, insoluble drugs may precipitate and form drug crystals, which limits the drug transmembrane absorption
On the other hand, the micellar solution formed by a large amount of surfactants in the preparation cannot inhibit the efflux of P-gp (surfactants can only inhibit the efflux of proteins when the concentration of micelles is lower than the critical micelle concentration). function), it will hinder the release of drugs from the micellar system and limit the small intestinal absorption of drugs

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
  • Supersaturated self-microemulsified administration system for insoluble anti-tumor drugs, and preparation method thereof
  • Supersaturated self-microemulsified administration system for insoluble anti-tumor drugs, and preparation method thereof
  • Supersaturated self-microemulsified administration system for insoluble anti-tumor drugs, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of supersaturated self-microemulsifying drug delivery system

[0029] Prescription composition:

[0030]

[0031] Weigh the prescription amount of each auxiliary material, stir evenly to obtain a uniform clear oily liquid, then add the prescription amount of medicine under stirring at room temperature, mix for about 1 hour to fully dissolve, make a soft capsule, and obtain a supersaturated self-microemulsifying drug. Medicine system soft capsules. Make 1000 soft capsules altogether.

[0032] Physicochemical properties of 9-nitrocamptothecin supersaturated self-microemulsifying drug delivery system:

[0033] Adopt the particle diameter, zeta-potential after the 9-nitrocamptothecin supersaturated self-microemulsification drug delivery system is diluted 250 times with pure water by laser scattering instrument, measure self-microemulsification time (such as figure 1 shown).

[0034] Table 1. In vitro characterization of 9-nitrocamptothecin super...

Embodiment 2

[0048] Preparation of supersaturated self-microemulsifying drug delivery system:

[0049] Prescription composition:

[0050]

[0051] Mix the prescribed amount of polyoxyethylene hydrogenated castor oil EL, polyethylene glycol-400, LAUROGLYCOL FCC, and hydroxypropyl methylcellulose, heat and stir at 35°C to mix the components, add the prescribed amount of paclitaxel, and stir to make the drug Completely dissolve to obtain a supersaturated self-microemulsifying drug delivery system, which is filled in soft capsules and made into 1000 soft capsules in total.

[0052] After testing, the results show that: (1) after preparing the drug into a self-microemulsified drug delivery system, using 0.1M hydrochloric acid as the dissolution medium, paclitaxel can dissolve more than 80% in 15 minutes in a supersaturated self-microemulsified drug delivery system, while the raw material drug capsule Almost no dissolution; (2) after the drug is prepared into a self-microemulsifying drug del...

Embodiment 3

[0053] Embodiment 3 is prepared from the microemulsion drug delivery system

[0054] prescription composition

[0055]

[0056]

[0057] Disperse 9-nitrocamptothecin in caprylic / capric macrogol glyceride (Labrasol), diethylene glycol monoethyl ether (Tanscutol), caprylic capric triglyceride (MIGLYOL 812N), β-cyclodextrin In the mixture, warm at 30°C to melt and mix the components, so that the drug is completely dissolved, and the supersaturated self-microemulsifying drug delivery system is obtained and filled in soft capsules. Made 1000 soft capsules altogether.

[0058] After testing, the results show that: (1) after the drug is prepared as a self-microemulsifying drug delivery system, 9-nitrocamptothecin can be dissolved by 80% in 15 minutes with 0.1M hydrochloric acid as the dissolution medium above, and the bulk drug capsule is almost not dissolved; (2) after the drug is prepared into a self-microemulsifying drug delivery system, the particle size after dispersion ...

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
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention belongs to the field of pharmaceutical preparation, and relates to a supersaturated self-microemulsified administration system for insoluble anticancer drugs, prepared from insoluble anti-tumor drugs, an emulsifier, a co-emulsifier, an oil phase and a crystallization inhibitor in different mass percents; and the administration system can be filled into soft capsules or hard capsules. The supersaturated self-microemulsified administration system is dispersible after oral administration to form microemulsion with the particle size of 10-100nm, thus inhibiting crystallization and separation of drugs, promoting absorption of drugs and improving the bioavailability of drugs. The administration system has the advantages of improving the solubility of the insoluble anticancer drugs in water, inhibiting the exocytosis of the intestinal epithelial cell p-glycoprotein on drugs, improving the bioavailability of drugs, eliminating the influence of foods on the absorption and bioavailability of drugs, and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a drug delivery system. Specifically, the invention relates to a supersaturated self-microemulsification drug delivery system for insoluble antitumor drugs and a preparation method thereof. Background technique [0002] 9-Nitrocamptothethin (9-NC) is a new semi-synthetic derivative of camptothecin, also known as rubitecan. Clinical pharmacological experiments have proved that it is less toxic than other camptothecin drugs that have been put into clinical use, and its unique advantage is that it is effective when taken orally. According to research reports, animal experiments have shown that it has strong anti-tumor activity on various cancer cells, especially on pancreatic cancer, ovarian cancer, and prostate cancer. It is expected to become a specific drug for the treatment of pancreatic cancer, ovarian cancer and prostate cancer. At present, the US Supergen ...

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
IPC IPC(8): A61K9/107A61K9/48A61K31/337A61K31/4745A61K45/00A61K47/32A61K47/34A61K47/38A61K47/40A61K47/44A61P35/00A61K47/26
Inventor 沙先谊吴娟方晓玲
Owner FUDAN UNIV
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