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

A kind of irinotecan hydrochloride composition and preparation method thereof

A technology for irinotecan hydrochloride and its composition, which is applied in the field of irinotecan hydrochloride composition and its preparation, can solve the problems of many adverse reactions and limited use, achieve simple and convenient preparation, improve stability, and overcome low encapsulation efficiency Effect

Active Publication Date: 2018-04-27
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the domestically marketed product is irinotecan hydrochloride injection, which has strong anticancer activity, but also has many adverse reactions. The common adverse reactions are anorexia, nausea, vomiting, diarrhea, leukopenia and neutropenia, and anemia And thrombocytopenia, alopecia and acetylcholinergic syndrome, these adverse reactions greatly limit the clinical use of the drug

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
  • A kind of irinotecan hydrochloride composition and preparation method thereof
  • A kind of irinotecan hydrochloride composition and preparation method thereof
  • A kind of irinotecan hydrochloride composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of irinotecan hydrochloride composition:

[0046] Dissolve 2g of soybean lecithin, 1g of cholesterol, and 0.5g of PEG-DSPE with 1.5ml of absolute ethanol sonically, inject it into 20ml of 300mM citric acid buffer (pH=3) preheated to 60°C, stir at high speed to obtain the primary product, and then Homogenize under high pressure 4 times at 20,000 psi, filter and sterilize, and dispense into vials of 2 ml / bottle to obtain a blank lipid nano-preparation (phospholipid concentration is 100 mg / ml).

[0047] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to obtain irinotecan hydrochloride solution.

[0048] Prepare sodium carbonate solution (0.5M), filter and sterilize, then pack in 8ml / bottles into vi...

Embodiment 2

[0052] The preparation of irinotecan hydrochloride composition:

[0053] Weigh 2g of HSPC, 0.2g of cholesterol, 0.3g of PEG-DSPE, and 0.3g of RGD-PEG-DSPE and dissolve them in 2ml of absolute ethanol, inject them into 30ml of 300mM copper sulfate solution, stir at high speed, and then dissolve them with polycarbonate with a pore size of 100nm Extrude the membrane for 4 times, then replace the outer aqueous phase with sucrose solution (300mM) by ultrafiltration (molecular weight of the ultrafiltration tube: 10K), filter and sterilize, and divide into vials of 4ml / bottle to obtain the blank fat Quality nano-preparation (phospholipid concentration of 50mg / ml).

[0054] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to o...

Embodiment 3

[0059] The preparation of irinotecan hydrochloride composition:

[0060] Weigh 2g of DSPC, 0.8g of cholesterol, 0.1g of FA-PEG-DSPE, and 0.2g of PEG-DSPE, dissolve them ultrasonically in 1.6ml of absolute ethanol, inject into 40ml of sbe-CD triethylamine solution (250mM), stir at high speed, and then The polycarbonate film of 100nm pore size was extruded 4 times, and the obtained preparation was dialyzed in normal saline for 24h, and after filtering and sterilizing, it was divided into vials at 4ml / bottle to obtain a blank lipid nano-preparation (the concentration of phospholipids was 50mg / ml).

[0061] Weigh 200mg of irinotecan hydrochloride (cpt-11), 9mg of lactic acid, and 450mg of sorbitol, add 20ml of water for injection to dissolve it ultrasonically, adjust the pH to 3-4 with hydrochloric acid (0.1M), and pack in 2ml / bottle in an anatomy , and then sterilized under high pressure at 121°C for 30 minutes to obtain irinotecan hydrochloride solution.

[0062] Prepare sodi...

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention relates to an irinotecan hydrochloride composition. It includes a blank lipid nano-preparation, irinotecan hydrochloride solution and pH adjustment solution; the blank lipid nano-preparation, irinotecan hydrochloride solution and pH adjustment solution are individually packaged, and the three components are mixed and incubated before clinical use. Actively loaded drugs are made into clinical drug-loaded nano-preparations. The present invention adopts the design of three bottles of independent packaging, and the medicine is not loaded into the lipid nano-preparation during the storage process, so the preparation does not have the problem of easy leakage of the existing preparation medicine, which greatly improves the stability of the preparation; before clinical use, The three components are mixed and incubated to make a drug-loaded nano-preparation, which is simple and convenient for clinical use. The invention also relates to a preparation method of the irinotecan hydrochloride composition, the preparation process is simple, the quality is easy to control, and it is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an irinotecan hydrochloride composition and a preparation method thereof. Background technique [0002] Irinotecan hydrochloride (1rinotecan, CPT-11) is a semi-synthetic water-soluble camptothecin derivative and an inhibitor of DNA topoisomerase I (Topo I). Irinotecan and its active metabolite SN-38 cause DNA single-strand breaks through the stable combination with the DNA-Topo-1 complex, resulting in irreversible damage to the DNA and death. Irinotecan is an effective drug for the treatment of metastatic colorectal cancer. It is still effective for fluorouracil-resistant cases and has a broad anti-tumor spectrum. Phase I and Phase II clinical research results show that the drug has a positive effect on chemotherapy-resistant tumors, such as non-small cell lung cancer, ovarian cancer and cervical cancer; Breast cancer, small cell lung cancer, skin cancer, ...

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 Patents(China)
IPC IPC(8): A61K9/00A61K31/4745A61K47/36A61K47/26A61K47/24A61P35/00
Inventor 李亚平陈伶俐樊继涛顾王文张志文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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