Capecitabine medicine carrier and preparation method thereof

A drug and carrier technology, applied in the field of capecitabine drug carrier and its preparation, can solve the problems of normal cell damage, frequent drug use, and long duration of the process, so as to maintain the activity of the drug, increase the circulation time in the body, and improve the utilization rate effect

Active Publication Date: 2014-12-31
广州智焜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the enzyme that activates 5-FU is not selective, it has greater damage to normal cells
Lu Ningning and others treated capecitabine alone or in combination with other drugs for cancer patients. Although the cancer treatment effect was stable and objectively relieved, the medication was frequent and the process lasted for a long time, and some diarrhea, moderate Adverse reactions such as granulocytopenia and nausea and vomiting

Method used

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  • Capecitabine medicine carrier and preparation method thereof
  • Capecitabine medicine carrier and preparation method thereof
  • Capecitabine medicine carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] (1) Synthesis of carboxyl-terminated polyethylene glycol

[0047] Dissolve 10.000g of polyethylene glycol (molecular mass: 2000Da), 0.502g of succinic anhydride in 30mL of dry chloroform, then add 1.151g of EDC·HCl, 0.122g of DMAP and 51uL of triethylamine. Stir the reaction at room temperature for 12h, then rotevaporate at 52°C to remove chloroform to obtain a residue; dissolve the residue in 35mL saturated NaHCO 3 , remove the white insoluble matter by suction filtration under reduced pressure; take the filtrate and wash it with 20mLCHCl 3 Extract the filtrate 3 times, take the water phase, adjust the pH to 2 with 0.1mol / L HCl, then transfer to a separatory funnel, add 20mL CHCl 3 Extract 3 times, combine extracts, add 1.200g anhydrous Na 2 SO 4 Dry until clarified, filter, take the filtrate, concentrate to about 3mL by rotary evaporation at 52°C, add 60mL of anhydrous ether to crystallize, put in the refrigerator at -4°C for 24 hours, filter, and vacuum dry at 25°...

Embodiment 2

[0073] (1) Synthesis of carboxyl-terminated polyethylene glycol

[0074] Dissolve 10.000g of polyethylene glycol (molecular mass: 4000Da), 0.625g of succinic anhydride in 30mL of dry chloroform, then add 0.575g of EDC·HCl, 0.061g of DMAP and 26uL of triethylamine. Stir the reaction at room temperature for 12h, then rotevaporate at 52°C to remove chloroform to obtain a residue; dissolve the residue in 35mL saturated NaHCO 3 , remove the white insoluble matter by suction filtration under reduced pressure, and take the filtrate; use 20mLCHCl 3 Extract the filtrate 3 times, take the water phase, adjust the pH to 2 with 0.1mol / L HCl, then transfer to a separatory funnel, add 20mL CHCl 3 Extract 3 times, combine extracts, add 1.200g anhydrous Na 2 SO 4 Dry until clarified, filter, take the filtrate, concentrate to about 3mL by rotary evaporation at 52°C, add 60mL of anhydrous ether to crystallize, put in the refrigerator at -4°C for 24 hours, filter, and vacuum dry at 25°C to obt...

Embodiment 3

[0099] (1) Synthesis of carboxyl-terminated polyethylene glycol

[0100] Dissolve 10.000g of polyethylene glycol (molecular mass: 10000Da), 0.301g of succinic anhydride in 30mL of dry chloroform, then add 0.288g of EDC·HCl, 0.122g of DMAP and 50uL of triethylamine. The reaction was stirred at room temperature for 12 h, then 53 ° C rotary evaporation, chloroform was removed to obtain a residue; the residue was dissolved in 25 mL saturated NaHCO 3 , remove the white insoluble matter by suction filtration under reduced pressure, and take the filtrate; use 20mLCHCl 3 Extract the filtrate 3 times, take the water phase, adjust the pH to 2 with 0.1mol / L HCl, then transfer to a separatory funnel, add 20mL CHCl 3 Extract 3 times, combine extracts, add 5g anhydrous Na 2 SO 4 Dry until clarified, filter, take the filtrate, concentrate to about 3mL by rotary evaporation at 53°C, add 60mL of anhydrous ether to crystallize, put in the refrigerator at -4°C for 24 hours, filter, and vacuum...

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Abstract

The invention discloses a capecitabine medicine carrier and a preparation method of the capecitabine medicine carrier. According to the capecitabine medicine carrier and the preparation method of the capecitabine medicine carrier, capecitabine is connected with macromolecule with good biocompatibility (BC), two hydroxyl functional groups exist in a cytidine structure in a capecitabine molecule, one of the two hydroxyl functional groups shows certain activity due to small steric hindrance, an esterification reaction occurs between the one hydroxyle functional group and an activated carboxyl compound under alkaline condition when the one hydroxyle functional group is catalyzed through catalyzer, and the capecitabine is connected with an amphipathicity compound in a chemical bonding mode to form an amphipathicity compound with one end hydrophobic and the other end hydrophilic. The amphipathicity compound with one end hydrophobic and the other end hydrophilic can be used for preparation of medicine carrying microspheres or medicine carrying nanoparticles. When the other end of a macromolecular compound connected with medicine is connected with monoclonal antibody (McAb), folic acid, transferring and the like which have tumor targeting functions, the macromolecular compound can leads the medicine to focus on a tumor position, medicine burst release is reduced, released medicine can also be compensated at a medicine release later stage, and the medicine release can be kept at a moderate level for a long time.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and in particular relates to a capecitabine drug carrier and a preparation method thereof. Background technique [0002] Capecitabine (trade name: Xeloda) is an oral cytotoxic preparation with selective effects on tumor cells, and it is a new prodrug of 5-fluorouracil (5-FU) developed by Roche, Switzerland . As a prodrug, capecitabine itself is inactive and has targeting properties to tumor tissues, and its metabolically generated active substance has a higher concentration than other tissues and plasma, and can be administered orally. It is a safe, effective, economical and adaptable drug. Strong antitumor drug. Due to the wide application and good curative effect of capecitabine, its clinical application and research have become a hot topic in recent years. Among them, capecitabine is used as a single drug or in combination with other drugs such as paclitaxel and doxorubicin to tr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/7068A61P35/00C08G81/00C08G65/48
Inventor 魏坤彭小敏
Owner 广州智焜生物科技有限公司
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