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Thermal gel controlled-release injection of platinum-containing antitumor drug and preparation method of thermal gel controlled-release injection

A technology for sustained-release injections and anti-tumor drugs, which can be used in anti-tumor drugs, medical preparations with non-active ingredients, drug combinations, etc.

Inactive Publication Date: 2015-02-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its hydrophilicity, platinum drugs will be released quickly if they are directly physically encapsulated in hydrogel, and have obvious burst release phenomenon, it is difficult to maintain a sufficient drug concentration in the body for a long time, so the ideal design The drug sustained release system is extremely challenging

Method used

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  • Thermal gel controlled-release injection of platinum-containing antitumor drug and preparation method of thermal gel controlled-release injection
  • Thermal gel controlled-release injection of platinum-containing antitumor drug and preparation method of thermal gel controlled-release injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1 Add 22.5 g MPEG (750) into a 250 mL three-neck flask, heat the oil bath to 130 °C, and vacuumize for 3 h while stirring to remove the water in MPEG, then add 47.6 g D,L-lactide (LA) and 60 mg stannous octoate (containing a small amount of toluene), the temperature of the oil bath was raised to 150 °C, and the reaction was continued for 12 h under an argon atmosphere. After the reaction is completed, vacuumize for 3 h to remove unreacted monomers and low-boiling products, pour out the reaction product while it is hot, wash it in water at 80 °C for several times, and then freeze-dry it to obtain an MPEG-PLA diblock copolymer (Copolymer-PLA). 1), the yield was about 85%, and it was stored at -20 ℃. The number-average and weight-average molecular weights of the diblock copolymers were determined by gel permeation chromatography (GPC) (using dimethylformamide (DMF) as the mobile phase and polymethyl methacrylate (PMMA) as the standard sample) ( M n , M w ) w...

Embodiment 2

[0070] Example 2 Add 22.5 g PEG (600) into a 250 mL three-neck flask, heat the oil bath to 130 °C, and vacuumize for 3 h while stirring to remove the water in the PEG, then add 42.0 g D,L-lactide (LA), 5.6 g glycolide (GA) and 60 mg stannous octoate (containing a small amount of toluene), the temperature of the oil bath was raised to 150 °C, and the reaction was continued for 12 h under an argon atmosphere. After the reaction is complete, vacuumize for 3 h to remove unreacted monomers and low-boiling products, pour out the reaction product while it is hot, dissolve it in dichloromethane solution, and then precipitate it with ether. The yield is about 85%. The product PLGA-PEG-PLGA triblock copolymer (Copolymer-3) was stored at -20 °C. Measure the number average and weight average molecular weight ( M n , M w ) were 1570 and 2120, respectively, and the molecular weight distribution coefficient ( M w / M n ) is 1.35.

Embodiment 3

[0071] Example 3 Add 15.0 g of MPEG (750) into a 250 mL three-neck flask, and vacuumize for 3 h at 130 °C while stirring to remove the water contained therein. Add 29.0 g caprolactone (CL) and 80 mg stannous octoate (containing a small amount of toluene), and react at 140 °C for 24 h under an argon atmosphere. After the reaction, vacuumize for 3 h to remove unreacted monomers and low-boiling products, then dissolve the initial product in dichloromethane solution, and then precipitate with ether, the yield is about 80%. The product MPEG-PCL diblock copolymer (Copolymer-5) was stored at -20°C. Measure the number average and weight average molecular weight ( M n , M w) are 1830 and 2520, respectively, and the molecular weight distribution coefficient ( M w / M n ) is 1.38.

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Abstract

The invention belongs to the field of new chemically synthesized drugs and medical preparations thereof, particularly discloses a thermal gel controlled-release injection of a platinum-containing antitumor drug and a preparation method of the thermal gel controlled-release injection. The thermal gel controlled-release injection consists of Pt(IV)-containing amphipathic segmented copolymer and a solvent, wherein the water system can generate phase transformation of thermal gelation with temperature rise to spontaneously form physical hydrogel; the bonded Pt(IV) complex is easily reduced into Pt(IV); the amphipathic segmented copolymer consists of a hydrophilic block and a hydrophobic block which can be degraded into polyester, wherein a functional group is connected at the terminal of the block copolymer. The controlled-release gel preparation disclosed by the invention can be used for prolonging the release period of the platinum antitumor drugs. By virtue of an injection way, the preparation is dosed in tumor, around tumor or in a postoperative tumor cavity; after the preparation is gelled in situ in the body, the bonded platinum drugs can be slowly released from the gel, so that the dosing frequency and the whole body toxic and side effects are lowered.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmaceutical preparations, and specifically relates to a thermotropic gel sustained-release injection of Pt (IV) antitumor drugs and a preparation method thereof. Background technique [0002] Cancer is one of the major killers that endanger human life and health. Up to now, surgery plus chemotherapy is still the main means of treating cancer. Traditional chemotherapy drugs often have serious side effects, and the effective concentration actually reaching the tumor site is low. Therefore, improving the enrichment of drugs in tumor sites to enhance the effect of chemotherapy is a current research hotspot. Among them, local tumor administration can artificially and passively target the drug to the tumor site, so that the local tumor concentration can be maintained at a high level, thereby improving the therapeutic effect and reducing systemic toxicity. [0003] Cisplatin (cis-dichlorodiammine ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/06A61K31/282A61K31/34A61P35/00
Inventor 丁建东俞麟沈文佳
Owner FUDAN UNIV
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