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A thermotropic gel sustained-release injection for combined administration and preparation method thereof

A slow-release injection and thermogenic gel technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of lack of interaction and achieve a significant sustained-release effect Effect

Active Publication Date: 2020-01-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the contrary, the loading of taxanes in pure amphiphilic block copolymer thermotropic hydrogels neither affects the phase transition temperature of the amphiphilic block copolymer thermotropic hydrogels, nor changes the carrier condensation temperature. Glue strength, revealing lack of above-mentioned interactions between drug and carrier

Method used

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  • A thermotropic gel sustained-release injection for combined administration and preparation method thereof
  • A thermotropic gel sustained-release injection for combined administration and preparation method thereof
  • A thermotropic gel sustained-release injection for combined administration and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1, 15 g of MPEG (750) was added to a 250 mL three-necked flask, heated in an oil bath to 130°C, and vacuumed for 3 h while stirring to remove water in the MPEG, and then 28.2 g of D,L-lactide ( LA) 3.8g lactide and 40 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 point products, pour out the reaction product while it is hot, wash it in 80°C water for several times, and then freeze-dry to obtain an MPEG-PLGA diblock copolymer (Copolymer- 1), the yield is about 70%, and it is stored at -20°C. 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) ( ...

Embodiment 2

[0075] 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 oil bath was heated 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

[0076] Example 3, 15.0 g of MPEG (750) was added into a 250 mL three-neck flask, and vacuumized at 130°C for 3 h 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 technical field of pharmaceutical preparations and particularly discloses a combinative-administration thermotropic gel sustained-release injection and a preparation method thereof. The thermotropic gel sustained-release injection is composed of a Pt(IV)-containing amphipathic segmented copolymer, taxane drugs and a solvent. By thermotropic gelatinization phase transformation along with temperature rise, physical hydrogel is formed spontaneously; the amphipathic segmented copolymer is formed by polyethylene glycol serving as a hydrophilic segment and degradable polyester serving as a hydrophobic segment, and functional groups can be connected to the tail end of the segmented copolymer. The gel sustained-release injection has advantages that release periods of platinum type antitumor drugs and taxane drugs can be remarkably prolonged, and synergistic release of the platinum type antitumor drugs and the taxane drugs can be realized; the injection is availablefor intratumoral, peritumoral and postoperation intralesional application by means of injection, and after in-vivo in-situ gelatinization of the injection, the bonded platinum type drugs and the coated taxane drugs can be slowly released from gel, and accordingly administration frequency and whole-body toxic and side effects can be reduced.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmaceutical preparations, and in particular relates to a thermotropic gel sustained-release injection and a preparation method thereof. Background technique [0002] Chemotherapy is one of the most common means of treating cancer. Because the pathogenesis of cancer is usually very complicated, it is often difficult to achieve the desired curative effect only by relying on a single anticancer drug for chemotherapy. Not only the drug utilization rate is low, the side effects are serious, but also drug resistance is easy to develop. Combination chemotherapy can exert synergistic interaction by using two or more drugs with different anti-cancer mechanisms, and has better therapeutic effect, lower dosage, and less toxic side effects than single-drug chemotherapy. Can overcome drug resistance. At present, various technical schemes of combined chemotherapy have been applied to the treatment of vari...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K47/59A61K47/58A61K47/69A61K9/06A61K33/243A61K31/555A61K31/337A61K31/282A61P35/00A61P7/04
CPCA61K9/0019A61K9/06A61K31/282A61K31/337A61K31/555A61K33/24A61K2300/00
Inventor 俞麟丁建东
Owner FUDAN UNIV
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