Thermo-sensitive self-assembled tri-block copolymer, pharmaceutical composition, and preparation method and application of pharmaceutical composition

A technology of copolymer and triblock, which is applied in the field of temperature-sensitive self-assembled triblock copolymer and pharmaceutical composition and preparation thereof, can solve the problem of difficulty in achieving drug release, limiting the loading of water-insoluble drugs, and poor hydrophilicity of the carrier. and other problems, to achieve the effect of accurate and controllable molecular weight of the product, good application value and good hydrophilic performance

Active Publication Date: 2013-01-02
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for the loading of water-insoluble drugs, since the PEG in the copolymer is a low-molecular-weight block, the hydrophilicity of the carrier is poor, and the micelles formed in water have a small hydrophobic area, which makes it difficult to disperse the water-insoluble drugs evenly, thus affecting the formulation. Appearance, which limits the loading capacity of water-insoluble drugs, and it is also difficult to achieve sustained and stable drug release. Therefore, the application of low-molecular-weight PEG PCL / PEG copolymers as temperature-sensitive carriers is greatly limited in the application of water-insoluble drugs.

Method used

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  • Thermo-sensitive self-assembled tri-block copolymer, pharmaceutical composition, and preparation method and application of pharmaceutical composition
  • Thermo-sensitive self-assembled tri-block copolymer, pharmaceutical composition, and preparation method and application of pharmaceutical composition
  • Thermo-sensitive self-assembled tri-block copolymer, pharmaceutical composition, and preparation method and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: PCL 1050 -PEG 6000 -PCL 1050 Synthesis of Triblock Copolymers

[0044] Configure 0.2 g / mL of stannous octoate toluene solution, weigh 6.0 g of polyethylene glycol with a number average molecular weight of 6000 and 2.1 g of caprolactone after dewatering and purification, add 0.12 mL of stannous octoate toluene solution, and place in a 100 mL circle In a bottom flask under nitrogen protection, react in an oil bath at 130°C for 24 hours.

[0045] After the reaction, the temperature of the flask was lowered to room temperature, and the reaction product was dissolved in 5 mL of anhydrous dichloromethane and then precipitated by magnetic stirring in 150 mL of ether. PCL 1050 -PEG 6000 -PCL 1050 . PCL 1050 -PEG 6000 -PCL 1050 The powder was dissolved in 5 mL of dimethylformamide (DMF), placed in a dialysis bag (MWCO=7000), dialyzed in 1 L of deionized water for 24 hours to remove residual small molecules, and freeze-dried to obtain purified PCL 1050 ...

Embodiment 2

[0048] Example 2: PCL 1250 -PEG 6000 -PCL 1250 Synthesis of Triblock Copolymers

[0049] Take by weighing 6.0 g of polyethylene glycol with a number-average molecular weight of 6000 and 2.5 g of caprolactone after dewatering and purification, add 0.15 mL of stannous octoate toluene solution configured in Example 1., place in a 100 mL round-bottomed flask, Under nitrogen protection, react in an oil bath at 130°C for 24 hours.

[0050] All the other aftertreatments are identical with embodiment 1, make PCL 1250 -PEG 6000 -PCL 1250 Triblock copolymer, yield 93.8%.

[0051] The NMR spectrum of the triblock copolymer is shown in Figure 4 (B), the number average molecular weight of the PCL block can be obtained by NMR calculation.

Embodiment 3

[0052] Example 3: PCL 1350 -PEG 6000 -PCL 1350 Synthesis of Triblock Copolymers

[0053] Take by weighing 6.0 g of polyethylene glycol with a number average molecular weight of 6000 after water removal and purification, and 2.7 g of caprolactone, add 0.17 mL of stannous octoate toluene solution configured in Example 1., place in a 100 mL round-bottomed flask, Under nitrogen protection, react in an oil bath at 130°C for 24 hours.

[0054] All the other aftertreatments are identical with embodiment 1, make PCL 1350 -PEG 6000 -PCL 1350 Triblock copolymer, yield 90.7%.

[0055] The NMR spectrum of the triblock copolymer is shown in Figure 4 (C), the number average molecular weight of the PCL block can be obtained by NMR calculation.

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Abstract

The invention provides a PCLm-PEG6000-PCLm thermo-sensitive self-assembled tri-block copolymer, wherein the copolymer presents two-phase transition characteristics, and can be applied to a controlled release drug delivery system as a drug carrier or can be applied to tissue engineering as a biodegradable material. The invention further provides a pharmaceutical composition containing the tri-block copolymer, and a preparation method and an application of the pharmaceutical composition. A system consisting of PCLm-PEG6000-PCLm tri-block copolymer and water can both load water-soluble drugs, and can efficiently load water-insoluble drugs, and has an excellent controlled-release effect.

Description

technical field [0001] The invention belongs to the field of medical polymer materials, and in particular relates to a temperature-sensitive self-assembled tri-block copolymer and a pharmaceutical composition as well as a preparation method and application thereof. Background technique [0002] In recent years, the use of environment-responsive polymers as drug carriers for smart drug delivery systems has become a research hotspot in the field of pharmacy. These polymers can change their physical or chemical properties with changes in environmental factors such as temperature, pH value, chemical structure, electron intensity, light or pressure. Among them, the temperature-responsive polymer material can be in a solution state at room temperature or slightly higher than body temperature after being dissolved in water, which is convenient for drug loading and administration. When it is injected into the human body, such as subcutaneous injection or intramuscular injection, du...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G63/08C08J3/03A61K47/34A61L27/18A61L27/50
Inventor 邱利焱吕辛怡
Owner ZHEJIANG UNIV
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