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Injectable hydrogel preparation of pegylated medicament

A technology of polyethylene glycol and hydrogel, which is applied in the direction of pharmaceutical formulation, drug delivery, and medical preparations of non-active ingredients, etc., to achieve the effect of easy use

Inactive Publication Date: 2007-05-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Injectable hydrogel preparation of pegylated medicament
  • Injectable hydrogel preparation of pegylated medicament

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Add 20g of polyethylene glycol (PEG, number average molecular weight 1500) into a 250ml three-necked flask, heat the oil bath to 150°C, and vacuum filter for three hours under stirring to remove the residual moisture in the PEG, and then add a molar ratio of 10 : 1 lactide (37.7g) and glycolide (3.0g), after heating under vacuum to make it melt completely, add 100μl of stannous octoate, the oil bath is heated up to 160 ℃, and continue to react under an argon atmosphere for 8 Hour. After the reaction was completed, vacuum filtration was performed for two hours to remove unreacted monomers and low-boiling products. Then dissolve the initial product in cold water (5°C-8°C). After it is completely dissolved, the solution is heated to 80°C. The product precipitates, and the upper solution is removed. Repeat the above steps once to obtain the product. The remaining water is frozen It was removed by drying with a yield of about 85%. pass 1 H-NMR determination of PLGA copoly...

Embodiment 2

[0040] Add 20g of polyethylene glycol (PEG, 1500) into a 250ml three-necked flask, then add 31.2g of DL-lactide and 6.3g of glycolide, heat it under vacuum to make it melt completely, add 100μl of stannous octoate, and put it in an oil bath The temperature was raised to 160° C., and the reaction was continued for 8 hours under an argon atmosphere. After the reaction was completed, vacuum filtration was performed for two hours to remove unreacted monomers and low-boiling products. Then dissolve the initial product in cold water (5°C-8°C). After it is completely dissolved, the solution is heated to 80°C. The product precipitates, and the upper solution is removed. Repeat the above steps once to obtain the product. The remaining water is frozen It was removed by drying with a yield of about 85%. Then under argon atmosphere, in 250ml there-necked flask, add the block copolymer of 10g, after 100ml dichloromethane solution dissolves, add equimolar succinic anhydride and anhydrous p...

Embodiment 3

[0042] The gelation behavior of the block copolymer in Example 1 in aqueous solutions with different concentrations was studied. Copolymer aqueous solutions with different weight percent concentrations from 10% to 30% were prepared, and the viscosity changes between 0°C and 60°C were measured. Gelation was defined by observing that no flow occurred within 30 seconds when the tube was inverted. Figure 1 is the phase diagram of the block copolymer in Example 1 with different concentrations of aqueous solution as the temperature changes. The reversibility of its gelation process can be clearly seen, and its gelation at human body temperature is very useful for injectable drug sustained-release systems.

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Abstract

The invention relates to a method for preparing injection aquagel agent which packs PEG drug, wherein said PEG drug is obtained by combining PEG decorator onto original drug molecule via covalence reaction; the carrier packing the drug is the mixture of degradable polymer and water; said degradable polymer is block copolymer or derivant whose hydrophilic section is PEG and hydrophobic section is degradable polyester. The inventive aquagel agent is fluid under body temperature; and it is gel at body temperature. It can be injected to release PEG drug for several days or several months.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and biological materials, and in particular relates to an injectable hydrogel preparation encapsulating polyethylene glycol (PEG) drugs and a preparation method thereof. Background technique [0002] In recent decades, pharmaceutical research has made great progress, especially through organic synthesis or genetic engineering, many striking new physiologically active substances have been obtained, and these drugs provide protection for human health and happiness. But medicines all have certain toxic and side effects, only when the blood drug concentration is maintained between the minimum effective concentration and the toxic concentration, the medicine can exert its drug effect. Therefore, when a new drug substance is successfully developed, it is necessary to develop a suitable route of administration and dosage form in order to maximize its therapeutic effect. [0003] Trad...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/48A61K47/34A61K47/59A61K47/60
Inventor 丁建东俞麟
Owner FUDAN UNIV
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