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Temp-sensitive, slow-releasing gel used for local injection, and its prepn. method

A slow-release gel and local injection technology, which is applied in the field of medicine, can solve problems such as incompatibility of infusion equipment, severe allergic reactions, and side effects of the gastrointestinal tract, and achieve the advantages of convenient administration, simple preparation process, and improved stability Effect

Inactive Publication Date: 2006-11-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many problems in this preparation, such as poor stability after dilution, severe allergic reactions, and incompatibility with infusion equipment made of polyoxyethylene, etc.
Similar to paclitaxel, non-steroidal anti-inflammatory drugs have very low solubility in water, and long-term use of non-steroidal anti-inflammatory drugs may cause serious gastrointestinal side effects

Method used

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  • Temp-sensitive, slow-releasing gel used for local injection, and its prepn. method
  • Temp-sensitive, slow-releasing gel used for local injection, and its prepn. method
  • Temp-sensitive, slow-releasing gel used for local injection, and its prepn. method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A PLGA-PEG-PLGA copolymer with a molecular weight of 4800 and a molar ratio of lactide and glycolide of 6 / 1 was dissolved in water, and prepared into solutions with concentrations of 15%, 17%, 23%, and 25%, respectively, and measured The gelling temperature of the copolymer solution. When the temperature rises, the copolymer solution shows the change of solution-gel-solution in turn, and its gelation temperature is between 30 and 37°C, and it can form a gel at body temperature (see figure 1 ).

Embodiment 2

[0027]Indomethacin, paclitaxel and PLGA-PEG-PLGA copolymer were dissolved in an organic solvent, and after the solvent was evaporated to dryness under reduced pressure, distilled water was added to dissolve. Indomethacin and paclitaxel are hydrophobic drugs and are barely tolerated in water. However, the solubility in 25% polymer solution was 13.7 mg / ml and 12.6 mg / ml, respectively. And after 3 months of storage, there are more than 90% of the original drug, and the stability of the drug is better.

Embodiment 3

[0029] The paclitaxel and PLGA-PEG-PLGA copolymer are dissolved in an organic solvent, evaporated to dryness, and then added water to prepare a concentration of 20%. Take 1ml of the copolymer solution, and after the gel is formed, add 3ml of phosphate buffer solution as the release medium. Sampling at 1, 4, 8, 12, 24 hours, then every 24 or 48 hours. Paclitaxel can be released continuously for about 30 days in vitro.

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Abstract

A temp-sensitive slow-release gel for local injection features that when its temp is lower than that of human body, it exists in liquid state and after it is injected into human body, it becomes gel for slowly releasing its medicine component. Its preparing process includes such steps preparing the temp-sensitive polymer as carrier from PLGA-PEG-PLGA block copolymer, PEG-PLGA-PEG block copolymer and poloxamer, dissolving it in water, and dissolving or dispersing the medicine in said aqueous solution.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a temperature-sensitive slow-release gel for local injection and a preparation method for local, joint cavity, parenteral and subcutaneous injection administration. Background technique [0002] In recent years, the sustained and controlled release drug delivery system for injections has developed rapidly. This drug delivery system has the following advantages: (1) Eliminate the peak-valley phenomenon caused by intermittent drug administration and uneven drug dosage, and achieve a near-constant rate. Sustained drug release and maintenance of therapeutic concentration, avoiding toxic and side effects caused by excessive drug concentration; (2) Because the injection route does not go through the gastrointestinal absorption process and the first-pass effect of the liver, the bioavailability is high and individual differences are small (3) It can be implanted at a fixed p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K45/00A61K47/10A61K47/34A61P23/00A61P29/00A61P35/00
Inventor 乔明曦陈大为赵秀丽
Owner SHENYANG PHARMA UNIVERSITY
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