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Thermosensitive gel for ropivacaine long-acting injection and preparation method thereof

A temperature-sensitive gel and ropivacaine technology, which is applied in the direction of medical preparations of non-active ingredients, pharmaceutical formulas, active ingredients of heterocyclic compounds, etc., can solve problems such as unsatisfactory drug release speed, residual organic solvents, and complicated preparation processes , to achieve the effects of easy diffusion, high encapsulation efficiency and simple preparation process

Active Publication Date: 2018-05-04
WUHAN GENERAL HOSPITAL OF GUANGZHOU MILITARY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] In order to prolong the administration interval of ropivacaine and reduce the inconvenience and potential safety hazards caused by catheter indwelling, the existing slow-release technology of ropivacaine has complicated preparation process, residual organic solvent, low encapsulation efficiency, and low release rate. In order to avoid problems such as unsatisfactory drug speed, the invention provides a thermosensitive gel for ropivacaine long-acting injection

Method used

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  • Thermosensitive gel for ropivacaine long-acting injection and preparation method thereof
  • Thermosensitive gel for ropivacaine long-acting injection and preparation method thereof
  • Thermosensitive gel for ropivacaine long-acting injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Take by weighing PLGA-PEG-PLGA copolymer (the mol ratio of lactide and glycolide=3:1, polyethylene glycol mass percent is 25%, polyethylene glycol number average molecular weight is 1000, Jinan Daigang Biotechnology Co., Ltd. product) 2.5g is placed in a beaker, and 8mL of sodium phosphate buffer solution of pH=8 is added (taking Na 2 HPO 4 12H 2 O5g, NaH 2 PO 4 2H 2 O 0.16g, add water to 1000mL), stir until the polymer is uniformly dispersed, store in a refrigerator at 4°C until the gel is fully swollen, and the PLGA-PEG-PLGA polymer gel solution is obtained. Slowly add 0.15 g of ropivacaine hydrochloride into the fully swollen PLGA-PEG-PLGA polymer gel solution, continue to stir evenly, add dropwise the above-mentioned sodium phosphate buffer solution of pH 8 to the 10 mL mark, and obtain the drug-containing ropivacaine Thermosensitive gel for pivacaine long-acting injection, finally filtered through a 0.2 μm microporous membrane to sterilize.

[0051] The tempe...

Embodiment 2

[0053] Take by weighing PLGA-PEG-PLGA copolymer (the mol ratio of lactide and glycolide=3:1, polyethylene glycol mass percent is 24%, polyethylene glycol number average molecular weight is 1000, Jinan Daigang Biotechnology Co., Ltd. product) 2g is placed in a beaker, and 8mL of sodium phosphate buffer solution of pH=8 is added (take Na 2 HPO 4 12H 2 O15g, NaH 2 PO 4 2H 2 O 0.5g, add water to 1000mL), stir until the polymer is uniformly dispersed, store in a refrigerator at 4°C until the gel is fully swollen, and the PLGA-PEG-PLGA polymer gel solution is obtained. Slowly add 0.15g of ropivacaine hydrochloride into the fully swollen PLGA-PEG-PLGA polymer gel solution, continue stirring evenly, add the above-mentioned sodium phosphate buffer solution dropwise to the 10mL mark, and obtain the drug-containing ropivacaine Thermosensitive gel for long-acting injection, finally filtered through a 0.2μm microporous membrane to sterilize.

[0054] The temperature-sensitive gel for...

Embodiment 3

[0056] Take by weighing PLGA-PEG-PLGA copolymer (the mol ratio of lactide and glycolide=2:1, polyethylene glycol mass percent is 22%, polyethylene glycol number average molecular weight is 1000, Jinan Dai Gang Biotechnology Co., Ltd. product) 1.5g is placed in a beaker, and 8mL of sodium phosphate buffer solution of pH=8 is added (taking Na 2 HPO 4 12H 2 O15g, NaH 2 PO 4 2H 2O 0.5g, add water to 1000mL), stir until the polymer is uniformly dispersed, store in a refrigerator at 4°C until the gel is fully swollen, and the PLGA-PEG-PLGA polymer gel solution is obtained. Slowly add 0.15g of ropivacaine hydrochloride into the fully swollen PLGA-PEG-PLGA polymer gel solution, continue stirring evenly, add the above-mentioned sodium phosphate buffer solution dropwise to the 10mL mark, and obtain the drug-containing ropivacaine Thermosensitive gel for long-acting injection, finally filtered through a 0.2μm microporous membrane to sterilize.

[0057] The temperature-sensitive gel...

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Abstract

The invention discloses a temperature-sensitive gel for ropivacaine long-acting injection and a preparation method thereof. The gel comprises main ingredients ropivacaine, ropivacaine hydrochloride or ropivacaine mesylate; Glycolide molar ratio 2-3:1, PLGA-PEG-PLGA copolymer with PEG molecular weight of 1000, PEG accounts for 18-30% of the total mass of the copolymer; water for injection, normal saline or pH adjustment solution. The preparation method is to fully swell the copolymer in a solvent, add the main drug, and sterilize through a filter membrane. The temperature-sensitive gel is convenient for administration, gels rapidly at body temperature and exerts a slow-release effect. The drug release in vitro is ≤35-45%, 48 hours ≥65%-75%, and 72 hours ≥80%, which is in line with local anesthetics. After a single injection of continuous analgesia 48h design requirements. Pharmacodynamic studies have shown that the ropivacaine temperature-sensitive gel group can significantly prolong the maintenance time of the drug effect, and can continuously exert an analgesic effect for 48 hours.

Description

technical field [0001] The invention relates to a temperature-sensitive gel for ropivacaine long-acting injection and a preparation method thereof. Background technique [0002] Postoperative pain can increase the burden on the cardiovascular system, reduce lung compliance, ventilation function and blood oxygenation function, and induce various complications. If acute postoperative pain cannot be controlled in the initial state, it may develop into chronic pain that lasts for half a year to several years. Effective postoperative analgesia can provide more favorable conditions for the rehabilitation of surgical patients. [0003] Postoperative pain can last for 48-72 hours, and the pain in this time period is the most difficult to control. Local anesthetics are the most direct postoperative analgesic method, but the half-life of clinically used local anesthetics is short, and it takes 4-6 hours One-time administration, at present, the drug effect is mainly maintained through...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K31/445A61K47/34A61P29/00
Inventor 符旭东曾慧琳郭家平刘宏施震
Owner WUHAN GENERAL HOSPITAL OF GUANGZHOU MILITARY
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