Temperature-sensitive gel containing ropivacaine and used for long-acting injection and preparation method of temperature-sensitive gel

A technology of ropivacaine and thermosensitive gel, applied in the field of thermosensitive gel for ropivacaine long-acting injection and its preparation, can solve the problems of unsatisfactory drug release speed, complicated preparation process, organic solvent residue, etc., and achieve easy diffusion out, the preparation process is simple, and the effect of high encapsulation efficiency

A technology of ropivacaine and thermosensitive gel, applied in the field of thermosensitive gel for ropivacaine long-acting injection and its preparation, can solve the problems of unsatisfactory drug release speed, complicated preparation process, organic solvent residue, etc., and achieve easy diffusion out, the preparation process is simple, and the effect of high encapsulation efficiency

CN104606129AActive Publication Date: 2015-05-13WUHAN GENERAL HOSPITAL OF GUANGZHOU MILITARY
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  • Temperature-sensitive gel containing ropivacaine and used for long-acting injection and preparation method of temperature-sensitive gel
  • Temperature-sensitive gel containing ropivacaine and used for long-acting injection and preparation method of temperature-sensitive gel
  • Temperature-sensitive gel containing ropivacaine and used for long-acting injection and preparation method of temperature-sensitive gel

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 temperature-sensitive gel containing ropivacaine and used for long-acting injection and a preparation method of the temperature-sensitive gel. The gel comprises a main drug ropivacaine, ropivacaine hydrochloride or ropivacaine mesylate, a PLGA (poly (lactic-co-glycolic acid)) -PEG (polyethylene glycol)-PLGA copolymer as well as water, normal saline or pH regulation solution for injection, wherein the mole ratio of lactide to glycolide is (2-3): 1, and the PEG molecular weight of the PLGA-PEG-PLGA copolymer is 1,000. The preparation method comprises the following steps: the copolymer is sufficiently swelled in a solvent firstly, then the main drug is added, and sterilization is performed through a filter membrane. The temperature-sensitive gel facilitates drug delivery and can gel rapidly at human body temperature so as to play a slow release role, smaller than or equal to 35%-45% of the drug is released in vitro after 12 h, larger than or equal to 65%-75% of the drug is released after 48 h, larger than or equal to 80% of the drug is released after 72 h, and the design requirement for postoperative continuous analgesia for 48 h through single injection of a local anesthesia drug is met. Pharmacodynamics study shows that a temperature-sensitive gel group containing ropivacaine can prolong the efficacy maintaining time remarkably and continuously play 48 h analgesic effect.

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

Patent Timeline
13 May 2015
Publication
CN104606129A
IPC
A61K9/06; A61K31/445; A61K47/34; A61P29/00
Inventors
符旭东; 曾慧琳