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Local analgesic drug entrapped near-infrared response lipid temperature-sensitive gel

A temperature-sensitive gel and near-infrared technology, which is applied in liposome delivery, drug photolysis in vivo, drug combination, etc., can solve problems such as short half-life, reduce toxic side effects, increase analgesic concentration, and relieve pain. clear effect

Active Publication Date: 2021-11-19
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Traditional local anesthetic preparations are injectable, but they still have limitations as a monotherapy, such as a relatively short half-life

Method used

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  • Local analgesic drug entrapped near-infrared response lipid temperature-sensitive gel
  • Local analgesic drug entrapped near-infrared response lipid temperature-sensitive gel
  • Local analgesic drug entrapped near-infrared response lipid temperature-sensitive gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh DSPC, Egg PC, cholesterol, Rop and PdPC(OBu)8 and ultrasonically disperse them in 1 mL of polar organic solvent at a mass ratio of 2:7:2:2:0.09 as the oil phase, and the oil phase solution is stirred under magnetic force Inject uniformly into 10mL PBS as the water phase within 40 s, stir at room temperature for 30 min to evaporate the solvent, and obtain a liposome solution; the concentration (w / v) is 2% chitosan (CS) 0.1M / v) is a 55% aqueous solution of β-glycerophosphate (β-GP) at a volume ratio of 3:1, mixed in an ice bath, and stirred for 30 minutes to obtain a gel matrix; the concentration (w / v ) into the 40% liposome solution, add the gel matrix, and stir evenly for 30 minutes to obtain.

Embodiment 2

[0030] Weigh DOPC, Egg PC, cholesterol, Rop and PdPC(OBu)8 and ultrasonically disperse them in 1 mL of polar organic solvent at a mass ratio of 2:7:2:2:0.09 as the oil phase, and put the oil phase solution under magnetic stirring Inject uniformly into 10mL PBS as the water phase within 40 s, stir at room temperature for 30 min to evaporate the solvent, and obtain a liposome solution; the concentration (w / v) is 2% chitosan (CS) 0.1M / v) is 55% β-glycerophosphate sodium (β-GP) aqueous solution at a volume ratio of 5:1, mixed under ice bath conditions, and stirred for 30 minutes to obtain a gel matrix; the concentration (w / v ) into the 40% liposome solution, add the gel matrix, and stir evenly for 30 minutes to obtain.

Embodiment 3

[0032] Weigh DLPC, Egg PC, cholesterol, Rop and PdPC(OBu)8 and ultrasonically disperse them in 1 mL of polar organic solvent at a mass ratio of 2:7:2:2:0.09 as the oil phase, and the oil phase solution is stirred under magnetic force Inject uniformly into 10mL PBS as the water phase within 40 s, stir at room temperature for 30 min to evaporate the solvent, and obtain a liposome solution; the concentration (w / v) is 2% chitosan (CS) 0.1M / v) is 55% β-glycerophosphate sodium (β-GP) aqueous solution at a volume ratio of 7:1, mixed under ice bath conditions, and stirred for 30 minutes to obtain a gel matrix; the concentration (w / v ) into the 40% liposome solution, add the gel matrix, and stir evenly for 30 minutes to obtain.

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Abstract

The invention discloses a local analgesic drug entrapped near-infrared response lipid temperature-sensitive gel, which can reduce and eliminate the toxic and side effects of the existing temperature-sensitive gel, prolong the slow release period, realize responsiveness and adjustable release, enable a patient to autonomously adjust the administration, greatly improve the treatment effect of pain and reduce the compliance of the patient. The composite drug delivery system is of a grid structure, the liposome is embedded in the system, the average particle size ranges from 150 nm to 200 nm, and the potential is about -2.88 mV; singlet oxygen is generated under the action of near infrared rays, so that a light response release behavior can be realized; the release behavior is first sudden release and then slow release, the slow release effect is obvious, meanwhile, near-infrared response can be achieved, the release rate is increased, and the analgesic concentration of ropivacaine is increased within a certain period of time.

Description

technical field [0001] The invention provides a near-infrared-responsive lipid body temperature-sensitive gel loaded with local analgesic drugs. The invention also discloses a preparation method thereof, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Pain is a common complaint after surgery. According to the duration and nature of pain, pain can be divided into acute and chronic. There are two main types of commonly used pain relief methods: drug and non-drug treatments. Non-drug treatments are mostly used in combination with other treatments, and can also be used alone for some mild symptoms of pain or discomfort. Common analgesic drugs in drug therapy include opioid analgesics, nonsteroidal anti-inflammatory drugs, and other adjuvant drugs. Among them, opioids are currently found to be the strongest analgesic drugs, mainly used for acute pain, moderate to severe pain, but opioids mainly come from the alkaloids and thei...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/06A61K9/127A61K31/167A61K31/245A61K31/445A61K41/00A61K47/24A61K47/28A61K47/36A61P23/02
CPCA61K41/0042A61K45/06A61K31/445A61K31/167A61K31/245A61K9/06A61K9/127A61K47/36A61K47/24A61K47/28A61P23/02A61K2300/00
Inventor 刘文华孟翔雪张释心孙凤英
Owner JILIN UNIV
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