Narcotic analgesic-loaded sustained-release microsphere and preparation method thereof and application thereof

A technology for sustained-release microspheres and analgesics, which is applied in anesthetics, pharmaceutical formulations, antipyretics, etc., can solve the problems of easy agglomeration and aggregation, difficulty in summarizing the release cycle, and high preparation costs, so as to ensure repeatability. , the effect of reducing drug escape and facilitating stability

Active Publication Date: 2018-12-18
INST OF PROCESS ENG CHINESE ACAD OF SCI +2
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (1) Due to the limitation of preparation technology (stirring, spraying, etc.), the particle size of the obtained narcotic analgesic microspheres is not uniform, resulting in poor repeatability between different batches, which interferes with subsequent research and drug efficacy, and the release cycle is difficult. Summarize the rules and make precise control;
[0008] (2) In the existing method, due to the instability of the system temperature during the preparation process, the molecular Brownian motion is intensified, causing a large number of drug molecules to escape;
[0009] (3) In the existing method, in order to reduce the escape of drug molecules to the water phase and improve the embedding rate, the water phase needs to be supersaturated with drugs in advance, resulting in high preparation costs;
[0010] (4) During the formation of drug-loaded

Method used

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  • Narcotic analgesic-loaded sustained-release microsphere and preparation method thereof and application thereof
  • Narcotic analgesic-loaded sustained-release microsphere and preparation method thereof and application thereof
  • Narcotic analgesic-loaded sustained-release microsphere and preparation method thereof and application thereof

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[0069] The invention also discloses a preparation method of sustained-release microspheres containing anesthetic and analgesics, which comprises the following steps:

[0070] Step A: Dissolve the stabilizer in water to form an aqueous phase (W), and add alkali or alkaline buffer to adjust the pH of the aqueous phase according to the acid dissociation constant (pKa value) of the selected narcotic analgesic molecule;

[0071] Step B, dissolving the degradable polymer material and anesthetic analgesics in at least one organic solvent to form an oil phase (O);

[0072] Step C: Inject the oil phase (O) obtained in step B into the water phase (W) obtained in step A for emulsification preparation to form an O / W pre-emulsion;

[0073] Step D, passing the O / W pre-emulsion obtained in step C through the microporous membrane with pressure to form a uniform O / W emulsion;

[0074] In step E, the O / W emulsion obtained in step D is volatilized and solidified under vacuum and negative pressure to obtai...

Example Embodiment

[0107] Example 1

[0108] A hydrophilic porous membrane with a pore size of 32 μm and a uniform pore size is soaked in water to fully wet the porous membrane. Dissolve 100 mg of ropivacaine free base with a concentration of 20 mg / mL after alkalization of ammonia in 5 mL of dichloromethane as the oil phase, and at the same time, 1 g of molecular weight of 20,000 (polylactic acid: polyglycolic acid = 50:50) The polylactic acid-polyglycolic acid copolymer (PLGA) is dissolved in the oil phase. Dissolve 1 g of polyvinyl alcohol (PVA) in 100 mL of distilled water and stir to form an aqueous phase. The oil phase and the water phase are slowly mixed and homogenized in an ice bath for 3 minutes to obtain an O / W pre-emulsion. Then press the pre-emulsion through the microporous membrane device (such as figure 1 ), the emulsion is obtained, and the film time of the emulsion is less than 10s, and then the emulsion is divided into two parts. One portion was stirred and solidified at room t...

Example Embodiment

[0111] Example 2

[0112] A hydrophilic porous membrane with a pore size of 30 μm and a uniform pore size is soaked in water to fully wet the porous membrane. Dissolve 100 mg of ropivacaine free base with a concentration of 20 mg / mL after alkalization of ammonia in 5 mL (dichloromethane: acetone = 3: 7) as the oil phase, and at the same time, 1 g of molecular weight of 20,000 (polylactic acid: Polylactic acid-polyglycolic acid copolymer (PLGA) with polyglycolic acid=75:25) is dissolved in the oil phase. 0.5 g of polyvinyl alcohol (PVA) was dissolved in 50 mL of alkaline tris buffer ((pH=9)) and stirred evenly as the water phase. The oil phase and the water phase are mixed homogeneously and emulsified in an ice water bath for 4 minutes to obtain an O / W type pre-emulsion. Then press the pre-emulsion through the microporous membrane device under the operating pressure of 500kPa to obtain the emulsion, the emulsion time is less than 10s, and then the emulsion is volatilized under n...

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Abstract

The invention discloses a narcotic analgesic-loaded sustained-release microsphere and a preparation method thereof and application thereof. The narcotic analgesic-loaded sustained-release microspherecan be continuously released for 1 to 7 days, the burst release rate is less than 20% within 0.5 hour, and the drug embedding rate is higher than 80%, so that high drug embedding rate and low burst release rate and sustained release can be realized. The method has simple process, the obtained product has uniform particle size, batches of products have good repeatability, and the preparation methodis easy for industrial production.

Description

technical field [0001] The present invention relates to the technical field of sustained-release medicaments, and more particularly to a sustained-release microsphere loaded with narcotic and analgesic drugs, its preparation method and application. Background technique [0002] As an innate feeling of the human body, pain plays an important role in avoiding injury and maintaining the endocrine environment of the human body. This is because when the body is stimulated or hurt, it can produce a defensive response, so that the body can avoid being hurt. On the other hand, pain such as neuralgia, cancer pain, low back pain, etc. not only bring suffering to patients, but also cause inconvenience in life, and also cause physiological dysfunction, and severe cases can lead to shock and death. [0003] In clinical treatment, narcotic analgesics can be used not only for surgical anesthesia, but also for pain control and relief. However, the action time of anesthetic analgesics curre...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K45/00A61P23/00A61P29/00
CPCA61K9/5026A61K9/5031A61K9/5089A61K45/00A61P23/00A61P29/00
Inventor 马光辉李勋韦祎苏志国吕丕平李杰杜文涛李莉娥符义刚吴有斌
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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