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A kind of preparation method of narcotic analgesic-loaded microspheres, product and use thereof

An analgesic and microsphere technology, which is applied in the field of preparation of narcotic analgesic-loaded microspheres, can solve the problems of low embedding rate, the advent of narcotic analgesic sustained-release microsphere products, and poor drug repeatability, etc. Repeatability, stability, and industrial scale-up effects

Active Publication Date: 2022-07-15
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current preparation technology of microspheres to load analgesics has the following problems: first, the particle size of the prepared microspheres is not uniform, resulting in poor reproducibility of drugs between batches; second, narcotic analgesics are chemical small molecules Drugs with extremely low molecular weight. During the preparation process, small molecular compounds are easy to escape to the water phase, resulting in low embedding rate; finally, the regulation of the release cycle of narcotic and analgesic sustained-release microspheres is a key factor restricting clinical application. In clinical practice, it is often necessary to achieve analgesic time of 3-7 days after surgery. During this period, the stable and accurate release of narcotic analgesics can not only prevent patients from postoperative pain, but also reduce drug accumulation due to too many injections. cardiovascular toxicity
Due to the constraints of the above problems, at present, there is no commercialized narcotic analgesic sustained-release microsphere product.

Method used

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  • A kind of preparation method of narcotic analgesic-loaded microspheres, product and use thereof
  • A kind of preparation method of narcotic analgesic-loaded microspheres, product and use thereof
  • A kind of preparation method of narcotic analgesic-loaded microspheres, product and use thereof

Examples

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Embodiment 1

[0101] This embodiment provides a preparation method of anesthesia-analgesic-loaded microspheres, and the preparation method of the anesthetic-analgesic-loaded microspheres includes the following steps:

[0102] (1) A hydrophilic porous membrane with a membrane pore size of 30 μm was soaked in water to fully wet the membrane surface. 75 mg of ropivacaine hydrochloride and 1.5 mg of gum arabic were dissolved in 1 mL of deionized water as the inner aqueous phase (W 1 ), 300 mg of polylactic acid-polyglycolic acid copolymer (PLGA) with a molecular weight of 20,000 (polylactic acid: polyglycolic acid in PLGA = 50:50, molar ratio) and 50 mg of soybean lecithin were dissolved in 10 mL of dichloromethane as oil phase (O). Dissolve 100 mg of polyvinyl alcohol (PVA) in 100 mL of distilled water and stir to be used as the outer water phase (W 2 );

[0103] (2) The inner water phase (W 1 ) was added to the oil phase (O), homogeneously emulsified in an ice bath at 0 °C for 2 min to ob...

Embodiment 2

[0108] This embodiment provides a preparation method of anesthesia-analgesic-loaded microspheres, and the preparation method of the anesthetic-analgesic-loaded microspheres includes the following steps:

[0109] (1) A hydrophilic porous membrane with a membrane pore size of 50 μm was soaked in water to fully wet the membrane surface. 50 mg of bupivacaine hydrochloride and 0.05 mg of casein were dissolved in 1 mL of deionized water as the inner aqueous phase (W 1 ), 800 mg of polylactic acid-polyglycolic acid copolymer (PLGA) with a molecular weight of 10,000 (polylactic acid: polyglycolic acid in PLGA = 50:50, molar ratio) and 30 mg of sucrose fatty acid ester were dissolved in 10 mL of ethyl acetate as the oil phase (O). Dissolve 500 mg of polyvinyl alcohol (PVA) in 50 mL of distilled water and stir to be used as the outer water phase (W 2 );

[0110] (2) The inner water phase (W 1 ) was added to the oil phase (O), homogeneously emulsified in an ice bath at 0 °C for 2 min...

Embodiment 3

[0115] This embodiment provides a preparation method of anesthesia-analgesic-loaded microspheres, and the preparation method of the anesthetic-analgesic-loaded microspheres includes the following steps:

[0116] (1) A hydrophilic porous membrane with a membrane pore size of 20 μm was soaked in water to fully wet the membrane surface. 30 mg of lidocaine hydrochloride and 0.3 mg of mannose were dissolved in 1 mL of deionized water as the inner aqueous phase (W 1), 5000 mg of polylactic acid-polyglycolic acid copolymer (PLGA) with a molecular weight of 30,000 (polylactic acid: polyglycolic acid = 75:25, molar ratio) and 50 mg of egg yolk lecithin were dissolved in 10 mL of dichloromethane as oil Phase (O). Dissolve 500 mg of polyvinyl alcohol (PVA) in 150 mL of distilled water and stir to be used as the outer water phase (W 2 );

[0117] (2) The inner water phase (W 1 ) was added to the oil phase (O), homogeneously emulsified in an ice bath at 5°C for 2 min to obtain W 1 / O ...

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Abstract

The invention provides a preparation method of microspheres loaded with anesthetic and analgesics, and its products and uses. The preparation method of the anesthetic and analgesic-loaded microspheres includes the following steps: (1) dissolving the anesthetic and analgesic drug in water to form an inner water phase; dissolving the degradable high molecular polymer and the oil phase emulsifier in an organic solvent to form an oil phase; dissolve the stabilizer in water to form an outer water phase; (2) mix the inner water phase and oil phase obtained in step (1), and obtain W after emulsification 1 / O type emulsion; (3) the outer water phase obtained in step (1) and the W obtained in step (2) 1 / O type emulsion mixed, emulsified to obtain W 1 / O / W 2 Type pre-recombination emulsion, filtered through a microporous membrane, and then solidified to obtain anesthetic and analgesic-loaded microspheres. The preparation method of the invention can effectively reduce the escape of drug molecules, improve the entrapment rate of the drug, and further increase the drug loading capacity. At the same time, the particle size and structure of the microspheres are controllable.

Description

technical field [0001] The invention relates to the technical field of sustained-release medicaments, in particular to a preparation method of anesthetic-analgesic-loaded microspheres, products and uses thereof. Background technique [0002] Pain is one of the common clinical manifestations of most diseases. Common pains include acute pain, chronic pain, and cancer pain. Acute pain is the body surface or visceral pain caused by external injury such as acute injury, surgery or disease, such as trauma, acute inflammation, surgery, myocardial infarction, organ perforation, etc. Chronic pain can sometimes last for more than a few months, with repeated episodes, and the disease progresses progressively. Cancer pain is a feeling caused by the information that the pain site needs to be repaired or mediated to the nerve center, which seriously affects the daily life of cancer patients, especially those with advanced cancer. With the improvement of the patient's requirements for t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/34A61K31/167A61K31/245A61K31/445A61K31/485A61K45/00A61K47/42A61K47/38A61K47/36A61P23/00
CPCA61K9/5031A61K45/00A61K31/445A61K31/245A61K31/167A61K31/485A61P23/00
Inventor 马光辉文康韦祎周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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