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

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...

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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 microspheres, the solvent evaporation method and solvent extraction method have a long solidification time and a large volume of the water phase, which causes the drug to diffuse to the water phase during the formation of the microspheres, and the embedding rate is low;

[0011] (5) For the slow-release microspheres loaded with analgesic drugs in the existing literature reports, the small molecule analgesic drugs are distributed on the surface of the microspheres in the form of crystals, so in the in vitro release process, the burst release is higher, and the later There is a plateau period in the release, and it is difficult to reach a therapeutically effective concentration;

[0012] (6) The microspheres prepared by the existing method have poor resuspension in aqueous solution, are easy to agglomerate and aggregate, and have the risk of clogging the needle

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