Local anesthesia pain relieving and slow-release medicine delivery system as well as preparation method and application thereof

Abstract

The invention discloses a novel local anesthesia pain relieving and slow-release medicine delivery system, which comprises an inner water phase, an outer water phase, an oil phase, an organic solvent,an isotonic regulator and a pH regulator, wherein the inner phase comprises a pain relieving agent, a medicine solvent and a medicine solubilizing agent; the pain relieving agent is selected from onekind of materials from bupivacaine, levobupivacaine, ropivacaine, lidocaine, bupivacaine or mepivacaine; the pain relieving agent is in a free alkali form or acid salt form; the medicine solvent is selected from N or P containing inorganic acid; the medicine solubilizing agent is selected from one or several kinds of materials from sugar or annular organic acid. The prepared muhivescular liposomes have high encapsulation rate, high medicine carrying capacity, uniform particle diameter and good slow release effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a local anesthesia analgesic slow-release drug delivery system and its preparation method and application. Background technique [0002] At present, clinical local anesthetic drugs mainly include esters and amides, and the action time of these drugs is generally less than 3 hours. If long-term analgesia is required, continuous administration is required to maintain an appropriate blood drug concentration. If such drugs are prepared into preparations with sustained release function, such as microspheres and multivesicular liposomes, the analgesic effect can last for a long time, and the tolerance of patients can also be improved. The Chinese patent whose patent number is CN102274183B proposes two kinds of multivesicular liposome preparation methods, the first method is to dissolve the active ingredient of the drug and the osmotic pressure regulator in water to make the inner wate...

AI Technical Summary

Problems solved by technology

This method is similar to the ordinary liposome pH gradient method or ion gradient drug loading. Since the multivesicular liposome is a structure in which most small capsules exist in a large capsule, when using this technology to load drugs, the outer layer must be small. Drugs are preferentially loaded into the vesicles, and after the drug is loaded in the outer vesicles, the osmotic pressure of the drug loaded into the vesicles in the inner layer of the large vesicles will decrease, so there must be some small vesicles in the large vesicles of multivesicular liposomes that are inactive. Drug filling, in addition, the difference between multivesicular liposomes and ordinary liposomes is that they contain oily components such as triglycerides, which exist in the skeleton structure of each capsule, and the patent is to dissolve the drug in the external water phase , then the water-based drug will inevitably be interfered by triglyceride during the process of entering the inner water phase from the outer water phase, and the drug cannot smoothly enter the interior of the multivesicular liposome, and the active ingredients of the drug described in this patent are mainly exenatide, Drugs unstable under alkaline conditions, such as topotecan

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