Sodium alginate modified ropivacaine hydrochloride multivesicular liposome microsphere as well as preparation method and application thereof

Abstract

The invention discloses a sodium alginate modified ropivacaine hydrochloride multivesicular liposome microsphere as well as a preparation method and an application thereof. The preparation method comprises the following steps: firstly, uniformly mixing and dispersing a nano calcium carbonate gel initiator into liquid paraffin, adding multivesicular liposome under the condition of uniform stirring, then adding a sodium alginate solution, and uniformly mixing; and then adjusting the pH value to 3.0-5.8, and rapidly initiating gelation reaction by free calcium ions to form the uniform gel-coated multi-vesicular liposome microspheres with a net-shaped cross-linked structure. The multi-vesicular liposome microsphere has the characteristics of clear structure, uniform particle size, stable state, long slow release time and the like. Compared with an existing preparation method, the preparation method has the advantages that the encapsulation effect of the final multi-vesicular liposome is guaranteed, the surface of the multi-vesicular liposome is uniformly covered with the sodium alginate, the problem that the sodium alginate is connected into a sheet is solved, the stability of the multi-vesicular liposome is enhanced, and therefore the slow release effect is improved. Meanwhile, the use amount of chloroform in the organic solvent can be reduced.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a sodium alginate-modified ropivacaine hydrochloride multivesicular liposome microsphere and a preparation method and application thereof. Background technique [0002] Ropivacaine (RPV) is a new type of long-acting amide local anesthetic, which has the advantages and characteristics of low toxicity to the heart and central nervous system, long duration of action, and separation of motor nerve and sensory nerve block. In the prevention and treatment of pain, ropivacaine can be used for labor analgesia, postoperative analgesia in upper and lower abdominal surgery and total knee replacement. Currently, ropivacaine preparations in clinical use are all injections. Pain relief usually lasts only about 5 hours after a single epidural injection. Continuous administration requires special devices such as catheters or infusion pumps built into the operation. The infusion p...

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Problems solved by technology

However, there are still many problems about the Rpv-MVLs-Alg prepared by the preparation method of sodium alginate-ropivacaine hydrochloride multivesicular liposomes at this stage. Gelling, leading to the problem of linking into sheets (Xu Wei, Yu Yang, Chen Yipeng, etc. Preparation and process optimization of amphotericin B liposome-microspheres [J]. Chinese Journal of Antibiotics, 2018, 43(07): 893 -900.)

For another example, when Dai Chuanyun etc. directly added calcium carbonate to the mixture of multivesicular liposomes and sodium alginate, the problem of uneven coating would occur, and even the particles would be too large, so it was not suitable for injection administration (Dai Chuanyun, Liu Huoan, Fu Ya, et al. Study on the physicochemical properties and preliminary stability of multivesicular liposome-sodium alginate microspheres[J]. China Pharmacy, 2008, (28): 2203-2205.)

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