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

A technology of ropivacaine hydrochloride and multivesicular liposome, which is applied in the field of ropivacaine hydrochloride multivesicular liposome microspheres and preparation thereof, can solve the problem of excessive gelation of sodium alginate and unsuitability for injection administration , uneven coating and other problems, to reduce the time and cost, ensure the effect and shape of the capsule, and improve the stability.

Active Publication Date: 2021-07-27
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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.)

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] The preparation method of Rpv-MVLs-Alg microspheres is as follows:

[0094] Step 1: Formation of water-in-oil colostrum (W / O)

[0095] Inject 4ml of the first water phase into the 4ml oil phase with a 5ml syringe. The rate of injecting the first water phase into the oil phase is 0.2mL / s, and keep shaking. Homogenize for 9 minutes to form water-in-oil colostrum. Wherein, the solvent of the first aqueous phase is water; the solute composition is as follows: 37.5 mg / ml ropivacaine hydrochloride, 31 mg / ml glucose. The organic solvent of the oil phase is dichloromethane-chloroform (3:1); the solute composition is as follows: 16mg / ml egg yolk lecithin (PC), 8mg / ml cholesterol (TH), 2.5mg / mL, dipalmitoylphosphatidylcholine Base (DPPC), 4 mg / mL triolein (TO).

[0096] Step 2: Formation of water-in-oil-in-water (W / O / W) double emulsion

[0097] Add the colostrum obtained in step 1 into 25 mL of the second aqueous phase, and homogenize at 4000 rpm for 45 seconds to form a wate...

Embodiment 2

[0122] The difference between the preparation method of Rpv-MVLs-Alg microspheres provided in this example and Example 1 is that the pH of the system was adjusted to 6.0 during the gelation reaction in step 4.2 of this example, and the prepared Rpv The morphology of -MVLs-Alg microspheres is as follows Figure 6 As shown, it can be seen that the gelation of sodium alginate in the Rpv-MVLs-Alg microspheres prepared in this example is not complete, resulting in uneven coverage around the multivesicular liposomes.

Embodiment 3

[0136]The difference between the preparation method of Rpv-MVLs in this example and Example 1 is that the nitrogen purging temperature used in this example is 45°C, and the morphology of the prepared Rpv-MVLs is as follows Figure 13 As shown, the results show that the particle size of the Rpv-MVLs prepared in this example is small, and although there are complete edges, there are many fragments and the shape is irregular.

[0137] In summary, the preparation method of Rpv-MVLs-Alg microspheres provided in the examples of the present invention is to improve gelation by mixing nano-calcium carbonate and liquid paraffin evenly, and then adding multivesicular liposomes and sodium alginate in sequence. The uniformity of the reaction enables the sodium alginate to evenly coat the surface of the multivesicular liposome after the gelation reaction, and improves the slow-release effect and stability of the common ropivacaine hydrochloride multivesicular liposome. Also by changing the ...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/36A61K9/127A61K31/445A61P23/02
CPCA61K31/445A61K9/1271A61K9/1277A61K9/5036A61P23/02
Inventor 刘美凤苏鹏文毛辉达
Owner SOUTH CHINA UNIV OF TECH
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