A kind of preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation

A multivesicular liposome and bupivacaine technology, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of sudden release and affect the therapeutic effect of drugs , the drug can not achieve the expected long-acting sustained-release effect and other problems, to achieve the effect of round shape and improve the long-acting sustained-release effect

Active Publication Date: 2021-01-01
GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Broken multivesicular liposomes will make the drug unable to achieve the expected long-term sustained release effect, or even burst release, which will affect the therapeutic effect of the drug

Method used

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  • A kind of preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation
  • A kind of preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation
  • A kind of preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] The preparation method of the bupivacaine multivesicular liposome provided by the present embodiment comprises the following steps:

[0070] 1 Formation of water-in-oil colostrum (W / O)

[0071] Mix 5mL of the first water phase and 25mL of the oil phase (the volume of the first water phase and the oil phase is 1:5), place in an ice bath, and shear at a speed of 16000rpm for 9min to form water-in-oil colostrum.

[0072] Wherein, the composition of the first aqueous phase is as follows:

[0073] The solvent is water;

[0074] The solutes were: 60 mg / mL bupivacaine, 150 mM glucuronic acid, 15 mM hydrochloric acid, and 20 mM phosphoric acid.

[0075] The composition of the oil phase is as follows:

[0076] Organic solvent is dichloromethane;

[0077] The solutes were: 18.6 mM DEPC, 4.2 mM DPPG and 30 mM cholesterol.

[0078] 2 plus neutral fat (TC)

[0079] Add 9 mg of TC to the colostrum obtained from the above steps (the mass ratio of the amount of TC added to the bu...

Embodiment 2

[0102] Such as Figure 5 As shown, the present embodiment provides the bupivacaine multivesicular liposome preparation device suitable for the preparation method of the bupivacaine multivesicular liposome described in Example 1, which includes:

[0103] The first water phase storage tank 1, the oil phase storage tank 2, the neutral fat storage tank 3, the first water phase storage tank control valve 4, the oil phase storage tank control valve 5, the neutral fat storage tank control valve 6, temperature control Device 7, colostrum reaction tank 8, colostrum flow rate control valve 9, second water phase storage tank 10, second water phase storage tank control valve 11, double milk reaction tank 12, double milk flow rate control valve 13, three-way device 14, a nitrogen generator 15, a nitrogen control valve 16, a third water phase storage tank 17, a third water phase storage tank control valve 18 and a multivesicular liposome receiving tank 19.

[0104] Wherein, the colostrum r...

Embodiment 3

[0124] The preparation method of the bupivacaine multivesicular liposome provided in this example is basically the same as that in Example 1, except that in this example, the organic solvent of the oil phase is chloroform. The morphological observation results of the bupivacaine multivesicular liposomes prepared by the present embodiment under a microscope are as follows: Figure 8 shown.

[0125] Figure 8 The results showed that the multivesicular liposomes prepared in this example did not contain phospholipid fragments and were round in shape.

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Abstract

The invention discloses a preparation method of bupivacaine multivesicular liposome and a bupivacaine multivesicular liposome preparation, and relates to the field of bupivacaine medicinal preparations. The preparation method of the bupivacaine multivesicular liposome comprises the following steps: adding a neutral fat into a preemulsion formed from an organic solvent-containing oil phase and a bupivacaine-containing first water phase to obtain a first solution for forming a compound emulsion. Compared with the conventional preparation method of the bupivacaine multivesicular liposome, the preparation method provided by the invention has the advantages as follows: through the step of adding the neutral fat into the preemulsion formed from the organic solvent-containing oil phase and the bupivacaine-containing first water phase, the problem of breakage of the multivesicular liposome in the subsequent organic solvent removing step can be overcome, so that the prepared multivesicular liposome is round in shape and basically free of phospholipid fragments, and thus the long-acting slow-release effect of a bupivacaine medicine is improved.

Description

Technical field [0001] The present invention relates to the field of bupivacaine pharmaceutical preparations, and specifically to a preparation method of bupivacaine multivesicular liposomes and a bupivacaine multivesicular liposome preparation. Background technique [0002] Bupivacaine is a BCS Class 1 drug with good water solubility but short half-life. In order to achieve long-acting and sustained-release effects for its injections, it is usually developed into a multivesicular liposome dosage form. [0003] The microstructure of multivesicular liposomes (MVLs) is that multiple liposomes aggregate into a spherical shape. Each liposome is composed of a hydrophobic membrane and an internal aqueous phase, and the drug is dissolved in the internal aqueous phase. Injectables can be formed by dispersing multivesicular liposomes in an aqueous phase. Multivesicular liposomes are a type of non-concentric honeycomb liposomes, which contain many large vesicles separated by lipid bi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/445A61K47/14
CPCA61K9/1273A61K9/1277A61K31/445A61K47/14
Inventor 王秋云
Owner GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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