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: 2018-05-29
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 sust

Method used

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  • Preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation
  • Preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation
  • Preparation method of bupivacaine multivesicular liposome and bupivacaine multivesicular liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0068] Example 1

[0069] The preparation method of bupivacaine multivesicular liposomes provided in this embodiment includes the following steps:

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

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

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

[0073] The solvent is water;

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

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

[0076] The organic solvent is dichloromethane;

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

[0078] 2 plus neutral fat (TC)

[0079] Add 9 mg of TC to the colostrum obtained by the above steps (the mass ratio of TC addition to the bupivacaine in the colostrum is 3:100),...

Example Embodiment

[0101] And figure 1 with figure 2 The morphological results of the bupivacaine multivesicular liposomes of Example 1 under the microscope are shown. It can be seen that the bupivacaine multivesicular liposomes of Example 1 are intact and undamaged before and after removing the organic solvent; The bupivacaine multivesicular liposomes of Comparative Example 1 were intact and undamaged before removing the organic solvent (such as image 3 Shown), but broken after being removed by organic solvent (such as Figure 4 As indicated by the arrow in). Example 2

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

[0103] First water phase storage tank 1, oil phase storage tank 2, neutral grease storage tank 3, first water phase storage tank control valve 4, oil phase storage tank control valve 5, neutral grease...

Example Embodiment

[0123] Example 3

[0124] The preparation method of bupivacaine multivesicular liposomes provided in this example is basically the same as that of 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 in this example under the microscope are as follows Figure 8 Shown.

[0125] Figure 8 The results show that the multivesicular liposome prepared in this example does not contain phospholipid fragments and has a round 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 invention relates to the field of bupivacaine pharmaceutical preparations, in particular to a preparation method of bupivacaine multivesicular liposomes and a bupivacaine multivesicular liposome preparation. Background technique [0002] Bupivacaine is a BCS 1 drug with good water solubility, but a short half-life. In order to achieve long-acting sustained-release effects in 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, and each liposome is composed of a hydrophobic membrane and an internal aqueous phase in which the drug is dissolved. Injectables can be formed by dispersing multivesicular liposomes in the aqueous phase. Multivesicular liposomes are non-concentric honeycomb liposomes, which have many large and small vesicles separated by lipid bilayers. This unique structure endows liposo...

Claims

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Application Information

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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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