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A kind of bupivacaine multivesicular liposome preparation device

A technology of bupivacaine and vesicular lipids, which is applied in the field of bupivacaine multivesicular liposome preparation devices, can solve the problem of sudden release, affecting drug treatment effect, lack of bupivacaine multivesicular liposomes, etc. problem, to achieve the effect of round shape

Active Publication Date: 2021-01-26
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
And there is currently a lack of equipment that can prepare bupivacaine multivesicular liposomes with complete morphology and no phospholipid fragments

Method used

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  • A kind of bupivacaine multivesicular liposome preparation device
  • A kind of bupivacaine multivesicular liposome preparation device
  • A kind of bupivacaine multivesicular liposome preparation device

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] The preparation method of the bupivacaine multivesicular liposome provided by the present embodiment comprises the following steps:

[0086] 1 Formation of water-in-oil colostrum (W / O)

[0087] 5 mL of the first water phase and 25 mL of the oil phase were mixed (the volume of the first water phase and the oil phase was 1:5), placed in an ice bath, and sheared at a speed of 16000 rpm for 9 min to form water-in-oil colostrum.

[0088] Wherein, the composition of the first aqueous phase is as follows:

[0089] The solvent is water;

[0090] The solutes were: 60 mg / mL bupivacaine, 150 mM glucuronic acid, 15 mM hydrochloric acid, and 20 mM phosphoric acid.

[0091] The composition of the oil phase is as follows:

[0092] Organic solvent is dichloromethane;

[0093] The solutes were: 18.6 mM DEPC, 4.2 mM DPPG and 30 mM cholesterol.

[0094] 2 plus neutral fat (TC)

[0095] Add 9 mg of TC to the colostrum obtained from the above steps (the mass ratio of the amount of TC ...

Embodiment 2

[0118] 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:

[0119] 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.

[0120] Wherein, the colostrum r...

Embodiment 3

[0139] 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.

[0140] 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 device for preparing bupivacaine multivesicle liposomes, and relates to the field of bupivacaine pharmaceutical preparations. The bupivacaine multivesicular liposome preparation device disclosed in the present invention includes a first mixed solution for receiving the first water phase containing bupivacaine and an oil phase containing an organic solvent and mixing the first mixed solution. A colostrum reaction tank for forming colostrum from a mixed solution; a neutral fat storage tank for storing neutral fat, and the neutral fat storage tank is connected with the colostrum reaction tank through a delivery pipeline, and the delivery pipeline is provided with a device for controlling the neutral fat The neutral fat storage tank control valve for fat delivery can independently add neutral fat to the colostrum reaction tank of the neutral fat storage tank control valve to make the colostrum mix, and then can prepare polycystic cells that do not contain phospholipid fragments and have a round shape Liposomes.

Description

technical field [0001] The invention relates to the field of bupivacaine pharmaceutical preparations, in particular to a preparation device for bupivacaine multivesicular liposomes. 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 liposomes with strong rigidity. When one of the vesicles r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/445A61K47/14A61J3/00
CPCA61J3/00A61K9/1271A61K31/445A61K47/14
Inventor 王秋云
Owner GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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