Bupivacaine multi-vesicular liposome preparing 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, the failure of the drug to achieve the expected long-term sustained release effect, and the lack of bupivacaine multi-vesicle liposomes. Eliminate problems such as vesicles and liposomes, and achieve the effect of round shape

Active Publication Date: 2018-06-15
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 therapeut

Method used

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  • Bupivacaine multi-vesicular liposome preparing device
  • Bupivacaine multi-vesicular liposome preparing device
  • Bupivacaine multi-vesicular liposome preparing 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 bupivacaine multi-vesicular liposome preparing device, and relates to the field of bupivacaine medicinal preparations. The disclosed bupivacaine multi-vesicular liposome preparing device comprises a primary emulsion reaction tank, which is used to receive a first water phase containing bupivacaine and an oil phase containing an organic solvent, wherein the first water phase and the oil phase are mixed in the reaction tank to form a first mixed solution and the first mixed solution forms primary emulsion in the reaction tank; and a neutral grease storing tank, which isused to store neutral grease. The neutral grease storing tank and the primary emulsion reaction tank are communicated through a delivery pipeline. The delivery pipeline is provided with a neutral grease storing tank control valve for controlling the delivery of neutral grease. Neutral grease in the neutral grease storing tank can be individually added into the primary emulsion reaction tank by the control valve and is mixed with the primary emulsion to prepare multi-vesicular liposome, which has the advantages that the liposome does not contain any phospholipid fragment and the shape of the liposome is round and regular.

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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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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