Multivesicular liposome for ocular vitreous injection and preparation method of multivesicular liposome

A technology of multivesicular liposomes and vitreous bodies, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to achieve good sustained release, improve compliance, and reduce medication pain Effect

Active Publication Date: 2017-07-07
YANTAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] There is no report on the application of multivesicular liposomes in the vitreous of the eye

Method used

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  • Multivesicular liposome for ocular vitreous injection and preparation method of multivesicular liposome

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Embodiment 1

[0041] A preparation method of multivesicular liposomes for ocular vitreous injection includes the following steps:

[0042] Accurately weigh dioleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, cholesterol, and triolein respectively 22mg, 6mg, 18mg, and 6mg into a 10ml beaker, add 3ml of chloroform to dissolve to obtain the lipid phase;

[0043] Combine the lipid phase obtained above with 4ml of 25mg / ml bevacizumab solution containing 7% sucrose and vortex to mix to form W / O colostrum;

[0044] Inject the colostrum obtained above into an aqueous solution containing 10ml of 4% glucose and 60mmol / L lysine, and vortex to mix to form a W / O / W double emulsion;

[0045] The double emulsion obtained above was quickly poured into 20ml of the external water phase, and rotary evaporated at about 37°C to remove the organic solvent chloroform, centrifuge at 1000r / min, discard the supernatant, and add proper amount of physiological saline to the lower sediment to obtain the polyamide of th...

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Abstract

The invention relates to a multivesicular liposome for ocular vitreous injection. The multivesicular liposome is prepared from the following components in parts by weight: 1 part of bevacizumab, 0.2-150 parts of lipid, 5-500 parts of an osmotic pressure regulator and 6-200 parts of a co-emulsifier. A preparation method of the multivesicular liposome for ocular vitreous injection comprises the steps of dispersing an inner water phase into a lipid phase according to the volume ratio of the inner water phase to the lipid phase of (1:1) to (1:10) to form a W/O primary emulsion; dispersing the W/O primary emulsion into an outer water phase according to the volume ratio of the W/O primary emulsion to the outer water phase of (1:1) to (1:5) to form a W/O/W compound emulsion; transferring the W/O/W compound emulsion to the outer water phase and removing an organic solvent in the compound emulsion; and centrifuging the obtained solution at 500-3,000rpm, taking lower sediments and adding normal saline for dispersion again to obtain the multivesicular liposome. According to the method provided by the invention, the prepared multivesicular liposome is high in encapsulation efficiency and has a good slow release effect, the particle sizes are 10-50 microns, the administration times are reduced and the compliance of a patient is improved.

Description

Technical field [0001] The present invention relates to a multivesicular liposome for ocular vitreous injection. The invention also relates to a preparation method of multivesicular liposome for ocular vitreous injection, which belongs to the field of pharmaceutical preparations. Background technique [0002] Age-related macular degeneration (hereinafter referred to as AMD) is the primary cause of irreversible visual impairment in the elderly, mainly due to aging changes in the structure of the macular area. Age-related macular degeneration mostly occurs over 45 years of age, and its prevalence increases with age. It is currently an important disease that causes blindness in the elderly. AMD is divided into dry (non-neovascular) and wet (neovascular). Dry AMD is the atrophy and degeneration of the macular area caused by the atrophy of retinal pigment epithelial cells and photoreceptor cells; wet AMD is mainly manifested by the destruction of the glass membrane and the formation ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/14A61K39/395A61P27/02A61P27/06A61P9/10
CPCA61K9/0002A61K9/0019A61K9/127A61K39/3955A61K47/14A61K47/24A61K47/28
Inventor 慕宏杰孙考祥王毅云
Owner YANTAI UNIV
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