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Lipid gel medicinal preparation, preparation method thereof and purpose thereof

A technology of pharmaceutical preparations and lipid gels, which is applied in the direction of drug combinations, pharmaceutical formulations, anesthetics, etc., to achieve the effects of cost reduction, high drug loading, and sustained and stable sustained release effect

Active Publication Date: 2014-04-09
SHANGHAI HENGRUI PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] HE Warriner et al reported in Science 16February 1996:Vol.271no.5251pp.969-973 that the gel with PEG-DMPE was added, the viscosity of the system increased with the increase of water content, but the maximum The water content is only 90%, no drug is loaded and contains amyl alcohol as a co-solvent

Method used

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  • Lipid gel medicinal preparation, preparation method thereof and purpose thereof
  • Lipid gel medicinal preparation, preparation method thereof and purpose thereof
  • Lipid gel medicinal preparation, preparation method thereof and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Prepare blank gel: 4g soybean phospholipid and 0.4g PEG-DSPE2000, add water for injection to the total weight of 100g, magnetically stir at 80°C for 0.5 hours, and no gel can be formed.

Embodiment 2

[0066] Prepare lipid gel according to the concentration of traditional VPG: prepare an aqueous solution of levobupivacaine hydrochloride, add 20g hydrogenated soybean phospholipid to it, the total weight is 100g, and the concentration of levobupivacaine hydrochloride is 50mg / g at 70℃ Stir under the blade for 2 hours, the viscosity is too high to be applied.

Embodiment 3

[0068] Prepare lipid gel according to the concentration of traditional VPG: prepare an aqueous solution of levobupivacaine hydrochloride, add 20g of soybean phospholipid to it, the total weight is 100g, and the concentration of levobupivacaine hydrochloride is 80mg / g at 70℃ Stir with the paddle for 2 hours, and the product is in the form of a gel with certain fluidity.

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PUM

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Abstract

The invention relates to a lipid gel medicinal preparation, a preparation method and a purpose. The lipid gel medicinal preparation comprises PEGylated phosphatide, non-PEGylated phosphatide, an active substance with effective treatment amount and a solvent, wherein the solvent contains water or physiological aqueous medium. The preparation method comprises the following steps: i) preparing an active substance solution; ii) mixing the above active substance solution with PEGylated phosphatide, non-PEGylated phosphatide, the solvent and other pharmaceutically acceptable accessory with a prescription amount; and iii) heating and mixing a solution obtained in the step ii), and fully swelling. The invention also comprises an application of the lipid gel in a slow release drug delivery system. The preparation has high maximum drug loading, is suitable for large scale production, and has the advantages of simple preparation method, low toxicity and obvious slow release effect.

Description

Technical field [0001] The invention relates to a lipid gel pharmaceutical preparation and its preparation method and application. Background technique [0002] The vesicular phospholipid gel (VPG) is a semi-solid phospholipid dispersion. It resembles vesicles in morphology, but is different from liposome gel and ordinary liposome compartment structure in the traditional sense. Due to the formation of a unique three-dimensional network structure, VPG can be used as a drug "reservoir" to control drug release. The increased phospholipid consistency reduces the spacing between adjacent vesicles. The final result is a certain volume of water phase in and between the closed vesicles, which is suitable for loading water-soluble, fat-soluble and amphiphilic drugs. Especially for water-soluble drugs, the almost equal volume of the water phase inside and outside the vesicle not only increases the encapsulation efficiency, but also the concentration of the inside and outside drugs tends ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K47/24A61K45/00A61P23/02
Inventor 仝新勇李立民董晓卉刘玉婵郭菲赵昊
Owner SHANGHAI HENGRUI PHARM CO LTD
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