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Phospholipid protein particle composite microsphere and preparation method thereof

A technology of protein particles and composite microspheres, applied in peptide/protein components, microcapsules, pharmaceutical formulations, etc., can solve the problems of protein drug activity decline, protein drug aggregation, burst release, etc., to achieve low burst release rate, drug package High sealing rate and solving the effect of high burst release rate

Active Publication Date: 2018-12-11
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, during the preparation process of the W / O / W double emulsion method, because the protein drug in the inner water phase is easy to leak into the outer water phase, it is easy to make the protein drug aggregate on the surface of the microspheres and cause a burst release.
On the other hand, as a biologically active agent with a relatively fragile structure, protein drugs will inevitably come into contact with organic solvents during the preparation of microspheres by the W / O / W double emulsion method, resulting in a decrease in the activity of protein drugs

Method used

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  • Phospholipid protein particle composite microsphere and preparation method thereof
  • Phospholipid protein particle composite microsphere and preparation method thereof
  • Phospholipid protein particle composite microsphere and preparation method thereof

Examples

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Embodiment 1

[0038] Embodiment 1: Preparation of phospholipid-protein microparticle composite microspheres of bovine serum albumin

[0039] The preparation method of the bovine serum albumin phospholipid protein particle composite microsphere of the present embodiment comprises the following steps:

[0040] 1. Preparation of phospholipid protein microparticles

[0041] Weigh an appropriate amount of water-soluble model protein drug bovine serum albumin and freeze-drying protective agent trehalose and dissolve them in ultrapure water to prepare a solution with a concentration of bovine serum albumin of 2 mg / mL and a concentration of trehalose of 1 mg / mL as the aqueous phase , Weigh an appropriate amount of soybean phosphatidylcholine and dissolve it in tert-butanol to prepare a tert-butanol solution with a phospholipid concentration of 50 mg / mL as the oil phase. Under the conditions of a water bath of 37° C. and a magnetic stirring rate of 1300 rpm, the oil phase was added dropwise to the ...

Embodiment 2

[0050] Embodiment 2: the preparation of the phospholipid protein particle composite microsphere of bovine serum albumin

[0051] The preparation method of the bovine serum albumin phospholipid protein particle composite microsphere of the present embodiment comprises the following steps:

[0052] 1. Preparation of phospholipid protein microparticles

[0053] Weigh an appropriate amount of water-soluble model protein drug bovine serum albumin and freeze-drying protective agent mannitol and dissolve them in ultrapure water to prepare a solution with a concentration of bovine serum albumin of 2 mg / mL and a concentration of mannitol of 1 mg / mL as the aqueous phase , Weigh an appropriate amount of soybean phosphatidylcholine and dissolve it in tert-butanol to prepare a tert-butanol solution with a phospholipid concentration of 50 mg / mL as the oil phase. Under the conditions of a water bath of 37° C. and a magnetic stirring rate of 1300 rpm, the oil phase was added dropwise to the ...

Embodiment 3

[0060] Example 3: Preparation of Thymopentin Phospholipid Protein Microparticle Composite Microspheres

[0061] The preparation method of the phospholipid protein particle composite microsphere of Thymopentin of the present embodiment comprises the steps:

[0062] 1. Preparation of phospholipid protein microparticles

[0063] Weigh an appropriate amount of water-soluble oligopeptide drug thymopentin and freeze-drying protective agent trehalose and dissolve them in ultrapure water to prepare a solution with a thymopentin concentration of 2 mg / mL and a trehalose concentration of 1 mg / mL as the aqueous phase, weighing An appropriate amount of soybean phosphatidylcholine was dissolved in tert-butanol to prepare a tert-butanol solution with a phospholipid concentration of 50 mg / mL as the oil phase. Under the conditions of a water bath of 37° C. and a magnetic stirring rate of 1300 rpm, the oil phase was added dropwise to the water phase, and the volume ratio of the oil phase to th...

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Abstract

The invention relates to a phospholipid protein particle composite microsphere and a preparation method thereof. The preparation method comprises the following steps: stirring and mixing protein or polypeptide water-soluble drugs, an aqueous solution of a freeze-drying protective additive and an alcoholic solution of phospholipid to obtain a lipid vesicle suspension of phospholipid protein; freeze-drying for removing the solvent to obtain phospholipid protein particles; uniformly dispersing the phospholipid protein particles into an organic solution of a polymer carrier material, then adding an aqueous solution containing an emulsifying agent, and shearing at a high speed to prepare emulsion of S / O / W; and carrying out the processes of solvent volatilization, microsphere curing and the like to form the phospholipid protein particle composite microsphere. The phospholipid protein particle composite microsphere prepared by the method provided by the invention has a high drug envelopment rate and a low sudden release rate, wherein the release rate at the first day is 9-15%; the release rate is stable and lasting, the slow release period of the preparation can reach 20-60 days, and the bioactivity of the drugs in the microsphere is high; and therefore, the phospholipid protein particle composite microsphere has practical values in clinical application.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a phospholipid protein particle composite microsphere and a preparation method thereof. Background technique [0002] With the rapid development of genomics, proteomics and biotechnology, the development of protein and peptide drugs has become one of the hot spots in the field of pharmaceutical research and development. As active substances with various metabolic functions in organisms, protein and peptide drugs are involved in various fields such as hormones, nerves, cell growth and reproduction. Compared with small molecule chemical drugs, protein drugs often have more significant curative effect, fewer adverse reactions and higher safety due to their high activity and high selectivity. Therefore, protein drugs have become the first-line drugs for the treatment of various diseases such as endocrine, infectious, metabolic and pain relief. [0003] Protein drugs are m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K45/00A61K47/34A61K47/24A61K38/38A61K38/08A61K38/23
CPCA61K9/5031A61K38/00A61K38/08A61K38/23A61K38/38A61K45/00A61K47/24
Inventor 潘昕陈龙楷冯地桑黄莹吴涵吴传斌
Owner SUN YAT SEN UNIV
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