Staphylococcus lysozyme local sustained release preparation, preparation method and application thereof

A technology for lysostaphin and sustained-release preparations, which are applied in the directions of antibacterial drugs, pharmaceutical formulations, and medical preparations with inactive ingredients, etc. , to achieve the effect of strong bactericidal effect, strong bactericidal effect, and strong drug release ability.

Inactive Publication Date: 2010-01-06
SHANGHAI HI TECH UNITED BIO TECHCAL RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Traditional drug preparation techniques, such as phase separation, spray drying, etc., are easy to denature and inactivate proteins, and it is difficult to meet the requirements of drug delivery for biomacromolecules.

Method used

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  • Staphylococcus lysozyme local sustained release preparation, preparation method and application thereof
  • Staphylococcus lysozyme local sustained release preparation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of embodiment 1 lysostaphin-PLA-PLGA microspheres

[0038] 1. Preparation of lysostaphin solution: Weigh 10 mg of lysostaphin freeze-dried powder, dissolve in 10 ml of dimethyl sulfoxide (DMSO) containing 10 mg of mannitol, and prepare 1 mg / ml of lysostaphin solution.

[0039] 2. Preparation of PLA-PLGA organic solution: weigh 0.4 gram of polylactic acid polymer with a molecular weight of 30,000-50,000, 0.1 gram of polylactic acid-glycolic acid with a molecular weight of 30,000-50,000 (wherein the ratio of lactic acid and glycolic acid is 75:25 ) polymer, dissolved in 10 milliliters of dichloromethane to prepare a 5% PLA-PLGA solution.

[0040] 3. Slowly add 5% PLA-PLGA solution to the prepared lysostaphin-DMSO solution drop by drop, set aside.

[0041] 4. Equilibrium supercritical CO 2 Fluid, process temperature 37°C, pressure 13.5MPa, CO 2 The flow rate is 20 g / min, and the above prepared lysostaphin solution is pumped in, and the lysostaphin-PLA-P...

Embodiment 2

[0043] The preparation of embodiment 2 lysostaphin-PLGA microspheres

[0044] 1. Preparation of lysostaphin solution: Weigh 20 mg of lysostaphin freeze-dried powder, dissolve in 10 ml of dimethyl sulfoxide (DMSO) containing 10 mg of mannitol, and prepare 1 mg / ml of lysostaphin solution.

[0045] 2. Preparation of PLGA organic solution: Weigh 0.5 grams of polylactic acid-glycolic acid (wherein the ratio of lactic acid and glycolic acid is 50:50) polymer with a molecular weight of 30,000-50,000, dissolve it in 10 milliliters of dichloromethane, and prepare 5% PLGA solution.

[0046] 3. Slowly add the 5% PLGA solution dropwise to the prepared lysostaphin-DMSO solution for later use.

[0047] 4. Equilibrium supercritical CO 2 Fluid, process temperature 37°C, pressure 13.5MPa, CO 2 The flow rate was 20 g / min, and the lysostaphin solution prepared above was pumped in, and the lysostaphin-PLGA microspheres were prepared by the supercritical anti-solvent method.

[0048] 5. After t...

Embodiment 3

[0049] The in vitro sustained release curve of embodiment 3 lysostaphin-PLA-PLGA microspheres

[0050] Weigh 5 mg of the microparticles prepared in Example 1, place in 10 ml of PBS buffer solution (pH 7.4), seal, shake at a constant temperature and speed (100 r·min −1 ) at 4° C. The buffer solution was taken regularly within three months, the enzyme activity of lysostaphin was detected, and the cumulative release percentage of lysostaphin was calculated. The in vitro drug release results of sustained-release lysostaphin microspheres are as follows: figure 1 Shown:

[0051] The results show that the release process of lysostaphin in vitro lasts up to three months, and the release rate is relatively stable, which can maintain the stable and long-term release of lysostaphin.

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Abstract

The invention discloses a staphylococcus lysozyme local sustained release preparation, a preparation method and application thereof. The preparation comprises the following components in percentage by weight: 1 to 10 percent of staphylococcus lysozyme, 1 to 10 percent of mannite, 0 to 90 percent of polylactic acid (PLA), and 5 to 95 percent of polylactide-co-glycolide (PLGA). The preparation takes the staphylococcus lysozyme as a bactericidal active component to obtain polylactide-co-glycolide (PLA-PLGA) polymer microspheres containing the staphylococcus lysozyme through supercritical fluid microparticle preparation technology. The preparation has good physical and chemical properties and strong sterilization effect, has adjustable time during the in vitro medicament release, ensures that the medicament release process can reach three days to three months, and has steady release rate.

Description

technical field [0001] The invention relates to a biological antibacterial slow-release preparation, in particular to a slow-release preparation of lysostaphin. Background technique [0002] Lysostaphin is an endopeptidase. The enzyme can cut the five-glycine peptide bond bridge structure in the peptidoglycan of the bacterial cell wall, thereby achieving the purpose of rapidly dissolving and killing the bacteria. In vitro pharmacodynamic studies have shown that lysostaphin has a good inhibitory effect on a variety of Staphylococcus aureus and Staphylococcus epidermidis, and has a good inhibitory effect on Corynebacterium pyogenes, Streptococcus and Pasteurella. Especially for drug-resistant Staphylococcus aureus, MRSA and "super bacteria" with multi-drug resistance, lysostaphin also has a strong bactericidal effect, because it can dissolve bacteria including growth stationary phase, Therefore, it is not easy to induce drug-resistant strains. [0003] It has been reported ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/48A61K47/34A61K9/16A61P31/04
Inventor 黄青山李莉
Owner SHANGHAI HI TECH UNITED BIO TECHCAL RES
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