Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Local sustained release preparation for preventing and treating osteomyelitis, preparation method and application thereof

A slow-release preparation, osteomyelitis technology, applied in the field of local slow-release preparations of lysostaphin, can solve the problems of reducing the strength of bone cement, and achieve the effect of fast degradation rate, high ratio and strong stability

Inactive Publication Date: 2010-01-06
SHANGHAI HI TECH UNITED BIO TECHCAL RES
View PDF1 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The invention patent "Application of lysostaphin in the preparation of drugs for treating osteomyelitis" (application number: 200610119208.0, publication number: CN101195027A) filed by the applicant on December 6, 2006 has disclosed that lysostaphin is used in the preparation of therapeutic Osteomyelitis medicine has a good application prospect, but because the invention mixes lysostaphin directly with drug carrier materials such as calcium phosphate bone cement, the calcium phosphate bone cement will release heat during the mixing process, and in a certain Can affect the biological activity of protein substances such as lysostaphin to a certain extent, so the bactericidal activity of the preparation prepared according to this method can generally only be maintained for about 3 days (the bacteriostasis test result of the 7th line 1 line of the CN101195027A instruction manual), and The direct mixing of biological protein macromolecules such as lysostaphin and bone cement and other carrier materials will affect the intermolecular force of calcium phosphate bone cement, thereby reducing the strength of bone cement after curing, so there are still some defects in clinical application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Local sustained release preparation for preventing and treating osteomyelitis, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 lysostaphin-polylactic acid microspheres

[0037] 1. Preparation of lysostaphin solution: Weigh 10 mg of lysostaphin freeze-dried powder, dissolve it in 10 ml of dimethyl sulfoxide (DMSO), and prepare a 1 mg / ml lysostaphin solution.

[0038] 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-polyglycolic acid with a molecular weight of 30,000-50,000 (wherein the ratio of lactic acid to glycolic acid is 75: 25) The polymer was dissolved in 10 ml of dichloromethane to prepare a 5% PLA-PLGA solution.

[0039] 3. Slowly add 5% PLA-PLGA solution to the prepared lysostaphin-DMSO solution drop by drop, set aside.

[0040] 4. Equilibrium supercritical CO 2 Fluid, process temperature 37°C, pressure 13.5MPa, CO 2 The flow rate is 20g / min, pumped through the nozzle, and the above-prepared lysostaphin solution is prepared by supercritical anti-s...

Embodiment 2

[0042] The preparation of embodiment 2 lysostaphin microspheres-calcium phosphate bone cement

[0043] 1. Take by weighing 6 grams of ultrafine α-tricalcium phosphate powder, 4 grams of ultrafine calcium hydrogen phosphate powder, and 1 gram of the lysostaphin-PLA-PLGA drug-loaded microspheres prepared in Example 1, mix evenly, and form solid phase powder;

[0044] 2. Prepare 2% Na 2 HPO 4 (pH6.5) liquid phase solidification solution, mix 4ml of liquid phase solidification solution with the solid phase powder prepared above to form a paste, pour it into the mold, put it in a 37°C, 100% humidity environment, and release the material after solidification Made into artificial bone blocks.

Embodiment 3

[0045] The in vitro sustained release curve of embodiment 3 lysostaphin-polylactic acid microspheres

[0046] Take the artificial bone block prepared in Example 2, weigh it, place it in 100ml of PBS buffer solution (pH7.4), seal it, and vibrate at a constant temperature and speed (100r·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:

[0047] The results show that the release process of lysostaphin in vitro lasts up to three months, the release rate is relatively stable, and it can maintain stable and long-term release at the administration site.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a local sustained release preparation for preventing and treating osteomyelitis, a preparation method and application thereof. The preparation comprises the following components in percentage by weight: 0.01 to 1 percent of staphylococcus lysozyme, 1 to 20 percent of polylactic acid (PLA), 0.5 to 10 percent of polylactide-co-glycolide (PLGA), and 70 to 90 percent of calcium phosphate cement (CPC). The preparation takes the staphylococcus lysozyme as a bactericidal active component to obtain PLA-PLGA polymer microspheres containing the staphylococcus lysozyme through supercritical fluid microparticle preparation technology, and the PLA-PLGA polymer microspheres are compounded with the calcium phosphate cement (CPC) to obtain a novel sustained release degradable antibacterial composite artificial bone carrying staphylococcus lysozyme microspheres. The preparation has good physical and chemical properties and strong sterilization effect, ensures that the in vitro medicament release process is long up to three months, has steady release rate, and can maintain steady and long-acting release at administration positions.

Description

technical field [0001] The invention relates to a biological antibacterial slow-release preparation, in particular to a local slow-release preparation of lysostaphin for preventing and treating osteomyelitis. Background technique [0002] Osteomyelitis is a common but difficult to cure disease of orthopedics. Bacterial infection is the direct cause of osteomyelitis. The most common pathogenic bacteria in suppurative osteomyelitis is Staphylococcus aureus, accounting for about 70% of the total infection cases, followed by hemolytic streptococcus and Pseudomonas aeruginosa. . Systemic antibiotics are the traditional approach to the treatment of osteomyelitis. However, the blood circulation of bone infection lesions is relatively poor. Even if large doses of antibiotics are applied systemically, it is difficult to achieve effective antibiotic concentrations in the local tissues of the lesions. In recent years, gentamicin PMMA bead chain topical sustained-release preparations...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K38/48A61K47/34A61K9/16A61L27/40A61L27/54A61P19/00A61P31/04A61K33/42
Inventor 黄青山李莉
Owner SHANGHAI HI TECH UNITED BIO TECHCAL RES
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products