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

A kind of hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application

A technology of hyaluronic acid and parecoxib, which is applied in the field of preparation of new sustained-release microspheres, which can solve the problems of repeated injections and achieve the effect of uniform size

Active Publication Date: 2022-04-19
STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
View PDF10 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Aiming at the problem that the drug injected into the joint cavity will be quickly metabolized and absorbed, and repeated injections are often required, the present invention provides a hyaluronic acid-parecoxib PLGA microsphere and its preparation method and 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
  • A kind of hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application
  • A kind of hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application
  • A kind of hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0036] A preparation method of hyaluronic acid-parecoxib PLGA microspheres, comprising the following steps:

[0037] a. Modify the hydrophilic hyaluronic acid, and transform it into an amphiphilic polymer by grafting hyaluronic acid with stearic acid, which is used as a surfactant in the subsequent microsphere preparation process;

[0038] b. Using double emulsification solvent volatilization method, dissolve PLGA in an appropriate amount of organic solvent, add a small amount of aqueous solution containing water-soluble drugs in proportion, add modified hyaluronic acid, and process it by ultrasonic or vibration to obtain the state Stable W / O emulsion;

[0039] c. Add a large amount of aqueous phase solution for the second emulsification treatment to obtain a W / O / W emulsion;

[0040] d. Remove the organic solvent by stirring and evaporating to obtain a microsphere suspension, and freeze-dry to obtain a microsphere powder.

[0041] Specifically, a preparation method of hyalur...

Embodiment 1

[0047] A preparation method of hyaluronic acid-parecoxib PLGA microspheres, comprising the following steps:

[0048] 1) Dissolve 200 mg of hyaluronic acid in 5 ml of deionized water, 80 mg of stearic acid in 25 ml of DMSO, add EDC to activate, mix the two solutions, add DMAP and stir overnight, precipitate with 300 ml of ethanol, and freeze-dry.

[0049] 2) Dissolve 40 mg parecoxib in 0.2 ml deionized water to form a uniform inner water phase, dissolve 240 mg PLGA in 2 ml dichloromethane as an oil phase, add the oil phase to the inner water phase, and add Amphiphilic hyaluronic acid (as surfactant).

[0050] 3) Immerse in an ice-water bath and stir for 1 min at high speed with a ultrasonic emulsifier to obtain colostrum. Drop the colostrum into 8ml of 4% PVA solution at a uniform speed and stir at high speed for 2 min to obtain double milk.

[0051]4) Transfer the double emulsion to a large volume of 100 ml 4% PVA aqueous solution, stir at a low speed for 3 hours to completel...

Embodiment 2

[0053] Example 2 Determination of drug loading and encapsulation efficiency

[0054] Weigh the weight of drug-loaded microspheres after lyophilization. Accurately weigh 20mg of microspheres and place them in a centrifuge tube, add 2ml of dichloromethane, and ultrasonically shake for 2 minutes to dissolve the microspheres; then dilute to 10ml with water, shake for 1 minute, let stand for 5 minutes, centrifuge at 10,000 rpm for 10 minutes, and take the supernatant solution; repeat the above steps twice, collect all the supernatant, and measure the absorbance value (A) with a UV spectrophotometer, drug loading = (mass of drug in microspheres / mass of drug-containing microspheres) × 100% , Encapsulation efficiency = (actual drug content in microspheres / theoretical drug content in microspheres) × 100%.

[0055] The drug loading rate of the microsphere obtained by the present invention is 20.95%, and the encapsulation rate is 54.70%.

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
encapsulation rateaaaaaaaaaa
Login to View More

Abstract

The invention discloses a hyaluronic acid-parecoxib PLGA microsphere and its preparation method and application. The invention modifies the hydrophilic hyaluronic acid, and grafts the hyaluronic acid with stearic acid to obtain the hyaluronic acid. It is transformed into an amphiphilic polymer as a surfactant, thereby reducing the interfacial tension of water and oil, which is conducive to better adsorption of drugs. Using double emulsification solvent volatilization method, dissolve PLGA in an appropriate amount of organic solvent, add a small amount of aqueous phase solution containing water-soluble drugs in proportion, add modified hyaluronic acid, and process it by ultrasonic or vibration to obtain a stable state. W / O emulsion, then add a large amount of water phase solution for the second emulsification treatment to obtain W / O / W emulsion, then remove the organic solvent by stirring and evaporating, and freeze-dry to obtain microsphere powder. The injection of the sustained-release microspheres of the present invention can effectively prolong the action time of the drug, reduce the toxicity and irritation of the drug, and release the drug slowly within a few weeks.

Description

technical field [0001] The invention belongs to the technical field of preparation of novel sustained-release microspheres for drug administration, and in particular relates to a hyaluronic acid-parecoxib PLGA microsphere and a preparation method and application thereof. Background technique [0002] As a new type of sustained-release preparation for controlled administration, microspheres can maintain long-term effective drug concentrations, reduce dosing frequency, and reduce drug toxicity and irritation. At present, for patients with temporomandibular joint pain, intra-articular injections of local anesthetics, non-steroidal anti-inflammatory drugs, hormones or hyaluronic acid have good curative effects. HA can nourish articular cartilage, reduce synovial inflammation and enhance joint lubrication. As a new type of non-steroidal anti-inflammatory drug, parecoxib is a potent and specific cyclooxygenase-2 inhibitor. Because of its good analgesic effect, good tolerance and ...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/36A61K47/34A61K31/42A61P29/00A61P19/02
CPCA61K9/5031A61K47/36A61K9/0019A61K31/42A61P29/00A61P19/02
Inventor 朱东望徐万宁白浩冉邓嘉胤
Owner STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com