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NSAID sustained-release nanoparticles and preparation method thereof

A nanoparticle and active component technology, applied in the field of medicine, can solve the problems of slow drug penetration through the skin, side effects, etc., achieve good sustained release effect, good biocompatibility, and improve medication compliance

Inactive Publication Date: 2018-08-28
HUMANWELL PURACAP PHARM WUHAN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First, the drug penetrates the skin very slowly (in μg / cm 2 / h is the unit of measurement)
Secondly, a large amount of skin penetration enhancers entering the host body may cause very serious side effects

Method used

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  • NSAID sustained-release nanoparticles and preparation method thereof
  • NSAID sustained-release nanoparticles and preparation method thereof
  • NSAID sustained-release nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 Preparation of NSAID sustained-release nanoparticles (indomethacin)

[0055] 1 Materials and equipment

[0056] 1.1 Polymers, proteins and materials in general

[0057]

[0058]

[0059] 1.2 Solvent

[0060]

[0061] 1.3 Equipment

[0062]

[0063]

[0064] 2 specific preparation steps:

[0065] PLGA nanoparticles loaded with NSAID (indomethacin) were prepared by single emulsion technique. 40 mg NSAID was dissolved in 2 ml PLGA (RG 504) in ethyl acetate (100 mg / ml). Then 4 ml of aqueous PVA (1% w / v) was added and the resulting o / w emulsion was sonicated on ice. The emulsion was diluted with 90 mL of PVA solution (0.3% w / v), and the solvent was quickly removed by rotary evaporation. Finally, the particles were isolated by centrifugation at 10,000 g (Beckman, Model J2-21 centrifuge) for half an hour and washed three times with water at the same centrifugation speed and processing time. Dried particles were collected by freeze drying.

[00...

Embodiment 2

[0071] Embodiment 2 prepares NSAID sustained-release nanoparticles (ketoprofen)

[0072] The specific preparation method is the same as in Example 1, except that indomethacin is replaced by ketoprofen.

Embodiment 3

[0073] Example 3 Characterization of General Evaluation Methods

[0074] 1. Characterization of nanoparticles

[0075] Laser diffraction analysis: Malvern Mastersizer 2000 was used to measure the particle size, and the Hydroμp sample dispersion unit was connected. 5-10 mg microparticles were dispersed in 1 ml deionized water and sonicated for 5 minutes before adding to the sample. The sample was added to the Mastersizer measuring cell, and the measurement process was controlled by Malvern Mastersizer 2000 software. Particle sizes were plotted as particle size distribution (by volume) and span values ​​were calculated. Span is a measure of the width of the volume distribution relative to the median diameter and is calculated as (D90%-D10%) / D50%. D90%, D50% and D10% are particle diameters measured at 90%, 50% and 10% volume distribution of cumulative particles, respectively. Samples were measured in triplicate.

[0076] Light Scattering Analysis

[0077] Particle size was ...

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Abstract

The invention discloses nonsteroidal anti-inflammatory drug (NSAID) sustained-release nanoparticles and a preparation method thereof, wherein the NSAID sustained-release nanoparticles contain an active component and a carrier, wherein the active component is NSAID, the carrier is polylactic acid polyglycolic acid copolymer (PLGA) nanoparticles, and the active component is loaded in the carrier. According to the present invention, the NSAID sustained-release nanoparticles have good biocompatibility and good slow-release effect, wherein the long-acting release time can reach 15-50 d.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to NSAID slow-release nanoparticles and a preparation method thereof. Background technique [0002] Certain NSAIDs have been used medicinally for over 100 years. NSAIDs are used to relieve the signs and symptoms of rheumatoid arthritis and osteoarthritis, relieve mild to moderate pain, reduce fever, and treat menstrual pain. They are the most widely used drugs in the world. However, the use of NSAIDs can produce many side effects, most notably gastrointestinal disturbances such as indigestion, heartburn, vomiting, gastric and duodenal bleeding, gastric ulcers and gastritis. Gastric and duodenal bleeding from NSAIDs is often painless but can cause blood in the stool and persistent iron deficiency anemia. The transdermal drug delivery system can help avoid direct drug damage to the gastrointestinal tract, as well as avoid drug inactivation caused by the "first-pass" e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/51A61K45/00A61K31/405A61K31/192A61K47/14A61K47/32A61P29/00A61P19/02A61P15/00
CPCA61K9/0002A61K9/0019A61K9/5123A61K9/5138A61K9/5146A61K31/192A61K31/405A61K45/00
Inventor 刘波叶翔沈福星
Owner HUMANWELL PURACAP PHARM WUHAN CO LTD
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