A kind of preparation method of fenofibrate nano freeze-dried composition

A technology of fenofibrate and composition, which is applied in the field of preparation of fenofibrate nano freeze-dried composition, can solve the problems of drug loss, long preparation time, and restrictions on popularization and use of fenofibrate nano preparations

Active Publication Date: 2021-09-10
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this technology has disadvantages such as very high preparation cost, long preparation time, drug loss caused by product adhesion, and product contamination caused by mechanical debris, which limits the further promotion and use of fenofibrate nano-preparation

Method used

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  • A kind of preparation method of fenofibrate nano freeze-dried composition
  • A kind of preparation method of fenofibrate nano freeze-dried composition
  • A kind of preparation method of fenofibrate nano freeze-dried composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Change temperature, stirring speed and stirring time to prepare nano-suspension and particle size potential measurement

[0023] (1) Weigh 10mg of fenofibrate, dissolve it in 1mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, quickly inject the organic phase into 10mL of water in a cold water bath at about 5°C, and continue stirring at 50rpm for 5 seconds to obtain Transparent, light blue opalescent fenofibrate nanosuspension, the concentration of fenofibrate is 1mg / mL, the measured average particle size is 299nm (PDI=0.134), and the average zeta potential tends to zero. Flocculate after half an hour at room temperature.

[0024] (2) Weigh 10mg of fenofibrate, dissolve it in 1mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, quickly inject the organic phase into 10mL of water in a cold water bath at about 5°C, and continue stirring at 100rpm for 5 seconds to obtain Transparent...

Embodiment 2

[0027] Example 2 Increase high-speed shearing to prepare nano-suspension and particle size potential measurement

[0028] (1) Weigh 10 mg of fenofibrate, dissolve it in 1 mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, quickly inject the organic phase into 10 mL of water in an ice-water bath (about 0°C), and continue stirring at 50 rpm for about In 10 seconds, the suspension was transferred to a high-speed shearing machine, and was sheared at 3000rpm for 3min to obtain transparent fenofibrate nanosuspension with light blue opalescence, and the concentration of fenofibrate was 1mg / mL, measured The average particle size is 168nm (PDI=0.098), and it flocculates after being left at room temperature for about 1 hour.

[0029] (2) Weigh 10mg of fenofibrate, dissolve it in 1mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, quickly inject the organic phase into 10mL of water in an ice-water bath (abo...

Embodiment 3

[0032] Example 3 Adding water phase stabilizer to prepare nanosuspension and particle size potential measurement

[0033] (1) Weigh 10mg of fenofibrate, dissolve it in 1mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, and quickly inject the organic phase into 10mL of 400% HPMC in an ice-water bath (about 0°C) -In the water phase of E5 and 400% SDS, continue stirring at 50rpm for about 10 seconds, transfer the suspension to a high-speed shearing machine, and shear at 3000rpm for 1min to obtain transparent, light blue opalescent fenofibrate nano Suspension, the concentration of fenofibrate is 1mg / mL, the measured average particle size is 208nm (PDI=0.210), the average zeta potential is -10.1mV, it can be stable for 3 hours at room temperature, and there is no obvious flocculation phenomenon.

[0034] (2) Weigh 10mg of fenofibrate, dissolve it in 1mL of absolute ethanol, heat and dissolve in a water bath at 60°C to form an organic phase, a...

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Abstract

The invention provides a fenofibrate nano freeze-dried composition and a preparation method thereof. The preparation method comprises: preparing a nano-suspension, and freeze-drying the suspension. The preparation method provided by the present invention does not need to micronize the raw material drug in advance, which greatly reduces the energy consumption required for the experiment; the experimental conditions of the present invention are mild and controllable, the preparation time is short, and the production cycle is greatly shortened; there is no need to use high-pressure homogenization or Methods such as mechanical grinding have low requirements on equipment, low energy consumption, and are not prone to debris pollution; they are simple to operate, have good reproducibility, low cost, and are easy to realize industrial scale-up production. In the nanosuspension prepared by the invention, the particle size of the drug nanoparticles in the suspension is controlled at 150-350nm, the dissolution and release are fast, the gastrointestinal transmembrane transport capacity of fenofibrate is greatly improved, and the absorption of fenofibrate is promoted. .

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of an insoluble drug fenofibrate nano freeze-dried composition, in particular to a preparation method of a fenofibrate nano freeze-dried composition. Background technique [0002] Fenofibrate (Fenofibrate; molecular formula: C 20 h 21 ClO 4 ; Molecular weight: 360.83; Chemical name: 2-methyl-2-[4-(4-chlorobenzoyl)phenoxy]propionic acid isopropyl ester). Fenofibrate is the third-generation phenoxyacetic acid blood lipid-regulating drug. The pharmacological effect is similar to that of clofibrate. It has the characteristics of good curative effect and less adverse reactions. Clinically, fenofibrate is the first choice for lowering triglycerides. As one of the drugs, it can also reduce the level of blood uric acid, and it also has a good effect on the treatment of type II diabetes and metabolic syndrome, and the market prospect is good. [0003] Fenofibrate i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/216A61K47/26A61K47/10A61K47/18A61P3/06
CPCA61K9/19A61K31/216A61K47/10A61K47/183A61K47/26A61P3/06
Inventor 胡富强孟廷廷袁弘敖嘉祺
Owner ZHEJIANG UNIV
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