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A kind of fenofibrate nano suspension and preparation method thereof

A nano-suspension and fenofibrate technology, applied in the field of medicine, can solve the problems of high cost, debris pollution of grinding machines, and restrictions on the popularization and use of fenofibrate, and achieve low preparation cost and mild preparation method conditions Effect

Active Publication Date: 2016-08-24
江苏一南生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The fenofibrate tablets currently on the market use grinding technology to reduce the particle size of fenofibrate raw materials to the nanometer level and prepare them into nanosuspensions, which improves the oral absorption of fenofibrate, but the cost of this technology Very high, and there will be debris pollution from the grinder, which limits the promotion and use of fenofibrate

Method used

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  • A kind of fenofibrate nano suspension and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0019] Dissolve 0.1 g of fenofibrate and 0.01 g of copovidone PVP S 630 in 25 mL of absolute ethanol, slowly add 0.01 g of PVP K-90 into 1000 mL of water, evaporate at 40°C, and evaporate the ethanol , to obtain fenofibrate nanosuspension, the concentration of fenofibrate is 0.1 mg / ml. The average particle size of the fenofibrate nanosuspension was measured, and the result was 362 nm, and the suspension remained stable within 48 h.

Embodiment 2

[0021] Dissolve 0.1 g of fenofibrate and 0.05 g of copovidone PVP S 630 in 50 mL of 95% ethanol, slowly add 0.05 g of PVP K-90 into 400 mL of water, evaporate at 40°C, and evaporate the ethanol , to obtain fenofibrate nanosuspension, the concentration of fenofibrate is 0.3 mg / ml. Measure the average particle diameter of fenofibrate nanosuspension, the result is 157 nm (the transmission electron microscope figure of fenofibrate nanosuspension is shown in figure 1 ), the suspension remained stable within 48 h.

Embodiment 3

[0023] Dissolve 0.1 g of fenofibrate and 0.02 g of copovidone PVP S 630 in 20 mL of absolute ethanol, slowly add 0.02 g of PVP K-90 into 200 mL of water, rotate to evaporate at 40°C, and evaporate the ethanol , to obtain fenofibrate nanosuspension, the concentration of fenofibrate is 0.5 mg / ml. The average particle size of the fenofibrate nanosuspension was measured, and the result was 383 nm, and the suspension remained stable within 48 h.

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Abstract

The invention belongs to the field of medical technology, and discloses a fenofibrate nano suspension and a preparation method of the fenofibrate nano suspension. As fenofibrate is merely dissolved in water, and the oral bioavailability is low, the popularization and application of the fenofibrate are limited. The fenofibrate nano suspension is characterized by containing fenofibrate, copovidone PVPS630 and povidone PVPK-90, and the mass ratio of the fenofibrate to the copovidone PVPS630 and the povidone PVPK-90 is (4-10):(1-2):(1-2). The preparation method of the nano suspension is moderate in condition and simple and controllable, and high oral bioavailability of the fenofibrate is achieved.

Description

technical field [0001] The invention relates to a fenofibrate nano-suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Fenofibrate is the third generation of clofibrate lipid-lowering drugs. Its main mechanism of action is to reduce the synthesis of cholesterol in cells by inhibiting HMG-CoA reductase, so as to achieve the purpose of lowering blood lipids. Due to the extremely low solubility of fenofibrate in water, the oral bioavailability is poor, which limits its full efficacy. Nanosuspension is a new nano-drug loading system for insoluble drugs that has emerged in recent years. Nanosuspension can improve the solubility and dissolution rate of insoluble drugs by reducing the drug particle size and increasing its specific surface area. Thereby improving its oral bioavailability and having good antitumor effect at the same time. The solubility of fenofibrate in water is very small, and the oral bioavaila...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/216A61K47/32A61P3/06
Inventor 罗瑞雪张振海
Owner 江苏一南生物科技有限公司
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