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Fenofibrate solid dispersion body, and preparation method and application thereof

A technology of solid dispersion and fenofibrate, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas. It can solve the problems of poor powder fluidity and achieve high dissolution rate, Improvement of wettability and improvement of in vitro dissolution effect

Active Publication Date: 2017-05-31
GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solid dispersion is mainly prepared from fenofibrate, mesoporous silica and polymer carrier materials, which can not only ensure the long-term stable and highly dispersed state of the drug, but also overcome the problem of poor fluidity of the mesoporous silica preparation powder. question

Method used

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  • Fenofibrate solid dispersion body, and preparation method and application thereof
  • Fenofibrate solid dispersion body, and preparation method and application thereof
  • Fenofibrate solid dispersion body, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of Mesoporous Silica SBA-15

[0040]Dissolve 8g of triblock copolymer polyvinyl ether-polypropylene ether-polyethylene (P123) in 363mL of 2mol / L hydrochloric acid, and stir at 40°C until the solution forms a light blue transparent homogeneous system. Under continuous stirring, slowly add 17.53g of tetraethyl orthosilicate (TEOS) dropwise, continue stirring for 24h, and move the reactant to the reaction solution for crystallization at 100°C for 48h. Then the product is taken out and cooled, collected by centrifugation, washed with water until neutral, washed with ethanol, and collected by centrifugation. The product was vacuum-dried at 40° C., and then calcined in a muffle furnace at 550° C. for 6 hours to remove the template agent P123 to obtain the mesoporous silica SBA-15.

[0041] The appearance and pore structure of the synthesized mesoporous silica SBA-15 were characterized by scanning electron microscope and transmission electron microscope...

Embodiment 2

[0043] Example 2: Preparation and phase characterization of fenofibrate solid dispersion

[0044] This embodiment prepares the solid dispersion of fenofibrate according to the weight ratio of raw materials shown in the table below:

[0045] prescription number Fenofibrate SBA-15 PVP / VA64 1 2 copies 1 copy 7 copies 2 2 copies 2 copies 6 servings 3 2 copies 3 copies 5 copies 4 2 copies 4 parts 4 parts

[0046] The preparation of the fenofibrate solid dispersion of the present embodiment comprises the following steps:

[0047] 1. Loading of fenofibrate

[0048] Dissolve fenofibrate in absolute ethanol, add mesoporous silica SBA-15 prepared in Example 1, stir magnetically for 6 hours, and remove ethanol by rotary evaporation to obtain drug-loaded SBA-15. SBA-15 is designated FNB-SBA-15.

[0049] 2. Preparation of fenofibrate solid dispersion by hot melt extrusion

[0050] Grind and mix FNB-SBA-15 and PVP / VA64, add the...

Embodiment 3

[0055] Embodiment 3: Investigation on the powder properties of fenofibrate solid dispersion

[0056] The powder properties of the fenofibrate solid dispersion prepared in Example 2 were investigated, mainly including the density, angle of repose and contact angle of the powder. The objects of investigation are fenofibrate solid dispersions FSP1, FSP2, FSP3, FSP4 and FNB-SBA-15 prepared according to Example 2 (the mass ratio of fenofibrate: SBA-15 is 2:4) and fenofibrate Special raw materials. The test method is as follows:

[0057] 1. Tap density and bulk density

[0058] The sample is passed through a 80-mesh sieve, and accurately weighed (W powder ), carefully transfer to a graduated cylinder, and record the initial volume of the sample (V o ), mechanically vibrate the measuring cylinder containing the sample powder, tap until the volume no longer changes, record the powder volume at this time (V f ). with the formula W powder / V o and W powder / V f Calculate the b...

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Abstract

The invention relates to a fenofibrate solid dispersion body, and a preparation method and application thereof. The fenofibrate solid dispersion body is mainly prepared from following raw materials: fenofibrate, mesoporous silica, and a macromolecule carrier material, wherein the content of fenofibrate (in mass) is 10-40%; the mass ratio of mesoporous silica to the macromolecule carrier material is 1:(0.2-10); the macromolecule carrier material is selected from at least one of copovidone, povidone, polyethylene glycol, and a polyethylene glycol / vinyl-epsilon-caprolactam / vinyl acetate copolymer. The fenofibrate solid dispersion body disclosed by the invention is good in in vitro dissolution effect, and high in vivo bioavailability; and by using the fenofibrate solid dispersion body, powder has high liquidity, and drugs have high physical stability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a fenofibrate solid dispersion and its preparation method and application. Background technique [0002] Fenofibrate (FNB), the chemical name is 2-methyl-2-(4-(4-chlorobenzoyl)phenoxy) isopropyl propionate, which is the second generation of phenoxyaromatic acids Blood lipid-lowering drugs are mainly used clinically to treat type IIa, IV, IIb, and type III hyperlipoproteinemia and endogenous hypertriglyceridemia, and are currently the most used drugs among fibrates. Fenofibrate has strong lipophilicity and low solubility in water, which leads to incomplete absorption of the drug in the gastrointestinal tract, and the absorption is greatly affected by food. The in vivo absorption of the drug with food and alone The rate difference is about 35%. In addition, fenofibrate has a liver first-pass effect, which all lead to its low bioavailability in vivo. Therefore, how to im...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/216A61K47/04A61K47/32A61P3/06
CPCA61K9/143A61K9/146A61K31/216
Inventor 吴传斌牛博艺吴巧利权桂兰潘昕
Owner GUANGZHOU ZHONGDA NANSHA TECH INNOVATION IND PARK
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