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A kind of magnetic fenofibrate-cyclodextrin inclusion compound

A technology of cyclodextrin inclusion compound and fenofibrate, which is applied in the direction of drug combination, drug delivery, organic active ingredients, etc., can solve the problems of low price, low inclusion efficiency, and short duration of blood drug concentration, etc. Achieve the effects of high inclusion rate, long dissolution time, and reduce the frequency of taking medicine

Active Publication Date: 2020-09-22
广东省药品检验所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] According to prior art reports, patent literature (CN102309476) reports a kind of fenofibrate composition, and is used as hard capsule, has used various pharmaceutical excipients, and the prepared fenofibrate has higher bioavailability, but The drug molecules cannot be released continuously, and the blood drug concentration of the prepared drug does not last long; the literature "Research on the inclusion of fenofibrate and two kinds of β-cyclodextrin water-soluble derivatives in aqueous solution, Gu Fugen, Zhongnan Pharmacy, 2013 ,4,11(4):258-260" reported that the inclusion of fenofibrate and β-cyclodextrin derivatives improved the solubility of fenofibrate, but due to the water solubility of cyclodextrin itself The performance is not as good as the solubility of its derivatives, and it cannot be directly used for inclusion, and its inclusion efficiency is very low. At this stage, cyclodextrin itself is rarely used for inclusion of drugs, and the price of cyclodextrin is relatively low on the market. Therefore, it is necessary to make full use of the cyclodextrin itself to include the drug and give full play to its inclusion performance

Method used

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  • A kind of magnetic fenofibrate-cyclodextrin inclusion compound
  • A kind of magnetic fenofibrate-cyclodextrin inclusion compound
  • A kind of magnetic fenofibrate-cyclodextrin inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: The fenofibrate-cyclodextrin inclusion compound comprises the following steps:

[0027] (1) Weigh 83 mg of fenofibrate, add appropriate amount of ethanol to dissolve;

[0028] (2) Weigh 1.3g of β-cyclodextrin, add 28mL of water to dissolve,

[0029] (3) Add the fenofibrate solution dropwise to the cyclodextrin solution under magnetic stirring, continue to stir for 2 hours, and filter to obtain clathrate A, wherein the stirring rate is 400rpm;

[0030] (4) Grinding the prepared clathrate A and sieving through 120 mesh;

[0031] (5) Mix and grind 6.5 mg of carboxymethyl cellulose, 13 mg of polyethylene glycol 400, 1.3 mg of ferric oxide powder and the above clathrate A, vibrate with a high-frequency ultrasonic device for 15 seconds every 3 minutes, and The oscillating frequency of the machine was 20KHz, and after grinding for 20 minutes, the fenofibrate-β-cyclodextrin inclusion compound was obtained by vacuum drying.

Embodiment 2

[0032] Embodiment 2: The fenofibrate-cyclodextrin inclusion compound comprises the following steps:

[0033] (1) Weigh 166 mg of fenofibrate, add appropriate amount of ethanol to dissolve;

[0034] (2) Weigh 1.4g of β-cyclodextrin, add 28mL of water to dissolve,

[0035] (3) Add the fenofibrate solution dropwise to the cyclodextrin solution under magnetic stirring, continue stirring for 3 hours, and filter to obtain clathrate A, wherein the stirring rate is 400 rpm;

[0036] (4) Grinding the prepared clathrate A and sieving through 120 mesh;

[0037] (5) Mix and grind 6.5 mg of carboxymethyl cellulose, 13 mg of polyethylene glycol 400, 0.8 mg of ferric oxide powder and the above-mentioned clathrate A, vibrate for 15 seconds with a high-frequency ultrasonicator every 3 minutes, and The oscillating frequency of the machine was 20KHz, and after grinding for 25 minutes, the fenofibrate-β-cyclodextrin inclusion compound was obtained by vacuum drying.

Embodiment 3

[0038] Embodiment 3: The fenofibrate-cyclodextrin inclusion compound comprises the following steps:

[0039] (1) Weigh 166 mg of fenofibrate, add appropriate amount of ethanol to dissolve;

[0040] (2) Weigh 1.3g of β-cyclodextrin, add 28mL of water to dissolve,

[0041] (3) Add the fenofibrate solution dropwise to the cyclodextrin solution under magnetic stirring, continue to stir for 4 hours, and filter to obtain clathrate A, wherein the stirring rate is 500rpm;

[0042] (4) Grinding the prepared clathrate A and sieving through 120 mesh;

[0043] (5) Mix and grind 10.0 mg of carboxymethyl cellulose, 20 mg of polyethylene glycol 400, 1.8 mg of ferric oxide powder and the above clathrate A, vibrate with a high-frequency ultrasonic device for 15 seconds every 3 minutes, and The oscillating frequency of the machine was 20KHz, and after grinding for 35 minutes, the fenofibrate-β-cyclodextrin inclusion compound was obtained by vacuum drying.

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PUM

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Abstract

The invention discloses a magnetic fenofibrate-cyclodextrin clathrate and a preparation method thereof. The magnetic fenofibrate-cyclodextrin clathrate comprises fenofibrate, beta-cyclodextrin, carboxymethyl cellulose, polyethylene glycol 400 and ferriferrous oxide. Compared with like products, the clathrate disclosed in the invention has the advantages of high clathration efficiency, good slow release effect on medicines, long-time release of the medicines, prolongation of the duration time of the medicines, and effective reduction of the medicine taking frequency.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a magnetic fenofibrate-cyclodextrin inclusion compound. Background technique [0002] Fenofibrate (FNB) is currently a commonly used blood lipid-lowering drug, which can reduce serum cholesterol, triacylglycerol and increase high-density lipoprotein. However, the drug is almost insoluble in water, and the release rate in pharmaceutical preparations is relatively slow, and the utilization rate in the human body is only 30%, and the effect of absorption is easily affected by food, and its therapeutic effect is obviously limited. [0003] β-cyclodextrin (β-CD) is a new type of pharmaceutical excipient, with a cone-shaped cylindrical three-dimensional structure, hydrophilic outside the ring, hydrophobic inside the ring, and can bind inorganic or organic compounds through weak van der Waals force. Synthetic inclusions. The special function of cyclodextrin makes it an inclu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/216A61K41/00A61K9/14A61P3/06
CPCA61K9/0002A61K9/146A61K31/216A61K41/00
Inventor 罗卓雅帅放文林生文王向锋章家伟王淼靳贵英
Owner 广东省药品检验所
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