Aspirin solid dispersion, as well as preparation method, pharmaceutical composition and use thereof

A technology of solid dispersion and aspirin, applied in the field of medicine, can solve the problems of increased incidence of toxic and side effects, reduced drug efficacy, long time consumption, etc.

Active Publication Date: 2012-07-04
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported that polylactic acid (Mw=62,000) was used as a drug carrier, and aspirin was made into sustained-release microspheres by solvent evaporation method, but the water phase was involved in the preparation process, and the preparation process took a long time, and aspirin was easily absorbed in water. Hydrolysis produces salicylic acid, resulting in low encapsulation efficiency, reduced drug efficacy, and increased incidence of toxic and side effects

Method used

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  • Aspirin solid dispersion, as well as preparation method, pharmaceutical composition and use thereof
  • Aspirin solid dispersion, as well as preparation method, pharmaceutical composition and use thereof
  • Aspirin solid dispersion, as well as preparation method, pharmaceutical composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Feeding amount:

[0080] Aspirin 0.15g

[0081] mPEG-PLA (Mw=2000 / 20000) 3.0g

[0082] Chloroform 30ml

[0083] Preparation method: Take mPEG-PLA, add chloroform, dissolve it by ultrasonication, add aspirin, dissolve it by ultrasonication, and spray dry. The air volume of the ring fan in the spray drying process is 90%, the nitrogen flow rate is 4L / min, the air inlet temperature is 35°C, and the peristaltic pump is used. Feed rate 20%. After the drying is completed, the solid dispersion is collected to obtain the obtained product.

[0084] Aspirin content: 4.5%.

[0085] In this example, the molecular structural formula of mPEG-PLA is

[0086]

[0087] Among them: m≈45, n≈276.

Embodiment 2

[0089] Feeding amount:

[0090] Aspirin 0.15g

[0091] Allanine derivatives of mPEG-PLA 3.0g

[0092] Chloroform 30ml

[0093] Note: The molecular structural formula of the aminopropionic acid derivative of mPEG-PLA is

[0094]

[0095] Where: m≈45, n≈276, R=-COCH 2 CH 2 NH 2

[0096] Preparation method: Take the aminopropionic acid derivative of mPEG-PLA, add chloroform, dissolve by ultrasonication, add aspirin, dissolve by ultrasonication, and spray dry. The air volume of the ring fan is 90%, the nitrogen flow rate is 4L / min, and the air inlet temperature is 35°C. Peristaltic pump feed rate 20%. After the drying is completed, the solid dispersion is collected to obtain the obtained product.

[0097] Aspirin content: 4.7%.

Embodiment 3

[0099] Feeding amount:

[0100] Aspirin 0.5g

[0101] mPEG-PLA (Mw=2000 / 80000) 5.0g

[0102] Cholesterol 0.25g

[0103] Dichloromethane 35ml

[0104] Preparation method: Take mPEG-PLA, add dichloromethane, dissolve it by ultrasonication, add cholesterol and aspirin in turn, dissolve it by ultrasonication, and spray dry. Pump feed rate 10%. After the drying is completed, the solid dispersion is collected to obtain the obtained product.

[0105] Aspirin content: 8.3%.

[0106] In this example, the molecular structural formula of mPEG-PLA is

[0107]

[0108] Among them: m≈45, n≈1104.

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PUM

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Abstract

The invention relates to an aspirin solid dispersion, as well as a preparation and use thereof. The aspirin solid dispersion provided by the invention is prepared by taking a methoxy-terminated polyethylene glycol-polylactic acid block copolymer and derivatives thereof, polylactic acid, a polylactic acid-glycollic acid copolymer or polycaprolactone as carrier materials and performing preparation through a solvent method or a hot melting method. According to the preparation method of the aspirin solid dispersion, provided by the invention, hydrolysis of aspirin can be avoided, and toxicity and side effects can be further reduced. The aspirin solid dispersion provided by the invention can be used for relieving fever, relieving pain, resisting rheumatic fever, resisting rheumatism or rheumatoid arthritis and resisting thrombus by subcutaneous or intramuscular injection.

Description

technical field [0001] The invention relates to the technical field of medicine. Specifically, the present invention relates to a solid dispersion of aspirin, and a preparation method and use of the solid dispersion. Background technique [0002] Aspirin is an antipyretic and analgesic with a long history, which was born on March 6, 1899. So far, aspirin has been used for a hundred years and has become one of the three classic drugs in the history of medicine. It is still the most widely used antipyretic, analgesic and anti-inflammatory drug in the world, and it is also used as a standard preparation for comparing and evaluating other drugs. Especially later, scientists discovered that aspirin also has antithrombotic effect in the body, it can inhibit the release reaction of platelets, inhibit the aggregation of platelets, and opened up a new era for the clinical prevention of cardiovascular and cerebrovascular diseases. [0003] Currently, the common clinical indications ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/616A61K47/34A61P29/00A61P19/02A61P19/04A61P7/02
Inventor 胡忍乐王九成焦亚奇丁多浩孙亚利夏磊吴建立
Owner XIAN LIBANG PHARMA TECH
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