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Aprepitant nano composition

A kind of aprepitant nanometer and nanometer composition technology, which is applied in the field of aprepitant nanometer composition and its preparation, and can solve the problems of reduced stability, increased production cost, product pollution and the like

Inactive Publication Date: 2016-08-24
北京乐嘉宝医药科技有限责任公司
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  • Application Information

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Problems solved by technology

Moreover, the nanotechnology significantly reduces the food effect of aprepitant, and the bioavailability of ordinary tablets will increase by 4 times in the fed state, while the bioavailability of the nanosized preparations before and after feeding has no significant change
However, there is a problem worthy of attention in the above-mentioned technology, that is, the quality and durability of the grinding media, and the product pollution caused by the wear of the grinding media during the preparation process; in addition, the media grinding method takes a long time, and a production cycle can be long Hours to days, which also brings inconvenience to production, resulting in increased production costs, and the risk of reduced stability and increased contamination

Method used

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Embodiment Construction

[0009] Purpose of the invention: provide a kind of aprepitant nano-composition with high solubility, good stability and high bioavailability and its preparation method, the aprepitant nano-composition can be effectively used for acute and delayed post-chemotherapy Nausea or vomiting attacks, can also be used for the treatment of major depressive disorder (accompanied by anxiety).

[0010] Technical solution: a novel aprepitant nano composition, characterized in that: the aprepitant nano composition includes aprepitant or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier and / or excipients.

[0011] The adjuvant includes the following components:

[0012] Emulsifiers, co-emulsifiers, oil phases, stabilizers, co-stabilizers and solid adsorbents.

[0013] Preferably, the nanocomposition has the following release characteristics, in a dissolution medium of 0.1 mol / L hydrochloric acid solution, at least 20% is released in 5 minutes, at least 7...

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Abstract

The invention discloses an aprepitant nano composition which is composed of aprepitant, an oil phase, an emulsifier, a co-emulsifier, a stabilizer, an auxiliary stabilizer and an optional solid adsorbent. The aprepitant nano composition significantly improves solubility, stability and bioavailability of the aprepitant.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a nano composition of aprepitant and a preparation method thereof. That is, the solubility, stability and bioavailability of aprepitant are improved by preparing nano-preparation of aprepitant. Background technique: [0002] Chemotherapy-induced nausea and vomiting (CINV) is the most common adverse reaction during the use of tumor chemotherapy drugs. This adverse reaction reduces the compliance of cancer patients and leads to unsatisfactory tumor control effects. disorders, malnutrition, and aspiration pneumonia. Therefore, timely and effective prevention and reduction of nausea and vomiting caused by chemotherapy, relief of patients' psychological pressure, and improvement of anti-tumor treatment effects are urgent problems to be solved in the process of cancer chemotherapy. [0003] Since the launch of ondansetron hydrochloride in 1990, "setron" drugs have been occupying the ...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K47/24A61K47/38A61K47/04A61P1/08A61P35/00A61P25/24A61P25/22B82Y5/00
Inventor 李馨儒刘艳杨卓理陈蒙蒙
Owner 北京乐嘉宝医药科技有限责任公司
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