Preparation method of aprepitant preparation

A prepitant and preparation technology, applied in the field of preparation of aprepitant micellar intravenous injection, can solve problems such as poor solubility of aprepitant, achieve good stability, mature technology, and overcome poor medication compliance

Inactive Publication Date: 2021-01-08
SUZHOU HAITE BIAO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the problem of poor solubility of aprepitant in water, and provide a preparation method of aprepitant micellar intravenous injection

Method used

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  • Preparation method of aprepitant preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] (1) Preparation of polyethylene glycol monomethyl ether-polylactic acid block polymer:

[0049](a) Weigh 51.07g of D,L-lactide and 50.57g of polyethylene glycol monomethyl ether 2000 for later use, dry polyethylene glycol monomethyl ether 2000 in vacuum at 100°C for 7 hours, replace with nitrogen, add D, For L-lactide, put in 0.2g catalyst stannous octoate, evacuate to a vacuum degree of 0.096Mpa, seal it, and keep the reaction temperature at about 100°C. Vacuumize the reactor to ensure a negative pressure in the reactor, seal it, heat up to 140°C, and react for 12 hours. After the reaction is completed, a light yellow, clear and viscous liquid is obtained.

[0050] (b) Add dichloromethane to the light yellow clear viscous liquid obtained in step (a), add 25ml of dichloromethane, stir for 30min; then add 510ml of anhydrous glacial ether, stir for 30min; then statically Set aside for 12 hours, vacuum-dried by suction filtration to obtain polyethylene glycol monomethyl e...

Embodiment 2

[0057] The preparation method of the aprepitant micelle preparation of the embodiment of the present invention comprises the following steps:

[0058] First, after mixing 0.02g of aprepitant and 0.156g of polyethylene glycol monomethyl ether polylactic acid block copolymer, add 5ml of acetonitrile solvent and stir until dissolved. During the stirring process, the temperature of the mixture is controlled at 20°C to 30°C between ℃.

[0059] Then, it was aseptically filtered with a 0.22 μm organic filter membrane into a dry and constant temperature eggplant-shaped bottle.

[0060] The solution formed above was heated in a water bath, the organic solvent was vacuum-dried, and the mixture was stirred at a high speed of 280 r / min, and the temperature was controlled between 50°C and 55°C. Prepare the gel mixture, then add 10ml of pure water phase to the above gel, and rotate at a high speed of 280r / min to form the aprepitant micelle preparation, which is then filtered through a 0.22...

Embodiment 3

[0062] The preparation method of the aprepitant milk preparation of the embodiment of the present invention comprises the following steps:

[0063] First, after mixing 0.02g of aprepitant and 0.156g of polyethylene glycol monomethyl ether polylactic acid block copolymer, add 5ml of acetonitrile solvent and stir until dissolved. During the stirring process, the temperature of the mixture is controlled at 20°C to 30°C between ℃.

[0064] Then, it was aseptically filtered with a 0.22 μm organic filter membrane into a dry and constant temperature eggplant-shaped bottle.

[0065] The solution formed above was heated in a water bath, the organic solvent was vacuum-dried, the mixture was stirred at a high speed at 200 r / min, and the temperature was controlled between 50°C and 55°C. Prepare the gel mixture, then add 2ml of the pure water phase to the above gel, and rotate at a high speed of 280r / min to form the aprepitant micelle preparation, which is then filtered through a 0.22 μm ...

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Abstract

The invention discloses a preparation method of an aprepitant micelle intravenous injection, and belongs to the field of pharmacy. The aprepitant micelle intravenous injection comprises the followingcomponents in percentage by mass: 2-10% of aprepitant and 90-98% of a surfactant. The micelle provided by the invention is used for clinically treating nausea and vomiting of tumor patients after chemotherapy, reducing nausea and vomiting in the early and middle stages of tumor chemotherapy, improving the immunity of tumor patients and improving the nutritional support of patients; and the acute and delayed nausea and vomiting caused by high-dose cisplatin combined high-dose sensitization cancer chemotherapy are reduced, and the rehabilitation of tumor patients is facilitated.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a preparation method of aprepitant micellar intravenous injection. Background technique [0002] Currently, chemotherapy is one of the main modalities for cancer treatment. However, the strong side effects of nausea and vomiting (Chemotherapy Nausea and Vomiting, CINV) caused by chemotherapy make patients suffer, and many people are discouraged from follow-up treatment. [0003] Aprepitant is a new generation of antiemetic drugs approved by the US FDA in 2003. Its main mechanism of action is different from traditional antiemetic drugs. It can cross the blood-brain barrier and interact with brain neurokinin-1 (NK-1 ) receptor binding, blocking the combination of NK-1 receptors and substance P (a neurokinin located in the neurons of the central and peripheral nervous systems, which can induce vomiting through the mediation of NK-1 receptors), Thereby inhibiting the vomiting ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/5377A61P1/08
CPCA61K9/1075A61K9/0019A61K47/34A61K31/5377A61P1/08
Inventor 阮君山杜鹏飞费芳张金海
Owner SUZHOU HAITE BIAO BIOLOGICAL TECH
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