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Peramivir pharmaceutical composition and preparation method thereof

A composition and medicine technology, applied in the field of peramivir pharmaceutical composition and preparation thereof, can solve the problems of high production cost and price of peramivir, and achieve the effects of good market prospect, simple process and low cost

Active Publication Date: 2022-03-15
朗天药业(湖北)有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the production cost and price of Peramivir are relatively high. As the demand for anti-influenza drugs in the market gradually increases, how to reduce the production cost of Peramivir has become an urgent task for those skilled in the art.

Method used

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Examples

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Effect test

preparation example Construction

[0032] The embodiment of this application provides a kind of preparation method of peramivir pharmaceutical composition, and preparation method comprises:

[0033] S100, dissolving peramivir in an organic solvent to obtain an oil phase solution;

[0034] S200, dissolving the excipient in water for injection to obtain an aqueous phase solution;

[0035] S300. Adding the aqueous phase solution into the oil phase solution dropwise, ultrasonic emulsification, and adding water for injection to obtain a peramivir pharmaceutical composition as an injection.

[0036] In some embodiments of the present application, the preparation method also includes:

[0037] S400. Sterilize and package the peramivir pharmaceutical composition.

[0038] It should be noted that the raw materials of peramivir used in the examples of this application can be purchased through commercial channels.

[0039] In some embodiments of the present application, S100 includes:

[0040] S110, according to the m...

Embodiment 1

[0068] This embodiment provides a preparation method of the peramivir pharmaceutical composition, specifically as follows.

[0069] S1-1. According to the mass ratio of peramivir:organic solvent=20:100, the peramivir was dissolved in the organic solvent at a temperature of 60° C. to obtain an oil phase solution. The organic solvent includes: nicotinamide, 5 parts by mass; polyoxyethylene castor oil, 45 parts by mass; ethyl oleate, 50 parts by mass.

[0070] S1-2. Dissolving the excipients in the water for injection according to the mass ratio of excipients: water for injection = 16:100 to obtain an aqueous phase solution. The auxiliary materials include: sodium sulfite, 8 parts by mass, and polysorbate, 8 parts by mass.

[0071] S1-3. According to the mass ratio of water phase solution: oil phase solution=40:100, the water phase solution is added dropwise into the oil phase solution and ultrasonically emulsified and supplemented with water for injection to obtain the peramivi...

Embodiment 2

[0073] This embodiment provides a preparation method of the peramivir pharmaceutical composition, specifically as follows.

[0074] S2-1. According to the mass ratio of peramivir: organic solvent = 30:100, the peramivir is dissolved in the organic solvent at a temperature of 65° C. to obtain an oil phase solution. The organic solvent includes: nicotinamide, 10 parts by mass; polyoxyethylene castor oil, 50 parts by mass; ethyl oleate, 40 parts by mass.

[0075] S2-2. Dissolving the excipients in the water for injection according to the mass ratio of excipients: water for injection = 20:100 to obtain an aqueous phase solution. The auxiliary materials include: sodium sulfite, 10 parts by mass, and polysorbate, 10 parts by mass.

[0076] S2-3, according to the mass ratio of water phase solution: oil phase solution=60:100, the water phase solution is added dropwise into the oil phase solution and ultrasonically emulsified and supplemented with water for injection to obtain the per...

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Abstract

The invention discloses a peramivir pharmaceutical composition and a preparation method thereof. The preparation method comprises the following steps: S100, dissolving peramivir in an organic solvent to obtain an oil phase solution; s200, dissolving the auxiliary materials in the water for injection to obtain a water-phase solution; and S300, dropwise adding the aqueous phase solution into the oil phase solution, and carrying out ultrasonic emulsification to obtain the peramivir pharmaceutical composition. The peramivir pharmaceutical composition obtained by the invention is simple in process and low in cost.

Description

technical field [0001] The application belongs to the technical field of medicinal chemistry, and in particular relates to a peramivir pharmaceutical composition and a preparation method thereof. Background technique [0002] The English name of Peramivir is Peramivirtrihydrate, and its chemical name is (1S, 2S, 3R, 4R, 1'S)-3-[(1'-acetylamino-2'-ethyl)butyl)]-4-[[ (aminoimino)methyl]amino]-2-hydroxycyclopentane-1-carboxylic acid trihydrate. [0003] Peramivir itself is a cyclopentane derivative neuraminidase inhibitor. The drug can effectively inhibit the replication and transmission process of various influenza virus strains, has the advantages of good tolerance, low toxicity, practical application for injection, etc., and is a promising anti-influenza drug. [0004] However, the production cost and price of peramivir are relatively high. As the market demand for anti-influenza drugs gradually increases, how to reduce the production cost of peramivir has become a top pri...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/44A61K47/14A61K47/22A61K47/02A61K47/26A61K31/196A61P31/16
CPCA61K9/08A61K9/0019A61K47/44A61K47/14A61K47/22A61K47/02A61K47/26A61K31/196A61P31/16
Inventor 蔡翔黎翩陈景丽陆文婷张友民蔡华冯廷松皮培培李英潘林方贤贵蔡和霖张显强
Owner 朗天药业(湖北)有限公司
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