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Oseltamivir phosphate dry suspension and preparation method thereof

A technology of oseltamivir phosphate and dry suspension, which is applied in the field of medicine and chemical industry, and can solve the problems of high cost, high control standard of excipients, and difficult to control or achieve

Inactive Publication Date: 2014-11-12
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Oseltamivir phosphate is easy to react with the reduced sugar alcohol in the composition. In order to overcome this technical problem in the prior art CN 101389323 A, in order to achieve the purpose of stabilizing the composition, it is required that the added excipients be selected from among 25 One or more sugars and sugar alcohols having an equilibrium moisture content of 1% by weight at ℃ and a relative humidity of 70%, and the content of glucose and mannose contained in the sugars and sugar alcohols as impurities relative to the sugars and sugar alcohols is Below 0.01% by weight, high quality requirements are required for the added sugar alcohols, so the control standards for auxiliary materials are very high, and it is not easy to control or achieve. In addition, the cost will also become higher due to the harsh quality requirements of auxiliary materials. Therefore, Not suitable for industrial production, cost saving

Method used

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  • Oseltamivir phosphate dry suspension and preparation method thereof
  • Oseltamivir phosphate dry suspension and preparation method thereof
  • Oseltamivir phosphate dry suspension and preparation method thereof

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specific Embodiment approach

[0068] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0069] In this embodiment, the percentages described in the specific embodiments are by mass ratio.

[0070] The reagents used in this example can be purchased from the market or can be prepared by the methods described in the present invention.

[0071] In this embodiment, sorbitol is purchased from Roquette, which meets the USP-NF excipient standard, wherein the limit of reducing sugar is less than 0.3% (calculated as sucrose)

Embodiment 1

[0073] prescription:

[0074] components

content

Oseltamivir Phosphate

3.5％

Mannitol

49.6％

Sorbitol

34.1％

xanthan gum

4.5％

Titanium dioxide

2.5％

Sodium citrate

4.0％

Citric Acid Monohydrate

0.8％

[0075] sodium benzoate

1.0％

total

100.0％

[0076] Preparation:

[0077]Weigh an appropriate amount of oseltamivir phosphate and auxiliary materials according to the prescription amount, add 3.5% oseltamivir phosphate, 34.1% sorbitol, 49.6% mannitol, 2.5% titanium dioxide, 4.0% sodium citrate, 0.8% a Hydrated citric acid, 1.0% sodium benzoate and 4.5% xanthan gum were uniformly mixed in a granulator, the blade speed of the granulator was 150rpm, the cutter speed was 3000rpm, and then passed through a 30-mesh sieve for 3 times.

Embodiment 2

[0079] prescription:

[0080] components

content

Oseltamivir Phosphate

3.8％

Mannitol

70.8％

Sorbitol

23.5％

Hydroxypropyl Cellulose

0.1％

Titanium dioxide

0.5％

Sodium citrate

1.0％

Citric Acid Monohydrate

0.2％

sodium benzoate

0.1％

total

100.0％

[0081] Preparation Process:

[0082] Weigh an appropriate amount of oseltamivir phosphate and auxiliary materials according to the prescription amount, add 3.8% oseltamivir phosphate, 23.5% sorbitol, 70.8% mannitol, 0.5% titanium dioxide, 1.0% sodium citrate, 0.2% a Hydrated citric acid, 0.1% sodium benzoate and 0.1% hydroxypropyl cellulose are mixed uniformly in a granulator, the blade speed of the granulator is 150rpm, the cutter speed is 3000rpm, and then passed through a 30-mesh sieve for 3 times.

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Abstract

The invention provides an oseltamivir phosphate dry suspension. The oseltamivir phosphate dry suspension comprises oseltamivir phosphate, filler not prone to reacting with the oseltamivir phosphate and other pharmaceutically acceptable accessories, wherein the filler is one or more of maltitol, xylitol and mannitol or is the composition of one or more of the maltitol, the xylitol and the mannitol and sorbitol, the content of the sorbitol in the whole composition is X, and X large than or equal to 0% and less than or equal to 75%. Meanwhile, the invention provides a preparation method of the oseltamivir phosphate dry suspension. Preferably, the preparation method is a step-by-step wet preparation method. The oseltamivir phosphate dry suspension is good in stability, low in cost, simple in preparation technology and capable of being produced in an industrial mode easily.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, and more specifically, to oseltamivir phosphate dry suspension and a preparation method thereof. Background technique [0002] Oseltamivir phosphate, chemical name (-)-(3R,4R,5S)-4-acetamide-5-amino-3-(1-ethylpropoxy)cyclohexyl-1-carboxylate ethyl ester phosphate. The chemical structural formula is as follows: [0003] [0004] Developed and launched by Roche, Switzerland, oseltamivir phosphate has a strong neuraminidase inhibitory activity and is effective against influenza A and B viruses. Information on its properties and preparation methods are disclosed in WO 1998007685 A1 and WO 1996026933 A1 middle. [0005] The currently marketed dosage forms of oseltamivir phosphate include granules, capsules, and dry suspensions. Granules or dry suspensions are suitable for preparation into liquid preparations before use, which is convenient for the elderly, children and people who a...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/215A61K47/26A61P31/16
CPCA61K31/215A61K9/0095A61K9/10A61K9/1623
Inventor 陆平林美王小芹黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD
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