Pharmaceutical composition for oral administration in powder formulation containing antiviral agent

A composition and drug technology, applied in the field of orally administered pharmaceutical compositions, can solve the problems of large volume, difficult storage and transportation, etc., and achieve the effects of reducing costs, preventing moisture changes, and improving medication compliance

Inactive Publication Date: 2022-01-18
DAE HWA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, pharmaceutical compositions in the form of syrups contain solvents (e.g., purified water), and thus are larger in volume than solid preparations, resulting in problems of difficulty in storage and transportation

Method used

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  • Pharmaceutical composition for oral administration in powder formulation containing antiviral agent
  • Pharmaceutical composition for oral administration in powder formulation containing antiviral agent
  • Pharmaceutical composition for oral administration in powder formulation containing antiviral agent

Examples

Experimental program
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Effect test

preparation example Construction

[0028] The present invention provides a pharmaceutical composition for oral administration in the form of a powder preparation, which is obtained by a preparation method comprising the following steps: (a) preparing zanamivir, triglyceride, an emulsion of acylglycerol, nonionic surfactant, sugar and water; and (b) subjecting the emulsion obtained in step (a) to freeze drying.

[0029] In the pharmaceutical composition of the present invention, zanamivir used as an active ingredient may be used in a therapeutically effective amount. For example, the pharmaceutical composition for oral administration in the powder form of the present invention may contain zanamivir in the range of 0.1-5 mg, preferably in the range of 1-5 mg, more preferably in the range of about 1 mg. amount of zanamivir, but is not limited to it.

[0030]In the pharmaceutical composition of the present invention, step (a) is a step of forming an emulsion, which can be achieved by including zana in the composit...

Embodiment 1

[0040] The preparation of embodiment 1. syrup

[0041] According to the ingredients and contents in Table 1 below, a syrup containing zanamivir was prepared. Sucrose was dissolved in purified water, then zanamivir was added, and stirred at 1000 rpm at 25° C. for 2 hours to dissolve until transparent. Add Captex in sequence TM 8000 (Abitec), Peceol TM (Jaffa Lion), Twain TM 80 (NOF), and stirred at 1000rpm to prepare a syrup.

[0042] [Table 1]

[0043]

[0044] The properties of the obtained syrup are as figure 1 shown. Such as figure 1 As shown in , the obtained syrup exhibited clear and transparent properties.

Embodiment 2

[0045] Example 2. Preparation of a pharmaceutical composition for oral administration in the form of a powder formulation

[0046] Mix the syrup obtained in Example 1 with purified water at a weight ratio of 1:3 to form an emulsion, then use liquid nitrogen to quickly freeze, and then freeze-dry at a temperature below -114°C and a pressure below 10 mTorr For about 5 hours, 7.871 g of the pharmaceutical composition in the form of a powder formulation was thus prepared.

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Abstract

The present invention provides a pharmaceutical composition for oral administration in a powder formulation, obtained by a preparation method comprising the steps of: (a) preparing an emulsion containing zanamivir as an active ingredient, triglycerides, acylglycerol, a non-ionic surfactant, sugars, and water. According to the present invention, the pharmaceutical composition can significantly increase the absorption level of zanamivir in the body, is a powder formulation, and is therefore easy to store and distribute, and can eliminate the use of functional packaging materials used to prevent changes in moisture.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for oral administration in the form of a powder formulation comprising an antiviral agent. In more detail, the present invention relates to a pharmaceutical composition for oral administration in the form of a powder formulation, which is prepared by adding zanamivir, triglycerides, acylglycerol, nonionic surface An emulsion of active agent, sugar and water is obtained by lyophilization. Background technique [0002] The chemical name of zanamivir is 5-(acetylamino)-4-{[amino(imino)methyl]amino}-2,6-anhydro-3,4,5-trideoxy-D -Glyceryl-D-galactose-2-enolic acid (5-(acetylamino)-4-{[amino(imino)methyl]amino}-2,6-anhydro-3,4,5-trideox y-D -glycero-D-galacto-non-2-enonic acid), and has the structure of the following chemical formula 1. [0003] <chemical formula 1> [0004] [0005] Zanamivir exhibits activity by binding to a conserved region of influenza virus neuraminidase, which p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/351A61K47/14A61K47/10A61K47/26A61P31/12
CPCA61K9/19A61K9/0053A61K31/351A61K47/14A61K47/10A61K47/26A61P31/12A61K9/0095A61K31/7012A61K9/107
Inventor 张准熙李仁铉孙旼希朴惠珍
Owner DAE HWA PHARMA
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