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Oral preparation containing darunavir

A technology of oral preparations, ritonavir, applied in the field of oral preparations

Inactive Publication Date: 2014-12-24
VIWIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the prior art discloses that ritonavir can be used to improve the pharmacokinetics of darunavir and tipinavir respectively, there is no report on the simultaneous use of effective doses and related preparations of the three

Method used

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  • Oral preparation containing darunavir
  • Oral preparation containing darunavir
  • Oral preparation containing darunavir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A tablet containing darunavir, with a total weight of about 800mg, which contains 370mg of darunavir, 180mg of tipinavir, 120mg of ritonavir, 110mg of corn starch, 8mg of micronized silica gel, and 12mg of crospovidone .

[0036]

Embodiment 2

[0038] A tablet containing darunavir, the total weight is about 800mg, which contains darunavir 350mg, tipinavir 180mg, ritonavir 120mg, sucrose 125mg, magnesium stearate 10mg, crospovidone 15mg.

[0039]

Embodiment 3

[0041] A tablet containing darunavir, with a total weight of about 1000mg, which contains 400mg of darunavir, 200mg of tipinavir, 130mg of ritonavir, 140mg of corn starch, 15mg of micropowder silica gel, cross-linked carboxymethyl Sodium cellulose 15mg, dextrin 100mg.

[0042]

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PUM

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Abstract

The invention discloses oral preparation containing darunavir and particularly relates to oral preparation containing the darunavir, tipranavir and ritonavir. Besides, the oral preparation can select one of a binder, a lubricant and a dispersing agent or the mixture of the binder, the lubricant and the dispersing agent according to the type of the preparation. The oral preparation which is used for treating aids and is formed by combining different effective doses is prepared by adjusting the contents of the darunavir, the tipranavir and the ritonavir; in the preparation, the content of the darunavir is preferable 300-1,000mg, the content of the tipranavir is preferable 150-600mg, and the content of the ritonavir is preferable 100-400mg; in the preparation, the total weight of the darunavir, the tipranavir and the ritonavir is preferable 650-1,800mg; the proportion of the binder is preferable 5-15 percent of the total weight of a unit preparation, the proportion of the lubricant is preferable 0.5-1.5 percent of the total weight of the unit preparation, and the proportion of the dispersing agent is preferable 1.5-3.5 percent of the total weight of the unit preparation.

Description

technical field [0001] The invention relates to an oral preparation containing darunavir for treating HIV, in particular to an oral preparation containing darunavir, ritonavir and tipinavir. Background technique [0002] Darunavir (English: Darunavir) has the structural formula shown in Formula I below. Darunavir is a protease inhibitor used to treat HIV infection in adults. Its side effects are small, but its bioavailability is low when used alone, and the effect of combined drugs is better. [0003] [0004] Tipanavir (English: Tipranavir) is a non-peptide protease inhibitor used to treat HIV infection. It works by inhibiting protease (an enzyme necessary for HIV replication) and can be used to inhibit the inhibition of other proteases. Replication of drug-resistant HIV viruses. Tipinavir was approved by the FDA in 2005 and approved for use in children in 2008. Its structural formula is shown in formula II. [0005] [0006] Ritonavir (English: Ritonavir) is a pe...

Claims

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Application Information

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IPC IPC(8): A61K31/635A61K9/20A61K9/48A61K9/14A61P31/18A61K31/44A61K31/427
Inventor 邢艳平魏彦君葛静茹
Owner VIWIT PHARMA
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