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Anti-malarial medicinal composition and preparation method and application thereof

A composition and anti-malarial technology, which is applied in the direction of drug combination, anti-infective drugs, and pharmaceutical formulations, can solve the problems of insufficient stability of compound solid preparations, low absorption rate of active components, and potential safety hazards, so as to facilitate absorption , release behavior is good, and the effect of ensuring safety

Active Publication Date: 2011-12-21
恩威医药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the extremely poor water solubility of artemether and lumefantrine, the absorption rate of the effective components of the compound product is low, making the drug effect of the compound solid preparation not stable enough, and its use is limited
Not only that, but in the production process of the compound solid preparation, it was also found that during the mixing process of lumefantrine and artemether, an explosion may occur, causing certain safety hazards in the production process

Method used

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  • Anti-malarial medicinal composition and preparation method and application thereof
  • Anti-malarial medicinal composition and preparation method and application thereof
  • Anti-malarial medicinal composition and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0045] The preparation of embodiment 1 pharmaceutical composition of the present invention

[0046] Take the raw and auxiliary materials according to the weight ratio stated in Table 1:

[0047] Table 1

[0048]

[0049] The raw and auxiliary materials used in the present invention can all be obtained by purchasing commercially available products, wherein, the purity of artemether and bemefluorenol is determined to be 98-102%.

[0050] Steps:

[0051] 1. The preparation method of artemether layer granules: mix artemether, lactose, and 80% povidone K30, and dissolve the remaining 20% ​​povidone K30 with an appropriate amount of water to make an aqueous solution, which is used as a binder for granulation. Made into soft materials, made into granules by a swinging granulator, dried at 50-60°C, granulated with a 20-mesh sieve, and set aside;

[0052] 2. The production method of benzfluorenol layer granules: mix benzfluorenol and pregelatinized starch, add appropriate amount ...

Embodiment 2

[0055] Embodiment 2 The screening of pharmaceutical composition prescription of the present invention

[0056] Because artemether and lumefantrine may explode during the mixing process, the present invention prepares the compound of artemether and lumefantrine into a double-layer tablet to avoid the mixing of the two, thereby avoiding the occurrence of accidents. Because artemether and lumefantrine have low solubility in water, it is very necessary to have a high requirement for dissolution rate when they are prepared into tablets. In this screening experiment, the type and dosage of the excipients of the pharmaceutical composition of the present invention were screened mainly by taking the disintegration time limit and dissolution rate of the tablet as indicators.

[0057] No. 1 preparation prescription: see embodiment 1.

[0058] Prescription of preparation No. 2:

[0059] Table 2

[0060]

[0061] Steps:

[0062]1. The production method of artemether layer granules: ...

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Abstract

The invention discloses an anti-malarial medicinal composition and a preparation method and application thereof. In the medicinal composition, artemether and lumefantrine are respectively pelletized and then are prepared into a double-layer sheet, so that the process of mixing the artemether and the lumefantrine is prevented, and the safety in the compound preparation process is ensured. In addition, the double-layer sheet can be quickly disintegrated by screening auxiliary materials in a specific preparation mode; and compared with the conventional compound tablet, the invention has the advantages that: the dissolution rate of the active ingredient of the medicinal composition is obviously improved, so that the medicinal composition has a better release behavior, contributes to the absorption of medicines better and has a better curative effect.

Description

technical field [0001] The invention relates to an anti-malarial pharmaceutical composition, a preparation method and application, and belongs to the field of medicines. Background technique [0002] Malaria is a parasitic disease transmitted by mosquitoes with high morbidity and mortality. Currently, artemisinin drugs are the most commonly used antimalarial drugs. Artemether, (3R, 5aS, 6R, 8aS, 9R, 10S, 12R, 12aR)-decahydro-10-methoxy-3,6,9-trimethyl-3,12-oxo bridge -12H-pyrano[4,3-j]-1,2-benzodisepin has a strong killing effect on Plasmodium schizonts, and is effective for multiple drug-resistant malaria and chloroquine-resistant falciparum malaria significantly. However, it has the disadvantages of short duration of action and high recurrence rate. And Lumefantrine, (9Z)-2,7-dichloro-9-[(4-chlorophenyl)methylene]-α-[(di-n-butylamino)methyl]-9H-fluorene -4-methanol kills malaria parasites cleanly and thoroughly, with high efficiency and low recurrence rate, but the ef...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/137A61K9/20A61P33/06
CPCY02A50/30
Inventor 薛刚薛飞代勇徐世军陈登志
Owner 恩威医药股份有限公司
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