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Orally administrable antimalarial combined preparation and preparation process thereof

A technology of drug administration and composition, applied in the field of antimalarial drug combination preparation and its preparation

Active Publication Date: 2010-12-15
SHIN POONG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the present inventors use pharmaceutically acceptable carriers, by mainly formulating with artemisinin or its derivatives (such as preparing them into microcapsules or eutectic mixtures, or coating them with coating agents, and then coating them Mixed with pyronaridine acid salt to prepare combination formulations) solves the problems of formulation stability, solubility and dissolution rate

Method used

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  • Orally administrable antimalarial combined preparation and preparation process thereof
  • Orally administrable antimalarial combined preparation and preparation process thereof
  • Orally administrable antimalarial combined preparation and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0020] Preparation Example 1: Preparation of Artesunate Microcapsules (1)

[0021] Ingredients Content

[0022] Artesunate 3g

[0023] Macrogol 10000 3g

[0024] Liquid paraffin 396g

[0025] Tween 80 4g

[0026] 3 g of artesunate and 3 g of polyethylene glycol were dissolved in 9 g of acetonitrile. This organic solution was dispersed in 396 g of liquid paraffin (containing 1% Tween 80) and stirred with a digital stirrer (IKA, EUROSTAR). After a suitable emulsion has thus been prepared, the solvent is evaporated until 40 to 60% of the acetonitrile has been completely removed therefrom. Therefore, the resulting suspension of microcapsules was centrifuged at 41 xg for 10 minutes. The supernatant was decanted, then the microcapsules were resuspended with 50 to 100 ml of wash water and filtered off slowly. During the filtration, the microcapsules were kept in suspension with slow stirring, and washing water was continuously added thereto to remove the acetonitrile held in t...

preparation Embodiment 2

[0027] Preparation Example 2: Preparation of Artesunate Microcapsules (2)

[0028] Ingredients Content

[0029] Artesunate 3g

[0030] Macrogol 10000 1.5g

[0031] Liquid paraffin 396g

[0032] Tween 80 4g

[0033] Using the above-mentioned ingredients, the microcapsule was prepared according to the same method as in Preparation Example 1.

preparation Embodiment 3

[0034]Preparation Example 3: Preparation of Artesunate Microcapsules (3)

[0035] Ingredients Content

[0036] Artesunate 3g

[0037] Macrogol 10000 6g

[0038] Liquid paraffin 396g

[0039] Tween 80 4g

[0040] Using the above-mentioned ingredients, the microcapsule was prepared according to the same method as in Preparation Example 1.

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Abstract

The present invention relates to an orally administrable antimalarial combined preparation containing artemisinine or its derivatives, and pyronaridine or its salts, as active ingredients, with pharmaceutically acceptable carriers, and to preparation process thereof.

Description

technical field [0001] The invention relates to an orally administrable antimalarial drug combination preparation and a preparation method thereof. The preparation contains artemisinin or its derivatives and pyronaridine or its salt as active ingredients and a pharmaceutically acceptable carrier. Background technique [0002] According to the report of the World Health Organization (WHO), there are about 3 to 5 million malaria patients in the world every year, and 90% of them are concentrated in Africa. Between 1.5 and 2.7 million people die from malaria every year, especially at least 1 million of them are African children under the age of 5. In particular, the sub-Saharan region showed the highest rates of infection, morbidity, and mortality. Today, malaria is made worse by resistance to antimalarial drugs, especially chloroquine and pyrimethamine / sulfadoxine, due to war, environmental damage, re-migration, climate change, etc. [0003] The treatment and prevention of ma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61P33/06
CPCA61K31/4375A61K31/357A61P33/06Y02A50/30A61K2300/00
Inventor 李星泰朴雨逸鲁政烈郑贤根李哲规全圣贤郑显圭
Owner SHIN POONG PHARMA CO LTD