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Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof

A technology for piperaquine phosphate tablets and dihydroartemisinin, applied in the field of medicine, can solve problems such as slow dissolution rate and achieve the effects of rapid dissolution, simple process and improved production efficiency

Active Publication Date: 2013-08-28
贝克诺顿(浙江)制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the deficiencies of the prior art, the inventor has done a lot of creative work to solve the problem of slow dissolution rate in the prior art

Method used

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  • Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof
  • Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof
  • Dihydroartemisinin piperaquine phosphate tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Preparation of Dihydroartemisinin Piperaquine Phosphate Tablets

[0026]

[0027] Preparation Process:

[0028] (1) Dissolve dihydroartemisinin and hydroxypropyl methylcellulose E5 in chloroform;

[0029] (2) Pass the piperaquine phosphate raw material through a 100-mesh sieve, disperse it in the above solution, and pulverize it through a colloid mill to obtain a suspension, the suspension D90=18.4 microns;

[0030] (3) Pass lactose and sodium carboxymethyl starch through a 100-mesh sieve, mix well, and set aside;

[0031] (4) Granulate the suspension in step (2) on the mixed excipients in step (3), dry at 40°C, granulate with a 16-mesh sieve, then add magnesium stearate, mix evenly and press into tablets.

Embodiment 2

[0032] Example 2 Preparation of Dihydroartemisinin Piperaquine Phosphate Tablets

[0033]

[0034] Preparation Process:

[0035] (1) Dissolve dihydroartemisinin and hydroxypropyl methylcellulose E5 in chloroform;

[0036] (2) Pass the piperaquine phosphate raw material through a 100-mesh sieve, disperse it in the above solution, and pulverize it through a colloid mill to obtain a suspension, the suspension D90=12.3 microns;

[0037] (3) Pass sucrose, lactose, sodium carboxymethyl starch and crospovidone through a 100-mesh sieve, mix well, and set aside;

[0038] (4) Granulate the suspension in step (2) on the mixed excipients in step (3), dry at 40°C, granulate with a 16-mesh sieve, then add magnesium stearate and micronized silica gel, mix evenly and press into tablets.

Embodiment 3

[0039] Example 3 Preparation of Dihydroartemisinin Piperaquine Phosphate Tablets

[0040]

[0041]

[0042] Preparation Process:

[0043] (1) Dissolve dihydroartemisinin and hydroxypropyl methylcellulose E5 in chloroform;

[0044] (2) Pass the piperaquine phosphate raw material through a 100-mesh sieve, disperse it in the above solution, and pulverize it through a colloid mill to obtain a suspension, the suspension D90=7.5 microns;

[0045] (3) Pass lactose and crospovidone through a 100-mesh sieve, mix well, and set aside;

[0046] (4) Granulate the suspension in step (2) on the mixed excipients in step (3), dry at 40°C, granulate with a 16-mesh sieve, then add magnesium stearate, mix evenly and press into tablets.

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Abstract

The invention discloses dihydroartemisinin piperaquine phosphate tablets and a preparation method thereof. The tablets are prepared from dihydroartemisinin, piperaquine phosphate, hydroxypropyl methyl cellulose E5, hydrophilic accessory and lubricating agent, wherein the weight ratio of the dihydroartemisinin to the hydroxypropyl methyl cellulose E5 is 1:(1-5). Solid dispersion of the dihydroartemisinin and pulverized piperaquine phosphate can be obtained by adopting one-step operation, so that the production efficiency is improved; and the tablets are dissolved quickly.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a dihydroartemisinin piperaquine phosphate tablet and a preparation method thereof. Background technique [0002] Dihydroartemisinin is the second-generation antimalarial drug of the artemisinin class and is the drug of choice for the treatment of malaria, especially multidrug-resistant falciparum malaria. WHO recommends the combination of artemisinin and other drugs to treat malaria, referred to as ACT therapy, as the first-line antimalarial drug. Dihydroartemisinin-piperaquine tablet is an excellent drug for treating various malaria, especially multidrug-resistant falciparum malaria. It is a compound preparation composed of dihydroartemisinin and piperaquine phosphate. In vitro pharmacodynamic studies have shown that the combination of dihydroartemisinin and piperaquine phosphate has a significant synergistic effect, which can delay the development of drug resista...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/20A61P33/06A61K31/357
CPCY02A50/30
Inventor 不公告发明人
Owner 贝克诺顿(浙江)制药有限公司
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