Method for preparing anti-malarial medicament with reversal of medicament resistance and multi-target effect

A drug resistance reversal and multi-target technology, which is applied to non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations, etc., to prolong half-life, improve drug bioavailability, good biodegradability and The effect of biocompatibility

Inactive Publication Date: 2010-01-27
黄云清
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, artemisinin monotherapy has already made malaria parasites resistant to drugs. WHO decided to limit the production and sales of artemisinin monotherapy, and began to advocate compound antimalarial drugs in 2001.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] A method for preparing an antimalarial drug with drug resistance reversal and multi-target effects, comprising the following steps:

[0032] Preparation of materials: preparation of carrier materials, framework materials, drugs and solvents, wherein the carrier materials are nano-magnetic biomaterials, that is, Fe with particle diameters between 2 and 20nm 3 o 4 Powder, the skeleton material is β-cyclodextrin, the solvent is water with a pH value of 6-7 and 50-95% ethanol, and the medicine is Chinese medicine extract and chemical medicine, wherein the Chinese medicine extract is composed of the following medicines in weight proportions : 10 parts of artemisinin, 10 parts of Anemarrhena, 10 parts of paeonol, 10 parts of buffalo horn, 10 parts of turtle shell, and the chemical medicine has the following drug composition of weight ratio: 40 parts of amodiaquine, 20 parts of chloroquine, primary ammonia 1 part of quinine;

[0033] Preparation of water-soluble traditional ...

Embodiment 2

[0038] A method for preparing an antimalarial drug with drug resistance reversal and multi-target effects, comprising the following steps:

[0039] Preparation of materials: preparation of carrier materials, framework materials, drugs and solvents, wherein the carrier materials are nano-magnetic biomaterials, that is, Fe with particle diameters between 2 and 20nm 3 o 4 Powder, the skeleton material is β-cyclodextrin, the solvent is water and ethanol, and the medicine is Chinese medicine extract and chemical medicine, wherein the Chinese medicine extract is composed of the following medicines in weight proportions: 30 parts of artemisinin, 30 parts of Anemarrhena, 30 parts of paeonol, 30 parts of buffalo horn, 30 parts of turtle shell, the chemical medicine has the following drug composition of weight ratio: 80 parts of amodiaquine, 40 parts of chloroquine, 20 parts of primaquine;

[0040] Preparation of water-soluble traditional Chinese medicine inclusion microspheres: add β-...

Embodiment 3

[0045] A method for preparing an antimalarial drug with drug resistance reversal and multi-target effects, comprising the following steps:

[0046] Preparation of materials: preparation of carrier materials, framework materials, drugs and solvents, wherein the carrier materials are nano-magnetic biomaterials, that is, Fe with particle diameters between 2 and 20nm 3 o 4 powder, the skeleton material is β-cyclodextrin, the solvent is water and ethanol, and the medicine is Chinese medicine extract and chemical medicine, wherein the Chinese medicine extract is composed of the following medicines by weight: 20 parts of artemisinin, 20 parts of Anemarrhena, 20 parts of paeonol, 20 parts of buffalo horn, 20 parts of turtle shell, the chemical drug has the following drug composition in weight proportion: 60 parts of amodiaquine, 30 parts of chloroquine, 10 parts of primaquine;

[0047] Preparation of water-soluble traditional Chinese medicine inclusion microspheres: add β-cyclodextri...

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Abstract

The invention discloses a method for preparing an anti-malarial medicament with reversal of medicament resistance and multi-target effect, which comprises the process flow of performing stock preparation, preparing water-soluble Chinese medicament inclusion microspheres, preparing alcohol-soluble Chinese medicament inclusion microspheres, and preparing water-soluble chemical medicament inclusion microspheres. The method takes beta-cyclodextrin as a framework material, and includes a nano-magnetic biomaterial (carrier material) and a pharmaceutical composition; and the medicament-loaded nano-magnetic microspheres can be quickly combined with target cells, penetrate target cell membranes to enter the cells, realize the transmembrane transport of medicament molecules, inhibit the gene expression and amplification of the target cells to ensure that the target cells degenerate, necrotize or apoptosize, and achieve the effect of the reversal of medicament resistance at the same time. An anti-malarial oral preparation interferes the processes of DNA replication and RNA transcription of schizonts of plasmodiums, kills schizonts of erythrocytic phases of the plasmodiums, and effectively kills exoerythrocyte stages of the plasmodiums and gametophytes of the plasmodiums at the same time; and at the same time, the anti-malarial oral preparation achieves the aims of preventing disease causes, and controlling the prevalence and propagation of malaria.

Description

technical field [0001] The present invention relates to a novel anti-malarial drug and its preparation method, in particular to an anti-malarial oral agent prepared by the new drug-loaded nano-magnetic microsphere technology of β-cyclodextrin inclusion nano-magnetic biological material and drug; In the process of schizont DNA replication and RNA transcription, multi-target attacks are carried out on the erythrocytic stage, extraerythrocytic stage and gametocytes of various malaria parasites, and drug resistance reversal is achieved. Background technique [0002] Malaria is an infectious disease transmitted by mosquitoes. The malaria parasites of mosquitoes can be divided into: Plasmodium vivax, Plasmodium falciparum, Plasmodium malariae and Plasmodium ovale. When the human body is onset, there are clinical symptoms such as regular chills, fever, and sweating, and signs such as splenomegaly. Plasmodium falciparum can cause cerebral malaria, which can lead to serious diseases...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/8964A61K47/48A61K47/02A61K9/16A61K9/48A61K9/28A61P33/06A61K35/32A61K35/56A61K31/55A61K31/47
CPCY02A50/30
Inventor 黄云清
Owner 黄云清
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