Use of indinavir sulfate and chloroquine in preparing compound antimalarial medicament

Abstract

The invention relates to an application of Indinavir used as chloroquine resistant reversal agent or chloroquine synergist in the preparation of a medicinal composite for curing malaria. The different concentration ratios between the Indinavir and the chloroquine in the cellular level detection ranges from 1:100 to 100:1, have synergistic effect to a sensitive strain 3D7, and a chloroquine drug-resistant strain Dd2, and show stronger synergistic effect to the chloroquine drug-resistant strain. In the model of Plasmodium chabaudi infection of a mouse, the standard 4-day suppressive test is adopted, with the discovery that the chloroquine antimalarial activity synergy of the Indinavir exhibits more obviously on the chloroquine drug-resistant strain. After the treatment, the composite medicine containing 100mg / kg of chloroquine and 1.8mg / kg of Indinavir can completely clear the chloroquine resistant strains of the Plasmodium chabaudi of the mouse, and the negative conversion rate of the plasmodium is 100 percent. The total dosage of the composite medicine applied to prevent and cure human malaria is as follows: 12mg / kg to 100mg / kg of the chloroquine and 60mg / kg to 500mg / kg of the Indinavir. The invention develops a new composite antimalarial and provides a foundation for the reapplication of the economical and practical chloroquine in the malaria treatment.

Description

[technical field] [0001] The invention relates to the preparation and application of a novel compound antimalarial medicine. Specifically, the present invention relates to the application of the combined compound of Indinavir (Indinavir) and chloroquine in the preparation of a pharmaceutical composition for treating malaria. [Background technique] [0002] Malaria is widely distributed in the world. It is the most serious insect-borne infectious disease that harms human beings and one of the three major infectious diseases in the world. At present, there are still about 2.4 billion people living in malaria-endemic areas in the world, and 300-500 million people get sick every year, of which 1.5-2.7 million people die; about 1 million deaths of children under the age of 5 are caused by malaria and other accompanying diseases. The incidence of malaria in tropical African countries exceeds 90% of the total number of malaria in the world. [0003] Chloroquine was once the most ...

AI Technical Summary

Problems solved by technology

In 2004 and 2005, some scholars found that some protease inhibitors could inhibit the growth of Plasmodium in the Plasmodium cultured in vitro, and carried out drug experiments of Saquinavir, Ritonavir and lopinavir in the mouse malaria model, but the results were not satisfactory

The World Health Organization (WHO) recommends that the total oral dose of chloroquine in the treatment of chloroquine-sensitive falciparum malaria is 25 mg / kg, but this dose can only slightly improve clinical symptoms and reduce peripheral blood asexual parasites in patients with chloroquine-resistant falciparum malaria Infection rate, but can not achieve curative effect

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