A method for improving the bioavailability of artemisinin drugs

A technology for artemisinin and drugs, which is applied in the field of improving the bioavailability of artemisinin drugs, and can solve problems such as low bioavailability, affecting drug efficacy, and unstable chemical properties

Inactive Publication Date: 2019-04-05
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2003, the traditional antimalarial drugs purchased by the WHO for US$ 41.4 million did not play their due role, while the new drug containing artemisinin purchased for another US$ 18.3 million had very good curative effect. Drug research turns to artemisinin derived from traditional Chinese medicine
[0006] Artemisinin and its analogues have always had their own defects, namely: generally low bioavailability, irregular absorption, and the existence of dioxygen bonds in the structure, resulting in unstable chemical properties and drug resistance, which have affected its The effect of medicine

Method used

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  • A method for improving the bioavailability of artemisinin drugs
  • A method for improving the bioavailability of artemisinin drugs
  • A method for improving the bioavailability of artemisinin drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Preparation of DHA bulk drug (dihydroartemisinin bulk drug) powder processed by SCF:

[0090] Supercritical fluid equipment of Tianjin Crystec Pharmaceutical Technology Co., Ltd. (composition: 200mL particle forming container, 50g / min-capacity CO 2 Pump). 2% DHA-ethanol solution (w / v), with CO 2 Pump into appropriate nozzles (coaxial nozzles), maintain a pressure of 85 bar (back pressure regulator control) and an operating temperature of 40°C, and finally collect the final powder in the forming chamber.

[0091] Characterization of SCF-treated DHA API powders:

[0092] (1) Powder X-ray Diffraction (PXRD) characterization: Simultaneously compare and investigate the DHA bulk drug, experimental instrument parameters: 40kV, 40mA; scanning speed 4θ / min. see results figure 1 . Both the DHA raw drug and the DHA raw drug treated with SCF have strong similar diffraction peaks at the same position, but the peak number and peak intensity are changed, and the crystallinity is ...

Embodiment 2

[0095] The preparation of the DHA+malic acid powder that SCF handles: the supercritical fluid equipment (composition: 200mL granule forming container, the CO of 50g / min-capacity 2 Pump). 12% (w / v) DHA and 8% (w / v) malic acid in dichloromethane-tetrahydrofuran (volume ratio 3:1) solution, with CO 2 Pump into appropriate nozzles, maintain a pressure of 85 bar and an operating temperature of 40°C, and finally collect the final powder in the forming chamber.

[0096] (1) Powder X-ray Diffraction (PXRD) characterization: Experimental instrument parameters: 40kV, 40mA; scanning speed 4θ / min. see results figure 1 , compared with the DHA bulk drug, there are stronger similar diffraction peaks at the same position, but the number of peaks and the intensity of the peaks change to some extent, and the crystallinity is stronger.

[0097] (2) Scanning electron microscope (SEM) characterization: see the results Figure 4 , all form good needle crystals, the average length of the "needle...

Embodiment 3

[0113] The preparation of the DHA+gentisic acid co-crystallization powder that SCF handles: the supercritical fluid equipment (composition: 200mL granule forming container, the CO of 50g / min-capacity 2 Pump). 5% DHA + 2% gentisic acid in dichloromethane, with CO 2 Pump into appropriate nozzles, maintain a pressure of 85 bar and an operating temperature of 36°C, and finally collect the final powder in the forming chamber. Scanning electron microscope (SEM) characterization results are shown in Figure 6 . The average crystal length is 71 μm, and the geometric equivalent diameter (particle size) is 10 μm.

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Abstract

The invention provides a method for improving bioavailability of artemisinin-based drugs and particularly provides a method for preparing artemisinin-based drug powder.The method for preparing the artemisinin-based drug powder includes the steps of dissolving artemisinin-based drug raw materials and optional second substances into organic solvents to form a first mixture; mixing the first mixture with supercritical fluids to form a second mixture, and enabling artemisinin-based drugs to separate out of the mixture so as to obtain the artemisinin-based drug powder.Compared with artemisinin-based drug powder prepared by a common method, the artemisinin-based drug powder prepared by the method is capable of improving stability and bioavailability of the artemisinin-based drugs.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, in particular, the invention relates to a method for improving the bioavailability of artemisinin drugs. Background technique [0002] In recent years, the spread of malaria has been on the rise again around the world. At present, the antimalarial drugs mainly used for prevention include pyrimethamine and proguanil; the antimalarial drugs mainly used for symptom control include chloroquine, quinine, piperaquine, hydroxypiperaquine, pyridine, pyronaridine, etc. Malaria is mainly distributed in a wide area between 60° north latitude and 40° south latitude, and is prevalent in 107 countries or regions in Asia, Africa, and Latin America. 40% of the world's population lives in malaria-endemic areas, about 2.1 billion Man is threatened by malaria. In 1998, WHO implemented the "Roll Back Malaria" plan, which planned to reduce the number of deaths from malaria by half within 12 years. But after a few...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/20A61K31/366A61K31/357A61P33/06A61P35/00A61P33/12A61P37/00A61P9/06A61P31/00
CPCY02A50/30Y02P20/54
Inventor 张继稳李海燕L·S·戴恩特尔D·M·莱杰顾景凯杨艳
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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