Method for improving bioavailability of artemisinin-based drugs

An artemisinin and drug technology, applied in the field of improving the bioavailability of artemisinin drugs, can solve the problems of low bioavailability, unstable chemical properties, affecting drug efficacy and the like

Inactive Publication Date: 2016-07-13
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +2
View PDF0 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2003, the traditional antimalarial drugs purchased by the WHO at a cost of US$41.4 million did not play their due role, while the new drug containing artemisinin purchased at an additional US$18.3 million had a very good curative effect. Drug research turns to artemisinin derived from tradit

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for improving bioavailability of artemisinin-based drugs
  • Method for improving bioavailability of artemisinin-based drugs
  • Method for improving bioavailability of artemisinin-based 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 DHA API, experimental instrument parameters: 40kV, 40mA; scanning speed 4θ / min. see results figure 1 . Both DHA API and SCF-treated DHA API have strong similar diffraction peaks at the same position, but the number of peaks and peak intensity have changed, and the crystallinity is strong.

[0093] (2) Scanni...

Embodiment 2

[0095] Preparation of DHA+malic acid powder treated by SCF: supercritical fluid equipment (composition: 200mL particle forming container, 50g / min-capacity CO 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 raw material drug, there are stronger similar diffraction peaks at the same position, but the peak number and peak intensity are changed, 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" crystal form is 82 μm, and the geome...

Embodiment 3

[0113] Preparation of DHA+gentisic acid co-crystallized powder processed by SCF: supercritical fluid equipment (composition: 200mL particle forming container, 50g / min-capacity CO 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Lengthaaaaaaaaaa
Lengthaaaaaaaaaa
Lengthaaaaaaaaaa
Login to view more

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, and 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, antimalarial drugs mainly used for prevention include pyrimethamine and proguanil; 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 halve the number of malaria deaths within 12 years. But after a few years, the number...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07D493/20A61K31/366A61K31/357A61P33/06A61P35/00A61P33/12A61P37/00A61P9/06A61P31/00
CPCY02P20/54Y02A50/30
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap