Dissolution, Bioavailability and Tissue Distribution of Artemisinin Microspheres Loaded With Porous Starch

doi:10.7525/j.issn.1673-5102.2019.04.015

Abstract

Abstract: To investigate the dissolution effect of artemisinin microspheres(ART-PS) loaded with porous starch in vitro compared with artemisinin, bioavailability and tissue distribution in rats, in the in vitro dissolution experiment, the dissolution effect of artemisinin was compared with that of artemisinin in water, artificial gastric juice and artificial intestinal fluid. In the in vivo bioavailability experiment, 18 rats were given artemisinin raw drug and porous starch loaded artemisinin microspheres respectively, and the blood drug concentrations at different time points were detected to investigate the differences in drug absorption and metabolism in rats. In the tissue distribution, the drug contents in heart, liver, spleen, lung, kidney and brain of 98 rats were detected at different points in time by gavage of porous starch loaded artemisinin microspheres and artemisinin active drugs. The dissolution rates of artemisinin microspheres loaded with porous starch in vitro were 4.04, 3.59 and 3.82 times higher than those of artemisinin in water, artificial gastric juice and artificial intestinal fluid, respectively. The blood content of artemisinin microspheres loaded with porous starch in rats was significantly higher than that of artemisinin, and the bioavailability was 2.90 times higher than that of artemisinin. In the results of tissue distribution, artemisinin microspheres loaded with porous starch and artemisinin active drugs were mainly distributed in the heart and liver, and the corresponding content of artemisinin active starch active microspheres in different tissues at different times was higher than that of active drugs. Compared with artemisinin, artemisinin microspheres loaded with porous starch have better dissolution effect in vitro and better absorption and release effect in vivo. The drug content in various tissues and organs is significantly higher than that of the original drug, providing an important theoretical basis for solving the limitation of artemisinin in practical application due to its insoluble in water.

Key words: artemisinin, dissolution, bioavailability

CLC Number:

Q949.95

ZHAO Xue, YANG Feng-Jian, GE Yun-Long, WANG Ling-Ling, LI Wen-Gang, DENG Yi-Ping, ZHAO Xiu-Hua. Dissolution, Bioavailability and Tissue Distribution of Artemisinin Microspheres Loaded With Porous Starch[J]. Bulletin of Botanical Research, 2019, 39(4): 604-612.

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