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Updated: Jun 21, 2026

Heterogeneous Removal of Water-Soluble Ruthenium Olefin Metathesis Catalyst from Aqueous Media Via Host-Guest Interaction

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Published on: August 23, 2018

Artemether/hydroxypropyl-beta-cyclodextrin host-guest system: characterization, phase-solubility and inclusion mode.

Bo Yang¹, Jun Lin, Yong Chen

¹School of Chemistry, Key Laboratory of Medicinal Chemistry for Natural Resource (Ministry of Education), Yunnan University, Kunming 650091, PR China.

Bioorganic & Medicinal Chemistry

|August 12, 2009

Summary

This study details an artemether (ATM) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) inclusion complex, enhancing ATM

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Published on: August 28, 2015

Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems
Medicinal Chemistry

Background:

Artemether (ATM) is a crucial antimalarial drug.
Improving ATM's water solubility and bioavailability is essential for effective malaria treatment.
Cyclodextrins are widely used to enhance drug properties.

Purpose of the Study:

To prepare and characterize an inclusion complex of artemether (ATM) with hydroxypropyl-beta-cyclodextrin (HPbetaCD).
To investigate the inclusion mechanism and assess the impact on ATM's physicochemical and pharmacokinetic properties.

Main Methods:

Phase-solubility studies were conducted to determine drug-excipient interactions.
(1)H NMR, 2D NMR (ROESY) spectroscopy were used to elucidate the inclusion complex structure.
Powder X-ray diffraction and thermal analysis confirmed complex formation.
Bioavailability was assessed in vivo.

Main Results:

The ATM-HPbetaCD complex demonstrated increased water solubility.
Phase-solubility diagram indicated an apparent binding constant of 220 M(-1).
NMR studies revealed a specific orientation of ATM within the HPbetaCD cavity.
Powder X-ray diffraction and thermal analysis confirmed the formation of a stable inclusion complex.
The complex resulted in a 1.81-fold enhancement in apparent bioavailability compared to free ATM.

Conclusions:

Hydroxypropyl-beta-cyclodextrin effectively forms an inclusion complex with artemether.
The complexation significantly enhances artemether's water solubility and bioavailability.
This formulation strategy holds promise for improving antimalarial drug efficacy.