Amorphous solid systems of poorly water-soluble drugs
5
Issued Date
2018
Resource Type
Language
eng
Rights
Mahidol University
Rights Holder(s)
Faculty of Pharmacy Mahidol University
Graduate School of Pharmaceutical Sciences Chiba University
Graduate School of Pharmaceutical Sciences Chiba University
Suggested Citation
Satit Puttipipatkhachorn, Waree Limwikrant, Nattawut Charoenthai, Kasama Pongsamart (2018). Amorphous solid systems of poorly water-soluble drugs. Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/25186
Title
Amorphous solid systems of poorly water-soluble drugs
Other Contributor(s)
Abstract
Most of active pharmaceutical ingredients (API) are poorly water-soluble and shows limited
dissolution rate which consequently affects drug absorption rate and bioavailability. This
leads to a challenging in product development in pharmaceutical industry. Regarding solid
state properties, API can be classified as crystalline and amorphous solids. Most marketed
pharmaceutical products consist of crystalline API because of their greater chemical stability
as compared to amorphous API. Amorphous solids exhibits a higher dissolution rate which is
a desirable pharmaceutical property, however, it will be eventually revert to the most stable
crystalline solids because of the higher molecular mobility and thermodynamic activity which
can be accelerated by moisture and temperature. Amorphous solid systems with improved
dissolution and good stability are desirable for product development. In this study, spray
drying, a common manufacturing process, was used to prepare the amorphous systems for
poorly water-soluble drugs by two approaches; molecular inclusion complexation using β-
cyclodextrin (β-CD) Molecular inclusion complex between dihydroartemisinin (DHA) and
β-CD was formed at 1:2 molar ratio and its spray-dried powder showed an amorphous system
with dramatically enhanced dissolution rate. It was chemically and physically stable with
remained antimalarial activity at 30 °C after 3 months storage. In conclusion, the amorphous
systems for poorly water-soluble drugs with improved dissolution rate and good stability
were successfully obtained by spray drying process.
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Description
The 3rd Chiba University-Mahidol University Joint Symposium
on Pharmaceutical Sciences. Hosted by Faculty of Pharmacy, Mahidol University
Thursday August 2, 2018