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Graduate seminar 1/2013

November 15, 2013

Title The application of polymer in stabilization of drug solubility in solid

dispersions

Speaker Miss Woralak Leelasornchai

Master of Sciences in Pharmaceutical chemistry and natural products /2ndyear

Advisor Asst. Prof. Dr. Soravoot Rujivipat

Co-advisor Asst. Prof. Dr. Waree Tiyaboonchai

Asst. Prof. Dr. A-nan Ounarun

Dr. Nutsawadee Apichartwattana

ABSTRACT

Low aqueous solubility is a common characteristic in todaysbiopharmaceuticswhichis a critical determinant of oral bioavailability [1]. There are many techniques which are used

to enhance the aqueous solubility like physical, chemical and others techniques. Solid

dispersion technology has been used for improving the dissolution rate and bioavailability of

poorly water soluble drugs [24]. Solid dispersions are typically prepared by incorporation of

the poorly soluble drug into a water-soluble carrier via melt-extrusion or coprecipitation

technique [5, 6], resulting in Such processes result in amorphous drug dispersions [7].

Although the amorphous drug dissolves faster compared to its crystalline alternatives, it is not

physically stable and may undergo unpredictable crystallization during the shelf-life [810].

The stabilization of amorphous drug solubility by the incorporation of polymer as

inhibitory effect has been introduced. The roles of polymer in stabilization mechanism could

be: to increasing glass transition temperature of miscible mixture (anti-platicization by the

polymer); specific drug-polymer interaction (e.g., hydrogen bonding, ion-dipole) [1113] and

an increase in the activation energy for nucleation or alteration of chemical potential of a

drug [14-15]. These results in a decrease in local molecular mobility at regular storage

temperatures, then the recrystallization would be decreased.

Keywords;solid dispersion, stabilization mechanism, anti-plasticization, drug-polymer

interaction, recrystallization

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Graduate seminar 1/2013

November 15, 2013

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