COMPARISON OF SOLID DISPERSION AND BALL MILLING TO IMPROVE EZETIMIBE DISSOLUTION
Ezetimibe belongs to the Biopharmaceutical Classification System (BCS) Class II which has high permeability, but low solubility. Ezetimibe is also very hydrophobic, causing many problems during formulation that leads to its poor dissolution profile. This research aims to improve the dissolutio...
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| Format: | Theses |
| Language: | Indonesia |
| Online Access: | https://digilib.itb.ac.id/gdl/view/76583 |
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| Institution: | Institut Teknologi Bandung |
| Language: | Indonesia |
| Summary: | Ezetimibe belongs to the Biopharmaceutical Classification System (BCS) Class II
which has high permeability, but low solubility. Ezetimibe is also very hydrophobic,
causing many problems during formulation that leads to its poor dissolution profile.
This research aims to improve the dissolution profile of ezetimibe using two
different methods that are solid dispersion formation and particle size reduction by
ball milling. The results of the subsequent treatment were compared with the
reference drug (Ezetrol®). Solid dispersion improved the dissolution rate of
ezetimibe but did not meet the similarity requirement with reference drug, indicated
by the value of the similarity factor (f2)?50. A similar dissolution profile was
achieved by ball-milling of ezetimibe with poloxamer 188 and crosspovidone. This
result can be seen from the percentage of drug that dissolved in 15 minutes for the
comparator product and the sample product was more than 85%. PXRD, DSC, and
SEM show that ball milling increased the dissolution due to surface activation. This
research shows that ball milling method can improve dissolution better than the
solid dispersion.
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