Crystal morphology engineering of pharmaceutical solids: tabletting performance enhancement

Sabiruddin Mirza, Inna Miroshnyk, Jyrki Heinämäki, Osmo Antikainen, Jukka Rantanen, Pia Vuorela, Heikki Vuorela, Jouko Yliruusi

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    Crystal morphology engineering of a macrolide antibiotic, erythromycin A dihydrate, was investigated as a tool for tailoring tabletting performance of pharmaceutical solids. Crystal habit modification was induced by using a common pharmaceutical excipient, hydroxypropyl cellulose, as an additive during crystallization from solution. Observed morphology of the crystals was compared with the predicted Bravais-Friedel-Donnay-Harker morphology. An analysis of the molecular arrangements along the three dominant crystal faces [(002), (011), and (101)] was carried out using molecular simulation and thus the nature of the host-additive interactions was deduced. The crystals with modified habit showed improved compaction properties as compared with those of unmodified crystals. Overall, the results of this study proved that crystal morphology engineering is a valuable tool for enhancing tabletting properties of active pharmaceutical ingredients and thus of utmost practical value.
    Original languageEnglish
    JournalAAPS PharmSciTech
    Issue number1
    Pages (from-to)113-119
    Number of pages7
    Publication statusPublished - 2009
    MoE publication typeA1 Journal article-refereed

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