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Title of Journal: Pharm Res

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Abbravation: Pharmaceutical Research

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Springer US

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DOI

10.1007/bf03162860

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1573-904X

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Effect of Polymer Additives on the Transformation

Authors: S Betigeri A Thakur R Shukla K Raghavan
Publish Date: 2007/10/12
Volume: 25, Issue: 5, Pages: 1043-1051
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Abstract

The conversion of anhydrate to dihydrate was monitored using differential scanning calorimetry powder Xray diffraction and polarized light microscopy Solubility and intrinsic dissolution studies were performed on anhydrate and dihydrate IR and NMR spectroscopy were used to probe the molecular interactions between BMS566394 and cellulose ether polymersThe anhydrate form of BMS566394 was readily transformed into the more stable dihydrate form in aqueous suspension The kinetic solubility and intrinsic dissolution rate of the anhydrate were ca fourfold that of the dihydrate Addition of cellulose ether polymers HPC HPMC MC inhibited anhydrate to dihydrate transformation in aqueous suspensions Hydrogen bonding interaction between the polar groups of the drug and polymers was inferred from infrared spectroscopy Solution NMR also indicated a hydrophobic interaction between the drug and polymer backboneThe authors wish to acknowledge MingHsing Huang and Scott Huffman for their help in IR studies Mingxin Qian for in vivo studies and Shelley Rabel for early characterization studies for the compound The single crystal analysis was conducted by Mary Malley

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