Effects of Cellulose Polymers on the Hydrate Transformation of the Drug Theophylline

Advisor Information

Alan Gift

Location

Dr. C.C. and Mabel L. Criss Library

Presentation Type

Poster

Start Date

7-3-2014 1:00 PM

End Date

7-3-2014 4:00 PM

Abstract

During the drug manufacturing process, active pharmaceutical ingredients (APIs) can potentially transform from the anhydrate to the hydrate form. This transformation can change the effectiveness of the drug, thus it is important to control the anhydrate-to-hydrate transformation. This research is focused on the inhibiting effects of cellulose based polymers on the transformation of the API theophylline. In-line Raman spectroscopy was used to record the anhydrate-to-hydrate transformation of theophylline by collecting spectra of the solutions every 30 seconds. A calibration model was used to construct transformation profiles by quantifying the percent transformation for each of the collected Raman spectra. The results showed that all cellulose polymers inhibited the transformation, and methylcellulose exhibited the greatest inhibition. To better understand the mechanism of inhibition, solubility and intrinsic dissolution experiments were performed on theophylline in the presence of these polymers. The results showed that these polymers had little to no influence on solubility and dissolution. These results indicate the inhibitory effects of these polymers are reducing the crystal growth rate of theophylline hydrate.

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COinS
 
Mar 7th, 1:00 PM Mar 7th, 4:00 PM

Effects of Cellulose Polymers on the Hydrate Transformation of the Drug Theophylline

Dr. C.C. and Mabel L. Criss Library

During the drug manufacturing process, active pharmaceutical ingredients (APIs) can potentially transform from the anhydrate to the hydrate form. This transformation can change the effectiveness of the drug, thus it is important to control the anhydrate-to-hydrate transformation. This research is focused on the inhibiting effects of cellulose based polymers on the transformation of the API theophylline. In-line Raman spectroscopy was used to record the anhydrate-to-hydrate transformation of theophylline by collecting spectra of the solutions every 30 seconds. A calibration model was used to construct transformation profiles by quantifying the percent transformation for each of the collected Raman spectra. The results showed that all cellulose polymers inhibited the transformation, and methylcellulose exhibited the greatest inhibition. To better understand the mechanism of inhibition, solubility and intrinsic dissolution experiments were performed on theophylline in the presence of these polymers. The results showed that these polymers had little to no influence on solubility and dissolution. These results indicate the inhibitory effects of these polymers are reducing the crystal growth rate of theophylline hydrate.