Manipulation of the Anhydrate to Hydrate Transformation of Theophylline Using Polymeric Excipients in Aqueous Slurries

Advisor Information

Alan Gift

Location

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

Presentation Type

Poster

Start Date

4-3-2016 10:45 AM

End Date

4-3-2016 12:15 PM

Abstract

Many chemical compounds can exist in either an anhydrate or hydrate form. The solid state form, anhydrate or hydrate, of an active pharmaceutical ingredient (API) influences its bioavailability, chemical stability, pharmacokinetics, and solubility. The hydrate form has a negative impact on all of these properties and so inhibiting the transformation is necessary. Aqueous slurries were prepared by adding a small amount of anhydrous theophylline to 50 mL of a dilute polymer solution. The pH of the solutions was varied from 2 to 7. The anhydrate to hydrate transformation was monitored using Raman spectroscopy. Additionally solubility tests and intrinsic dissolution tests were performed to quantify how the polymer effects the stages of transformation. The transformation of theophylline was determined to be pH dependent with the slowest transformations occurring at the lowest pHs.

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Mar 4th, 10:45 AM Mar 4th, 12:15 PM

Manipulation of the Anhydrate to Hydrate Transformation of Theophylline Using Polymeric Excipients in Aqueous Slurries

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

Many chemical compounds can exist in either an anhydrate or hydrate form. The solid state form, anhydrate or hydrate, of an active pharmaceutical ingredient (API) influences its bioavailability, chemical stability, pharmacokinetics, and solubility. The hydrate form has a negative impact on all of these properties and so inhibiting the transformation is necessary. Aqueous slurries were prepared by adding a small amount of anhydrous theophylline to 50 mL of a dilute polymer solution. The pH of the solutions was varied from 2 to 7. The anhydrate to hydrate transformation was monitored using Raman spectroscopy. Additionally solubility tests and intrinsic dissolution tests were performed to quantify how the polymer effects the stages of transformation. The transformation of theophylline was determined to be pH dependent with the slowest transformations occurring at the lowest pHs.