The Use of a Polymer Excipient to Inhibit the Hydrate Transformation of Carbamazepine

Advisor Information

Alan Gift

Location

Milo Bail Student Center Ballroom

Presentation Type

Poster

Start Date

8-3-2013 9:00 AM

End Date

8-3-2013 12:00 PM

Abstract

Solid active pharmaceutical ingredients (APIs) are formed into tablets through a process called wet granulation. This process introduces an aqueous solution that contains a binding agent. However, if the API is an anhydrate crystal, this process may transform it to its hydrate state, which can affect its bioavailability, solubility, and stability. Polymeric excipients have shown to inhibit the transformation of an API to the hydrate form. Different aqueous slurries containing polyvinyl alcohol (PVA) have been examined to understand its inhibitory effects on the anhydrate-to-hydrate crystal transformation of carbamazepine. Each slurry mixture contained 1.0 gram of carbamazepine in 50 mL of an aqueous polymer solution (0.01 mg/mL) and was mixed with an overhead stirrer. Kinetic data was collected with an in-line Raman spectrometer and analyzed with multi-variate software. A variety of polymer solutions of polyvinyl alcohol with different chain lengths and percent hydration values were investigated. The results showed significant increase in transformation time for all of the PVA solutions compared to transformation of carbamazepine in pure water. Many of the PVA solutions showed similar results at inhibiting the carbamazepine transformation, but the PVA solution with the longer chain length and lowest percent hydration showed the least inhibition. More PVA solutions will be examined to determine how these properties affect the of carbamazepine transformation.

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Mar 8th, 9:00 AM Mar 8th, 12:00 PM

The Use of a Polymer Excipient to Inhibit the Hydrate Transformation of Carbamazepine

Milo Bail Student Center Ballroom

Solid active pharmaceutical ingredients (APIs) are formed into tablets through a process called wet granulation. This process introduces an aqueous solution that contains a binding agent. However, if the API is an anhydrate crystal, this process may transform it to its hydrate state, which can affect its bioavailability, solubility, and stability. Polymeric excipients have shown to inhibit the transformation of an API to the hydrate form. Different aqueous slurries containing polyvinyl alcohol (PVA) have been examined to understand its inhibitory effects on the anhydrate-to-hydrate crystal transformation of carbamazepine. Each slurry mixture contained 1.0 gram of carbamazepine in 50 mL of an aqueous polymer solution (0.01 mg/mL) and was mixed with an overhead stirrer. Kinetic data was collected with an in-line Raman spectrometer and analyzed with multi-variate software. A variety of polymer solutions of polyvinyl alcohol with different chain lengths and percent hydration values were investigated. The results showed significant increase in transformation time for all of the PVA solutions compared to transformation of carbamazepine in pure water. Many of the PVA solutions showed similar results at inhibiting the carbamazepine transformation, but the PVA solution with the longer chain length and lowest percent hydration showed the least inhibition. More PVA solutions will be examined to determine how these properties affect the of carbamazepine transformation.