The Influence of Cellulosic Polymer's Variables on Dissolution/Solubility of Amorphous Felodipine and Crystallization Inhibition from a Supersaturated State.

The Influence of Cellulosic Polymer's Variables on Dissolution/Solubility of Amorphous Felodipine and Crystallization Inhibition from a Supersaturated State.
AAPS PharmSciTech. 2018 Dec 17;20(1):12
Authors: Shi NQ, Jin Y, Zhang Y, Che XX, Xiao X, Cui GH, Chen YZ, Feng B, Li ZQ, Qi XR
Abstract
The collective impact of cellulosic polymers on the dissolution, solubility, and crystallization inhibition of amorphous active pharmaceutical ingredients (APIs) is still far from being adequately understood. The goal of this research was to explore the influence of cellulosic polymers and incubation conditions on enhancement of solubility and dissolution of amorphous felodipine, while inhibiting crystallization of the drug from a supersaturated state. Variables, including cellulosic polymer type, amount, ionic strength, and viscosity, were evaluated for effects on API dissolution/solubility and crystallization processes. Water-soluble cellulosic polymers, including HPMC E15, HPMC E5, HPMC K100-LV, L-HPC, and MC, were studied. All cellulosic polymers could extend API dissolution and solubility to various extents by delaying crystallization and prolonging supersaturation duration, with their effectiveness ranked from greatest to least as HPMC E15 > HPMC E5 > HPMC K100-LV > L-HPC > MC. Decreased polymer amount, lower ionic strength, or higher polymer viscosity tended to decrease dissolution/solubility and promote crysta...

Source: AAPS PharmSciTech - December 17, 2018 Category: Drugs & Pharmacology Authors: Shi NQ, Jin Y, Zhang Y, Che XX, Xiao X, Cui GH, Chen YZ, Feng B, Li ZQ, Qi XR Tags: AAPS PharmSciTech Source Type: research