Partially hydrolyzed polyvinyl alcohol for fusion-based pharmaceutical formulation processes: evaluation of suitable plasticizers

Publication date: Available online 5 February 2020Source: International Journal of PharmaceuticsAuthor(s): Konstantinos Katopodis, Afroditi Kapourani, Elisavet Vardaka, Anna Karagianni, Christina Chorianopoulou, Konstantinos N. Kontogiannopoulos, Dimitrios N. Bikiaris, Kyriakos Kachrimanis, Panagiotis BarmpalexisAbstractThe present study evaluates the effect of several pharmaceutical plasticizers on the thermo-physical and physicochemical properties of partially hydrolyzed poly(vinyl alcohol) (PVA) used in fusion-based pharmaceutical formulation processes. Specifically, the effect of mannitol (MAN), sorbitol (SOR), sucrose (SUC), anhydrous citric acid (CA), triethyl citrate (TEC) and low-molecular weight polyethylene glycol (PEG400) on PVA’s melting properties, physical state and thermal degradation was evaluated via differential scanning calorimetry (DSC), powder X-ray diffractometry (pXRD) and thermo-gravimetric analysis (TGA). Results showed that the use of MAN, SOR, SUC and PEG400 led to the reduction of PVA’s melting onset temperature, while MAN, SUC, CA and SOR were amorphously dispersed within PVA’s matrix, and the addition of SUC and CA resulted in significant reduction of PVA’s crystallinity. TGA results showed the formation of thermally highly unstable PVA mixtures in the cases of CA and TEC (degradation started from ∼150 oC and ∼125 oC, respectively), while significant molecular interactions were identified by FTIR in the cases of PVA-MAN, PVA-SOR and P...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research