Open AccessA case study exploring the impact of an oxygen barrier coating on formulation stability, in‐vitro dissolution and bioperformance
Author(s) -
Mann James C.,
Mitra Amitava,
Pygall Samuel R.
Publication year - 2012
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/j.2042-7158.2011.01372.x
Subject(s) - dissolution , coating , oxygen , chemistry , chemical engineering , materials science , nanotechnology , engineering , organic chemistry
Objectives The impact of a carmellose sodium (sodium carboxymethycellulose)‐based coat (Opaglos 2) on the stability of an oxygen‐sensitive compound A and in‐vitro dissolution and bioperformance of compound B has been investigated. Methods Tablets containing compounds A and B were coated with various weight gains of Opaglos 2 and a comparative elegance coating (poly(vinyl alcohol)‐based Opadry II). Film‐coated tablets were assessed for oxidative degradation under accelerated stability conditions (30°C/65% RH and 40°C/75% RH). Key findings An apparent rank order of restriction of oxygen (O 2 ) permeability afforded by the coatings was observed, with only higher Opaglos 2 coating weight gains (6 and 8% w/w) providing adequate oxidative degradation stability for up to 52 weeks. Improved stability at the higher coating weight gains was attributed to incomplete polymeric film formation at lower coating weight gains. The 6% and 8% w/w Opaglos 2 formulations showed dissolution retardation compared with elegance‐coated formulations in USP dissolution apparatus II, predicting significant impact on formulation bioperformance. However, pharmacokinetic studies in Beagle dogs showed similar bioperformance for all formulations. Conclusions The Opaglos 2 coating system evaluated in these studies afforded adequate protection from oxidative degradation with no negative impact on bioperformance as compared to elegance coating. However, further studies are needed using several compounds to assess the broader applicability of these coatings.