Chitinosan-drug complexes: effect of electrolyte on naproxen release in vitro.
The purpose of this study was to examine the potential use of electrolytes to control naproxen sodium (I) release from chitinosan (II) tablets. An ANOVA was employed to evaluate the effects of molecular weight (MW) of II, electrolyte valence (EV), and pH of the dissolution medium on I's release. The intrinsic dissolution rates and saturation solubilities of I were determined at each of the pHs used. Directly compressed tablets were prepared from admixtures containing: I, NaCl, CaCl(2), or AlCl(3), Mg stearate, and II. The tablets were characterized for their dimensions, crushing strengths, friability, disintegration times, and in vitro dissolution profiles. The slopes of the log-log cumulative percent released-time curves (t=0-5 h) were compared using ANOVA. Based on the ANOVA, each of the variables-chitinosans, EVs, and pHs-significantly affected drug release (P<0.05). Besides the poor aqueous solubility of I, the factors possibly affecting drug release included: (a) the formation of a rate-limiting II gel barrier; (b) the interaction of I with ionized amino groups of II; (c) the effect of electrolyte on the II's gel barrier formation; and/or (d) decreased aqueous solubility of I in the presence of electrolyte.
Rege
Pankaj R
PR
Department of Medicinal Chemistry and Pharmaceutics, Duquesne University, Pittsburgh, PA 15282, USA. pankaj.rege@bms.com
Shukla
Dhruti J
DJ
Block
Lawrence H
LH
D002686:Chitin / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D004573:Electrolytes / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D009288:Naproxen / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D014783:Viscosity
D004573:Electrolytes; D013607:Tablets; D002686:Chitin; D009288:Naproxen