Interaction of two diclofenac acid salts with copolymers of ammoniomethacrylate: effect of additives and release profiles.
The copolymer of ammoniomethacrylate Eudragit RL (ERL) interacted with diclofenac acid salts (sodium and diethylamine salts) in aqueous solutions, forming a complex. Sorption experiments were done in aqueous solutions of either sodium lauryl sulfate (SLS), Tween 20, or Tween 80. The SLS competed strongly with the drug, even at low concentrations, and reduced significantly the amount of drug sorbed by ERL. Tweens at high concentrations exhibited two phase profiles: the sorption phase, which was short and during which drug concentration dropped sharply, and the release phase, during which the drug was released slowly over 24 hr and which was accompanied by dispersion of ERL particles into the colloidal dispersion. The interaction was dependent on temperature, ionic strength, and nature of the additives. The extent of interaction in water and phosphate buffer solutions was in the following order: water > pH 6 > pH 7-8. In-vitro dissolution studies of the dried complex were done over 24 hr. In water, the drug remained bound to the polymer. In aqueous surfactant solutions (SLS, Tween 20, and Tween 80) and phosphate buffer at pH 6.8, a linear relationship between drug concentration and the square root of time was obtained, indicating a matrix diffusion-controlled mechanism. However, 100% release was not reached, and resorption was observed in the phosphate buffer solution.
Khalil
E
E
Faculty of Pharmacy, University of Jordan, Amman, Jordan.
Sallam
A
A
D000327:Adsorption; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry; D004008:Diclofenac / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006863:Hydrogen-Ion Concentration; D009994:Osmolar Concentration; D011108:Polymers / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013696:Temperature; D013997:Time Factors
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011108:Polymers; D011136:Polysorbates; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; D004008:Diclofenac; D012967:Sodium Dodecyl Sulfate