Drug volume fraction profile in the gel phase and drug release kinetics inhydroxypropylmethyl cellulose matrices containing a soluble drug

In the present work, the drug volume fraction profiles of a colored and ver y soluble drug, buflomedil pyridoxal phosphate, in the gel layer of initial ly glassy hydroxypropylmethyl cellulose matrices were studied, using image analysis of pictures of the matrices during swelling and release. The goal was to correlate the drug release kinetics with the dynamic behavior of the drug gradient in the gel layer. An inert (nonswellable) matrix, manufactur ed by substituting hydroxypropylmethyl cellulose with an inert polymer and containing the same amount of buflomedil pyridoxal phosphate, was prepared as well. The drug color gradient in the partially extracted region and the flux of this matrix were compared to the swellable matrix. The drug gradien t in the dissolved drug gel layer of swellable matrices was observed. It wa s demonstrated that drug release kinetics does not only depend on drug diff usion and matrix erosion, but also on drug dissolution in the gel and on po lymer relaxation. (C) 1999 Published by Elsevier Science B.V. All rights re served.