Formulation and Investigation of Eroding Hydrophilic Matrix Systems

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On the basis of this study the following can be con cluded: •There is a correlation between the wetting properti es of powder mixtures and the erosion of inert comprimates. •Factors which increase wetting time are relevant for temperature elevation during the formulation of this system. The effect of operational factors can be predicted from the results of such preformulation studies. •The composition applied was appropriate for the incorporation of LA. It can be processed into the granulating fluid (up to concentration of 15%). The presence of LA in the granulating fluid altered significantly neither the particle size distribution, nor the mechanical properties of the granules. The shape of the tablets constantly changed during the dissolution, the main alteration could be seen after 4 h. Erosion and change in shape were very similar for each of the samples. •The pH-decreasing effect of the tablets was influenced by the concentration of LA applied in the granulating fluid. Erosion is the main parameter responsible for the liberation of LA from this system in the first partof dissolution. This phenomenon increased the possibility of detachment of LA from the insoluble carrier. When the concentration of LA reached a given level, the more readily liberating sites were saturated. In the second stage of dissolution the relevance of erosion was lower and the slower process became more important. Finally, it can be stated that a controlled release intravaginal matrix tablet can be formulated from the matrix former HPMC and the carrier MCC to ensure a long-acting preparation containing LA. In addition, there was no sign of matrix destruction caused by the LA as a strong acid.

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