PubMed · 4721645
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J E Rees. 1973. Physico-mechanical pre-formulation studies.. https://pubmed.ncbi.nlm.nih.gov/4721645/
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Theoretical descriptions of solvent and solubility properties, important for a rational development of liquid dosage forms, have so far not proved completely satisfying. In this work, the modified Debye equation according to Leuenberger, which was introduced earlier for the description of polar and nonpolar pure liquids, is extended to liquid binary mixtures. Between 290.7 and 343.2 K, several binary aqueous systems were investigated. The values of (E(i)/E) (E(i)=internal electric field, E=external electric field), calculated by means of the modified Debye equation, were compared to the correlation factor g of the Kirkwood-Fröhlich equation, which describes the molecules' preference for either parallel or nonparallel alignment. The previously found correlation between /m/ of (E(i)/E)=m(1/T)+b (T=temperature) and the Hildebrand solubility parameter delta for pure liquids was investigated for binary mixtures. Furthermore, the applicability of percolation theory to the description of binary liquid mixtures was examined. This new approach allows the description of irregular solutions and provides a useful tool for a more rational design of liquid dosage forms.
The influence of in situ plasticization of chlorpheniramine maleate (CPM) on Eudragit RS PO from hot-melt extruded matrix tablets, and from compressed granules prepared by thermal processing was investigated. CPM was studied as both a model drug substance and as a solid-state plasticizer for the acrylic polymer. Triethyl citrate (TEC) was incorporated into the polymer blend as a liquid plasticizer for the polymer. The influence of TEC and CPM concentration on the dissolution properties of CPM tablets was investigated. The glass transition temperature (T(g)) of the samples was determined by modulated differential scanning calorimetry (MDSC). The morphologies of the granules formed by hot-melt extrusion and hot-melt granulation processes were investigated by scanning electron microscopy. The addition of 12% TEC to the polymer reduced the T(g) by 32.5 degrees C, while the reduction in the T(g) for the same level of CPM was 16.4 degrees C. The effect of TEC levels on drug release was dependent on the tablet preparation method. At high TEC levels, the release rate of CPM decreased in tablets prepared by direct compression and tablets made from compressed granules that had been prepared by high shear hot-melt granulation. However, the CPM release rate increased from hot-melt extruded tablets with increasing blends of plasticizer in the extruded tablets. An increase in the CPM content in the tablets resulted in an increase in the drug release rate. During high shear hot-melt granulation, the model drug adhered to the polymer to form a porous discontinuous structure. Following hot-melt extrusion, the drug was distributed at a molecular level in the continuous polymeric structure. The influence of both CPM and TEC levels on the drug release rate from these polymeric drug delivery systems was shown to be a function of whether the granules or tablets were formed by either hot-melt granulation or hot-melt extrusion, as well as the plasticization effects of both TEC and CPM on the acrylic polymer.