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Characterization of supersaturated lidocaine/polyacrylate pressure sensitive adhesive systems: thermal analysis and FT-IR.

Supersaturated and crystallized lidocaine (LC)/pressure sensitive adhesive (PSA) systems have been studied by differential scanning calorimetry (DSC) and FT-IR with the objective of characterizing the thermodynamic states and compatibility of the two-component systems. Analysis of the phase behavior of LC/DT2287 systems indicates that LC and DT2287 are thermodynamically miscible within the composition range containing less than approximately 20% w/w LC, beyond which LC may crystallize from the blends forming a separated crystalline phase. The composition dependence of the glass transition temperature (T(g)) was used to characterize the physical and thermodynamic states of the supersaturated systems. The Fox, Gordon-Taylor, Kwei, Kovacs, and Brekner, Schneider and Cantow (BSC) equations were employed to conduct the analysis. It was found that the PSA in the supersaturated LC/PSA systems underwent significant entropic relaxation upon mixing. LC in the miscible systems is absorbed into and swells the polymer network of the PSA, thereby exhibiting reduced molecular mobility, while the PSA attains significant molecular conformation relaxation and entropy increase. It was also found that LC molecules extensively participate in molecular relaxation of the PSA throughout the composition range studied. The molecular mobility of LC is inhibited as the volume fraction of DT2287 increases, suggesting that the PSA molecular network reduces the molecular mobility of LC by closely involving LC molecules in its relaxation, and thereby may enhancing the physical stability of the systems. No strong intermolecular interactions between the two components were found based upon the results of T(g)-composition analysis, and was confirmed by FT-IR studies. This indicates that the analysis based on the BSC equation provides more precise characterization of polymer systems than the T(g) -composition analysis based on other equations cited.

Acrylic Resins↗

Evidence that (+)-bupranolol interacts directly with myocardial beta-adrenoceptors. Control of optical purity with differential thermal analysis.

Melting points measured with the capillary method were 150.5 degree C, 150.5 degree C and 224.0 degree C for hydrochlorides of (+)-bupranolol, (-)-bupranolol and (+/-)-bupranolol, respectively. The large difference in melting points of 73.5 degree C prompted us to determine possible contaminations of (+)-bupranolol with traces of (-)-bupranolol using differential scanning calorimetry. We detected as little as 0.001% (-)-bupranolol in a standard mixture of (+)-bupranolol and (-)-bupranolol. A batch of (+)-bupranolol not measurably contaminated with (-)-bupranolol (optically purity greater than 99.999%) was used in pharmacological and biochemical assays. The affinities of (-)-bupranolol and (+)-bupranolol were determined functionally by the blockade of isoprenaline stimulation of spontaneously beating rat right atria and electrically driven kitten papillary muscles; and directly by inhibition of binding of 3H-(-)-propranolol to kitten ventricle membrane particles. In all 3 systems the enantiomeric (-)/(+) affinity ratio was 50--120 for bupranolol. These experiments prove that (+)-bupranolol itself binds to the beta-adrenoceptors of mammalian myocardium.

Animals↗