Preparation and evaluation in vitro of polycarbonate microspheres containing local anesthetics.
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Biomedical subjects
Publications and source records attributed to K Juni.
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Compressed tablets were prepared from theophylline and hydroxypropylcellulose. Effects of the viscosity grades of the polymer, the mixing ratios of two polymers with different viscosity grades, and the polymer contents in the tablets on release patterns of theophylline were examined in vitro. Release rate was decreased with increasing viscosity designation and polymer contents in the tablets. In salivary level profiles of theophylline following oral administration of sustained-release tablets to five human volunteers, a low but sustained level was noted indicating sustained release of the drug from the tablets in vivo.
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The local anesthetic effect of tetracaine in polylactic acid microspheres was compared with that of tetracaine hydrochloride solutions. As a first step, the local anesthetic effect of 0.1 ml tetracaine hydrochloride solutions was examined at four concentrations in vivo. Then, the local anesthetic effect of 0.2 ml tetracaine hydrochloride solutions was compared with that of 0.1 ml tetracaine hydrochloride solutions. The more the amount of tetracaine, the stronger and longer was the local anesthetic effect. The local anesthetic effect of tetracaine in microspheres was much longer and lasted over 100 h.
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Dry agar beads containing theophylline were prepared. The release rate of theophylline from the agar beads in vitro was smaller than the dissolution rate of the drug from pure drug powders. The salivary levels of the drug following oral administration of the agar beads to three healthy volunteers were determined by reversed-phase high pressure liquid chromatography. Results of pharmacokinetic analyses indicated sustained absorption of the drug following the administration of the agar beads.
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The effects of caffeine, beta-cyclodextrin, and povidone on the permeation behavior of butamben from saturated solutions in these complexing agents through a dimethyl polysiloxane membrane were investigated at 30 degrees. In all systems, these agents increased the rate of release over the plain saturated drug solution. The effect was more pronounced with caffeine and beta-cyclodextrin than with povidone. Interpretation of these results with the aid of solubility data for the corresponding systems led to the following generalization. For a fixed total (free and complexed) amount of drug available for release, sustained release is associated with systems containing more stable complexes. The practical value of this approach to the controlled release of drug is discussed.
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