Showing papers in "Journal of Pharmaceutical Sciences in 1994"

TL;DR: The results of pharmacokinetic analysis suggested that small PEG tended to freely translocate from the circulation to extravascular tissues and to return to the blood circulation again by diffusion, whereas large PEG translocated more slowly to extraVascular tissues.

TL;DR: A general linear solvation energy equation has been used to analyze published partition coefficients in the systems water-octanol, water-hexadecane), water-alkane, and water-cyclohexane and shows that solute hydrogen-bond basicity, dipolarity/polarizability and size are significant factors that influence the delta log P parameter.

TL;DR: It was shown that in both samples significant crystallization to the most stable polymorphic form occurred over several days when stored below Tg, and in some cases this process was preceded by the relaxation of one amorphous form to the other.

TL;DR: The pH of the extracapsular environment was found to affect the release of albumin significantly and a combination of high and low molecular weight chitosan gave the best results for reducing elution ofalbumin in the first 4 h and increasing elution in the following 20 h.

TL;DR: Solute dipolarity/polarizability, hydrogen-bond acidity, and hydrogen- bond basicity favor blood, and solute size, as Vx, favors brain, so that log BB values themselves may be obtained simply from knowledge of solute molecular structure.

TL;DR: It is suggested that in vitro dissolution tests of hard gelatin-containing dosage forms be conducted in two stages, one in a dissolution medium without enzymes and secondly in dissolution media containing enzymes prior to in vivo evaluation, to constitute a better indication of the in vivo behavior of gelatin-encapsulated formulations.

TL;DR: Reduced variability in the pharmacokinetics of cyclosporine following oral administration of Sandimmune Neoral provides a more predictable and consistent concentration-time profile.

TL;DR: This approach was used to quantify the relationship between permeant radius and transepithelial electrical resistance and to analyze changes in junctional pore size as a function of pharmacological perturbation, such as in the use of absorption promoters or adjuvants.

TL;DR: A symposium devoted to classic and new approaches in the use of liposomal systems was organized and chaired by M. Mezei and E. Touitou and focused on liposomes as tools in the mechanistic study of absorption promoters and interaction with the human skin.

TL;DR: An ultrafiltration system was evaluated for the free-fraction measurement of SPECT radiotracers used in functional brain imaging and provided rapid results, demonstrated minor analytical errors, revealed generally good correlation with equilibrium dialysis, and allowed excellent precision.

TL;DR: This review focuses upon one aspect of this problem, namely aggregation of solid proteins under pharmaceutically relevant conditions (elevated temperature and water activity).

TL;DR: The results show that all the optimized F forms do lastingly float upon the gastric contents, whereas the NF forms sink rapidly after ingestion, whereas in upright subjects, the F forms are consequently protected against postprandial emptying.

TL;DR: The floating dosage form was found to be a feasible approach in delivering furosemide to the upper gastrointestinal tract to maximize drug absorption and to develop and optimize in vitro a monolithic modified-release dosage form (MMR).

TL;DR: It is shown that molecules bearing highly charged oxygen or nitrogen atoms tend to have high activity, and that the enzyme can accommodate molecules of only a limited size.

TL;DR: In this article, a quantum chemical (AM1) combined with a classical study of structure-activity relationships for 1,4-dihydropyridines (nifedipine analogues) was performed.

TL;DR: The absorption of peptide and protein agents by rat lung following their intratracheal administration was investigated, and a negative association between molecular weight and bioavailability was noted.

TL;DR: In this paper, a spontaneous emulsification solvent diffusion mathod was used to prepare nanospheres with L-lactide/glycolide copolymer (PLGA) for peptide drugs.

TL;DR: Dissociation constants (pKaS) of acidic, basic, and amphoteric pharmaceuticals were exactly determined by capillary electrophoresis, and the obtained pKa values were highly consistent with the values determined by conventional methods.

TL;DR: The results of this study indicate that dextran conjugates may be useful in selectively delivering glucocorticoids to the large intestine for the treatment of colitis.

TL;DR: The pKa and log P of 20 compounds, including six substituted phenols, two substituted quinolines, N-methylaniline, five barbiturate derivatives, two phenothiazines, and several other molecules of pharmaceutical interest, were determined by the potentiometric technique at 25 degrees C and ionic strength 0.1 M.

TL;DR: Thirty-two aryl-substituted 2-benzothiazolamines have been tested for their ability to modulate sodium flux in rat cortical slices and showed a trend toward increasing potency as sodium flux inhibitors with increasing lipophilicity, decreasing size, and increasing electron withdrawal of the benzo ring substituents.

TL;DR: Sulfated polysaccharides and citrate are found to be effective in increasing the melting temperature of rhKGF or preventing its aggregation and negatively charged small ions, such as phosphate, also have moderate stabilizing effects on rhK GF.

TL;DR: The lipid emulsion particles described in this study have a potential use as targetable carriers for site-specific drug delivery and may be suitable for dispersing and stability properties of parenteral drug carriers.

TL;DR: It is found that the extent of solubilization strongly depends on the solute hydrophobicity and the ethanol concentration in the solvent mixture, and patterns of deviation from the log-linear model are related to the structure and hydrophobia of the solutes.

TL;DR: A computer optimization technique based on response surface methodology was applied for the optimization of a hydrogel formulation containing indomethacin as a model drug and the predicted response values for the optimum formulation have been successfully validated in a repeated in vivo percutaneous absorption study.

TL;DR: Why HDL-associated AmpB causes reduced renal toxicity may be due to its lack of interaction with renal cells because of the absence of HDL receptors, and the role of LTP on the distribution of AmpB to HDL and LDL was investigated.

TL;DR: The theory suggests that transdermal transport in the presence of an electrical field may occur through corneocytes of the stratum corneum, and confirms the importance of a shunt route for small ion transport, as well as an intercellular route of transport for passive diffusion of noncharged substances.

TL;DR: The effects of molecular weight (M(r) on the serum and urine pharmacokinetics and tissue distribution of dextrans, potential macromolecular carriers for drug delivery, were studied in rats and the liver, spleen, and kidney accumulation of FDs demonstrated a significant degree of M( r) dependency.

TL;DR: Topotecan's half-life in human plasma (pH 7.6) can be enhanced dramatically by packaging the drug within the aqueous, pH 5-adjusted confines of lipid vesicles composed of diasteroylphosphatidylcholine.

TL;DR: Interestingly, unlike irreversible protein aggregates, the insulin powders recover essentially full biological activity on reconstitution, and are suggestive of extensive beta-sheet-mediated intermolecular interactions in precipitate states, consistent with analyses of irreversible protein aggregate/fibril states.