By determining the degree of irritation caused in the derma by solutions of substances in common pharmaceutical use, it can be shown that these solutions may be divided into two categories: those which exert an osmotic pressure (because they do not pass through the cell membrane) and those which exert no osmotic pressure (because they do pass through the cell membrane). Injectable solutions prepared with substances of the second group must be rendered isotonic by the addition of the same quantity of a product not freely diffusible through the cell membrane which would be necessary to render distilled water isotonic. Furthermore, it has been demonstrated that slightly hypertonic solutions are better tolerated than isotonic solutions and, hence, when desiring to prepare a well tolerated injectable solution of a substance whose osmotic pressure is not known and cannot be determined by a biological method, 0.9 per cent of NaCl may be added.
The results of a study of the anatomy of the stem of Morinda citrifolia L. are described. A preliminary report of the pharmacodynamic study of a 95 per cent alcoholic extract of the root on the isolated uterine horn of an albino rat showed some measure of sedation using doses of 1 to 5,000 to 1 to 36,000. A water decoction of the crude whole root, injected intravenously in the anesthetized dog, in a dose representing 4 Gm. produced a marked lowering of blood pressure which lasted approximately twenty-six minutes. It appears that the hypotensor activity resides in the water-soluble fraction of the root of Morinda citrifolia. The results of in vivo experiments gave evidence of a low order of toxicity of Morinda citrifolia root.
The plan of this investigation was to complex tetracaine HCl and some related local anesthetics with certain metal ions; and to determine the most acceptable complexing metal ions, the stability constants of the metal complexes under varying conditions, and the biological significance of such complexes.
An improved synthesis of benzofuran-2-carboxaldehyde and 2-methylbenzofuran-3-carboxaldehyde and the preparation of twenty-three new derivatives are reported. They were evaluated against three pathogenic fungi, together with some other derivatives which have been described in the literature. Some of these compounds showed significant in vitro antifungal activity. Of all the compounds tested, including the standard, undecylenic acid, benzofuran-2-carboxaldehyde exhibited high activity in every case against all three organisms. A discussion of the activity and structure relationship is based on the data resulting from this investigation. Further studies seem to be warranted.
A procedure for the determination of sodium pentobarbital and sodium thiopental under rigidly standardized conditions of extraction, using Allen's absorption factor, is described. This method makes possible the reliable quantitative determination of 1 mcg./ml. or smaller concentration differences. In an appendix Allen's absorption factor for sodium pentobarbital is derived.
A homolog of acetylsalicylic acid, β -( o -ace-toxyphenyl)propionic acid, has been made successfully. Its toxicity and, analgesic properties have been determined on rats. It has been found to have analgesic properties in rheumatic patients. No free salicylic acid is eliminated in the urine. It appears that this compound does not exert its analgesic properties as a salicylate.
Three plastic syringes were evaluated as to their ability to bind a number of weak organic acids. Polyethylene and polystyrene syringes did not interact with any of the seven agents included in the binding study. Benzoic acid, m-hydroxybenzoic acid, p-aminobeazoic acid, and salicylic acid were bound to various degrees by the nylon syringes. No interaction was noted with any of the syringes and acetylsalicylic acid, phénobarbital, or barbital. The degree of binding was influenced by concentration, temperature, and diffusion.
When tropine is esterified with an appropriate acid, an active antispasmodic results. In order to study a change in the linkage between the nitrogen ring system and the acid moiety, a series of glycidic esters was prepared utilizing tropinone as the starting ketone in the Darzens condensation. Another series was prepared utilizing 1-methyl-4-piperidone.
A number of 4-diethylamino-2-butynyl esters and 1,4-bis-N-substituted amino-2-butynes were prepared. The compounds, in the form of their hydrochloride and/or methiodide salts, were tested in vitro against three fungi causing dermatomycoses. Several compounds exhibited good activity in comparison to the control compound, sodium undecylenate. The most effective compound in this investigation was 4- diethylamino-2-butynyl o-toluate hydrochloride.
Available indicator extraction methods were inadequate for the determination of isopropamide iodide in the presence of amine bases. The substance was complexed with methyl orange in pH 10.2 buffer and extracted into chloroform. Re-extraction of the color into 1 N hydrochloric acid and its spectrophotometric determination gave quantitative results. Calibration curves for other short chain quaternary amines were determined and compared to a known solution of methyl orange. Agreement with the theoretical value was obtained down to tetra-n-propyl ammonium iodide. Application of the method to the determination of isopropamide iodide in a pharmaceutical preparation gave results ranging from 98.7 to 101.3 per cent of the theoretical amount present.
A method is presented which describes a revised sugar coating procedure. The procedure eliminates the rounding and smoothing operations usually employed in pan-coated tablets. The resulting coating is approximately one-half as thick as the standard method and coating time is greatly reduced.
An easily constructed apparatus for the uniform agitation of solute-solvent combinations is described. It can be used effectively in many laboratory mixing problems.
