Fumio Ueda

Release of Nicotinamide from Fatty Acid-Nicotinamide Equimolar Complexes.

The release behavior of nicotinamide (NAA) from fatty acid (FA)-NAA equimolar complexes was examined in a JP XI dissolution test apparatus in JP XI disintegration test medium No. 1 (pH 1.2) at 37°C where the carbon number of FA is 14-18. The time required for 50% or 80% of NAA to release (T50 or T80) was measured, and the effect of the constituent FA on T50 or T80 was investigated. The values of T50 or T80 for FA-NAA formed with odd-numberd FA were larger than those for FA-NAA formed with even-numbered FA whose alkyl chain length is one more carbon number longer, though the values of T50 of T80 increased rather regularly with an increase of the alkyl chain length for only even-numbered or odd-numbered FA. The values of T50 and T80 for FA-NAA formed with heptadecanoic acid (C17-NAA) were about 36 and 102 min, respectively, suggesting that C17-NAA may be applicable to the preparetion of a sustained-release drug formulation.

Hygroscopicity and Dissolution of Thiamine Disulfide-Higher Fatty Acids Complexes

The hygroscopicity of the complexes composed of thiamine disulfide (TDS) and higher fatty acids and the dissolution of TDS from the complexes were studied. The hygroscopicity of TDS was reduced dramatically by the formation of the (fatty acid) 6 (TDS) complexes. Regarding the dissolution of TDS from the complexes, plots of T 50 or T 80 (the time required for 50% or 80% of TDS to dissolve, respectively) against the carbon numbers of the constituent fatty acids showed a zig-zag pattern, and C17 fatty acid gave the longest T 50 and T 80

Researches on Chemotherapeutic Drugs against Viruses. XXV. Studies on the Syntheses and Antiviral Effect of 2-Dimethylaminoethyl Alkylphenyl Ethers

2-Dimethylaminoethyl phenyl ether, having alkyl chain of 8∼14 carbon atoms on the benzene ring in ortho- or para-position, were synthesized by condensation of alkylphenol with 2-dimethylaminoethyl chloride. The antiviral effects of these compounds were tested against the Nakayama strain of Japanese B encephalitis virus and the Lansing strain of poliomyelitis virus. 2-Dimethylaminoethyl o-octylphenyl ether and p-octylphenyl ether had antiviral activity against the Nakayama strain in vivo. 2-Dimethylaminoethyl o-octylphenyl ether, o-decylphenyl ether, and p-octylphenyl ether had antiviral activity against the Lansing strain in vitro.