Bansal P C, Pitman I H, Higuchi T
J Pharm Sci. 1981 Aug;70(8):855-7. doi: 10.1002/jps.2600700804.
Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher water solubilities and faster dissolution rates than the parent drugs, and they appear to be potentially useful as prodrugs.
制备了1-羟甲基别嘌醇、1,5-二羟甲基别嘌醇、1-羟甲基格鲁米特和1-羟甲基苯巴比妥的固体样品，并计算了它们由甲醛与别嘌醇、格鲁米特或苯巴比妥形成时的平衡常数。N-羟甲基衍生物比母体药物具有更高的水溶性和更快的溶解速率，它们似乎有可能作为前药使用。
