Rao K V, Kailasam S, Menon N K, Radhakrishna S
Bull World Health Organ. 1971;45(5):625-32.
This paper reports the gross and rapid condensation of isoniazid in a commercial black-currant-flavoured syrup. In vitro studies showed that the condensation was due, at least partly, to the glucose contained in the syrup, paper chromatography having demonstrated the presence of D(+)-glucose isonicotinoyl hydrazone. Controlled studies in human beings showed that the absorption of isoniazid from the preparation was considerably impaired by this condensation.It is concluded that sugars such as glucose, fructose, and sucrose-especially glucose-should not be used in isoniazid syrup preparations, and it is suggested that sorbitol, a stable non-carbonyl compound, might be a suitable substitute.
本文报道了异烟肼在一种市售黑加仑味糖浆中的大量快速缩合现象。体外研究表明，这种缩合至少部分是由于糖浆中所含的葡萄糖引起的，纸色谱法已证明存在D(+)-葡萄糖异烟酰腙。人体对照研究表明，这种缩合会显著损害异烟肼从该制剂中的吸收。结论是，葡萄糖、果糖和蔗糖等糖类——尤其是葡萄糖——不应用于异烟肼糖浆制剂中，建议使用山梨醇，一种稳定的非羰基化合物，可能是合适的替代品。
