Furuta S, Toyama S, Miwa M, Sano H
Central Research Laboratories, Zeria Pharmaceutical Co. Ltd., Saitama, Japan.
J Pharm Pharmacol. 1995 Aug;47(8):632-6. doi: 10.1111/j.2042-7158.1995.tb05849.x.
The disposition of polaprezinc in the rat gastrointestinal tract was studied by a double tracer method using [14C]- and [65Zn]polaprezinc. At 0.5 h after oral administration of [14C]-,[65Zn]polaprezinc to rats, the 14C-radioactivity in the gastric contents was comparable with the 65Zn-radioactivity. However, a significant difference was observed in the time course of changes in gastric contents between 14C- and 65Zn-radioactivity over 1 h after administration, indicating that polaprezinc existed in complex form at 0.5 h after administration and was dissociated to L-carnosine and zinc in the gastrointestinal tract as a function of time. The adhesion of zinc to stomach mucosa after oral administration of polaprezinc to rats was significantly increased by treatment with cimetidine. These results suggest that the adhesion of zinc to gastric tissues is increased by inhibiting the dissociation of polaprezinc, and that H2-receptor antagonists, such as cimetidine, may increase anti-ulcer effects of polaprezinc.
采用双示踪法,使用[¹⁴C] - 和[⁶⁵Zn]波拉佐辛研究了波拉佐辛在大鼠胃肠道中的分布情况。给大鼠口服[¹⁴C] - 、[⁶⁵Zn]波拉佐辛后0.5小时,胃内容物中的¹⁴C放射性与⁶⁵Zn放射性相当。然而,给药后1小时内,胃内容物中¹⁴C和⁶⁵Zn放射性的变化时间过程存在显著差异,这表明波拉佐辛在给药后0.5小时以复合物形式存在,并随时间在胃肠道中解离为L - 肌肽和锌。给大鼠口服波拉佐辛后,西咪替丁治疗显著增加了锌对胃黏膜的黏附。这些结果表明,通过抑制波拉佐辛的解离可增加锌对胃组织的黏附,并且西咪替丁等H2受体拮抗剂可能会增强波拉佐辛的抗溃疡作用。