Fugono Jun, Yasui Hiroyuki, Sakurai Hiromu
Department of Analytical and Bioinorganic Chemistry, Kyoto Pharmaceutical University, Kyoto, Japan.
J Pharm Pharmacol. 2005 May;57(5):665-9. doi: 10.1211/0022357055993.
Chronic oral administration of vanadyl sulfate has recently been shown to improve the state of type 2 diabetic subjects. Mild gastrointestinal symptoms and side effects, however, have been observed in some subjects. To find safer and more effective dosages, we have developed an enteric-coated capsule containing solid vanadyl sulfate (ECC/VS), which enhances the bioavailability of vanadyl sulfate to almost double that of vanadyl sulfate solution. ECC/VS was chronically administered to treat streptozotocin-induced diabetic rats (STZ-rats), an animal model of type 1 diabetes mellitus, and an equivalent blood-glucose-lowering effect was observed at half the doses of vanadyl sulfate alone. In addition, we observed almost the same total vanadium levels in the serum after chronic administration of ECC/VS as those of vanadyl sulfate alone, suggesting that plasma vanadium levels correlate with the hypoglycaemic activity of vanadyl sulfate. These results indicate that oral ECC/VS improves the diabetic state by enhancing the uptake of vanadium in STZ-rats. These findings will be useful in designing clinical trials of vanadyl sulfate for diabetic subjects.
最近研究表明，长期口服硫酸氧钒可改善2型糖尿病患者的状况。然而，部分患者出现了轻微的胃肠道症状和副作用。为了找到更安全、有效的剂量，我们研发了一种含有固体硫酸氧钒的肠溶胶囊（ECC/VS），它能使硫酸氧钒的生物利用度提高至硫酸氧钒溶液的近两倍。将ECC/VS长期用于治疗链脲佐菌素诱导的糖尿病大鼠（STZ大鼠），这是1型糖尿病的动物模型，观察到在硫酸氧钒剂量减半的情况下，血糖降低效果相同。此外，我们发现长期服用ECC/VS后血清中的总钒水平与单独服用硫酸氧钒时几乎相同，这表明血浆钒水平与硫酸氧钒的降血糖活性相关。这些结果表明，口服ECC/VS可通过增强STZ大鼠对钒的摄取来改善糖尿病状态。这些发现将有助于设计针对糖尿病患者的硫酸氧钒临床试验。
