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[3H]血管加压素在布拉特洛维大鼠体内用于研究从Accurel/火棉胶装置进行控释的体内研究。

The use of [3H]vasopressin for in-vivo studies of controlled delivery from an Accurel/collodion device in the Brattleboro rat.

作者信息

Kruisbrink J, Boer G J

出版信息

J Pharm Pharmacol. 1986 Dec;38(12):893-7. doi: 10.1111/j.2042-7158.1986.tb03378.x.

Abstract

Accurel polypropylene/collodion controlled drug-delivery devices containing 22 micrograms [3H]vasopressin (VP) were implanted s.c. in VP-deficient Brattleboro rats. This caused a decrease in their urine production for at least 50 days, at which time the Accurel device was removed. Release of VP was followed by measurements of tritium radioactivity and by radioimmunoassay of VP in the urine. These parameters showed a constant pattern during the whole period. After re-implantation of the Accurel devices in another group of Brattleboro rats, release of VP continued to give the same level of urine production as during the last period of the first implantation. It is concluded that release of VP in-vivo is not influenced by encapsulation of the Accurel polymer by connective tissue, or that adaptation of the kidney adds to the maintenance of the urine production at this low level. In-vivo release rate is calculated to be about 1% of the original load each day. The in-vitro release in a flow cell system appeared to produce the same release rate which indicates that these data have a predictive value for the in-vivo situation.

摘要

将含有22微克[³H]血管加压素(VP)的Accurel聚丙烯/火棉胶控释给药装置皮下植入VP缺乏的布拉特洛维大鼠体内。这导致它们的尿量减少至少50天,此时将Accurel装置取出。通过测量氚放射性以及对尿液中的VP进行放射免疫测定来跟踪VP的释放。这些参数在整个期间呈现出恒定模式。在另一组布拉特洛维大鼠中重新植入Accurel装置后,VP的释放继续产生与首次植入最后阶段相同水平的尿量。得出的结论是,体内VP的释放不受结缔组织对Accurel聚合物的包裹影响,或者肾脏的适应性有助于将尿量维持在这个低水平。体内释放速率经计算约为每日原始负载量的1%。流动池系统中的体外释放似乎产生相同的释放速率,这表明这些数据对体内情况具有预测价值。

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