Regdon G, Erös I, Gombkötö Z, Németh J, Regdon G, Vernyik A, Sallai J
Szent-Györgyi Albert Orvostudományi Egyetem Gyógyszertechnológiai Intézet, Szeged.
Acta Pharm Hung. 1998 Jul;68(4):224-8.
The factors influencing in vitro liberation (Part 1) and in vivo absorption (Part 2) from trimethoprim-containing rectal suppositories and the authors' results related to them are reported in this two-part publication. Special emphasis was laid on selecting the optimal suppository base which is harmless physiologically yet not indifferent pharmacologically. From among the 24 compositions studied, a lipophilic mixture containing a surface active additive (Witepsol W 35) and a hydrophilic (Macrogolum) mixture were found to be the best in all respects. Liberation from the trimethoprim-containing rectal suppositories was measured with in vitro dynamic diffusion and spectrophotometrically. A power relation was found to exist between the quantity of the released pharmacon and the diffusion time, and a significant negative exponential relation was observed between the doses and their respective in vitro availability values.
本文分两部分发表，报道了影响含甲氧苄啶直肠栓剂体外释放（第一部分）和体内吸收（第二部分）的因素以及作者与之相关的研究结果。特别强调了选择生理无害但药理并非惰性的最佳栓剂基质。在所研究的24种配方中，发现含有表面活性添加剂（Witepsol W 35）的亲脂性混合物和亲水性（聚乙二醇）混合物在各方面都是最佳的。采用体外动态扩散和分光光度法测定了含甲氧苄啶直肠栓剂的释放情况。发现释放药物的量与扩散时间之间存在幂函数关系，并且观察到剂量与其各自的体外可用性值之间存在显著的负指数关系。
