[Experiences with the rectal use of a chemotherapeutic agent. 1. In vitro biopharmaceutical examinations; selection of the optimal vehicle].
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.
Regdon
G
G
Szent-Györgyi Albert Orvostudományi Egyetem Gyógyszertechnológiai Intézet, Szeged.
Erös
I
I
Gombkötö
Z
Z
Németh
J
J
Regdon
G
G
Vernyik
A
A
Sallai
J
J
D000285:Administration, Rectal; D002626:Chemistry, Pharmaceutical; D004058:Diffusion; D006801:Humans; D013053:Spectrophotometry; D013488:Suppositories; D014295:Trimethoprim / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
D013488:Suppositories; D014295:Trimethoprim