Preparation of a 35S Labelled Trimeprazine Tartrate Sustained Action Product for its Evaluation in Man

Abstract

Multi‐pellet sustained action capsules containing radiochemically labelled drug were prepared by a pan coating procedure. Pellets of varying lipid thickness were prepared, and mixed in different proportions to obtain products having variable in vitro release characteristics. Capsules were prepared from these pellets for administration to man. Oral doses of 5 mg. of labelled trimeprazine were given in a non‐sustained release form at 0, 4, and 8 hours. Other subjects received single 15 mg. oral doses of labelled trimeprazine in sustained action capsules. The 35S activity was determined in blood and urine at selected times. Sustained action capsules were prepared which when evaluated in man gave data for 35S activity in blood and urine which were comparable to that observed for three divided doses of non‐sustained release drug administered at 0, 4, and 8 hours.

Absorption efficiency and excretion profile of a prolonged‐action form of chlorpromazine

“…Urine was collected from each patient as follows: on days 1 and 10, at intervals of 0 to 3, 3 to 6, 6 to 9, 9 to 12, and 12 to 24 hours. On days 8,9,11,12, and 13 the total urinary output was collected, that is, o to 24 hours. Days 12 and 13 were the first and second "rest" days.…”

Comparative study in man of the absorption and excretion of amobarbital-14C from sustained-release and nonsustained-release dosage forms

“…However, conventional bioanalytic techniques to measure levels of amobarbital and its metabolites in blood and urine are not sufficiently sensitive to accurately measure drug concentration from a 30-mg. dose, so it was necessary t o label the amobarbital with a radioactive carbon atom. The utility of this technique for evaluating pelleted sustained-release preparations has been reported previously (2)(3)(4).…”

Reduced Side Effects following Administration of a New Anorectic Agent, 4′-Chloro-2-(ethylamino)propiophenone, in Timed-Release Form

“…In Vitro Release-Nontimed-release medicated pellets were prepared as previously reported (1,2) and made to assay from 32 to 74% SK&F 70948. A portion of these pellets was retained, and the remaining pellets were coated with approximately 4% paraffin wax and varying increments of glyceryl stearate to prolong drug release.…”

“…These compounds were synthesized by the condensation of a ketone with a desired amine according to the procedure described in the literature (1). Preliminary pharmacological studies indicate only insignificant antianxiety properties.…”