PREPARATION OF A 35S LABELLED TRIMEPRAZINE TARTRATE SUSTAINED ACTION PRODUCT FOR ITS EVALUATION IN MAN

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.