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.
Tablets and capsules of a combination product containing triamterene and hydrochlorothiazide in a 2:1 ratio were compared in a series of short‐term studies with male volunteers. The tablet caused approximately twice as much excretion of hydrochlorothiazide and 3 times as much triamterene as the capsule. These studies provide further evidence of the importance of the dosage forms in the effectiveness of drugs.
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