TY - JOUR
T1 - Pharmacokinetics of octreotide acetate long acting release (OALAR) in volunteers
AU - Anthony, L. B.
AU - Petryk, L.
AU - Olejarczyk, J.
AU - Foulds, E. C.
AU - Schran, H. F.
PY - 1997
Y1 - 1997
N2 - To develop a long acting formulation of octreotide (Sandostatin®), a double-blind placebo controlled trial of single IM doses of OALAR was performed in 48 subjects (males=11). Serum was collected, octreotide levels measured using RIA and pharmacokinetic analyses performed as follows: means (+/- S.E.) Dose Tmax Cmax>24 hr AUC(0-44D) (mg) (hr) (pg/ml) (pg × hr/ml) 1.5 544 (104) 40 (27) 19,462 (6,224) 3.0 632 (197) 315 (280) 54,481(16,937) 6.0 437 (169) 230 (97) 108,548 (14,129) 12 452 (177) 1,097 (268) 385,735 (20,550) 20 656 (91) 1,457 (142) 818,711 (56,124) 30 532 (107) 2,812 (209) 1.42 E 6(2.89 E 5) AUC and Cmax>24 hr correlated to dose and could be described by a simple linear model. Sustained serum levels for 37-76 days occurred with the 2 higher doses and decreased 55 days post injection with serum levels detectable up to 100 days. Assuming a minimal effective level of 1 ng/ml, the 30 mg dose could provide therapeutic hormonal suppression from 9 to 45 days.
AB - To develop a long acting formulation of octreotide (Sandostatin®), a double-blind placebo controlled trial of single IM doses of OALAR was performed in 48 subjects (males=11). Serum was collected, octreotide levels measured using RIA and pharmacokinetic analyses performed as follows: means (+/- S.E.) Dose Tmax Cmax>24 hr AUC(0-44D) (mg) (hr) (pg/ml) (pg × hr/ml) 1.5 544 (104) 40 (27) 19,462 (6,224) 3.0 632 (197) 315 (280) 54,481(16,937) 6.0 437 (169) 230 (97) 108,548 (14,129) 12 452 (177) 1,097 (268) 385,735 (20,550) 20 656 (91) 1,457 (142) 818,711 (56,124) 30 532 (107) 2,812 (209) 1.42 E 6(2.89 E 5) AUC and Cmax>24 hr correlated to dose and could be described by a simple linear model. Sustained serum levels for 37-76 days occurred with the 2 higher doses and decreased 55 days post injection with serum levels detectable up to 100 days. Assuming a minimal effective level of 1 ng/ml, the 30 mg dose could provide therapeutic hormonal suppression from 9 to 45 days.
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M3 - Article
AN - SCOPUS:33748961508
SN - 0009-9236
VL - 61
SP - 144
JO - Clinical Pharmacology and Therapeutics
JF - Clinical Pharmacology and Therapeutics
IS - 2
ER -