Octreotide Acetate

Sandostatin® (octreotide acetate) Injection, a cyclic octapeptide prepared as a clear sterile solution of octreotide, acetate salt, in a buffered lactic acid solution for administration by deep subcutaneous (intrafat) or intravenous injection. Octreotide acetate, known chemically as L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]-, cyclic (2→7)-disulfide; [R-(R*, R*)] acetate salt, is a long-acting octapeptide with pharmacologic actions mimicking those of the natural hormone somatostatin.

Sandostatin (octreotide acetate) Injection is available as: sterile 1-mL ampuls in 3 strengths, containing 50, 100, or 500 mcg octreotide (as acetate), and sterile 5-mL multi-dose vials in 2 strengths, containing 200 and 1000 mcg/mL of octreotide (as acetate).

Each ampul also contains:

lactic acid, USP............................................. 3.4 mg
mannitol, USP................................................ 45 mg
sodium bicarbonate, USP .............................. qs to pH 4.2 ±0.3
water for injection, USP...................................qs to 1 mL

Each mL of the multi-dose vials also contains:

lactic acid, USP ............................................. 3.4 mg
mannitol, USP................................................. 45 mg
phenol, USP....................................................5.0 mg
sodium bicarbonate, USP ............................... qs to pH 4.2 ±0.3
water for injection, USP...................................qs to 1 mL

Lactic acid and sodium bicarbonate are added to provide a buffered solution, pH to 4.2 ±0.3.

The molecular weight of octreotide acetate is 1019.3 (free peptide, C49H66N10O10S2) and its amino acid sequence is:

H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol,
xCH3COOH           where x = 1.4 to 2.5