
Chemical Name:Octreotide acetate
CAS:83150-76-9
Molecular Formula:C<sub>49</sub>H<sub>66</sub>N<sub>10</sub>O<sub>10</sub>S<sub>2</sub>·C<sub>2</sub>H<sub>4</sub>O<sub>2</sub>
Molecular Weight:1019.24 g/mol (free base: 931.61 g/mol)
Appearance:White or almost white powder
Solubility:Freely soluble in water; slightly soluble in ethanol
Stability:Stable at 2–8°C; protect from light and moisture
Mode of Action:Synthetic somatostatin analog; binds to somatostatin receptors (SSTR2/SSTR5) to inhibit growth hormone, glucagon, and insulin secretion.
Pharmacological Use:Treatment of acromegaly, neuroendocrine tumors (e.g., carcinoid syndrome), and esophageal varices bleeding.
Half-life:1.5–2 hours (subcutaneous); prolonged-release formulations available

Octreotide acetate is a synthetic analog of somatostatin with prolonged activity and selective binding to SSTR2/SSTR5 receptors. Its clinical applications include:
Acromegaly: Suppresses growth hormone secretion.
Neuroendocrine Tumors: Controls symptoms (e.g., flushing/diarrhea in carcinoid syndrome).
GI Bleeding: Reduces portal hypertension in esophageal varices.
Advantages over Somatostatin:
Longer half-life (allows 2–3 daily SC injections or monthly depot formulations).
Higher specificity for target receptors.

Test Parameter | Specification | Test Method | Reference Standard |
---|
Appearance | White to off-white lyophilized powder | Visual inspection | EP/USP |
Identification | Complies (HPLC retention time + MS) | HPLC-PDA/MS | EP/USP |
Assay (HPLC) | 95.0%~105.0% (anhydrous basis) | RP-HPLC (C18, 220nm) | EP/USP |
Related Substances | Total impurities ≤ 3.0% Any single ≤ 1.5% | Gradient HPLC | ICH Q3A/B |
Acetate Content | 5.0%~12.0% | Ion chromatography | EP |
Water Content | ≤ 8.0% | Karl Fischer | EP/USP <921> |
pH (1% solution) | 3.5~5.5 | Potentiometry | EP/USP <791> |
Heavy Metals | ≤ 20 ppm | ICP-MS | USP <232>/EP 2.4.8 |
Residual Solvents | Meets ICH Q3C Class 2/3 limits | GC-FID | ICH Q3C |
Microbial Limits | TAMC ≤ 100 CFU/g TYMC ≤ 50 CFU/g | Membrane filtration | EP/USP <61> |
Endotoxin | < 50 IU/mg | LAL test (gel clot) | EP/USP <85> |
Specific Rotation | -30° to -45° (c=1 in water) | Polarimetry | EP/USP <781> |
Peptide Content | ≥ 90.0% | Amino acid analysis | EP |
Biological Potency | 90%~115% of label claim | Cell-based bioassay (SSTR2/SSTR5) | EP/In-house validated |
