Fospropofol is a water-soluble phosphate prodrug of propofol developed for intravenous administration. It is rapidly converted in the body to propofol, the active anesthetic compound. Fospropofol has been investigated and developed as an intravenous sedative-hypnotic agent for monitored anesthesia care and procedural sedation.
Fospropofol is a specialized pharmaceutical active ingredient belonging to the anesthetic drug class. Its phosphate ester structure provides substantially greater water solubility than propofol, supporting development of aqueous injectable formulations.
CAS Number: 102010-04-6
Molecular Formula: C13H19Na2O6P
Molecular Weight: 348.24 g/mol
Development Code: GPI 15715
Drug Class: General Anesthetic / Sedative-Hypnotic
Chemical Class: Phosphate Prodrug
Active Metabolite: Propofol
Route: Intravenous
Fospropofol is a prodrug that is converted by alkaline phosphatase to propofol. Propofol enhances inhibitory neurotransmission primarily through modulation of GABA-A receptors in the central nervous system. This produces sedation and hypnosis.
Fospropofol has been developed for intravenous sedation in patients undergoing diagnostic or therapeutic procedures. Its water-soluble prodrug design was intended to provide an alternative to the lipid emulsion formulation traditionally used for propofol.
Fospropofol differs from propofol by the addition of a phosphate group that significantly increases water solubility. Following administration, enzymatic cleavage of the phosphate group releases propofol, which produces the principal sedative-hypnotic effect.
Fospropofol is a phosphate-containing prodrug and is substantially more water soluble than propofol. The disodium salt is associated with the molecular formula C13H19Na2O6P and molecular weight 348.24 g/mol.
Fospropofol API quality assessment may include identification by IR and chromatographic techniques, HPLC assay, related substances, water content, residual solvents, inorganic phosphate, elemental impurities and other applicable pharmaceutical quality-control tests.
Fospropofol should be stored in tightly closed containers under controlled pharmaceutical conditions and protected from excessive heat, moisture and direct light. Storage conditions should follow the applicable validated stability data and product specification.
Fospropofol represents a prodrug approach to improving the formulation properties of propofol. Conversion to propofol after administration allows the pharmacological effects of propofol to be obtained while using a water-soluble phosphate prodrug.
Fospropofol is a water-soluble phosphate prodrug of propofol developed for intravenous sedation. It is identified by CAS Number 102010-04-6, with molecular formula C13H19Na2O6P and molecular weight 348.24 g/mol. It is primarily associated with anesthetic and procedural sedation applications.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | Conforms by IR and HPLC |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 1.0% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 4.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |