WebJan 1, 2024 · Phosphate ester group. Phosphate esters are the most commonly used for prodrug synthesis to increase the solubility of poorly water-soluble orally administered drugs as well as for drugs that are administered parenterally (Stella and Nti-Addae, 2007). The phosphate prodrug is acted upon by endogenous phosphatase enzymes like alkaline ... WebOnce the prodrug gets into the systemic circulation or target tissues, the ester prodrug moiety may be cleaved through an enzymatic and/or chemical process to release the corresponding free acid of phosphinate, phosphonate, or phosphate to achieve the desirable biological effect.
Neurotherapeutic Potential of Water-Soluble pH-Responsive Prodrugs …
WebEster and phosphate hydrolysis are widely used in prodrug design because of their simplicity, but such approaches are relatively ineffective for targeting drugs to specific sites. The activation of prodrugs by the cytochrome P450 system provides a highly versatile approach to prodrug design that is particularly adaptable for targeting drug ... WebAug 28, 2008 · Preformulation studies were performed on a hemiglutarate ester prodrug of Δ 9-tetrahydrocannabinol (THC-HG), to facilitate the development of stable formulations by hot-melt methods.The various studies performed included solid-state thermal characterization, pKa, logP, aqueous and pH dependent solubility, pH stability and effect … smart and light
Oral phosphate prodrugs: Absorption rate limit considerations.
Webtriphenylethylene phosphate prodrug, TAT-59, were also conducted in the rat intestinal perfusion model. Finally, the utility of a phosphate ester prodrug strategy for entacapone to increase that drugs systemic levels was evaluated in rats. MATERIALS AND METHODS Materials TAT-59 and its parent drug, DP-TAT-59, were gifts of WebGW433908 is the water-soluble, phosphate ester prodrug of the human immunodeficiency virus type 1 protease inhibitor amprenavir (APV). A high-yield synthesis of GW433908 is achieved by phosphorylation of the penultimate precursor of APV with phosphorous oxychloride (POCl(3)) in pyridine. WebPhosphate ester prodrugs of propofol (fospropofol, HX0969W) were designed to avoid the unsatisfactory water solubility of the parent drug. However, in previous clinical trials, there … hill country apothecary bee cave