Biomaterial Database

Aggregation behavior of fosinopril sodium--a new angiotensin-converting enzyme inhibitor. 1995

Z Wang, and K R Morris, and B Chu

Department of Chemistry, State University of New York, Stony Brook 11794-3400, USA.

Fosinopril sodium is an effective new angiotensin-converting enzyme (ACE) inhibitor that is very useful for the clinical treatment of hypertension. After oral administration, fosinopril sodium is only partially absorbed (about one third of the drug). We studied the solution behavior of fosinopril sodium in aqueous media by a combination of high-resolution nuclear magnetic resonance (NMR) spectroscopy and laser light scattering (LLS). LLS characterizes the self-association properties of fosinopril sodium in solution, and NMR chemical shifts provide information on molecular conformation and interactions. The results revealed that fosinopril sodium has a micelle-like self-association behavior with a critical micelle concentration (cmc) approximately 1.5 mg/mL. Hydrophobic interactions could induce formation of micellar aggregates, which had a narrow hydrodynamic size distribution, with an average diameter of approximately 150 nm at concentrations above the cmc. The surface activity and self-association of fosinopril sodium may be responsible for its early observed concentration-dependent stability in aqueous solution, unexpected decrease in solubility in the presence of metal ions, as well as the limited absorption in clinical studies.

UI	MeSH Term	Description	Entries
D007834	Lasers	An optical source that emits photons in a coherent beam. Light Amplification by Stimulated Emission of Radiation (LASER) is brought about using devices that transform light of varying frequencies into a single intense, nearly nondivergent beam of monochromatic radiation. Lasers operate in the infrared, visible, ultraviolet, or X-ray regions of the spectrum.	Masers,Continuous Wave Lasers,Pulsed Lasers,Q-Switched Lasers,Continuous Wave Laser,Laser,Laser, Continuous Wave,Laser, Pulsed,Laser, Q-Switched,Lasers, Continuous Wave,Lasers, Pulsed,Lasers, Q-Switched,Maser,Pulsed Laser,Q Switched Lasers,Q-Switched Laser
D008823	Micelles	Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS.	Micelle
D009682	Magnetic Resonance Spectroscopy	Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).	In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D012964	Sodium	A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.	Sodium Ion Level,Sodium-23,Ion Level, Sodium,Level, Sodium Ion,Sodium 23
D014867	Water	A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)	Hydrogen Oxide
D017328	Fosinopril	A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.	Fosenopril,Dynacil,Fosinil,Fosinopril Sodium,Fosinopril, (1(S(R)),2 alpha,4 alpha)-(D-Pro)-Isomer,Fosinopril, (1(S(R)),2 alpha,4 beta)-Isomer,Fosinopril, (1(S(S)),2 alpha,4 beta)-Isomer,Fosinorm,Fositens,Fozitec,Hiperlex,Monopril,Newace,SQ-28,555,SQ-28555,Staril,Tenso Stop,Tensocardil,SQ 28,555,SQ 28555,SQ28,555,SQ28555,Sodium, Fosinopril