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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Kumpulainen, Hanna Järvinen, Tomi Mannila, Anne Leppänen, Jukka Nevalainen, Tapio Mäntylä, Antti Vepsäläinen, Jouko Rautio, Jarkko |
| Description | Country affiliation: Finland Author Affiliation: Kumpulainen H ( Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FI-70211 Kuopio, Finland. Hanna.Kumpulainen@uku.fi) |
| Abstract | A novel ethyl dioxy phosphate prodrug of propofol (3) was synthesized and characterized in vitro and in vivo as safer alternative for phosphonooxymethyl prodrugs. The synthesis of 3 was achieved via vinyl and 1-chloroethyl ether intermediates, followed by addition of phosphate group. Aqueous solubility and chemical stability of 3 was determined in buffer solutions and the bioconversion of 3 to propofol was determined in vitro and in vivo. The results show that 3 greatly enhanced the aqueous solubility of propofol (solubility over 10 mg/mL) and the stability in buffer solution (t1/2=5.2+/-0.2 days at pH 7.4, r.t.) was sufficient for i.v. administration. The enzymatic hydrolysis of 3 to propofol was extremely rapid in vitro (t1/2=21+/-3s) and 3 was readily converted to propofol in vivo in rats. During bioconversion, 3 releases acetaldehyde, a less toxic compound than the formaldehyde released from the phosphonooxymethyl prodrug of propofol (Aquavan), currently undergoing clinical trials. The maximum plasma concentration of propofol, 3.0+/-0.2 microg/mL, was reached within 2.1+/-0.8 min after the i.v. administration of 3. The present study indicates that ethyl dioxy phosphate represents a potentially useful water-soluble prodrug structure suitable for i.v. administration. |
| File Format | HTM / HTML |
| ISSN | 09280987 |
| Issue Number | 2-3 |
| Volume Number | 34 |
| e-ISSN | 18790720 |
| Journal | European Journal of Pharmaceutical Sciences |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2008-07-03 |
| Publisher Place | Netherlands |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Chemistry Discipline Pharmacology Anesthetics, Intravenous Chemical Synthesis Prodrugs Propofol Alkaline Phosphatase Chemistry Pharmacology Animals Buffers Chromatography, High Pressure Liquid Chromatography, Thin Layer Hydrolysis Indicators And Reagents Magnetic Resonance Spectroscopy Male Phosphates Rats Rats, Wistar Solubility Solutions Spectrophotometry, Ultraviolet Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmaceutical Science |
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