Pharmacokinetics of methoxyflurane after its intra-dermal injection as lecithin-coated microdroplets

作者: Michael Y. Wu , Jonas Johansson , Norman H. Altman , Duncan H. Haynes , Vera Fiserova-Bergerova

DOI: 10.1016/0168-3659(89)90028-X

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摘要: Abstract Recent studies (D.H. Haynes and A.F. Kirkpatrick, Anesthesiology, 63 (1985) 490–499) have shown that general anesthetic oils such as methoxyflurane (MOF) can be incorporated into lecithin-coated microdroplets of ca. 1000 A diameter. Intradermal injection selected inhalation anesthetics results in reversible local anesthesia. The present study gives information on the time course absorption, distribution, elimination MOF its metabolites for intradermal 20 mg microdroplet-associated rat tails. Following microdroplets, bulk injected amount is absorbed blood. absorption biphasic with half-times 2 h 450 h. levels blood tissue peak within 3 after injection. concentrations 6 Studies body burden suggest lung a major pathway, clearing much two-thirds MOF. This direct contrast to fate administered by inhalation, which metabolism pathway. With microdroplet administration, offluoride plasma are an order magnitude smaller than non-effect associated anesthesia nephrotoxicity, respectively. would appear provide sufficient margin safety any known adverse effect low noninjected tissues partly attributed dose requirement respiratory-circulatory system allows significant removed from exhalation before it reaches other tissues.

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